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1.
J Am Vet Med Assoc ; 262(8): 1-7, 2024 Aug 01.
Artículo en Inglés | MEDLINE | ID: mdl-38503053

RESUMEN

OBJECTIVE: To describe the effect of different substance combinations administered through mesotherapy in dogs with hip osteoarthritis. ANIMALS: 104 dogs. METHODS: In this retrospective study, 4 groups (dogs treated with a combination of lidocaine, piroxicam, and thiocolchicoside [MG]; dogs treated with lidocaine, piroxicam, and Traumeel [TG]; dogs treated with lidocaine, piroxicam, and glucosamine [GG]; and dogs treated with the same combination as in MG combined with a photobiomodulation session [MPG]) were set. For all groups, the same treatment frequency was followed. Response to treatment was measured with the Canine Brief Pain Inventory (divided into pain interference score and pain severity score), Liverpool Osteoarthritis in Dogs (LOAD), and Canine Orthopedic Index (divided into function, gait, stiffness, and quality of life) before treatment and 15, 30, 60, 90, and 120 days after treatment. Cox proportional hazard regression analysis was used to investigate the influence of treatment, age, sex, body weight, breed, and Orthopedic Foundation for Animals score. RESULTS: Dogs had a mean age of 7.6 ± 3.1 years and body weight of 28.6 ± 5.5 kg. Hip osteoarthritis was classified as mild (4), moderate (70), or severe (30). Greater improvements were observed in MG and MPG. Kaplan-Meier estimators showed MG and MPG had longer periods with clinically significant results. Treatment was the covariable that contributed more frequently to the outcomes observed. CLINICAL RELEVANCE: The combination used in MG, particularly combined with photobiomodulation, produced longer-lasting clinically significant results.


Asunto(s)
Enfermedades de los Perros , Mesoterapia , Piroxicam , Animales , Perros , Enfermedades de los Perros/tratamiento farmacológico , Enfermedades de los Perros/terapia , Estudios Retrospectivos , Masculino , Femenino , Piroxicam/uso terapéutico , Piroxicam/administración & dosificación , Piroxicam/análogos & derivados , Mesoterapia/veterinaria , Colchicina/uso terapéutico , Colchicina/administración & dosificación , Lidocaína/uso terapéutico , Lidocaína/administración & dosificación , Quimioterapia Combinada/veterinaria , Osteoartritis/veterinaria , Osteoartritis/tratamiento farmacológico , Glucosamina/uso terapéutico , Glucosamina/administración & dosificación , Extractos Vegetales/uso terapéutico , Extractos Vegetales/administración & dosificación , Osteoartritis de la Cadera/veterinaria , Osteoartritis de la Cadera/tratamiento farmacológico , Antiinflamatorios no Esteroideos/uso terapéutico , Antiinflamatorios no Esteroideos/administración & dosificación , Terapia por Luz de Baja Intensidad/veterinaria
2.
AAPS PharmSciTech ; 25(1): 18, 2024 Jan 23.
Artículo en Inglés | MEDLINE | ID: mdl-38263347

RESUMEN

Due to tenoxicam (TX)'s poor aqueous solubility (0.072 mg/ml), it is poorly absorbable in the GIT, and the long-term oral administration of TX may cause severe GIT disturbances. Topical administration of TX can help in bypassing the GIT adverse effects. Therefore, in the present work, we constructed different pluronic/lecithin organogels (PLOs) for topical delivery of TX. PLO was constructed simply via direct mixing of an aqueous pluronic solution with lecithin solution. The prepared PLO formulations were characterized for their physicochemical properties including pH, drug content, visual inspection, viscosity, and spreadability. Also, the in vitro release and kinetic studies were carried out to investigate the mechanism of drug release. Moreover, the in vivo studies were carried out by investigating the anti-inflammatory and analgesic activities using albino male rats. The results showed that the modified PLOs have good physicochemical properties. The viscosity of the modified gels is a direct proportionality with both lecithin and pluronic concentrations. Also, subsequently, the drug release rate is directly proportional to gel viscosity. Moreover, the in vivo studies showed that the modified PLOs (F19) showed a significant ( < 0.05%) paw edema inhibition and pain analgesia compared with other investigated groups. Also, the results indicated that the increase in dose is accompanied by higher activity and a longer duration of action which extended to 12 h. Hence, the modified PLOs are promising safe candidates or vehicles for effective TX loading with sustained delivery behavior.


Asunto(s)
Lecitinas , Piroxicam/análogos & derivados , Poloxámero , Animales , Ratas , Cinética , Inflamación , Dolor
3.
Biomed Res Int ; 2022: 1546734, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-35958816

RESUMEN

Lornoxicam is a potent oxicam-class nonsteroidal anti-inflammatory drug (NSAID) with analgesic, anti-inflammatory, and antipyretic effects. Its impacts on many biological functions are not fully understood. We measured various biomarkers in male albino rats provided an oral aqueous ginger extract before IM administration of therapeutic and 2× the therapeutic doses of lornoxicam. The aqueous ginger plant extract was characterized by mass spectroscopy, and its effects were determined by examining free radical scavenging activity, blood parameters, renal and hepatic function, semen quality, proinflammatory cytokines, antioxidant markers, and histopathology. Rats administered lornoxicam had significantly higher liver and kidney function biomarker values, TNF-α, interleukin-6, and sperm abnormalities than the control rats. The overall erythrocyte count, packed cell volume, prostaglandin, and sperm counts were all considerably lower in the experimental animals. Histological changes were found in the liver, spleen, and testes of rats administered lornoxicam alone. In rats, pretreatment with ginger extract reduced the majority of the negative effects of conventional and high dosages of lornoxicam.


