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1.
Postgrad Med ; 132(1): 28-36, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31900074

RESUMO

Interest in and use of topical analgesics has been increasing, presumably due to their potential utility for relief of acute and chronic pain. Topically applied agents with analgesic properties can target peripheral nociceptive pathways while minimizing absorption into the plasma that leads to potential systemic adverse effects.Clinical trials have found 5% lidocaine patches to be effective and well tolerated for the treatment of post-herpetic neuralgia (PHN) with a minimal risk of toxicity or drug-drug interactions. With this patch formulation, the penetration of lidocaine into the skin produces an analgesic effect without producing a complete sensory block. Use of topical lidocaine is supported by clinical practice guidelines, including first-line treatment by the American Academy of Neurology (guidelines retired 2018), the European Federation of Neurological Societies and second-line by the Canadian Pain Society.FDA approved 5% lidocaine patches in 1999, and a 1.8% topical lidocaine system in 2018 - both indicated for the treatment of pain secondary to PHN. The 1.8% system offers a more efficient delivery of lidocaine that is bioequivalent to 5% lidocaine patches, but with a 19-fold decrease in drug load (i.e., 36 mg versus 700 mg) as well as superior adhesion that allows the patch to maintain contact with the skin during the 12-h administration period.Although topical lidocaine formulations have advanced over time and play an important role in the treatment of PHN, a variety of other conditions that respond to topical lidocaine have been reported in the literature including PHN, lower back pain, carpal tunnel syndrome, diabetic peripheral neuropathy, and osteoarthritis joint pain. Other neuropathic or nociceptive pain syndromes may respond to topical lidocaine in select cases and warrant further study. Clinicians should consider local anesthetics and other topical agents as part of their multimodal treatments of acute and chronic pain.


Assuntos
Analgésicos/administração & dosagem , Lidocaína/administração & dosagem , Administração Cutânea , Analgésicos/uso terapêutico , Humanos , Lidocaína/uso terapêutico , Neuralgia/tratamento farmacológico , Adesivo Transdérmico
2.
AAPS PharmSciTech ; 20(8): 322, 2019 Oct 24.
Artigo em Inglês | MEDLINE | ID: mdl-31650263

RESUMO

The objectives of this work were to prepare a 5 wt% lidocaine-diclofenac ionic liquid drug-loaded gelatin/poly(vinyl alcohol) transdermal patch using a freeze/thaw method and to evaluate its physicochemical properties, in vitro release of lidocaine and diclofenac, and stability test. The lidocaine-diclofenac ionic liquid drug was produced by the ion pair reaction between the hydrochloride salts of lidocaine and the sodium salts of diclofenac. The thermal properties of the final drug product were significantly changed from the primary drugs. The ionic liquid drug could be dissolved in water and mixed in a polymer solution. The resulting transdermal patch was then exposed to 10 cycles of freezing and thawing preparation at - 20°C for 8 h and at 25°C for 4 h, respectively. As a result, it was found that the lidocaine-diclofenac ionic liquid drug-loaded transdermal patch showed good physicochemical properties and could feasibly be used in pharmaceutical applications. The lidocaine-diclofenac ionic liquid drug was not affected by the properties of the transdermal patch due to the lack of chemical interaction between polymer base and drug. The high drug release values of both lidocaine and diclofenac were controlled by the gelatin/poly(vinyl alcohol) transdermal patch. The patch showed good stability over the study period of 3 months when kept at 4°C or under ambient temperature.


Assuntos
Diclofenaco/farmacocinética , Gelatina/farmacocinética , Líquidos Iônicos/farmacocinética , Lidocaína/farmacocinética , Álcool de Polivinil/farmacocinética , Adesivo Transdérmico , Administração Cutânea , Anestésicos Locais/química , Anestésicos Locais/farmacocinética , Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/farmacocinética , Preparações de Ação Retardada/química , Preparações de Ação Retardada/farmacocinética , Diclofenaco/química , Combinação de Medicamentos , Liberação Controlada de Fármacos , Congelamento , Gelatina/química , Líquidos Iônicos/química , Lidocaína/química , Álcool de Polivinil/química
3.
Ned Tijdschr Geneeskd ; 1632019 09 16.
Artigo em Holandês | MEDLINE | ID: mdl-31556491

