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1.
J Dairy Sci ; 102(8): 6959-6970, 2019 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-31255265

RESUMO

In this paper, we report the physicochemical and sensory properties of milk supplemented with a powder of microencapsulated lactase. The core material was lactase (ß-galactosidase), the primary coating material was medium-chain triglyceride (MCT), and the secondary (enteric) coating material was either hydroxypropyl methylcellulose phthalate (HPMCP) or shellac, comparing both against market milk as a control. The physicochemical properties of both types of microcapsules were analyzed, including the particle size, zeta potential, and in vitro release behavior. To survey the stability of the microcapsules in milk during storage, we studied the residual lactose content and pH. Furthermore, to determine the properties of milk supplemented with the microcapsules, changes in color and sensory properties were evaluated during storage. The particle sizes (volume-weighted mean; D[4,3]) of the microcapsules coated with HPMCP or shellac were 2,836 and 7,834 nm, respectively, and the zeta potential of the capsules coated with shellac was higher than the zeta potential of those coated with HPMCP. The pH levels of milk supplemented with the lactase microcapsules were similar to those of the control (unsupplemented market milk); however, for milk supplemented with HPMCP-coated microcapsules, the pH was slightly lower. The core material, lactase, was released from the microcapsules during 12-d storage, and 18.82 and 35.09% of lactose was hydrolyzed in the samples for HPMCP- and shellac-coated microcapsules, respectively. The sensory characteristics of milk containing microcapsules coated with HPMCP did not show significant differences from the control, in terms of sweetness or off-taste, until 8 d of storage. However, shellac-coated microcapsules showed significant difference in sweetness and off-taste at d 8 and 6 of storage, respectively. The color of milk containing HPMCP-coated microcapsules did not show a significant difference during storage. However, that containing shellac-coated microcapsules was somewhat higher in color values than others. In particular, it showed significance from 0 to 4 d storage in L* and C* values. In conclusion, a powder of lactase microcapsules coated with HPMCP can be suitable as a supplement for milk.


Assuntos
Suplementos Nutricionais , Kluyveromyces/enzimologia , Lactase/administração & dosagem , Metilcelulose/análogos & derivados , Leite/química , Animais , Cápsulas , Fenômenos Químicos , Composição de Medicamentos/veterinária , Proteínas Fúngicas/administração & dosagem , Hidrólise , Lactose/metabolismo , Metilcelulose/química , Leite/metabolismo , Tamanho da Partícula , Pós , Resinas Vegetais/química , Paladar , Triglicerídeos/química
2.
Vet Parasitol ; 270 Suppl 1: S58-S63, 2019 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-31182302

RESUMO

The efficacy of three consecutive monthly treatments with a novel topical product (Revolution® Plus/Stronghold® Plus, Zoetis) containing selamectin in combination with the isoxazoline, sarolaner, was compared with that of another topical isoxazoline, fluralaner [Bravecto® (fluralaner topical solution) for Cats, Merck] against Ixodes scapularis ticks on cats. Twenty-four cats were ranked by pre-treatment tick counts to form groups of three and were randomly allocated to be treated with placebo, the minimum label dosage of Revolution® Plus (6 mg/kg selamectin plus 1 mg/kg sarolaner) or the minimum label dosage of Bravecto® for Cats (40 mg/kg fluralaner) within the groups. On Days 0, 30, and 60, each cat in the placebo and Revolution® Plus-treated groups was treated topically, whereas cats in the Bravecto® for Cats-treated group were treated topically once on Day 0 with fluralaner and, subsequently, these animals were treated with the placebo on Days 30 and 60 to maintain masking. Doses were calculated based on weight to provide the minimum label dosage for each product; the calculated volume of product to be administered was rounded off to the nearest 0.1 mL. The selamectin plus sarolaner-treated cats received effective dosages of 5.29-7.12 mg/kg selamectin and 0.88-1.19 mg/kg sarolaner, while the fluralaner cats received dosages of 35.21-43.16 mg/kg fluralaner. Cats were infested with approximately 50 unfed viable adult I. scapularis ticks on Days 5, 12, 26, 40, 54, 68, 82, and 88. Efficacy was assessed at 48 h after each infestation. There were no adverse reactions to any treatment during the study. The placebo-treated cats maintained adequate tick infestations throughout the study. Three monthly treatments with selamectin plus sarolaner (Revolution® Plus) resulted in high and consistent efficacy against I. scapularis for up to 30 days after each treatment. Based on geometric means, efficacy was ≥99.1% at all time points assessed. Treatment with fluralaner (Bravecto® for Cats) provided high and consistent efficacy of ≥99.3% up to Day 70. On Day 84, efficacy was 90.1%; however, cats from which ticks were recovered on Day 84 had received approximately 4%-12% less than the minimum dosage of 40 mg/kg fluralaner. Three consecutive monthly treatments with Revolution® Plus or a single treatment with Bravecto® for Cats provided >90% control of I. scapularis ticks over a 12-week time period.


Assuntos
Antiparasitários/administração & dosagem , Azetidinas/administração & dosagem , Doenças do Gato/tratamento farmacológico , Isoxazóis/administração & dosagem , Ivermectina/análogos & derivados , Compostos de Espiro/administração & dosagem , Controle de Ácaros e Carrapatos , Infestações por Carrapato/veterinária , Administração Tópica , Animais , Gatos , Composição de Medicamentos/veterinária , Feminino , Ivermectina/administração & dosagem , Ixodes/efeitos dos fármacos , Masculino , Infestações por Carrapato/tratamento farmacológico , Resultado do Tratamento
3.
Vet Parasitol ; 270 Suppl 1: S38-S44, 2019 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-31104940

