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Improving Tenoxicam Solubility and Bioavailability by Cosolvent System

机译:通过助溶剂系统提高替诺昔康的溶解度和生物利用度

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摘要

The formulation study of tenoxicam, a poorly water-soluble drug, was developed by use of a ternary cosolvent system and has significantly enhanced the solubility. Additionally, the relative bioavailability of testing formulation was also evaluated by New Zealand rabbit with a single i.m. injection. The three-phase diagram for dimethylsulfoxide (DMSO)/propylene glycol/water, DMSO/ethanol/water, and DMSO/polyethoxylated castor oil/ethanol system was developed. The volume ratio of 5:4:1 in the DMSO/polyethoxylated castor oil/ethanol system resulted in a more suitable vehicle than other systems, with a high solubility (20.73 mg/ml) and low viscosity (10.0 Cp). A pharmacokinetic study of bioequivalence (Frel = 0.89) was also obtained. The present study not only provides a novel strategy improving tenoxicam solubility but also helps further scientific knowledge for the development of parenteral formulations.
机译:使用三元助溶剂系统开发了水溶性较差的药物替诺昔康的制剂研究,该研究显着提高了溶解度。另外,还通过一个单一的i.m.的新西兰兔来评估测试制剂的相对生物利用度。注射。建立了二甲基亚砜(DMSO)/丙二醇/水,DMSO /乙醇/水和DMSO /聚乙氧基化蓖麻油/乙醇系统的三相图。 DMSO /聚乙氧基化蓖麻油/乙醇系统中5:4:1的体积比比其他系统更适合使用赋形剂,具有高溶解度(20.73 mg / ml)和低粘度(10.0Cp)。还进行了生物等效性的药代动力学研究(Frel = 0.89)。本研究不仅提供了改善替诺昔康溶解度的新策略,而且还为肠胃外制剂的开发提供了进一步的科学知识。

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