RESUMO

The most common side effects of transdermal patches are mechanical reactions caused by applying or removing the transdermal patch, or by excessive perspiration under the patch. Allergic contact dermatitis (type IV allergic reaction) is the most commonly occurring hypersensitivity reaction and can be caused by the active substance or by excipients. Type I allergic reactions such as urticaria, bronchospasm and angioedema are rare and usually caused by the active substance in the patch. Allergy testing to determine the allergen is indicated following a type I allergic reaction, or after a type IV allergic reaction that requires an alternative for the patch. It is important to document hypersensitivity reactions in the electronic patient records in order to prevent a hypersensitivity reaction in the future.


Assuntos
Dermatite Alérgica de Contato/etiologia , Excipientes/efeitos adversos , Adesivo Transdérmico/efeitos adversos , Angioedema/etiologia , Dermatite Alérgica de Contato/diagnóstico , Feminino , Humanos , Masculino , Testes Cutâneos , Urticária/etiologia
4.
Forensic Sci Int ; 302: 109896, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31426021

RESUMO

BACKGROUND: Interpretation of postmortem fentanyl concentrations after transdermal application remains a challenge. There are indications that fentanyl shows relevant postmortem redistribution. The aim of this study was to investigate the time course of these changes and to develop recommendations for toxicological case work. MATERIAL AND METHOD: Blood specimens were collected from palliative care patients who were treated with fentanyl transdermal patches. Antemortem reference samples (ethylenediaminetetraacetic acid (EDTA) and serum specimens) were collected at stable dose rates. Postmortem femoral venous blood specimens were collected at four postmortem time-points: 2hpm (hours postmortem), 6-8hpm, 11-16hpm and approximately 24hpm. Liquid chromatography tandem mass spectrometry was applied to quantify fentanyl and norfentanyl. RESULTS: Ten patients were included in the study (8 men, 2 women). Fentanyl patches with delivery rates of 12-150µg/h were applied. Antemortem fentanyl levels in EDTA samples varied between 0.19 and 4.64µg/L. At 6 to 8hpm, blood concentrations of fentanyl were already significantly (p=0.05) higher in postmortem samples compared to the paired antemortem reference. On average, the antemortem concentration (range: 0.19-4.64µg/L) increased 3-fold within 6-8hpm (range: 0.4-14.9µg/L), and 5.5-fold within 24hpm (range: 0.39-21.88µg/L). Norfentanyl concentrations increased significantly (p=0.01) within 6-8hpm, too. In half of the patients, norfentanyl concentrations were below fentanyl concentrations, antemortem as well as postmortem. CONCLUSION: Postmortem fentanyl concentrations increased quickly. As early as 6-8h after death, postmortem concentrations differ significantly from antemortem ones. Our results strongly indicate that postmortem blood concentrations of fentanyl after transdermal application should be interpreted carefully.


Assuntos
Analgésicos Opioides/sangue , Fentanila/sangue , Mudanças Depois da Morte , Adesivo Transdérmico , Idoso , Analgésicos Opioides/administração & dosagem , Cromatografia Líquida , Ácido Edético , Feminino , Fentanila/administração & dosagem , Fentanila/análogos & derivados , Toxicologia Forense , Humanos , Masculino , Pessoa de Meia-Idade , Espectrometria de Massas em Tandem
5.
J Forensic Sci ; 64(6): 1936-1942, 2019 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-31340064

RESUMO

Fentanyl transdermal patches have been used to treat cancer- and noncancer-related chronic pain. However, its inappropriate or illegal application may cause fatal poisoning. We herein present the case of a Japanese woman in her 40s who was found dead with seven 25-µg/h fentanyl transdermal patches on her body. We established a detailed toxicological analysis procedure to quantify fentanyl, and its metabolite norfentanyl, and other drugs (acetaminophen, allylisopropylacetylurea, celecoxib, estazolam, promethazine, and sertraline) in human whole blood by ultra-high-performance liquid chromatography-tandem mass spectrometry. The measured fentanyl and norfentanyl concentrations in the femoral and cardiac blood were 0.051 and 0.072 µg/mL and 0.033 and 0.076 µg/mL, respectively. The decedent's fentanyl concentrations were consistent with previously reported postmortem blood levels for fatal cases of poisoning by fentanyl transdermal patches. Based on the decedent's case history, autopsy findings, and toxicological analyses, the cause of death was identified as intoxication with transdermal fentanyl.