RESUMO

The efficacy and safety of a new topical formulation containing selamectin plus sarolaner (Revolution® Plus / Stronghold® Plus, Zoetis) was evaluated for the prevention of heartworm (Dirofilaria immitis) disease and the treatment of roundworm infection in cats enrolled as veterinary patients in two field studies conducted in Japan. In the heartworm field study, 91 cats negative for D. immitis antigen and anti-D. immitis antibody were enrolled and received 9 monthly topical treatments with selamectin plus sarolaner during the period of April to December 2015. Efficacy was assessed by testing post-treatment blood samples collected 8, 12, and 15 months after initiation of treatment for the presence of D. immitis antigen and anti-D. immitis antibody. Eighty-seven cats completed the entire study and were included in the determination of efficacy. No D. immitis antigen or anti-D. immitis antibody were detected in any of the post-treatment samples. In the roundworm field study, completed in the period from April to November 2015, 64 cats with ≥100 roundworm eggs per gram (EPG) of feces were enrolled and allocated randomly in a 1:1 ratio, to receive either selamectin plus sarolaner or emodepside plus praziquantel (Profender®, Bayer). Treatments were administered topically on Days 0 and 30, and efficacy was assessed by fecal EPG counts conducted on Days 14, 30, and 60. All cats completed the entire study. At enrollment, all cats were infected with Toxocara cati. Compared to pre-treatment, geometric mean T. cati EPG counts on Days 14, 30, and 60 were reduced by >99.9% in both treatment groups. There were no treatment-related adverse events in either study. Monthly topical administration of Revolution® Plus / Stronghold® Plus providing a minimum of 6 mg/kg selamectin and 1 mg/kg sarolaner was safe and effective in the prevention of heartworm disease and the treatment of roundworm infection in cats enrolled as veterinary patients in Japan.


Assuntos
Antiparasitários/administração & dosagem , Azetidinas/administração & dosagem , Doenças do Gato/prevenção & controle , Dirofilariose/prevenção & controle , Enteropatias Parasitárias/veterinária , Ivermectina/análogos & derivados , Infecções por Nematoides/veterinária , Compostos de Espiro/administração & dosagem , Administração Tópica , Animais , Doenças do Gato/tratamento farmacológico , Doenças do Gato/parasitologia , Gatos , Dirofilaria immitis/efeitos dos fármacos , Dirofilaria immitis/imunologia , Dirofilariose/tratamento farmacológico , Dirofilariose/parasitologia , Composição de Medicamentos/veterinária , Feminino , Helmintíase/tratamento farmacológico , Helmintíase/parasitologia , Helmintíase/prevenção & controle , Enteropatias Parasitárias/tratamento farmacológico , Enteropatias Parasitárias/parasitologia , Enteropatias Parasitárias/prevenção & controle , Ivermectina/administração & dosagem , Masculino , Infecções por Nematoides/tratamento farmacológico , Infecções por Nematoides/parasitologia , Infecções por Nematoides/prevenção & controle , Contagem de Ovos de Parasitas/veterinária , Distribuição Aleatória , Toxocara/efeitos dos fármacos , Resultado do Tratamento
4.
Vet Parasitol ; 270 Suppl 1: S52-S57, 2019 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-31133494

RESUMO

In a controlled laboratory study, the efficacy against fleas, Ctenocephalides felis, of a single treatment of fluralaner topical solution (Bravecto® for Cats, Merck) was compared with that of three consecutive monthly topical treatments with selamectin and sarolaner (Revolution® Plus, Zoetis). Twenty-four domestic short hair cats were ranked based on host suitability flea counts to form groups of three and were randomly assigned within group to one of three treatments. The first group received a topical treatment with (a) placebo (vehicle control for Revolution® Plus) on Days 0, 30, and 60, (b) 6 mg/kg selamectin and 1 mg/kg sarolaner on Days 0, 30, and 60, or (c) 40 mg/kg fluralaner on Day 0 and placebo (vehicle control for Revolution® Plus) on Days 30 and 60. Because doses were rounded off, the selamectin plus sarolaner-treated cats received effective dosages of 5.25-6.60 mg/kg selamectin and 0.88-1.10 mg/kg sarolaner, while the fluralaner-treated cats received dosages of 34.71-43.08 mg/kg fluralaner. All cats were infested with 100 (±5) fleas on Day -1 and at biweekly intervals after that, from Day 13 to Day 89. Flea comb counts were conducted 24 hours after treatment or after re-infestation. There were no adverse events related to treatment during the study. Except for a single cat from which 20 fleas were recovered on Day 90, all other placebo-treated cats had at least 48 fleas at each count, indicating adequacy of infestation of the controls. Based on geometric mean live flea counts, three consecutive monthly treatments with Revolution® Plus resulted in consistent and high efficacy of ≥98.6% compared with placebo throughout the study. A single treatment with Bravecto® for Cats provided consistent and high efficacy of ≥94.6% on all count days during a period of 12 weeks, the approved duration of efficacy for the product. Based on the efficacy results of the study, both products were equivalent in their ability to control fleas on cats. Use of Bravecto® for Cats every 12 weeks or the consecutive monthly use of Revolution® Plus is expected to provide extended high residual kill over the respective labeled durations of efficacy of the two products.


Assuntos
Antiparasitários/administração & dosagem , Azetidinas/administração & dosagem , Doenças do Gato/tratamento farmacológico , Infestações por Pulgas/veterinária , Inseticidas/administração & dosagem , Isoxazóis/administração & dosagem , Ivermectina/análogos & derivados , Compostos de Espiro/administração & dosagem , Administração Tópica , Animais , Gatos , Ctenocephalides/efeitos dos fármacos , Composição de Medicamentos/veterinária , Feminino , Infestações por Pulgas/tratamento farmacológico , Ivermectina/administração & dosagem , Masculino , Distribuição Aleatória , Resultado do Tratamento
5.
J Vet Sci ; 20(2): e16, 2019 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-30944538

RESUMO

We prepared a polymorphic form of valnemulin hydrogen tartrate (Form I) to overcome the instability and irritating odor of valnemulin hydrochloride that affect its use in the production and application of veterinary drugs. The physicochemical properties of Form I were characterized by scanning electron microscopy, X-ray powder diffraction, infrared spectroscopy, differential scanning calorimetry, and thermogravimetric analysis. The results showed the crystal structure and thermal properties of Form I were very different from those of a commercially available form of valnemulin hydrogen tartrate (Form II). Form I and Form II were more stable than valnemulin hydrochloride after storage under irradiation and high humidity conditions, respectively. The solubility of Form I was 2.6 times that of Form II, and Form I was selected for use in pharmaceutical kinetics experiments in vivo. Compared to valnemulin hydrochloride, after oral administration at a dose of 10 mg/kg in pigs, Form I had similar pharmaceutical kinetic behavior but a slightly higher area under the concentration-time curve from time zero to the last measurable concentration. Consequently, Form I should be suitable for the development of simple formulations and be effective in the clinical application of veterinary drugs.


