Phutane P, Shidhaye S, Lotlikar V, Ghule A, Sutar S, Kadam V
Department of Pharmaceutics, Bharati Vidyapeeth's College of Pharmacy, Sector 8, C.B.D. Belapur, Navi Mumbai - 400 614, India.
J Young Pharm. 2010 Jan;2(1):35-41. doi: 10.4103/0975-1483.62210.
The objective of the current investigation is to reduce dosing frequency and improve patient compliance by designing and systematically evaluating sustained release microspheres of Glipizide. An anti-diabetic drug, Glipizide, is delivered through the microparticulate system using ethyl cellulose as the controlled release polymer. Microspheres were developed by the emulsion solvent diffusion-evaporation technique by using the modified ethanol,-dichloromethane co-solvent system. The polymer mixture of ethyl cellulose and Eudragit(®) S100 was used in different ratios (1:0, 1:1, 2:3, 1:4 and 0:1) to formulate batches F1 to F5. The resulting microspheres were evaluated for particle size, densities, flow properties, morphology, recovery yield, drug content, and in vitro drug release behavior. The formulated microspheres were discrete, spherical with relatively smooth surface, and with good flow properties. Among different formulations, the fabricated microspheres of batch F3 had shown the optimum percent drug encapsulation of microspheres and the sustained release of the Glipizide for about 12 h. Release pattern of Glipizide from microspheres of batch F3 followed Korsmeyers-peppas model and zero-order release kinetic model. The value of 'n' was found to be 0.960, which indicates that the drug release was followed by anomalous (non-fickian) diffusion. The data obtained thus suggest that a microparticulate system can be successfully designed for sustained delivery of Glipizide and to improve dosage form characteristics for easy formulation.
当前研究的目的是通过设计并系统评估格列吡嗪缓释微球来降低给药频率并提高患者依从性。格列吡嗪是一种抗糖尿病药物,通过使用乙基纤维素作为控释聚合物的微粒系统来递送。采用改良的乙醇 - 二氯甲烷共溶剂体系,通过乳液溶剂扩散 - 蒸发技术制备微球。将乙基纤维素和尤特奇(®)S100的聚合物混合物以不同比例(1:0、1:1、2:3、1:4和0:1)用于配制批次F1至F5。对所得微球进行粒度、密度、流动性、形态、回收率、药物含量和体外药物释放行为的评估。所制备的微球呈离散的球形,表面相对光滑,流动性良好。在不同配方中,批次F3制备的微球显示出微球最佳的药物包封率以及格列吡嗪约12小时的持续释放。批次F3微球中格列吡嗪的释放模式符合Korsmeyers - peppas模型和零级释放动力学模型。“n”值为0.960,表明药物释放遵循非菲克(反常)扩散。因此获得的数据表明,可以成功设计微粒系统用于格列吡嗪的持续递送,并改善剂型特性以利于制剂制备。