Assuntos
Analgésicos Opioides/envenenamento , Fentanila/envenenamento , Adesivo Transdérmico , Adulto , Analgésicos Opioides/sangue , Cromatografia Líquida de Alta Pressão , Feminino , Fentanila/sangue , Humanos , Japão , Uso Indevido de Medicamentos sob Prescrição , Espectrometria de Massas em Tandem
6.
J Opioid Manag ; 15(2): 147-158, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31343716

RESUMO

Transdermal buprenorphine (TDB) has demonstrated effectiveness in treating a range of chronic pain conditions, including cancer pain, nociceptive pain, and neuropathic pain and has a favorable safety profile. Worldwide, clinical experience of its use is relatively limited. There is considerable misunderstanding about the pharmacology, mechanism of action, and safety of buprenorphine. There is also limited guidance on the appropriate use of TDB for chronic pain management. This article presents an overview of TDB and also provides practical recommendations for its use as part of a multifaceted strategy in chronic cancer and non-cancer pain.


Assuntos
Analgésicos Opioides/administração & dosagem , Buprenorfina/administração & dosagem , Dor Crônica , Neoplasias/complicações , Analgésicos Opioides/uso terapêutico , Buprenorfina/uso terapêutico , Dor Crônica/tratamento farmacológico , Dor Crônica/etiologia , Humanos , Manejo da Dor , Medição da Dor , Adesivo Transdérmico
8.
Forensic Sci Int ; 302: 109858, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31279508

RESUMO

Fentanyl is a potent synthetic opioid with a variety of possible applications. Transdermal fentanyl patches are regularly prescribed for patients with severe chronic or cancer-related pain. The potential for abuse is well-known and cases associated with illicit fentanyl intake are common. Fentanyl related fatalities due to unintentional misuse are relatively rare. This study focused on those instances and their identification in forensic examinations and adds new cases and consolidates the existing femoral blood concentrations in the event of fatal fentanyl patch misapplications. A total of 35 cases between 2010 and 2018 in which transdermal fentanyl patches were detected during forensic autopsies were identified and reviewed for the frequency of unspecific macroscopic signs of opioid intoxication. Furthermore, a detailed examination is presented for 11 cases in which toxicological results were available. The cause of death was eventually considered to be related to fentanyl patch misuse in 5 of these 11 cases. Co-administered drugs and signs of opioid intoxication, especially pulmonary edema, were frequently found. Lastly, it is advised to include norfentanyl and hair analysis in the interpretation of post-mortem fentanyl concentrations.


Assuntos
Analgésicos Opioides/efeitos adversos , Fentanila/efeitos adversos , Transtornos Relacionados ao Uso de Opioides/complicações , Uso Indevido de Medicamentos sob Prescrição , Adesivo Transdérmico/efeitos adversos , Adolescente , Adulto , Idoso , Analgésicos Opioides/análise , Analgésicos Opioides/envenenamento , Cromatografia Líquida , Feminino , Fentanila/análogos & derivados , Fentanila/análise , Fentanila/envenenamento , Cabelo/química , Humanos , Masculino , Espectrometria de Massas , Edema Pulmonar/patologia , Estudos Retrospectivos , Retenção Urinária/patologia
9.
J Med Microbiol ; 68(9): 1314-1319, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31274404