Assuntos
Antibacterianos/química , Animais , Antibacterianos/farmacocinética , Antibacterianos/uso terapêutico , Varredura Diferencial de Calorimetria , Cristalização , Diterpenos/química , Diterpenos/farmacocinética , Diterpenos/uso terapêutico , Composição de Medicamentos/veterinária , Masculino , Microscopia Eletrônica de Varredura , Espectroscopia de Infravermelho com Transformada de Fourier , Suínos , Tartaratos/química , Tartaratos/uso terapêutico , Termogravimetria , Difração de Raios X
6.
Vet Parasitol ; 270 Suppl 1: S12-S18, 2019 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-30914264

RESUMO

The efficacy of a single application of a new topical formulation containing selamectin plus sarolaner (Revolution® Plus / Stronghold® Plus, Zoetis) was evaluated against fleas and ticks infesting cats enrolled as veterinary patients in two field studies conducted in Japan and against Haemaphysalis longicornis ticks on cats in a laboratory study. In the laboratory study, sixteen cats were ranked based on pre-treatment tick counts and allocated randomly to treatment on Day 0 with either selamectin plus sarolaner or placebo. Cats were infested with adult H. longicornis on Days -2, 5, 12, 19, 26 and 33. Efficacy relative to placebo was based on live attached tick counts conducted 48 h after treatment and subsequent re-infestations. Selamectin plus sarolaner reduced live, attached H. longicornis counts by 96.4% within 48 h of treatment, and by ≥91.7% within 48 h of weekly re-infestation for 35 days, based on arithmetic means. In the field studies, 67 client-owned cats harboring six or more live fleas and 63 cats harboring four or more live attached ticks were enrolled to evaluate selamectin plus sarolaner for efficacy and safety compared with a registered product. Cats were allocated randomly to treatment with selamectin plus sarolaner or fipronil plus (S)-methoprene based on order of presentation. Treatment was administered once on Day 0 and efficacy was assessed by parasite counts conducted on Days 14 and 30 compared to the pre-treatment count. In the flea field study, live flea counts on Days 14 and 30 were reduced by 99.5% and 99.9% in the selamectin plus sarolaner group, and by 97.6% and 98.6% in the fipronil plus (S)-methoprene group, based on least squares mean percentage reductions. Clinical signs typically associated with flea allergy dermatitis improved following treatment. In the tick field study, live tick counts on Days 14 and 30 were reduced by 97.5% and 97.7% in the selamectin plus sarolaner group, and by 91.5% and 93.4% in the fipronil plus (S)-methoprene group, based on least squares mean percentage reductions. Selamectin plus sarolaner was determined to be non-inferior to fipronil plus (S)-methoprene in both field studies. There were no treatment-related adverse events in any study. A single topical dose of Revolution® Plus / Stronghold® Plus providing a minimum dosage of 6.0 mg/kg selamectin and 1.0 mg/kg sarolaner was confirmed to be effective against H. longicornis ticks on cats for one month and safe and effective in the treatment of fleas and ticks on cats enrolled as veterinary patients in Japan.


Assuntos
Azetidinas/administração & dosagem , Doenças do Gato/tratamento farmacológico , Infestações por Pulgas/veterinária , Ivermectina/análogos & derivados , Compostos de Espiro/administração & dosagem , Controle de Ácaros e Carrapatos , Infestações por Carrapato/veterinária , Acaricidas/administração & dosagem , Administração Tópica , Animais , Doenças do Gato/prevenção & controle , Gatos , Composição de Medicamentos/veterinária , Feminino , Infestações por Pulgas/tratamento farmacológico , Infestações por Pulgas/prevenção & controle , Inseticidas/administração & dosagem , Ivermectina/administração & dosagem , Japão , Masculino , Metoprene/administração & dosagem , Pirazóis/administração & dosagem , Distribuição Aleatória , Sifonápteros/efeitos dos fármacos , Infestações por Carrapato/tratamento farmacológico , Infestações por Carrapato/prevenção & controle , Carrapatos/efeitos dos fármacos , Resultado do Tratamento
7.
Vet Parasitol ; 270 Suppl 1: S19-S25, 2019 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-30470637

RESUMO

The efficacy of a single topical application of a combination product containing selamectin and sarolaner (selamectin/sarolaner; Revolution® Plus/Stronghold® Plus) was evaluated in seven laboratory studies against Ixodes scapularis (three studies), Dermacentor variabilis (two studies), or Amblyomma maculatum (two studies). In each study, cats were randomly allocated to treatment groups based on pre-treatment host-suitability tick counts. On Days -2, 5, 12, 19, 26 and 33, the cats were infested with unfed adult ticks. On Day 0, cats were treated with either a placebo (vehicle control) or with the spot-on solution at the minimum dose of 6.0 mg selamectin and 1.0 mg sarolaner/kg bodyweight. In one study with I. scapularis and one with D. variabilis an additional group of cats was treated with selamectin alone (Revolution®, Zoetis) at 6.0 mg/kg bodyweight. Tick counts were conducted after treatment and after each weekly re-infestation and efficacy determined relative to placebo-treated animals. There were no treatment-related adverse reactions in any of the studies. Geometric mean live tick counts were significantly (P < 0.05) lower in the selamectin/sarolaner-treated groups compared to the geometric mean tick counts in the placebo-treated groups at all time-points in all studies. For all species, a single topical administration of the selamectin/sarolaner combination resulted in>90% efficacy against existing infestations based on geometric means. Efficacy against weekly re-infestations was >90% based on geometric means for at least 5 weeks for I. scapularis and D. variabilis, and for at least 4 weeks against A. maculatum. Selamectin alone had no efficacy against I. scapularis, where counts on selamectin-treated cats were not significantly different from placebo at all time points (P > 0.05), and for D. variabilis, counts were not significantly different from placebo at 2, 3 and 5 weeks after treatment (P > 0.05) and efficacy was never greater than 85%. Thus, the activity of the sarolaner against three common tick species found on cats in the US is complementary to the existing broad-spectrum parasite control of selamectin. The inclusion of sarolaner with selamectin in a combination product (Revolution® Plus/Stronghold® Plus) provides for the treatment of existing tick infestations and gives at least one month of control against re-infestation following a single topical application.


