Department of Pharmaceutics and Pharmaceutical Technology, S.K. Patel College of Pharmaceutical Education and Research, Ganpat University, Kherva, Gujarat, India.
Drug Dev Ind Pharm. 2011 Oct;37(10):1244-52. doi: 10.3109/03639045.2011.567274. Epub 2011 Apr 6.
The goal of diabetes therapy today is to achieve and maintain as near normal glycemia as possible to prevent the long-term microvascular and macrovascular complications of an elevated blood glucose. A newly developed inlay osmotic pump tablet (IOPT) can deliver glipizide (GLZ) and metformin HCl (MET) gradually in controlled manner. The aim of present investigation was to prepare the IOPT that can deliver >75% of GLZ in 2 h, whereas MET released after 2 h and sustained up to 12 h. In the present work, HP-β-CD was used to modify the solubility of GLZ before incorporating in the osmotic system and MET was spray-dried with HPMC A15C to modify its release profile, flow property, and compressibility. Various parameters mainly G(75%) (75% GLZ release), t(LMET) (lag time of MET release from device), Q(10 h) (percent of MET released within 10 h), and RSQ(ZERO) (R(2) of release data fitted to zero-order equation) were used to compare different formulations. The effects of different formulation variables, that is, osmagents, concentration of hydrophilic polymer, diameter of drug releasing orifice, and coating composition on the drug release profile were investigated. The release rate of GLZ could be effectively modified by the addition of sodium carbonate and sodium chloride, whereas the release rate of MET was adjusted by dual-coating system and by addition of hydrophilic polymer. The developed inlay osmotic system could be effective in the multidrug therapy of diabetes by delivering both drugs in a controlled manner.
目前糖尿病治疗的目标是尽可能实现并维持接近正常的血糖水平，以预防高血糖引起的长期微血管和大血管并发症。一种新开发的嵌入式渗透泵片剂（IOPT）可以逐渐以受控的方式输送格列吡嗪（GLZ）和盐酸二甲双胍（MET）。本研究的目的是制备能够在 2 小时内释放超过 75% GLZ 的 IOPT，而 MET 在 2 小时后释放并持续 12 小时。在本工作中，使用 HP-β-CD 来提高 GLZ 的溶解度，然后将其纳入渗透系统，使用 HPMC A15C 对 MET 进行喷雾干燥以改变其释放特性、流变性和可压缩性。主要使用各种参数（即 G(75%)（75% GLZ 的释放）、t(LMET)（从装置中释放 MET 的滞后时间）、Q(10 h)（10 小时内释放的 MET 的百分比）和 RSQ(ZERO)（拟合至零阶方程的释放数据的 R(2)）来比较不同的配方。考察了不同制剂变量（即渗透压剂、亲水性聚合物浓度、药物释放孔的直径和包衣组成）对药物释放曲线的影响。通过添加碳酸钠和氯化钠，可以有效地调节 GLZ 的释放速率，而通过双重包衣系统和添加亲水性聚合物可以调节 MET 的释放速率。开发的嵌入式渗透系统可以通过以受控方式输送两种药物，从而有效用于糖尿病的多药物治疗。