RESUMO

Introduction. Current intradermal tuberculin skin tests for latent tuberculosis infection (LTBI) based on purified protein derivative (PPD) have poor specificity.Aims. Developing a better skin test antigen as well as a simple skin patch test may improve and facilitate diagnostic performance.Methodology. Defined recombinant antigens that were unique to Mycobacterium tuberculosis (MTB), including two potential latency-associated antigens (ESAT-6 and Rv2653c) and five DosR-encoded latency proteins (Rv1996, Rv2031c, Rv2032, DevR and Rv3716c), were used as diagnostic skin test reagents in comparison with a standard PPD. The performance of the skin tests based on the detection of delayed-type hypersensitivity (DTH) reaction in guinea pigs sensitized to MTB and M. bovis bacille Calmette-Guérin (BCG) vaccine was evaluated.Results. The latency antigens Rv1996, Rv2031c, Rv2032 and Rv2653c and the ESAT-6 protein elicited less reactive DTH skin responses in MTB-sensitized guinea pigs than those resulting from PPD, but elicited no response in BCG-vaccinated guinea pigs. The remaining two latency antigens (DevR and Rv3716c) elicited DTH responses in both groups of animals, as did PPD. The reactivity of PPD in BCG-vaccinated guinea pigs was greater than that of any of the selected skin test reagents. Using stronger concentrations of selected skin test reagents in the patch test led to increased DTH responses that were comparable to those elicited by PPD in guinea pigs sensitized with MTB.Conclusion. Transdermal application of defined purified antigens might be a promising method for LTBI screening.


Assuntos
Hipersensibilidade Tardia/imunologia , Tuberculose Latente/diagnóstico , Mycobacterium tuberculosis/imunologia , Testes Cutâneos/métodos , Adesivo Transdérmico , Animais , Antígenos de Bactérias/imunologia , Vacina BCG/imunologia , Feminino , Cobaias , Indicadores e Reagentes , Mycobacterium tuberculosis/isolamento & purificação , Testes Cutâneos/normas , Tuberculina/imunologia
10.
Int J Pharm ; 567: 118489, 2019 Aug 15.
Artigo em Inglês | MEDLINE | ID: mdl-31276760

RESUMO

This study systematically demonstrated the antigenicity kinetics of HBV vaccine microneedles (MNs) during the fabrication, application and storage. To improve the stability of HBsAg in a microneedle patch, several selected saccharides were added to the MN formulations as stabilizers. According to the experimental data, no significant decrease of the bio-activity of HBsAg antigen was found during the microneedle fabrication process. And then immune effects of HBsAg added with different sugars were tested. Chitosan and trehalose loaded HBsAg MNs enhanced the antibody levels to approximately 1.5-fold and 2-fold of the plain HBsAg MNs respectively while sucrose and glucose were not obviously beneficial. During the short-term storage under 60 °C, the antigenicity of HBsAg MNs encapsulated with glucose and chitosan declined sharply in 24 h and hardly left after 7 days. As for the groups of HBsAg MNs added with sucrose and trehalose, approximately 90% of HBsAg initial antigenicity maintained, which could be attributed to the protective function of non-reductive disaccharides. As for the long-term storage experiments, the pharmacological activity of HBsAg antigen protected by sucrose and trehalose slightly reduced in 3 months except for the samples under 60 °C. In extreme condition, trehalose performed even better protection function than sucrose, of which the antigenicity of HBsAg in MNs left approximately 81% and 63% of its initial, respectively. These results confirmed that trehalose loaded HBsAg MNs enabled stable encapsulation and storage of HBsAg antigen and realized reasonable enhancement of immune effect in a relatively painless, safe, and convenient manner.


Assuntos
Antígenos de Superfície da Hepatite B/administração & dosagem , Vacinas contra Hepatite B/administração & dosagem , Trealose/administração & dosagem , Animais , Quitosana/administração & dosagem , Estabilidade de Medicamentos , Feminino , Anticorpos Anti-Hepatite B/sangue , Cinética , Camundongos Endogâmicos BALB C , Microinjeções , Agulhas , Sacarose/administração & dosagem , Adesivo Transdérmico
11.
Int J Biol Macromol ; 138: 704-717, 2019 Oct 01.
Artigo em Inglês | MEDLINE | ID: mdl-31344412

