Improving Tenoxicam Solubility and Bioavailability by Cosolvent System

被引：53
|
作者：
Yeh, Ming-Kung [2 ]
Chang, Li-Chien [3 ]
Chiou, Andy Hong-Jey [1 ]
机构：
[1] Natl Def Med Ctr, Inst Prevent Med, Taipei 90048700, Taiwan
[2] Tri Serv Gen Hosp, Dept Pharm Practice, Taipei, Taiwan
[3] Natl Def Med Ctr, Sch Pharm, Taipei 90048700, Taiwan
来源：
AAPS PHARMSCITECH | 2009年 / 10卷 / 01期
关键词：
bioavailability; cosolvent system; pharmacokinetics; poorly water-soluble drug; solubility; tenoxicam; FORMULATION; BUSULFAN; PHARMACOKINETICS; PACLITAXEL;
D O I：
10.1208/s12249-009-9189-2
中图分类号：
R9 [药学];
学科分类号：
1007 ;
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 (F (rel) = 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.
引用
收藏
页码：166 / 171
页数：6
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