Asunto(s)
Antiinflamatorios , Rizoma , Zingiber officinale , Animales , Masculino , Antiinflamatorios/efectos adversos , Antiinflamatorios/farmacología , Zingiber officinale/química , Piroxicam/análogos & derivados , Extractos Vegetales/farmacología , Plantas Medicinales/química , Rizoma/química , Análisis de Semen , Ratas
4.
Am J Emerg Med ; 38(7): 1431-1435, 2020 07.
Artículo en Inglés | MEDLINE | ID: mdl-31859197

RESUMEN

INTRODUCTION: Musculoskeletal pain such as low back pain (LBP) are routinely encountered in the ED and contribute to ED overcrowding. The aim of our study was to compare the efficiency of mesotherapy with systemic therapy in pain control in patients with lumbar disk herniation. METHODS: We conducted this prospective parallel randomized controlled trial with the patients admitted to the emergency department with low back pain related to herniated lumbar disk. Mesotherapy was performed to one group, while intravenous dexketoprofen was administered to the control group. Changes in pain intensity at 15th minute, 30th minute, 60th minute and 24th hours after treatment using Visual Analogue Scale (VAS), need to use analgesic drug within 24 h after treatment, and adverse effect of the treatment methods were compared between groups. RESULTS: The decreases in pain intensity were statistically significantly higher in mesotherapy group for all time intervals. The need to use analgesics was statistically significantly three fold higher in the systemic therapy group. There was no statistically significant difference in having any adverse effect between study groups during one-week follow-up period. CONCLUSIONS: Changes in medical practices, from the systemic administration of NSAIDs to the minimally invasive techniques such as mesotherapy with potent efficacy and minimal side effects, may enhance the ability of EDs to meet the waiting time targets and improve patient's satisfaction.


Asunto(s)
Anestésicos Locales/uso terapéutico , Antiinflamatorios no Esteroideos/uso terapéutico , Dolor de la Región Lumbar/terapia , Mesoterapia , Adulto , Colchicina/análogos & derivados , Colchicina/uso terapéutico , Servicio de Urgencia en Hospital , Femenino , Humanos , Desplazamiento del Disco Intervertebral/complicaciones , Cetoprofeno/uso terapéutico , Lidocaína/uso terapéutico , Dolor de la Región Lumbar/etiología , Masculino , Persona de Mediana Edad , Piroxicam/análogos & derivados , Piroxicam/uso terapéutico , Estudios Prospectivos , Escala Visual Analógica
6.
Am J Emerg Med ; 37(11): 2061-2065, 2019 11.
Artículo en Inglés | MEDLINE | ID: mdl-30876777

RESUMEN

INTRODUCTION: Acute musculoskeletal injuries are one of the most common painful presentation when admission to the emergency department. The aim of the study is to compare the tenoxicam mesotherapy with intravenous dexketoprofen in pain control in patients with acute musculoskeletal injury. METHODS: This parallel randomized controlled trial was conducted with the patients admitted to the emergency department with musculoskeletal injury. Intravenous dexketoprofen was administered to the control group, and mesotherapy treatment was performed to the other group. Differences between 10th, 30th, 60th and 120th minutes VAS scores and on the admission VAS score, clinically meaningful change in pain intensity, and adverse effect of the procedures were compared among groups. THE RESULTS: The differences in VAS scores and the presence of clinically meaningful change in pain intensity were statistically significantly higher in mesotherapy group than the systemic therapy group in all time periods. During one-week follow-up period, there was no reported adverse effect neither in mesotherapy group nor in the systemic therapy group. CONCLUSIONS: The mesotherapy treatment may be superior than the systemic therapy for pain relief in musculoskeletal injury in short term follow-up in emergency department settings.


Asunto(s)
Antiinflamatorios no Esteroideos/administración & dosificación , Cetoprofeno/análogos & derivados , Mesoterapia , Dolor Musculoesquelético/tratamiento farmacológico , Piroxicam/análogos & derivados , Trometamina/administración & dosificación , Adolescente , Adulto , Anciano , Anciano de 80 o más Años , Antiinflamatorios no Esteroideos/uso terapéutico , Servicio de Urgencia en Hospital , Femenino , Estudios de Seguimiento , Humanos , Inyecciones Intravenosas , Cetoprofeno/administración & dosificación , Cetoprofeno/uso terapéutico , Masculino , Persona de Mediana Edad , Piroxicam/administración & dosificación , Piroxicam/uso terapéutico , Estudios Prospectivos , Resultado del Tratamiento , Trometamina/uso terapéutico , Adulto Joven
7.
Curr Drug Deliv ; 16(1): 66-78, 2019.
Artículo en Inglés | MEDLINE | ID: mdl-30264681

RESUMEN

OBJECTIVE: The focus of this study was to develop in situ injectable implants of Lornoxicam which could provide sustained drug release. METHODS: Biodegradable in situ injectable implants were prepared by polymer precipitation method using polylactide-co-glycolide (PLGA). An optimized formulation was obtained on the basis of drug entrapment efficiency, gelling behavior and in vitro drug release. The compatibility of the formulation ingredients were tested by Fourier transform infrared (FT-IR) spectroscopy, and differential scanning colorimetry (DSC). SEM study was performed to characterize in vivo behavior of in situ implant. Pharmacokinetic study and in vivo gelling study of the optimized formulation were performed on Sprague-Dawley rats. Stability testing of optimized formulation was also performed. RESULTS: The drug entrapment efficiency increased and burst release decreased with an increase in the polymer concentration. Sustained drug release was obtained up to five days. SEM photomicrographs indicated uniform gel formation. Chemical interaction between the components of the formulation was not observed by FT-IR and DSC study. Pharmacokinetic studies of the optimized formulation revealed that the maximum plasma concentration (Cmax), time to achieve Cmax (Tmax) and area under plasma concentration curve (AUC) were significantly higher than the marketed intramuscular injection of lornoxicam. Stability study of optimized batch showed no change in physical and chemical characteristics. CONCLUSION: Lornoxicam can be successfully formulated as in situ injectable implant that provides long-term management of inflammatory disorders with improved patient compliance.