RESUMO

Wound healing is a complex multistep process. Wound healing materials should have good antibacterial activity against wound infection causing microbes. Curcumin has effective antimicrobial activity, anti-inflammatory and antioxidant property. Titanium dioxide (TiO2) is a biocompatible, nontoxic material used for many biomedical applications. The Usage of curcumin tagged TiO2 nanoparticles for wound healing activity is promising due to the properties of both curcumin and TiO2. We have synthesized curcumin tagged TiO2 nanoparticles. The synthesized materials are characterized with XRD, FTIR and TEM. TiO2-Cur nanocomposite was incorporated into poly vinyl alcohol (PVA) and sodium alginate (SA) patch. The PVA/SA/TiO2-Cur patch was prepared by gel casting method. Antibacterial efficiency of PVA/SA/TiO2-Cur patch was analyzed. Further, in vivo studies conducted on Wister rats confirmed the enhanced wound healing property of the PVA/SA/TiO2-Cur patch. Our results suggest that this could be an ideal biomaterial for wound dressing applications.


Assuntos
Alginatos , Materiais Biocompatíveis/química , Curcumina , Álcool de Polivinil , Titânio , Adesivo Transdérmico , Cicatrização , Alginatos/química , Animais , Antibacterianos/química , Antibacterianos/farmacologia , Linhagem Celular , Fenômenos Químicos , Curcumina/química , Fenômenos Mecânicos , Camundongos , Nanocompostos/química , Nanopartículas/química , Álcool de Polivinil/química , Ratos , Pele/metabolismo , Pele/patologia , Pele/ultraestrutura , Análise Espectral , Titânio/química
12.
Acta Pharm ; 69(2): 197-215, 2019 Jun 01.
Artigo em Inglês | MEDLINE | ID: mdl-31259729

RESUMO

Use of transdermal patches can evade many issues associated with oral drug delivery, such as first-pass hepatic metabolism, enzymatic digestion attack, drug hydrolysis and degradation in acidic media, drug fluctuations, and gastrointestinal irritation. This article reviews various transdermal patches available in the market, types, structural components, polymer role, and the required assessment tools. Although transdermal patches have medical applications for smoking cessation, pain relief, osteoporosis, contraception, motion sickness, angina pectoris, and cardiac disorders, advances in formulation development are ongoing to make transdermal patches capable of delivering more challenging drugs. Transdermal patches can be tailored and developed according to the physicochemical properties of active and inactive components, and applicability for long-term use. Therefore, a number of chemical approaches and physical techniques for transdermal patch development are under investigation.


Assuntos
Sistemas de Liberação de Medicamentos , Preparações Farmacêuticas/administração & dosagem , Adesivo Transdérmico , Administração Cutânea , Desenho de Drogas , Desenvolvimento de Medicamentos , Humanos , Preparações Farmacêuticas/química
13.
Adv Mater ; 31(30): e1901051, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-31165524

RESUMO

Insulin-dependent patients with diabetes mellitus require multiple daily injections of exogenous insulin to combat hyperglycemia. However, administration of excess insulin can lead to hypoglycemia, a life-threatening condition characterized by abnormally low blood glucose levels (BGLs). To prevent hypoglycemia associated with intensive insulin therapy, a "smart" composite microneedle (cMN) patch is developed, which releases native glucagon at low glucose levels. The cMN patch is composed of a photo-crosslinked methacrylated hyaluronic acid (MeHA) microneedle array with embedded multifunctional microgels. The microgels incorporate zwitterionic moieties that stabilize loaded glucagon and phenylboronic acid moieties that provide glucose-dependent volume change to facilitate glucagon release. Hypoglycemia-triggered release of structurally unchanged glucagon from the cMN patch is demonstrated in vitro and in a rat model of type 1 diabetes (T1D). Transdermal application of the patch prevented insulin-induced hypoglycemia in the diabetic rats. This work is the first demonstration of a glucose-responsive glucagon-delivery MN patch for the prevention of hypoglycemia, which has a tremendous potential to reduce the dangers of intensive insulin therapy and improve the quality of life of patients with diabetes and their caregivers.