Assuntos
Acaricidas/administração & dosagem , Azetidinas/administração & dosagem , Doenças do Gato/tratamento farmacológico , Ivermectina/análogos & derivados , Compostos de Espiro/administração & dosagem , Controle de Ácaros e Carrapatos , Infestações por Carrapato/veterinária , Animais , Gatos , Composição de Medicamentos/veterinária , Feminino , Ivermectina/administração & dosagem , Ixodidae/efeitos dos fármacos , Masculino , Infestações por Carrapato/tratamento farmacológico , Estados Unidos
8.
Vet Parasitol ; 270 Suppl 1: S31-S37, 2019 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-30466895

RESUMO

Cytauxzoonosis, caused by infection with Cytauxzoon felis, is the most severe tick-borne disease of cats. The purpose of our study was to determine the efficacy of selamectin (6.0 mg/kg) plus sarolaner (1.0 mg/kg) formulated in combination (Revolution® Plus / Stronghold® Plus, Zoetis) applied topically once a month on cats for three months against induced infestations of Amblyomma americanum adults and to evaluate the effectiveness of the product in preventing the transmission of C. felis. This study was conducted in two phases. Sixteen cats were dosed with selamectin/sarolaner or a placebo (vehicle control) on Days 0, 28, and 56. In phase 1, each cat was infested with 50 (±5) unfed adult A. americanum on Day 4 and tick counts were conducted on Day 6 (48 h post infestation) and Day 7 (72 h post infestation) to evaluate acaricidal efficacy. In phase 2, to confirm acaricidal efficacy and evaluate prevention of C. felis transmission, each cat was infested on Day 60 with 50 (±5) adult A. americanum acquisition fed as nymphs on two C. felis-infected donor cats. Tick counts were conducted on Day 62 (48 h post infestation) and Day 63 (72 h post infestation). Blood samples were collected on Days -9, 60, 70, 76, and 90 and tested for infection with C. felis. Placebo cats were adequately infested on all count days, with least squares (geometric) mean live tick counts ranging from 34.0 (28.8) to 46.1 (46.0). Treatment reduced the least squares (geometric) mean counts compared to placebo by 27.1 (32.1)% and 90.4 (96.8)% on Days 6 and 7, respectively. The corresponding percent reductions were 56.4 (60.6)% and 94.7 (97.3)% on Days 62 and 63, respectively. Least squares mean counts were significantly lower in the treated group compared with the placebo group on all count days (P ≤ 0.0286). All cats were negative for C. felis by PCR prior to study start. In phase 2, seven cats in the control group and no cats in the selamectin/sarolaner group became infected with C. felis (P = 0.0017). Topical treatment with selamectin/sarolaner was >90% effective in reducing A. americanum tick counts 72 h after infestation and prevented the transmission of C. felis from infected ticks following the third of three monthly treatments. Revolution® Plus / Stronghold® Plus offers an option for the control of A. americanum infestations on cats and for preventing the transmission of C. felis to cats.


Assuntos
Antiparasitários/administração & dosagem , Azetidinas/administração & dosagem , Doenças do Gato/prevenção & controle , Ivermectina/análogos & derivados , Infecções Protozoárias em Animais/prevenção & controle , Compostos de Espiro/administração & dosagem , Controle de Ácaros e Carrapatos , Infestações por Carrapato/veterinária , Administração Tópica , Animais , Vetores Aracnídeos/efeitos dos fármacos , Vetores Aracnídeos/parasitologia , Doenças do Gato/tratamento farmacológico , Doenças do Gato/parasitologia , Doenças do Gato/transmissão , Gatos , Composição de Medicamentos/veterinária , Ivermectina/administração & dosagem , Ixodidae/efeitos dos fármacos , Ixodidae/parasitologia , Ninfa , Piroplasmida/efeitos dos fármacos , Piroplasmida/fisiologia , Infecções Protozoárias em Animais/parasitologia , Infecções Protozoárias em Animais/transmissão , Infestações por Carrapato/tratamento farmacológico , Resultado do Tratamento
9.
Vet Parasitol ; 270 Suppl 1: S26-S30, 2019 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-30563718

RESUMO

The speed of kill of a novel, topical product containing selamectin in combination with sarolaner (selamectin/sarolaner; Revolution® Plus/Stronghold® Plus) was evaluated against Ixodes scapularis ticks on cats. Sixteen cats were randomly allocated to a treatment group and treated topically on Day 0 with either placebo (vehicle control) or 6 mg/kg selamectin plus 1 mg/kg sarolaner. Cats were infested with approximately 50 unfed viable adult I. scapularis ticks on Days -2, 7, 14, 21, 28 and 35. Efficacy was assessed at 4, 8, 12, 24, 48 and 72 h after treatment on Day 0 and at 4, 8, 12 and 24 h after post-treatment re-infestations. There were no adverse reactions to the topical treatment with selamectin/sarolaner. Placebo-treated cats maintained tick infestations throughout the study. Treatment with selamectin/sarolaner significantly reduced tick counts within 12 h (P < 0.0001) and resulted in 100% efficacy by 24 h. For subsequent re-infestations, live tick counts were significantly reduced by 12 h after infestation on Day 7 (P = 0.0120) and by 24 h for Days 14-35 (P < 0.0001). At 24 h after the post-treatment re-infestations, efficacy based on geometric (arithmetic) means was ≥96.1% (94.5%) through Day 21, 75.3% (67.7%) on Day 28 and 66.4% (56.4%) on Day 35. Thus, a single topical dose of Revolution® Plus/Stronghold® Plus at the recommended minimum dose started killing ticks within 12-24 hours after treatment and re-infestations for up to 5 weeks. High acaricidal efficacy (≥90% reduction in tick burden) was achieved within 24 h after treatment and subsequent re-infestations for at least three weeks.