Asunto(s)
Implantes Absorbibles , Antiinflamatorios no Esteroideos/farmacología , Artritis/terapia , Piroxicam/análogos & derivados , Animales , Antiinflamatorios no Esteroideos/química , Rastreo Diferencial de Calorimetría , Preparaciones de Acción Retardada/química , Preparaciones de Acción Retardada/farmacología , Composición de Medicamentos/métodos , Evaluación Preclínica de Medicamentos , Estabilidad de Medicamentos , Excipientes/química , Inyecciones Intraarticulares , Masculino , Microscopía Electrónica de Rastreo , Modelos Animales , Piroxicam/química , Piroxicam/farmacología , Copolímero de Ácido Poliláctico-Ácido Poliglicólico/química , Ratas , Ratas Sprague-Dawley , Espectroscopía Infrarroja por Transformada de Fourier
8.
Curr Drug Deliv ; 15(3): 424-435, 2018.
Artículo en Inglés | MEDLINE | ID: mdl-29219057

RESUMEN

BACKGROUND: Ethosomes, a novel type of percutaneous drug delivery carrier with a lipid bilayer structure, penetrate the skin barrier due to their deformability and malleability, and presence of ethanol that fluidizes lipids in the skin. In order to further enhance the delivery of drugs through the skin, penetration enhancers are widely used. OBJECTIVE: The objective of this work was to develop an optimized formulation of lornoxicam ethosomal gels, investigate skin permeability with the addition of penetration enhancers, and evaluate the invivo pharmacodynamics of these formulations. METHODS: Lornoxicam ethosomes were prepared by the ethanol injection method and optimized using the orthogonal design method. Lornoxicam ethosomal gels with enhancers were prepared and optimized using in-vitro transdermal delivery experiments. Experiments on lornoxicam ethosomal gels containing various enhancers such as azone, menthol, lauryl alcohol, and oleic acid were conducted using vertical Franz diffusion cells to measure the percutaneous permeability of the different formulations. Furthermore, the in-vivo analgesic effects of the optimized lornoxicam ethosomal gels were examined using the hot-plate and acetic acid-induced writhing tests. Anti-inflammatory activity was investigated using the dimethylbenzene-induced mouse ear swelling method. RESULTS: The results showed that compared to other formulations, the optimized lornoxicam ethosomal gels with 5 % menthol significantly increased transdermal penetration. Meanwhile, the optimized lornoxicam ethosomal gels showed remarkably anti-nociceptive and anti-inflammatory activity compared with the plain lornoxicam gels. CONCLUSION: These results suggest that the optimized ethosomal gel formulated in this study is a promising lornoxicam carrier in transdermal delivery systems to enhance anti-nociceptive and antiinflammatory efficiency.


Asunto(s)
Analgésicos/administración & dosificación , Antiinflamatorios no Esteroideos/administración & dosificación , Mentol/administración & dosificación , Piroxicam/análogos & derivados , Ácido Acético , Analgésicos/química , Analgésicos/farmacocinética , Analgésicos/uso terapéutico , Animales , Antiinflamatorios no Esteroideos/química , Antiinflamatorios no Esteroideos/farmacocinética , Antiinflamatorios no Esteroideos/uso terapéutico , Colesterol/química , Composición de Medicamentos , Sistemas de Liberación de Medicamentos , Edema/inducido químicamente , Edema/tratamiento farmacológico , Etanol/química , Femenino , Geles , Calor/efectos adversos , Lecitinas/química , Liposomas , Mentol/química , Mentol/farmacocinética , Mentol/uso terapéutico , Ratones Endogámicos BALB C , Dolor/tratamiento farmacológico , Dolor/etiología , Piroxicam/administración & dosificación , Piroxicam/química , Piroxicam/farmacocinética , Piroxicam/uso terapéutico , Absorción Cutánea , Xilenos
9.
Drug Deliv Transl Res ; 6(4): 342-53, 2016 08.
Artículo en Inglés | MEDLINE | ID: mdl-27371394

RESUMEN

The present study investigates the drug delivery potential of polymer lipid hybrid nanocomposites (Lecithmer®) composed of poly(D,L-lactide-co-glycolide (PLGA) and soya lecithin. Core-shell structure of Lecithmer was evident from cryo-TEM images. Daunorubicin (DNR) and lornoxicam (LNX)-incorporated Lecithmer nanocomposites were evaluated for anticancer and anti-inflammatory activity. DNR- and LNX-loaded Lecithmer had mean particle size of ∼335 and ∼282.7 nm, respectively. Lecithmer formulated with different cationic lipids resulted in lower particle size (∼120 nm) and positive zeta potential. Entrapment efficiency of DNR and LNX was 93.16 and 88.59 %, respectively. In vitro release of DNR from Lecithmer was slower compared to PLGA nanoparticles. DNR release from Lecithmer was significantly higher at pH 5.5 (80.96 %) as compared to pH 7.4 (55.95 %), providing advantage for selective tumor therapy. Similarly, sustained release of LNX (30 % in 10 h) was observed at pH 7.4. DNR in Lecithmer showed superior cytotoxicity on human erythroleukemic K562 cells. Pharmacokinetic study in Wistar rats with i.v. administered DNR-loaded Lecithmer showed higher volume of distribution, lower elimination rate constant, and longer half-life (81.68 L, 0.3535 h(-1), 1.96 h) as compared to DNR solution (57.46 L, 0.4237 h(-1), 1.635 h). Pharmacodynamic evaluation of orally administered LNX-loaded Lecithmer showed superior anti-inflammatory activity with maximum inhibition of 81.2 % vis-à-vis 53.57 % in case of LNX suspension. In light of these results, Lecithmer can be envisaged as a promising nanosystem for parenteral as well as oral drug delivery.