Assuntos
Glicemia/metabolismo , Glucagon/administração & dosagem , Hipoglicemia/tratamento farmacológico , Agulhas , Animais , Reagentes para Ligações Cruzadas/química , Diabetes Mellitus Experimental/tratamento farmacológico , Diabetes Mellitus Experimental/metabolismo , Diabetes Mellitus Tipo 1/tratamento farmacológico , Diabetes Mellitus Tipo 1/metabolismo , Liberação Controlada de Fármacos , Géis , Humanos , Ácido Hialurônico/análogos & derivados , Ácido Hialurônico/química , Hipoglicemia/induzido quimicamente , Hipoglicemiantes/efeitos adversos , Insulina/efeitos adversos , Metacrilatos/química , Processos Fotoquímicos , Polimerização , Ratos , Adesivo Transdérmico
14.
Curr Pain Headache Rep ; 23(7): 50, 2019 Jun 21.
Artigo em Inglês | MEDLINE | ID: mdl-31227918

RESUMO

PURPOSE OF REVIEW: The administration of a transdermal fentanyl patch can be complicated with different pharmacokinetics than other fentanyl preparations. RECENT FINDINGS: The medical condition and baseline opioid requirements must all be carefully considered when dosing a fentanyl patch. An advantage of the fentanyl patch is its ability to bypass the gastrointestinal tract and in many patients, provide effective analgesia with minimal side effects. Fentanyl patches must be carefully administered since morbidity and/or mortality can result from the following: Giving higher doses than a patient needs, combining the medication with potent sedatives, or heating a fentanyl patch. The use of a transdermal fentanyl patch for the treatment of acute postoperative pain is not recommended and any patient undergoing a surgical procedure should have the fentanyl patch removed preoperatively. The current manuscript discusses the history of fentanyl and the fentanyl patch, as well as perioperative considerations, contraindications, current clinical efficacy, and clinical adversities related to the transdermal fentanyl patch. Regarding the heating of a transdermal fentanyl patch, which significantly increases blood levels of fentanyl, it is of the utmost importance that the patch be removed prior to surgery.


Assuntos
Analgésicos Opioides/administração & dosagem , Consenso , Fentanila/administração & dosagem , Dor Pós-Operatória/cirurgia , Adesivo Transdérmico , Analgésicos Opioides/uso terapêutico , Fentanila/uso terapêutico , Humanos , Morfina/uso terapêutico , Medição da Dor , Adesivo Transdérmico/efeitos adversos , Resultado do Tratamento
15.
Eur J Contracept Reprod Health Care ; 24(3): 209-215, 2019 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-31066303

RESUMO

Purpose: Prior studies evaluating the effect of administered progestogens on peak cervical mucus have not controlled for the influence of endogenous hormones. To address this, we treated women with a gonadotropin-releasing hormone (GnRH) agonist to suppress the hypothalamus-pituitary-ovarian (HPO) axis and used transdermal oestradiol replacement to stimulate peak cervical mucus and then evaluated the effects of an oral progestin or oestradiol withdrawal. Materials and methods: We used a crossover design to examine cervical mucus changes in women receiving transdermal oestradiol replacement following intramuscular administration of leuprolide acetate. After increasing oestradiol patches to mid-cycle levels, subjects were assigned to either 0.35 mg oral norethindrone with continuation of the patches (NET) or oestradiol withdrawal by patch removal (E2WD). We collected serum and cervical mucus samples at 0, 2, 4, 6, 22 and 24 h following the intervention. Results: We analysed 12 cycles (6 NET, 6 E2WD) from three subjects. Baseline cervical mucus scores were favourable to sperm penetration [NET median 11, interquartile range (9-12), E2WD 13 (12-13)]. Two hours after removal of oestradiol patch or administration of norethindrone, cervical mucus scores declined [NET 8.5 (4-9), E2WD 10.5 (10-12)]. Low cervical mucus scores persisted at 24 h with NET [8.0 (7-8)] but not E2WD [10.5 (8-11)]. Conclusions: We observed a rapid decline in cervical mucus Insler scores following administration of a single dose of oral norethindrone, and scores remained lower and unfavourable through 24 h. Oestradiol withdrawal did not result in similar unfavourable changes.