Assuntos
Acaricidas/administração & dosagem , Azetidinas/administração & dosagem , Doenças do Gato/tratamento farmacológico , Ivermectina/análogos & derivados , Ixodes/efeitos dos fármacos , Compostos de Espiro/administração & dosagem , Controle de Ácaros e Carrapatos , Infestações por Carrapato/veterinária , Administração Tópica , Animais , Gatos , Composição de Medicamentos/veterinária , Feminino , Ivermectina/administração & dosagem , Masculino , Infestações por Carrapato/tratamento farmacológico , Resultado do Tratamento
10.
Vet Parasitol ; 270 Suppl 1: S3-S11, 2019 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-30579753

RESUMO

Two randomised, single-masked, multi-center field studies were conducted in the United States in cats presented as veterinary patients. The first study evaluated the efficacy and safety of a topically applied formulation of selamectin plus sarolaner (Revolution® Plus/Stronghold® Plus, Zoetis) against natural flea infestations; the second study evaluated its efficacy against natural ear mite infestations. The product was administered topically by the cats' owners at the dose range provided in the market product of 6.0-12.0 mg selamectin and 1.0-2.0 mg sarolaner per kg bodyweight. Imidacloprid plus moxidectin (Advantage® Multi for Cats, Bayer) was used as a positive control in both studies at the label dosage. In the flea study, treatments were administered on Days 0, 30, and 60. Efficacy was calculated based on the mean percent reduction of live flea counts on Days 30, 60, and 90 relative to the pre-treatment count. In the ear mite study, a single treatment was applied on Day 0 and efficacy was determined on Days 14 and 30 based on the presence or absence of ear mites. In both studies, patients were randomly allocated to treatments in the ratio of 2:1, selamectin plus sarolaner: imidacloprid plus moxidectin. In the two studies, 405 cats received treatment with selamectin plus sarolaner; of these, 256 cats received three monthly treatments in the flea study. There were no serious adverse reactions to treatment with selamectin plus sarolaner; health issues noted were typical of the normal ailments or minor traumatic injuries expected in the general cat population and were similar in both treatment groups. Efficacy against fleas based on geometric (arithmetic) means was 97.2% (95.9%), 99.5% (99.4%), and 99.8% (99.8%) in the selamectin plus sarolaner group and was 79.7% (70.5%), 91.4% (77.3%), and 95.5% (87.4%) in the imidacloprid plus moxidectin group on Days 30, 60, and 90, respectively. Flea counts for the selamectin plus sarolaner group were significantly lower than the counts for the imidacloprid plus moxidectin group at all time-points after treatment administration on Day 0 (P < 0.001). Treatment reduced the clinical signs of flea allergy dermatitis (alopecia, dermatitis/pyodermatitis, erythema, pruritus, scaling, and papules) in affected cats by 86.7%-100% in the selamectin plus sarolaner group and by 66.7%-100% in the imidacloprid plus moxidectin group. In the ear mite study, a single application of selamectin plus sarolaner resulted in the clearance of mites from 87.5% of cats within 14 days and 94.4% of cats within 30 days of treatment. The respective percentages of mite-free cats in the imidacloprid plus moxidectin group were 64.0% and 72.0%. There were significantly more cats with no mites noted in the selamectin plus sarolaner group than in the imidacloprid plus moxidectin group on Day 14 and Day 30 (P ≤ 0.018). Selamectin plus sarolaner (Revolution® Plus/Stronghold® Plus) administered topically at monthly intervals for three months was well tolerated and highly effective for the treatment and prevention of natural infestations of fleas on cats presented as veterinary patients. Clinical signs of flea allergy dermatitis improved in affected cats following treatment administration. A single topical treatment was also safe and highly effective for the treatment of ear mite infestations in naturally infested cats.


Assuntos
Acaricidas/administração & dosagem , Azetidinas/administração & dosagem , Doenças do Gato/tratamento farmacológico , Infestações por Pulgas/veterinária , Inseticidas/administração & dosagem , Ivermectina/análogos & derivados , Infestações por Ácaros/veterinária , Compostos de Espiro/administração & dosagem , Administração Tópica , Animais , Doenças do Gato/prevenção & controle , Gatos , Composição de Medicamentos/veterinária , Feminino , Infestações por Pulgas/tratamento farmacológico , Infestações por Pulgas/prevenção & controle , Ivermectina/administração & dosagem , Macrolídeos/administração & dosagem , Masculino , Infestações por Ácaros/tratamento farmacológico , Infestações por Ácaros/prevenção & controle , Ácaros/efeitos dos fármacos , Neonicotinoides/administração & dosagem , Nitrocompostos/administração & dosagem , Distribuição Aleatória , Sifonápteros/efeitos dos fármacos
11.
J Sci Food Agric ; 99(3): 1078-1087, 2019 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-30022472

RESUMO

BACKGROUND: The high ureolytic activity of rumen microbiota is a concern when urea is used in ruminant feed, because it leads to fast urea conversion, resulting in possible intoxication and lower nitrogen utilization. This study intended to microencapsulate urea using carnauba wax to obtain slow-release systems in the rumen. The experiment was conducted in a randomized block design, arranged in a 3 × 2 factorial, with the urea encapsulated with carnauba wax in ratios of 1 : 2; 1 : 3, and 1 : 4 (UME 2; UME 3, and UME 4) and two particles sizes (small, PS ; and large, PL ). RESULTS: All formulations showed excellent properties, including inhibition of urea hygroscopicity. The formulation UME 2 exhibited the greatest yield (91.6%) and microencapsulation efficiency (99.6%) values, whereas the formulation UME 4 presented the greatest thermal stability (259.5 °C) and lowest moisture content (1.81%). The UME 2 formulation presented a slower release than the other UME formulations studied. CONCLUSION: The production of urea microspheres using carnauba wax was successful for all microencapsulated systems developed, evidencing the promising potential for use in ruminant animal diets. The UME 2 formulation with large particles is the most recommended because it permitted greater resistance to microbial attack, allowing a slower release of urea into the rumen, reducing the risk of intoxication or ruminal alkalosis. © 2018 Society of Chemical Industry.