Asunto(s)
Daunorrubicina/farmacología , Lecitinas/farmacocinética , Nanocompuestos/química , Piroxicam/análogos & derivados , Poliésteres/farmacocinética , Animales , Supervivencia Celular/efectos de los fármacos , Células Cultivadas , Preparaciones de Acción Retardada/síntesis química , Preparaciones de Acción Retardada/farmacocinética , Preparaciones de Acción Retardada/farmacología , Sistemas de Liberación de Medicamentos , Liberación de Fármacos , Edema/prevención & control , Humanos , Ácido Láctico/química , Ácido Láctico/farmacocinética , Lecitinas/sangre , Lecitinas/química , Masculino , Nanocompuestos/ultraestructura , Piroxicam/farmacología , Ácido Poliglicólico/química , Ácido Poliglicólico/farmacocinética , Copolímero de Ácido Poliláctico-Ácido Poliglicólico , Ratas
10.
Drug Deliv Transl Res ; 6(5): 511-8, 2016 10.
Artículo en Inglés | MEDLINE | ID: mdl-27255375

RESUMEN

Proniosomes are the new generation provesicular drug delivery system of non-ionic surfactant, lecithin and cholesterol which upon reconstitution get converted into niosomes. The objective of current study was to develop stable and sustain transdermal delivery system for lornoxicam. Lornoxicam-loaded topically applied proniosomal gel was formulated, optimized, and evaluated with the aim to deliver drug transdermally. Lornoxicam-loaded proniosomal gels were prepared that contained Lutrol F68 and lecithin as surfactants, cholesterol as a stabilizer, and minimal amount of ethanol and trace water. The resultant lornoxicam-loaded proniosomal gel were assessed for stability and the proniosomes-derived niosomes were characterized for morphology, size, zeta potential, and entrapment efficiency, which revealed that they were suitable for skin application. The coacervation phase separation technique was used in formulation of lornoxicam proniosomal gel and the gel was further assessed for in vitro permeation of lornoxicam through the freshly excised rat skin and the cumulative permeation amount of lornoxicam from proniosome, all exhibited significant increase as compared to 1.0 % lornoxicam-loaded pure gel. The optimized F5 batch had shown maximum entrapment efficiency up to 66.98 %. It has shown sustained drug release for more than 24 h. The skin permeability of proniosomal gel was found to be 59.73 %. The SEM and zeta potential studies showed formation of good and stable vesicles. Thus, proniosomes proved to have better potential for transdermal delivery of lornoxicam over conventional gel formulations.


Asunto(s)
Sistemas de Liberación de Medicamentos/métodos , Liposomas/química , Piroxicam/análogos & derivados , Administración Cutánea , Animales , Colesterol/química , Liberación de Fármacos , Estabilidad de Medicamentos , Geles/química , Lecitinas/química , Liposomas/ultraestructura , Masculino , Tamaño de la Partícula , Piroxicam/administración & dosificación , Piroxicam/química , Piroxicam/farmacocinética , Polietilenglicoles/química , Ratas , Absorción Cutánea , Propiedades de Superficie
11.
J Oral Maxillofac Surg ; 74(10): 1946.e1-6, 2016 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-27311846

RESUMEN

PURPOSE: The aim of the present study was to compare the effects of daily single-dose use of flurbiprofen, diclofenac sodium, and tenoxicam on pain, swelling, and trismus that occur after surgical extraction of impacted wisdom teeth using local anesthesia. MATERIALS AND METHODS: The present study included 3 groups with 30 patients in each group. Those volunteering to participate in this double-blind randomized study (n = 90) were selected from a patient population with an indication for extraction of impacted wisdom teeth. Group 1 patients received 200 mg flurbiprofen, group 2 patients received 100 mg diclofenac sodium, and group 3 patients received 20 mg tenoxicam. All doses were once a day, starting preoperatively. Pain was evaluated postoperatively at 1, 2, 3, 6, 8, and 24 hours and at 2 and 7 days using a visual analog scale (VAS). For comparison with the preoperative measurements, the patients were invited to postoperative follow-up visits 2 and 7 days after extraction to evaluate for swelling and trismus. The statistical analysis was performed using descriptive statistics in SAS, version 9.4 (SAS Institute, Cary, NC), software. Statistical analysis of the pain, swelling, and trismus data was performed using the Kruskal-Wallis, Dunn, and Wilcoxon-Mann-Whitney U tests. The statistical level of significance was accepted at P = .05 and power of 0.80. RESULTS: Clinically, tenoxicam showed better analgesic and anti-inflammatory efficacy compared with diclofenac sodium and, in particular, flurbiprofen. Although the VAS scores in the evaluation of pain showed statistically significant differences at 2 days, no statistically significant difference was found for swelling and trismus. CONCLUSIONS: Our study evaluated the analgesic and anti-inflammatory effects with a daily single dose of flurbiprofen, diclofenac sodium, and tenoxicam. Daily 20 mg tenoxicam can be accepted as an adequate and safe option for patients after a surgical procedure.


