ABSTRACT
Objective: This study was undertaken to determine the bioavailability of ondansetron gel in experimental animals and humans applying UPLC as an analytical tool and evaluation of the antiemetic effect of ondansetron gel in cisplatin-induced emesis in rats. Methods: Ondansetron gel (F13: sodium alginate 7% w/w) was used, marketed I. V. ondansetron (Zofran) ® was chosen as reference. The bioavailability study in rabbits was selected as a parallel design using nine healthy rabbits divided into three groups whereas, bioavailability study in humans was an open-label, wherein 6 healthy subjects administered ondansetron gel. The potential effect of ondansetron gel was evaluated for the prevention of different phases of emesis motivated by exposure to antineoplastic drugs (cisplatin) by determination of body weight loss, water and food intake applying kaolin-pica model in rats using seventy-two rats divided into six groups. Results: Ondansetron gel (0.5%) showed detectable plasma concentration 22.833±2.17 ng/m1 after ¼ h and 419.55±2.17 ng/ml after 1-h post-treatment in rabbits and human respectively and concentration was maintained above-reported minimum effective concentration for more than 2.5 h for rabbits and 7 h for humans compared to 1.75 h after I. V. administration. The ondansetron gel significantly reduces all phases of cisplatin-induced emesis and a decrease in body weight, water, and food consumption was significantly attenuated. Conclusion: Based on the high efficacy of gel on emesis induced by cisplatin, and its high bioavailability, transdermal ondansetron gel could be a promising convenient system to prevent nausea and vomiting following administration of antineoplastic drugs.
ABSTRACT
In the present study transdermal Lisinopril proniosomal gels was formulated by using Lecithin, Cholesterol as encapsulating agents, Surfactant, Span and permeation enhancers. The study methodology encompasses compatibility studies using FTIR spectra, evaluation of proniosomal gels for pH determination, Viscosity, Vesicle size analysis, rate of spontaneity, encapsulation efficiency, in vitro skin permeation studies and stability studies. The preliminary compatibility studies conducted revealed that there no interaction between Lisinopril and excipients which was as evident from FTIR spectral studies. The physical characterization of proniosomal gels was found to be within the acceptable limits. It was observed that the gel formulations showed good spreadability and viscosity. Determination of vesicle size was found to be 20.10-26.23μm. The proniosomes showed spherical and homogenous structure in optical microscopy. All formulations showed zero order drug release by diffusion mechanism. The stability studies showed that proniosomal gels were stable at 4 to 80C and 25±20C. The above results indicated that the proniosomal gels of could be formulated for controlled release of Lisinopril. The proniosomal gels are suitable for Lisinopril once a day controlled release formulation.
ABSTRACT
AIM: To study the absorption and distribution characteristics of oxybutynin (OXY) oral tablet and transdermal gel. METHODS: A single dose of 0.1 g OXY transdermal gel (2 mg OXY) was applied to abdominal area about 4 cm2 and 0.5 mg immediate-release tablet was orally given to 48 rats in a randomized, open-label, control design test. The plasma, bladder and liver tissue were collected, disposed and analyzed and OXY pharmacokinetic parameters were calculated and evaluated. RESULTS: The Cmax of OXY transdermal gel and oral tablets in bladder are approximately 800 and 70 times higher than those in plasma. The plasma half life of OXY gel delayed 5.99 h, tablets 2.18 h. CONCLUSION: OXY gel show better pharmacokinetic properties, characterized with long half life and high target organ concentrations than those of tablets.