Assuntos
Composição de Medicamentos/veterinária , Ureia/administração & dosagem , Ceras/química , Ração Animal/análise , Animais , Dieta/veterinária , Composição de Medicamentos/métodos , Masculino , Rúmen/efeitos dos fármacos , Rúmen/metabolismo , Carneiro Doméstico , Ureia/química , Ureia/farmacocinética
12.
J Vet Med Sci ; 80(12): 1847-1852, 2018 Dec 11.
Artigo em Inglês | MEDLINE | ID: mdl-30381675

RESUMO

The purpose of this study was to evaluate the bioequivalence of 5% ceftiofur hydrochloride sterile suspension in two formulations, a test formulation (Saifukang 5% CEF, Hvsen) and a reference formulation (Excenel®RTU 5% CEF, Pfizer). Twenty-four healthy pigs were assigned to a two-period, two-treatment crossover parallel trial, and both formulations were administered at a single intramuscular dose of 5 mg/kg weight, with a 7-day washout period. Blood samples were collected consecutively for up to 144 hr after administration. The concentrations of ceftiofur- and desfuroylceftiofur-related metabolites in the plasma were determined by high-performance liquid chromatography. In addition, the major pharmacokinetic parameters (Cmax, AUC0-t and AUC0-∞) were computed and compared via analysis of variance, with 90% confidence intervals. Bioequivalence evaluation of Tmax was statistically analyzed with the nonparametric test. The comparison values between test and reference formulation for AUC0-t, AUC0-∞, Cmax, and Tmax were 376.7 ± 75.3 µg·hr/ml, 390.5 ± 78.6 µg·hr/ml, 385.9 ± 79.2 µg·hr/ml, 402.7 ± 80.4 µg·hr/ml, 34.6 ± 5.5 µg/ml, 36.1 ± 6.2 µg/ml, 1.27 ± 0.18 hr, and 1.26 ± 0.21 hr, respectively, and we observed no significant differences between the two formulations. The 90% CI values were within the recommended range of 80-125% (P>0.05), and the relative bioavailability of the test product was 96.47 ± 10.92% according to AUC0-t values. Based on our results, the two formulations exhibit comparable pharmacokinetic profiles, and the test product is bioequivalent to the reference formulation.


Assuntos
Antibacterianos/farmacocinética , Cefalosporinas/farmacocinética , Suínos/metabolismo , Animais , Cromatografia Líquida de Alta Pressão/veterinária , Estudos Cross-Over , Composição de Medicamentos/veterinária , Feminino , Masculino , Equivalência Terapêutica
13.
Parasit Vectors ; 11(1): 508, 2018 Sep 12.
Artigo em Inglês | MEDLINE | ID: mdl-30208937

RESUMO

BACKGROUND: Pyrethroids are the most common class of insecticide used worldwide for indoor residual spraying (IRS) against malaria vectors. Water-dispersible granules (WG) are a pyrethroid formulation to be applied after disintegration and dispersion in water with less risks of inhalation than using the usual wettable powder (WP) formulation. The objective of this small-scale field study was to evaluate efficacy and duration of insecticidal action of a new alpha-cypermethrin WG (250 g a.i./kg) against susceptible Anopheles gambiae in comparison with the WHO reference product (alpha-cypermethrin WP, 50 g a.i./kg) on the most common indoor surfaces in Benin. METHODS: Both formulations were applied at two target-dose concentrations in houses made of mud and cement in the Tokoli village in southern Benin. We measured the applied dose of insecticide by chemical analysis of filter paper samples collected from the sprayed inner walls. We recorded An. gambiae mortality and knock-down rates every 15 days during 6 months using standard WHO bioassays. RESULTS: The alpha-cypermethrin WG formulation did not last as long as the WP formulation on both surfaces. The difference is higher with the 30 mg/m2 concentration for which the WP formulation reached the 80% mortality threshold during 2 months on the mud-plastered walls (3 months on cement) whereas the WG formulation last only one month (2 months on cement). CONCLUSIONS: The new WG formulation has a shorter efficacy than the WHO recommended WP formulation. In this trial, both the WG and WP formulations had low durations of efficacy that would need at least two rounds of spray to cover the entire transmission season.


Assuntos
Anopheles/efeitos dos fármacos , Inseticidas/farmacologia , Malária/prevenção & controle , Controle de Mosquitos/métodos , Mosquitos Vetores/efeitos dos fármacos , Piretrinas/farmacologia , Animais , Anopheles/parasitologia , Composição de Medicamentos/veterinária , Feminino , Habitação , Malária/transmissão , Mosquitos Vetores/parasitologia , Água
14.
Vet Parasitol ; 260: 38-44, 2018 Aug 30.
Artigo em Inglês | MEDLINE | ID: mdl-30197011

RESUMO

The effective dose of an injectable prodrug, named compound alpha prodrug, against immature and adult Fasciola hepatica in experimentally infected sheep was determined. In a first experiment, 30 sheep were infected with Fasciola hepatica on day 0 and 50. After microscopic detection of faecal eggs on day 80, groups (n = 6) 1 to 3 were treated with 6, 8 and 10 mg/kg of the experimental water-soluble prodrug compound alpha intramuscularly, respectively. Group 4 was treated with closantel and group 5 remained untreated. Copromicroscopical examinations were made on day 0, 80 and 108. On day 110, trematodes were collected from the bile ducts. Fasciolicide efficacy was assessed as a percentage of fluke-egg and adult-fluke reduction. Fluke length was also recorded. In a second experiment aimed to assess the fasciolicide activity of compound alpha prodrug against four-week-old flukes, 12 sheep were infected on day 0 and allocated into two groups (n = 6). On day 50 post infection, group A was treated with the experimental water-soluble prodrug compound alpha at 6 mg/kg/IM and B remained untreated. Fasciolicide activity was assessed on day 80 after collection, microscopic observation and measurement of flukes present in the parenchyma for immature stages and on day 108 for adults. Egg output decreased 91.2, 96.0, 98.8 and 94.9% for groups 1, 2, 3 and 4, respectively. Compound alpha prodrug cleared 97.6%, 98.51% and 100% of adult stages in a dose-dependent manner. Closantel killed 81.95% flukes. Regarding the second experiment, 81.2% efficacy was achieved. Immature flukes were significantly smaller in the treated group. It is concluded that the intramuscular application of compound alpha prodrug exerted fasciolicide efficacy against adults of Fasciola hepatica.