Asunto(s)
Antiinflamatorios no Esteroideos/administración & dosificación , Diclofenaco/administración & dosificación , Edema/tratamiento farmacológico , Flurbiprofeno/administración & dosificación , Tercer Molar/cirugía , Dolor Postoperatorio/tratamiento farmacológico , Piroxicam/análogos & derivados , Diente Impactado/cirugía , Trismo/tratamiento farmacológico , Adolescente , Adulto , Anestesia Dental , Anestesia Local , Método Doble Ciego , Femenino , Humanos , Masculino , Dimensión del Dolor , Piroxicam/administración & dosificación , Resultado del Tratamiento
12.
Int Braz J Urol ; 41(4): 669-75, 2015.
Artículo en Inglés | MEDLINE | ID: mdl-26401858

RESUMEN

PURPOSE: We compared the effects of local levobupivacaine infiltration, intravenous paracetamol, intravenous lornoxicam treatments on postoperative analgesia in patients submitted to transperitoneal laparoscopic renal and adrenal surgery. MATERIALS AND METHODS: Sixty adult patients 26 and 70 years who underwent laparoscopic renal and adrenal surgery were randomized into three groups with 20 patients each: Group 1 received local 20 mL of levobupivacaine 0.25% infiltration to the trocar incisions before skin closure. In group 2, 1g paracetamol was given to the patients intravenously 30 minutes before extubation and 5 g paracetamol was given intravenously in the 24 postoperative period. In group 3, 8 mg lornoxicam i.v. was given 30 minutes before extubation and 8 mg lornoxicam i.v. was given in the 24 postoperative period. In the postoperative period, pain scores, cumulative tramadol, and additional pethidine consumption were evaluated. RESULTS: Postoperative pain scores significantly reduced in each group (p < 0.05). Although pain levels of the groups were not significantly different at 1, 2, 4, 8, 12 and 24 hours postoperatively, cumulative tramadol consumptions were higher in group 1 than the others. (Group 1 = 370.6 ± 121.6 mg, Group 2: 220.9 ± 92.5mg, Group 3 = 240.7 ± 100.4 mg.) (p < 0.005). The average dose of pethidine administered was significantly lower in groups 2 and 3 compared with group 1 (Group 1: 145 mg, Group 2: 100mg, Group 3: 100mg) (p = 0.024). CONCLUSIONS: Levobupivacaine treated group required significantly more intravenous tramadol when compared with paracetamol and lornoxicam groups in patients submitted to transperitoneal laparoscopic renal and adrenal surgery.


Asunto(s)
Glándulas Suprarrenales/cirugía , Riñón/cirugía , Laparoscopía/métodos , Manejo del Dolor/métodos , Dolor Postoperatorio/tratamiento farmacológico , Acetaminofén/administración & dosificación , Acetaminofén/uso terapéutico , Administración Intravenosa , Adulto , Analgésicos no Narcóticos/uso terapéutico , Anestesia Local/métodos , Anestésicos Locales/uso terapéutico , Antiinflamatorios no Esteroideos/uso terapéutico , Bupivacaína/análogos & derivados , Bupivacaína/uso terapéutico , Femenino , Humanos , Levobupivacaína , Masculino , Persona de Mediana Edad , Dimensión del Dolor/métodos , Piroxicam/administración & dosificación , Piroxicam/análogos & derivados , Piroxicam/uso terapéutico , Escala Visual Analógica
13.
Int. braz. j. urol ; 41(4): 669-675, July-Aug. 2015. tab
Artículo en Inglés | LILACS | ID: lil-763070

RESUMEN

ABSTRACTPurpose:We compared the effects of local levobupivacaine infiltration, intravenous paracetamol, intravenous lornoxicam treatments on postoperative analgesia in patients submitted to transperitoneal laparoscopic renal and adrenal surgery.Materials and Methods:Sixty adult patients 26 and 70 years who underwent laparoscopic renal and adrenal surgery were randomized into three groups with 20 patients each: Group 1 received local 20mL of levobupivacaine 0.25% infiltration to the trocar incisions before skin closure. In group 2, 1g paracetamol was given to the patients intravenously 30 minutes before extubation and 5g paracetamol was given intravenoulsy in the 24 postoperative period. In group 3, 8mg lornoxicam i.v. was given 30 minutes before extubation and 8mg lornoxicam i.v. was given in the 24 postoperative period. In the postoperative period, pain scores, cumulative tramadol, and additional pethidine consumption were evaluated.Results:Postoperative pain scores significantly reduced in each group (p < 0.05). Although pain levels of the groups were not significantly different at 1, 2, 4, 8, 12 and 24 hours postoperatively, cumulative tramadol consumptions were higher in group 1 than the others. (Group 1 = 370.6 ± 121.6mg, Group 2: 220.9 ± 92.5mg, Group 3 = 240.7 ± 100.4mg.) (p < 0.005). The average dose of pethidine administered was significantly lower in groups 2 and 3 compared with group 1 (Group 1: 145mg, Group 2: 100mg, Group 3: 100mg) (p = 0.024).Conclusions:Levobupivacaine treated group required significantly more intravenous tramadol when compared with paracetamol and lornoxicam groups in patients submitted to transperitoneal laparoscopic renal and adrenal surgery.


