吡格列酮自微乳化给药体系的研制与表征

P. Hyma , K. Abbulu
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引用次数: 17

摘要

本研究的目的是研制吡格列酮水溶性较差药物的自微乳化给药系统。大约40%的新候选药物水溶性较差,口服给药往往伴随着低生物利用度、高体内和体内变异性以及缺乏剂量比例的影响。疏水药物通常可以溶解在微乳液中,使其被包裹成细小的小球,使药物在肠道中保持不溶解,避免了溶解步骤,这往往限制了疏水药物的吸收速度。对吡格列酮的最大溶解度进行了相溶解度研究。以Tween 80(表面活性剂)、聚乙二醇400(共表面活性剂)和棉籽油含量最高。构建三元相图评价微乳区域。FTIR分析了药物与辅料的相互作用。优化后的SMEDDS平均粒径小于200 nm, zeta电位为负。并与市售片剂进行了溶出度比较;结果表明,所研制的吡格列酮溶出度比市售片提高了2 ~ 3倍。对球的形状和形态进行了扫描电镜研究。因此,SMEDDS可被视为目前吡格列酮制剂的新颖和商业上可行的替代品。
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Formulation and characterisation of self-microemulsifying drug delivery system of pioglitazone

The aim of the study was to develop self-microemulsifying drug delivery system (SMEDDS) of a poorly water soluble drug, pioglitazone. Approximately 40% of new drug candidates have poor water solubility and the oral delivery of such drugs is frequently associated with implications of low bioavailability, high intra- and intersubject variability and lack of dose proportionality. Hydrophobic drugs can often be dissolved in microemulsion allowing them to be encapsulated in the form of fine globules, so that drug remains undissolved in the gut avoiding the dissolution step, which frequently limit the rate of absorption of hydrophobic drugs. Phase solubility studies were conducted for the maximum solubility of pioglitazone. Highest was found in Tween 80 (surfactant) polyethylene glycol 400 (cosurfactant) and cottonseed oil. Ternary phase diagrams were constructed to evaluate microemulsion regions. FTIR analysis was done for investigating the drug–excipient interactions. The mean globule size of SMEDDS was observed to be below 200 nm for the optimized formulations and the zeta potential was negative. The dissolution of emulsion formulations was compared with commercial tablets; the results indicated that the rate of dissolution of developed formulations containing pioglitazone was 2 to 3 folds increased compared with that of commercial tablets. SEM studies were done for the shape and morphology of the globules. Thus, SMEDDS can be regarded as novel and commercially feasible alternative to the current pioglitazone formulations.

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