Assuntos
Anti-Helmínticos/uso terapêutico , Composição de Medicamentos/veterinária , Fasciola hepatica/efeitos dos fármacos , Fasciolíase/veterinária , Pró-Fármacos/uso terapêutico , Doenças dos Ovinos/tratamento farmacológico , Animais , Anti-Helmínticos/administração & dosagem , Anti-Helmínticos/química , Anti-Helmínticos/isolamento & purificação , Fasciolíase/tratamento farmacológico , Fasciolíase/parasitologia , Fezes/parasitologia , Injeções Intramusculares , Contagem de Ovos de Parasitas , Pró-Fármacos/administração & dosagem , Pró-Fármacos/efeitos adversos , Pró-Fármacos/química , Ovinos , Doenças dos Ovinos/parasitologia , Solubilidade
15.
Vet Clin North Am Exot Anim Pract ; 21(2): 195-214, 2018 May.
Artigo em Inglês | MEDLINE | ID: mdl-29655467

RESUMO

Extralabel drug use is the use of a Food and Drug Administration (FDA)-approved drug in a manner different from what is stipulated on the approved label. Compounding is the process of preparing a medication in a manner not indicated on the label to create a formulation specifically tailored to the needs of an individual patient. Extralabel drug use and compounding are vital aspects of safe and effective drug delivery to patients in exotic animal practice. There are few FDA-approved drugs for exotic animal species, and many approved drugs for other species are not available in suitable formulations for use in exotic animals.


Assuntos
Animais Exóticos/fisiologia , Sistemas de Liberação de Medicamentos/veterinária , Uso Off-Label/veterinária , Drogas Veterinárias/administração & dosagem , Drogas Veterinárias/química , Animais , Composição de Medicamentos/veterinária
16.
J Vet Pharmacol Ther ; 41(4): 572-580, 2018 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-29500829

RESUMO

The objective of this work was to manufacture an enteric formulation of florfenicol (FF) using hot-melt extrusion (HME) technology and to evaluate its in vitro dissolution and in vivo pharmacokinetics. For the HME process, hypromellose acetate succinate LG (HPMCAS-LG) was the enteric polymer mixed with FF, and the two components were extruded with a standard screw configuration at a speed of 50 rpm. Differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), powder X-ray diffraction (PXRD), and Fourier transform infrared spectroscopy (FT-IR) were performed to characterize the HME extrudate. The release percentage of the enteric formulation in the acidic stage was <10% of the loaded FF, whereas that in the phosphate buffer stage was >80%. Pharmacokinetic evaluations in swine revealed that the enteric formulation had a longer t1/2λ and MRT than commercially available FF powder (FULAIKA® ), indicating that the novel formulation exhibited enteric and sustained release properties. Compared with the commercial product, the relative bioavailability of the enteric formulation reached up to 117.2%. This study suggests that this formulation may have potential for future commercialization.


Assuntos
Antibacterianos/farmacocinética , Composição de Medicamentos/veterinária , Tianfenicol/análogos & derivados , Administração Oral , Animais , Antibacterianos/administração & dosagem , Antibacterianos/sangue , Antibacterianos/química , Varredura Diferencial de Calorimetria/veterinária , Composição de Medicamentos/métodos , Temperatura Alta , Injeções Intravenosas/veterinária , Espectroscopia de Infravermelho com Transformada de Fourier/veterinária , Suínos , Termogravimetria , Tianfenicol/administração & dosagem , Tianfenicol/sangue , Tianfenicol/química , Tianfenicol/farmacocinética , Difração de Raios X/veterinária
17.
J Vet Pharmacol Ther ; 41(1): e16-e21, 2018 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-28815733

RESUMO

This study was conducted to compare the pharmacokinetic profiles of conventional (Fungizone® ) and liposomal amphotericin B (AmBisome® ) formulations in order to predict their therapeutic properties, and evaluate their potential differences in veterinary treatment. For this purpose, twelve healthy mixed breed dogs received both drugs at a dose of 0.6 mg/kg by intravenous infusion over a 4-min period in a total volume of 40 ml. Blood samples were collected at 0, 0.5, 1, 1.5, 2, 3, 4, 8, 12, 24, 48, 72 and 96 hr after dosing, and concentrations of drug in plasma were determined by high-performance liquid chromatography (HPLC). Pharmacokinetics was described by a two-compartment model. Although both formulations were administered at the same doses (0.6 mg/kg), the plasma pharmacokinetics of liposomal amphotericin B differed significantly from those of amphotericin B deoxycholate in healthy dogs (p < .05). Liposomal amphotericin B showed markedly higher peak plasma concentrations (approximately ninefold greater) and higher area under the plasma concentration curve values (approximately 14-fold higher) compared to conventional formulation. It is concluded that AmBisome® reached higher plasma concentration and lower distribution volume and had a longer half-life compared to Fungizone® , and therefore, AmBisome® is reported to be an appropriate and effective choice for the treatment of systemic mycotic infections in dogs.