Asunto(s)
Adulto , Femenino , Humanos , Masculino , Persona de Mediana Edad , Glándulas Suprarrenales/cirugía , Riñón/cirugía , Laparoscopía/métodos , Manejo del Dolor/métodos , Dolor Postoperatorio/tratamiento farmacológico , Administración Intravenosa , Acetaminofén/administración & dosificación , Acetaminofén/uso terapéutico , Analgésicos no Narcóticos/uso terapéutico , Anestesia Local/métodos , Anestésicos Locales/uso terapéutico , Antiinflamatorios no Esteroideos/uso terapéutico , Bupivacaína/análogos & derivados , Bupivacaína/uso terapéutico , Dimensión del Dolor/métodos , Piroxicam/administración & dosificación , Piroxicam/análogos & derivados , Piroxicam/uso terapéutico , Escala Visual Analógica
14.
Pak J Pharm Sci ; 28(1): 185-93, 2015 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-25553695

RESUMEN

In this present research work, we have designed a pulsincap formulation comprising mini-tablets, which to the best of our knowledge this combination has not been reported yet. We successfully combined the advantages of mini-tablets technology to meet the optimized requirements of our pulsincap formulation. Our main aim was to target lornoxicam to treat rheumatoid arthritis as per the chronotherapeutic pattern of the disease. Directly compressing method was used to prepare mini-tablets. The drug, polymers and combine mixtures of drug and polymers was evaluated for pre-formulation testing. Prepared mini-tablets were also evaluated for physicochemical, dissolution and stability studies. From FTIR and DSC evaluation, we found no interaction between the drug and polymers used. For mini-tablets, all the physico-chemical parameters were in limit. The mini-tablets of lornoxicam were filled into an insoluble body of capsule, and its opening was sealed by plugging it with a polymer. The complete capsule body after sealing with a cap was given enteric coating. Different polymers in various concentrations were used as a plug, to identify the most suitable which gives a complete lag time of 5 hours when combined with 5% CAP coating. HPMC-K100M in 30% and sodium alginate in 40% concentrations were identified as the most suitable plugs. Our optimized pulsincap formulations releases lornoxicam after a lag time of 5 hrs and maximum portion of the drug will be released in the early morning hours. It was also found to be stable for a period of 6 months as per ICH guidelines.


Asunto(s)
Antirreumáticos/administración & dosificación , Artritis Reumatoide/tratamiento farmacológico , Cronoterapia de Medicamentos , Piroxicam/análogos & derivados , Administración Oral , Alginatos/química , Antirreumáticos/química , Rastreo Diferencial de Calorimetría , Química Farmacéutica , Estabilidad de Medicamentos , Ácido Glucurónico/química , Ácidos Hexurónicos/química , Humanos , Derivados de la Hipromelosa/química , Cinética , Piroxicam/administración & dosificación , Piroxicam/química , Polvos , Solubilidad , Espectroscopía Infrarroja por Transformada de Fourier , Comprimidos
15.
Arch Pharm Res ; 38(5): 801-12, 2015.
Artículo en Inglés | MEDLINE | ID: mdl-24752862

RESUMEN

The objective of this study was to improve the dissolution and subsequently the therapeutic efficacy of poorly water soluble BCS class-II drugs meloxicam and tenoxicam, by lipid semi solid matrix (SSM) systems filled in hard gelatin capsules by liquid fill technology. The present research involved preparation of SSM formulations using Gelucire 44/14 as a carrier due to its self emulsifying, wetting and hydrophilic properties. The SSM capsules were characterized by assay, in vitro dissolution studies, moisture uptake, FTIR and DSC. The optimized formulations were also evaluated for their in vivo anti inflammatory activity in rat model. Six to ten fold enhancement in vitro drug release, in both acidic and basic media, was obtained with formulations containing drug to carrier in 1:6 ratio. The absence of drug peak in DSC scans indicated complete dissolution of the drug in carrier, while IR revealed no chemical interaction of pure drug and Gelucire 44/14. The optimized SSM formulations of meloxicam and tenoxicam showed a rapid decrease in paw edema with a significant increase in anti-inflammatory activity. The SSM formulations were successful in providing rapid release of drugs with improved dissolution and in vivo anti-inflammatory activity by liquid fill technology in hard gelatin capsules.


Asunto(s)
Antiinflamatorios no Esteroideos/química , Antiinflamatorios no Esteroideos/metabolismo , Piroxicam/análogos & derivados , Tiazinas/química , Tiazinas/metabolismo , Tiazoles/química , Tiazoles/metabolismo , Animales , Cápsulas , Química Farmacéutica , Evaluación Preclínica de Medicamentos/métodos , Masculino , Meloxicam , Piroxicam/química , Piroxicam/metabolismo , Ratas , Ratas Wistar , Solubilidad
16.
Artículo en Ruso | MEDLINE | ID: mdl-24874317

RESUMEN

OBJECTIVE: Acute cervical pain is one of the most common reasons for a visit to a doctor and temporal disability. We studied efficacy and safety of the nonsteroid anti-inflammatory drug tenoxicam (texamen) in the treatment of acute cervical pain in myofascial syndrome. MATERIAL AND METHODS: A trial included 50 people (42 women and 8 men, mean age 42,2±6,8 years) with acute cephalgia. A main group (30 patients) received tenoxicam in dose 20 mg daily in the morning during 7 days with simultaneous therapeutic exercises with elements of postisometric relaxation of cervical muscles. A control group (20 patients) received myorelaxants and massage of a cervical-collar zone. RESULTS: The analgesic effect was more rapid in patients treated with texamen compared to controls. Statistically significant differences were seen in 1-3 days of treatment. In the main group, the analgesic effect long, only 16,6% of patients reported the aggravation of pain in the evening hours during the first day of treatment and 10% in the 2nd day; 23,3% patients of the main group used an additional dose of texamen, another nonsteroid anti-inflammatory drug (ibuprofen) or triptan to stop pain. CONCLUSION: The introduction of nonsteroid anti-inflammatory drugs, in particular texamen, in the complex treatment of acute cephalgia can significantly reduce pain syndrome.