Assuntos
Muco do Colo Uterino/efeitos dos fármacos , Colo do Útero , Anticoncepcionais Orais Hormonais/farmacologia , Estradiol/farmacologia , Leuprolida/farmacologia , Progestinas/farmacologia , Adulto , Estudos Cross-Over , Estradiol/administração & dosagem , Estradiol/sangue , Feminino , Fármacos para a Fertilidade Feminina/farmacologia , Humanos , Muco , Noretindrona/sangue , Noretindrona/farmacologia , Projetos Piloto , Progesterona/sangue , Adesivo Transdérmico , Adulto Jovem
16.
Biomed Res Int ; 2019: 9346567, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31073531

RESUMO

Background: Repairs of large to massive rotator cuff tears have a high failure rate. We investigated the efficacy of a novel, reinforced, low immunogenic, porcine small intestine submucosa (SIS) patch to repair a supraspinatus tendon defect in a rabbit model. We hypothesized that the histological and biomechanical results of SIS patch repair would be comparable with those of autologous fascia lata (FL) repair. Methods: The study mainly comprised two parts. First, the characteristics of the SIS patch were evaluated, including its micromorphology, mechanical properties, and immunogenic properties. Second, a supraspinatus tendon defect model was created in 36 rabbits (72 shoulders). The bilateral shoulders were randomly chosen to undergo repair using either a SIS patch (SIS group) or autologous FL (FL group). At 4, 8, and 12 weeks, histological analysis was performed using four shoulders from each group, and biomechanical tests were performed using eight shoulders from each group. Results: The SIS patch was a three-dimensional construct mainly composed of collagen fibers. The mean single and double suture retention loads of the SIS patch were 48.6 ± 5.8 N and 117.9 ± 2.7 N, respectively. The DNA content in the SIS patch was 53.9 ± 10.9 ng/mg dry weight. Both the histological score and ultimate load to failure increased in a time-dependent manner in both groups, with no significant differences between the SIS and FL groups at 12 weeks. Conclusion: Repair of a large supraspinatus tendon defect using a reinforced, low immunogenic, SIS patch achieves similar effects as autologous FL in a rabbit model. This novel patch might be useful to be employed as a structural tissue replacement in medical activities.


Assuntos
Mucosa Intestinal/ultraestrutura , Intestino Delgado/ultraestrutura , Lesões do Manguito Rotador/terapia , Traumatismos dos Tendões/terapia , Animais , Tecido Conjuntivo/transplante , Modelos Animais de Doenças , Humanos , Mucosa Intestinal/química , Intestino Delgado/química , Coelhos , Manguito Rotador/fisiopatologia , Lesões do Manguito Rotador/fisiopatologia , Articulação do Ombro/crescimento & desenvolvimento , Articulação do Ombro/lesões , Suínos , Traumatismos dos Tendões/fisiopatologia , Adesivo Transdérmico , Cicatrização
17.
AAPS PharmSciTech ; 20(5): 174, 2019 Apr 25.
Artigo em Inglês | MEDLINE | ID: mdl-31028490

RESUMO

Chemical penetration enhancers are widely used in transdermal drug delivery system. However, few studies have focused on changes of concentration in chemical penetration enhancers. In this study, the effect of concentrations of enhancers on drug release and its mechanism were investigated. Zolmitriptan (ZOL) was used as a model drug and isopropyl palmitate (IPP) was used as a model enhancer to investigate drug release behaviors in pressure-sensitive adhesives (PSAs). The IPP concentrations were 2, 5, 10, 12, and 15%. Drug release percents increased by 4.8, 11.5, 16, 15.1, and 14.8%, respectively. Interestingly, the linear relationship between concentrations of IPP and release percents was improved in the 0-10% and remained unchanged in the 10-15%. Moreover, thermal and rheology studies were performed to investigate changes of the fluidity of PSAs. FT-IR and molecular dynamics simulation were conducted to confirm the interaction strength among ZOL, IPP, and PSAs. The results elucidated that IPP increased fluidity of PSAs and vied for drug from PSAs. As a result, the interaction among three components played a major role in changing release behaviors of ZOL, but the increased fluidity only worked in the concentration of less than 10%.