Assuntos
Anfotericina B/farmacocinética , Antifúngicos/farmacocinética , Anfotericina B/administração & dosagem , Anfotericina B/sangue , Animais , Antifúngicos/administração & dosagem , Antifúngicos/sangue , Cães , Composição de Medicamentos/veterinária , Infusões Intravenosas/veterinária , Masculino
18.
Am J Vet Res ; 79(1): 107-114, 2018 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-29287162

RESUMO

OBJECTIVE To compare the pharmacokinetics of 2 commercial florfenicol formulations following IM and SC administration to sheep. ANIMALS 16 healthy adult mixed-breed sheep. PROCEDURES In a crossover study, sheep were randomly assigned to receive florfenicol formulation A or B at a single dose of 20 mg/kg, IM, or 40 mg/kg, SC. After a 2-week washout period, each sheep was administered the opposite formulation at the same dose and administration route as the initial formulation. Blood samples were collected immediately before and at predetermined times for 24 hours after each florfenicol administration. Plasma florfenicol concentrations were determined by high-performance liquid chromatography. Pharmacokinetic parameters were estimated by noncompartmental methods and compared between the 2 formulations at each dose and route of administration. RESULTS Median maximum plasma concentration, elimination half-life, and area under the concentration-time curve from time 0 to the last quantifiable measurement for florfenicol were 3.76 µg/mL, 13.44 hours, and 24.88 µg•h/mL, respectively, for formulation A and 7.72 µg/mL, 5.98 hours, and 41.53 µg•h/mL, respectively, for formulation B following administration of 20 mg of florfenicol/kg, IM, and 2.63 µg/mL, 12.48 hours, and 31.63 µg•h/mL, respectively, for formulation A and 4.70 µg/mL, 16.60 hours, and 48.32 µg•h/mL, respectively, for formulation B following administration of 40 mg of florfenicol/kg, SC. CONCLUSIONS AND CLINICAL RELEVANCE Results indicated that both formulations achieved plasma florfenicol concentrations expected to be therapeutic for respiratory tract disease caused by Mannheimia haemolytica or Pasteurella spp at both doses and administration routes evaluated.


Assuntos
Antibacterianos/farmacocinética , Ovinos/metabolismo , Tianfenicol/análogos & derivados , Animais , Área Sob a Curva , Cromatografia Líquida de Alta Pressão/veterinária , Estudos Cross-Over , Composição de Medicamentos/veterinária , Meia-Vida , Injeções Intramusculares/veterinária , Injeções Subcutâneas/veterinária , Masculino , Tianfenicol/administração & dosagem , Tianfenicol/farmacocinética
19.
Fish Shellfish Immunol ; 73: 112-120, 2018 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-29208500

RESUMO

Polysaccharide from red seaweed Gracilaria folifera has an interesting functional property of antioxidant activity and prebiotic effect. A feeding trial experiment was directed to examine the effect of probiotic bacteria Bacillus vireti 01 microencapsulated with G. folifera polysaccharide against freshwater prawn M. rosenbergii. Three different feeding trials were conducted for 15 days. The first group contained prawns fed with commercial diet. The second group was comprised of Aeromonas hydrophila challenged prawns fed with commercial feed. The third group consisted of A. hydrophila challenged prawns fed with microencapsulated probiotic-polysaccharide. Survival percentage was significantly decreased in prawns of group2 as compared to that of group1 and group3 prawns (p < 0.0001). The immunological parameters and antioxidant activities (p < 0.001) were found to be increased in group three prawns which were fed with encapsulated probiotic-seaweed polysaccharide and challenged with A. hydrophila as compared to that of group1 and group2. Tissue necrosis, fused lamella, haemocyte infiltration and damage of hepatopancreas lumen and tubule were noted in group2 prawns. There was no histological changes were observed in group3 prawns in which the histological architecture was similar to the control group1. The results suggested that combination of encapsulated probiotic B. vireti 01 and seaweed polysaccharide as dietary feed showed an enhancement of immune response, antioxidant activity and disease resistant of M. rosenbergii against A. hydrophila.


Assuntos
Alginatos/farmacologia , Bacillus/química , Quitosana/farmacologia , Doenças dos Peixes/imunologia , Gracilaria/química , Palaemonidae/imunologia , Probióticos/farmacologia , Aeromonas hydrophila/fisiologia , Alginatos/administração & dosagem , Animais , Antioxidantes/metabolismo , Quitosana/administração & dosagem , Resistência à Doença/efeitos dos fármacos , Composição de Medicamentos/veterinária , Ácido Glucurônico/administração & dosagem , Ácido Glucurônico/farmacologia , Infecções por Bactérias Gram-Negativas/imunologia , Ácidos Hexurônicos/administração & dosagem , Ácidos Hexurônicos/farmacologia , Imunidade Inata/efeitos dos fármacos , Palaemonidae/efeitos dos fármacos , Extratos Vegetais/administração & dosagem , Extratos Vegetais/farmacologia , Polissacarídeos/administração & dosagem , Polissacarídeos/farmacologia , Probióticos/administração & dosagem
20.
J Vet Intern Med ; 32(1): 469-473, 2018 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-29114956

RESUMO

BACKGROUND: Periodic lack of availability and high cost of commercially produced isotonic fluids for intravenous (IV) use in horses have increasingly led to use of home-made or commercially compound fluids by veterinarians. Data regarding the quality control and safety of compounded fluids would be of benefit to equine veterinarians. OBJECTIVES: To compare electrolyte concentrations, sterility, and endotoxin contamination of commercially available fluids to 2 forms of compounded isotonic crystalloid fluids intended for IV use in horses. METHODS: Prospective study. Two methods of preparing compounded crystalloids formulated to replicate commercial Plasma-Lyte A (Abbott, Chicago, IL) were compared. One formulation was prepared by a hand-mixed method involving chlorinated drinking water commonly employed by equine practitioners, and the other was prepared by means of ingredients obtained from a commercial compounding pharmacy. The variables for comparison were electrolyte concentrations, sterility, and presence of endotoxin contamination. RESULTS: Electrolyte concentrations were consistent within each product but different between types of fluids (P < 0.0001). Hand-mixed fluids had significantly more bacterial contamination compared to commercial Plasma-Lyte A (P = 0.0014). One of the hand-mixed fluid samples had detectable endotoxin contamination. CONCLUSIONS AND CLINICAL IMPORTANCE: Chlorinated drinking water is not an acceptable source of water to compound isotonic fluids for IV administration. Equine practitioners should be aware of this risk and obtain the informed consent of their clients.


Assuntos
Composição de Medicamentos/veterinária , Eletrólitos/normas , Cavalos , Infusões Intravenosas/veterinária , Soluções Isotônicas/farmacologia , Controle de Qualidade , Animais , Soluções Cristaloides , Composição de Medicamentos/métodos , Contaminação de Medicamentos , Endotoxinas/análise , Infusões Intravenosas/normas , Soluções Isotônicas/química , Água/química
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