Asunto(s)
Dolor Agudo/tratamiento farmacológico , Antiinflamatorios no Esteroideos/uso terapéutico , Dolor de Cuello/tratamiento farmacológico , Piroxicam/análogos & derivados , Adulto , Método Doble Ciego , Femenino , Humanos , Ibuprofeno/uso terapéutico , Masculino , Persona de Mediana Edad , Dimensión del Dolor , Piroxicam/uso terapéutico
17.
Pharm Res ; 31(8): 1946-57, 2014 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-24522816

RESUMEN

PURPOSE: The advent of cocrystals has demonstrated a growing need for efficient and comprehensive coformer screening in search of better development forms, including salt forms. Here, we investigated a coformer screening system for salts and cocrystals based on binary phase diagrams using thermal analysis and examined the effectiveness of the method. METHODS: Indomethacin and tenoxicam were used as models of active pharmaceutical ingredients (APIs). Physical mixtures of an API and 42 kinds of coformers were analyzed using Differential Scanning Calorimetry (DSC) and X-ray DSC. We also conducted coformer screening using a conventional slurry method and compared these results with those from the thermal analysis method and previous studies. RESULTS: Compared with the slurry method, the thermal analysis method was a high-performance screening system, particularly for APIs with low solubility and/or propensity to form solvates. However, this method faced hurdles for screening coformers combined with an API in the presence of kinetic hindrance for salt or cocrystal formation during heating or if there is degradation near the metastable eutectic temperature. CONCLUSIONS: The thermal analysis and slurry methods are considered complementary to each other for coformer screening. Feasibility of the thermal analysis method in drug discovery practice is ensured given its small scale and high throughput.


Asunto(s)
Análisis Diferencial Térmico/métodos , Indometacina/análisis , Piroxicam/análogos & derivados , Combinación de Medicamentos , Evaluación Preclínica de Medicamentos/métodos , Indometacina/química , Piroxicam/análisis , Piroxicam/química , Difracción de Polvo/métodos , Difracción de Rayos X
18.
Cochrane Database Syst Rev ; (5): CD005277, 2012 May 16.
Artículo en Inglés | MEDLINE | ID: mdl-22592704

RESUMEN

BACKGROUND: Decompression illness (DCI) is due to bubble formation in the blood or tissues following the breathing of compressed gas. Clinically, DCI may range from a trivial illness to loss of consciousness, death or paralysis. Recompression is the universally accepted standard treatment of DCI. When recompression is delayed, a number of strategies have been suggested in order to improve the outcome. OBJECTIVES: To examine the effectiveness and safety of both recompression and adjunctive therapies in the treatment of DCI. SEARCH METHODS: In our previous update we searched until October 2009. In this version we searched CENTRAL (The Cochrane Library, October 2011); MEDLINE (1966 to October 2011); CINAHL (1982 to October 2011); EMBASE (1980 to October 2011); the Database of Randomised Controlled Trials in Hyperbaric Medicine (October 2011); and handsearched journals and texts. SELECTION CRITERIA: We included randomized controlled trials that compared the effect of any recompression schedule or adjunctive therapy with a standard recompression schedule. We did not apply language restrictions. DATA COLLECTION AND ANALYSIS: Three authors extracted the data independently. We assessed each trial for internal validity and resolved differences by discussion. Data were entered into RevMan 5.1. MAIN RESULTS: Two randomized controlled trials enrolling a total of 268 patients satisfied the inclusion criteria. The risk of bias for Drewry 1994 was unclear as this study was presented as an abstract, while Bennett 2003 was rated as at low risk. Pooling of data was not possible. In one study there was no evidence of improved effectiveness with the addition of a non-steroidal anti-inflammatory drug (tenoxicam) to routine recompression therapy (at six weeks: relative risk (RR) 1.04, 95% confidence interval (CI) 0.90 to 1.20, P = 0.58) but there was a reduction in the number of compressions required when tenoxicam was added from three to two (P = 0.01, 95% CI 0 to 1). In the other study, the odds of multiple recompressions were lower with a helium and oxygen (heliox) table compared to an oxygen treatment table (RR 0.56, 95% CI 0.31 to 1.00, P = 0.05). AUTHORS' CONCLUSIONS: Recompression therapy is standard for the treatment of DCI, but there is no randomized controlled trial evidence for its use. Both the addition of a non-steroidal anti-inflammatory drug (NSAID) and the use of heliox may reduce the number of recompressions required, but neither improve the odds of recovery. The application of either of these strategies may be justified. The modest number of patients studied demands a cautious interpretation. Benefits may be largely economic and an economic analysis should be undertaken. There is a case for large randomized trials of high methodological rigour in order to define any benefit from the use of different breathing gases and pressure profiles during recompression therapy.


Asunto(s)
Enfermedad de Descompresión/terapia , Oxigenoterapia Hiperbárica/métodos , Antiinflamatorios no Esteroideos/uso terapéutico , Humanos , Piroxicam/análogos & derivados , Piroxicam/uso terapéutico , Ensayos Clínicos Controlados Aleatorios como Asunto , Retratamiento/métodos
19.
Zhong Yao Cai ; 33(6): 1019-23, 2010 Jun.
Artículo en Chino | MEDLINE | ID: mdl-21049628