Assuntos
Liberação Controlada de Fármacos , Palmitatos/química , Adesivo Transdérmico , Adesivos , Administração Cutânea , Animais , Sistemas de Liberação de Medicamentos , Masculino , Simulação de Dinâmica Molecular , Oxazolidinonas/administração & dosagem , Oxazolidinonas/química , Palmitatos/farmacologia , Ratos , Absorção Cutânea/efeitos dos fármacos , Triptaminas/administração & dosagem , Triptaminas/química
18.
Acta Biochim Pol ; 66(2): 167-172, 2019 Apr 15.
Artigo em Inglês | MEDLINE | ID: mdl-30986279

RESUMO

The present clinical trial investigates the sustaining anesthetic effect of Ropivacaine when administered as epidural injection followed by transdermal patch with and without Reverse electrodialysis (RED) system in order to maintain anesthesia in children. It also focuses on rate of release of drug in-vitro when administered with RED system. The transdermal patch of Ropivacaine was prepared using evaporation technique enclosing 25 mg of Local anesthetic Ropivacaine. Thus prepared patches were evaluated for physical parameters like folding endurance, tensile strength, in vitro drug release etc. The thicknesses of the patches were in the range of 0.02 ±0.006 to 0.04 ± 0.007 mm with 95.79 ±1.85 to 97.45±0.07 % drug content. The average weight and tensile strength was found to be 0.15±0.2 to 0.17±0.18 gm and 0.42±0.006 to 0.58±0.002 kg/cm2. The folding endurance of the patches was in range of 155.21 ±0.2 to 167± 0.29 and content of moisture was 1.43±0.23 % to 2.97±0.23 %. The formulation shows In - vitro release in Phosphate buffer pH 7.4 as 55.56 % to 89.23 ± 0.24 % in 24 hr with reverse electrodialysis system attached and 43.76 % to 81.23 ± 0.14 % in 24 hr without reverse electrodialysis system. The children of different age groups, different body weight with no premedication of anesthetic of analgesic were selected as subjects with written informed consent and divided into two groups depending upon RED system to be attached or not. The patches with and without RED system were attached to forearm of subjects and trial is run. The results obtained showed that patch when attached with reverse electrodialysis system showed greater potential for thermal threshold, lowering of cool sensation and depth of pain. Keywords: Child Anesthesia, Iontophoresis, Reverse Electrodialysis ,Ropivacaine, Transdermal Patch.


Assuntos
Anestésicos Locais/uso terapêutico , Sistemas de Liberação de Medicamentos/métodos , Iontoforese/métodos , Dor/tratamento farmacológico , Ropivacaina/uso terapêutico , Adesivo Transdérmico , Administração Cutânea , Anestésicos Locais/administração & dosagem , Animais , Criança , Pré-Escolar , Diálise/métodos , Composição de Medicamentos , Liberação Controlada de Fármacos , Feminino , Humanos , Masculino , Ropivacaina/administração & dosagem , Pele/efeitos dos fármacos , Suínos , Resultado do Tratamento
20.
Int J Pharm ; 564: 485-491, 2019 Jun 10.
Artigo em Inglês | MEDLINE | ID: mdl-31026490

RESUMO

The use of opioids for treating acute and chronic pain condition is a common clinical practice. When delivered systemically, the analgesic activity is mediated through the central pathway, which although effective, leads to various adverse effects such as dependence, abuse and respiratory depression. Fentanyl is an opioid analgesic that is available as injection and transdermal patch products for the management of acute and chronic pain. These products require stringent regulatory controls and label warnings on disposal due to the abuse potential associated. This research project evaluated the regional antinociceptive efficacy of fentanyl delivered from soluble microneedles. The microneedle patches were formulated with relatively less drug loading as compared to patches intended for systemic delivery and were tested for their antinociceptive activity in rats by measuring the paw withdrawal latency when exposed to a thermal stimulus. The results indicate that regional delivery of fentanyl mediated through soluble microneedles provides an effective antinociceptive activity. The onset of analgesic activity was faster with microneedle patch (0.5 h) when compared to the adhesive dermal patch (6 h). This study thus demonstrates the effectiveness of microneedle mediated pain management for immediate pain relief.


Assuntos
Analgésicos Opioides/administração & dosagem , Fentanila/administração & dosagem , Microinjeções , Agulhas , Dor/tratamento farmacológico , Adesivo Transdérmico , Analgésicos Opioides/química , Animais , Liberação Controlada de Fármacos , Fentanila/química , Masculino , Ratos Sprague-Dawley , Pele/metabolismo
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