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Formulation and evaluation of Thiocolchicoside Topical Gel by using different method

机译:不同方法对硫秋水仙苷外用凝胶的配制与评价

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Thiocolchicoside used for the effective treatment of muscle spasm, cramps, musculoskeletal and neuromuscular disorders. It is available in market in the form of capsules and injection. The major problem associated with thiocolchicoside is it's bioavailability which is very low i.e. 25-30% only so in order to minimize drug loss due to first pass metabolism, and overcome problem associated with low bioavailability of drug there is a need to formulate semisolid preparation in the form of gel so we try to formulate and evaluate thiocolchicoside gel using different polymer and comparative study of their drug release. In vitro release of thiocolchicoside gel from three different polymers i.e. carbapol, HPMC, and Na CMC to an aqueous receptor phase through goat skin was monitored spectrophotometrically at a wavelength of 259nm. This study was conducted to develop gel formulation of thiocolchicoside using three types of gelling agent i.e. carbopol, HPMC, Na CMC. Effect of penetration enhancer (propylene glycol) on the release has been studied. The gels were evaluated for physical appearance, rheological behaviour, drug release, and stability. Drug release from all gelling agent through goat skin was evaluated using keshary-chien diffusion cell. All gels show acceptable physical properties concerning colour, homogenity, consistancy spredability and pH value. Among all gel formulation carbapol showed superior drug release then followed by Na CMC and HPMC. Drug release decreased with increased in the polymer concentration. Drug release was not linearly proportional with the conc. of penetration enhancer or co-solvent stability studies showed that the physical appearance, rheological properties and drug release remained unchanged upon storage for two month at ambient condition.
机译:硫秋水仙苷可有效治疗肌肉痉挛,抽筋,肌肉骨骼和神经肌肉疾病。它以胶囊和注射剂的形式在市场上出售。与硫代秋水仙苷有关的主要问题是其生物利用度非常低,即仅为25%至30%,因此,为了最大程度地减少由于首过代谢引起的药物损失,并克服与药物的生物利用度低有关的问题,需要配制半固体制剂。凝胶形式,因此我们尝试使用不同的聚合物来配制和评估硫代秋水仙碱凝胶,并对它们的药物释放进行比较研究。通过分光光度法在259nm的波长下监测了硫代秋水仙苷凝胶从三种不同的聚合物,即卡巴普尔,HPMC和Na CMC通过山羊皮肤向水性受体相的体外释放。进行该研究以开发使用三种类型的胶凝剂即卡波姆,HPMC,Na CMC的硫代秋水仙苷的凝胶制剂。已经研究了渗透促进剂(丙二醇)对释放的影响。评价凝胶的物理外观,流变行为,药物释放和稳定性。使用keshary-chien扩散池评估了从所有胶凝剂通过山羊皮肤释放的药物。所有凝胶均显示出可接受的有关颜色,均匀性,稠度和pH值的物理性质。在所有凝胶制剂中,carbapol显示出更高的药物释放,其次是Na CMC和HPMC。药物释放随着聚合物浓度的增加而降低。药物释放与浓度不成线性比例。渗透促进剂或助溶剂稳定性研究表明,在环境条件下储存两个月后,其物理外观,流变性质和药物释放均保持不变。

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