RESUMEN

OBJECTIVE: To explore the role of Tong Mai Tang & Lornoxicam on the serum concentrations of tumor necrosis factor alpha (TNF-alpha), interleukin (IL-6) , D-dipolymer( D-Di), Platelet count (PLC) in treatment of femoral shaft fracture among period surgery time. METHODS: We selected 120 cases of traumatic femoral shaft fracture patients according to the inclusion criteria and exclusion criteria, which were randomized dividend into four groups (I, II, III, IV respectively) of the same size based on the random number table method of 30 patients each. Therapeutic methods of four groups following as: Group I, Tpanax Notoginseng Pills PO; Group II, Tpanax Notoginseng Pills PO, Lornoxicam For Injection, 8 mg IM; Group III, Tpanax Notoginseng Pills PO, Tong Mai Decoctions 200 mL PO; Group IV, Tpanax Notoginseng Pills PO, Lornoxicam For Injection 8 mg IM, Tong Mai Decoctions 200 mL PO. The above medications were administered to the four groups after admission to hospital the next day. Peripheral blood samples were taken for immune determination of pro-inflammatory cytokines of TNF-alpha, IL-6, D-Di, PLC in blood serum on the 2nd and 6th day before operation and on the 8th and 13th day after operation in the morning. And all patients received liver and kidney function examination 2nd and 13th day after admission. Analysis of variance and least significant difference-test were done with the help of SPSS 17.0 statistic software. RESULTS: The difference among four groups in TNF-alpha and IL-6 were significant (P < 0.05). And there were also significant statistic difference between group II/III/IV and group I group (P < 0.05). But the difference between group II and group III was insignificant (P > 0.05). However, the group contrast result between group IV and group II/III had statistics difference (P < 0.05). The difference in D-Di PLC at 6th day and 8th day were significant (P < 0.05). The group comparisons in group I/II/IV were also significant. There were non-statistics significance in group II compared 6th day/8th day with 2nd day (P > 0.05). The comparison between the 13th day with the first three time sections had statistics significance. And there were statistics significance at the 13th day between group IV and group II (P < 0.05). CONCLUSION: The serum concentrations of TNF-alpha, IL-6, D-Di and PLC level were significantly increased in peroperative period, These results seem to indicate that the Tong Mai Decoctions & Lornoxicam may play an important role in inhibiting the release of TNF-alpha, IL-6, D-Di and PLC into the blood stream and decreasing the incunabula complication at early traumatic stage. The Tong Mai Decoctions & Lornoxicam was the worth promoting screened China and the West union medication combination.


Asunto(s)
Medicamentos Herbarios Chinos/administración & dosificación , Fracturas del Fémur/tratamiento farmacológico , Interleucina-6/sangre , Piroxicam/análogos & derivados , Factor de Necrosis Tumoral alfa/sangre , Adulto , Combinación de Medicamentos , Quimioterapia Combinada , Medicamentos Herbarios Chinos/farmacología , Femenino , Fracturas del Fémur/sangre , Fracturas Cerradas/sangre , Fracturas Cerradas/tratamiento farmacológico , Humanos , Masculino , Persona de Mediana Edad , Atención Perioperativa , Piroxicam/administración & dosificación , Piroxicam/farmacología , Recuento de Plaquetas , Resultado del Tratamiento , Trombosis de la Vena/prevención & control , Adulto Joven
20.
Neuropharmacology ; 59(3): 149-59, 2010 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-20450924

RESUMEN

Treatment of the autoimmune demyelinating disease multiple sclerosis (MS) requires therapies that both limit and repair damage. While several immunomodulatory treatments exist to limit damage there are currently no treatments that promote the regenerative process of remyelination. A rapid way of screening potential pro-remyelination compounds is therefore required. The use of larval zebrafish in a drug reprofiling screen allows rapid in vivo screening and has been used successfully in the past as an efficient way of identifying new indications for existing drugs. A novel screening platform for potential pro-myelination compounds was developed using zebrafish larvae. Two percent of compounds screened from reprofiling libraries altered oligodendrocyte lineage cell recruitment and/or proliferation, as measured by the numbers of dorsally migrated spinal cord olig2(+) cells. Selective screening identified three compounds that altered levels of myelination, as measured by whole larvae myelin basic protein (mbp) transcript levels; the src family kinase inhibitor PP2, a biogenic amine and a thioxanthene. As well as many previously unrecognised compounds, identified compounds included those with previously known effects on myelin and/or the oligodendrocyte lineage, such as a PPAR agonist, steroid hormones and src family kinase inhibitors. As well as providing methods for further assessment of potentially beneficial compounds, this screen has highlighted 25 targets that are able to alter oligodendrocyte lineage cell recruitment or proliferation and/or mbp transcript levels in vivo and are worthy of further investigation for their potential effects on remyelination.


Asunto(s)
Diferenciación Celular/efectos de los fármacos , Inhibidores Enzimáticos/farmacología , Regulación del Desarrollo de la Expresión Génica/efectos de los fármacos , Modelos Animales , Proteína Básica de Mielina/metabolismo , Oligodendroglía/metabolismo , Análisis de Varianza , Animales , Animales Modificados Genéticamente , Antiinflamatorios no Esteroideos/farmacología , Factores de Transcripción con Motivo Hélice-Asa-Hélice Básico/genética , Factores de Transcripción con Motivo Hélice-Asa-Hélice Básico/metabolismo , Recuento de Células/métodos , Diferenciación Celular/fisiología , Evaluación Preclínica de Medicamentos , Embrión no Mamífero , Regulación del Desarrollo de la Expresión Génica/fisiología , Proteínas Fluorescentes Verdes/genética , Proteína Básica de Mielina/genética , Proteínas del Tejido Nervioso/genética , Proteínas del Tejido Nervioso/metabolismo , Factor de Transcripción 2 de los Oligodendrocitos , Oligodendroglía/efectos de los fármacos , Piroxicam/análogos & derivados , Piroxicam/farmacología , Médula Espinal/citología , Pez Cebra , Proteínas de Pez Cebra/genética , Proteínas de Pez Cebra/metabolismo
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