Department of Pharmaceutics, C.L. Baid Metha College of Pharmacy, Thoraipakkam, Chennai, Tamilnadu, India.
Lipids Health Dis. 2011 Apr 11;10:51. doi: 10.1186/1476-511X-10-51.
A system that can deliver multi-drug at a prolonged rate is very important for the treatment of various chronic diseases such as diabetes, asthma and heart disease. Controlled porosity osmotic pump tablet (CPOP) system was designed to deliver Nifedipine (NP) and Metoprolol (MP) in a controlled manner up to 12 h. It was prepared by incorporating drugs in the core and coated with various types (PVP, PEG-400 and HPMC) and levels (30, 40 and 50% w/w of polymer) of pore former at a weight gain of 8, 12 & 15%.
Formulation variables like type and level of pore former and percent weight gain of membrane was found to affect the drug release from the developed formulations. Drug release was inversely proportional to the membrane weight but directly related to the level of pore former. Burst strength of the exhausted shell was inversely proportional to the level of pore former, but directly affected by the membrane weight. Results of scanning electron microscopy (SEM) studies showed the formation of pores in the membrane from where the drug release occurred. Dissolution models were applied to drug release data in order to establish the mechanism of drug release kinetics. In vitro release kinetics was subjected to superposition method to predict in vivo performance of the developed formulation.
The developed osmotic system is effective in the multi-drug therapy of hypertension by delivering both drugs in a controlled manner.
对于治疗糖尿病、哮喘和心脏病等各种慢性疾病，能够以延长的速率输送多种药物的系统非常重要。控释渗透泵片（CPOP）系统旨在以受控方式输送硝苯地平（NP）和酒石酸美托洛尔（MP），时间长达 12 小时。通过将药物掺入芯中，并在增重 8、12 和 15%的情况下，用各种类型（PVP、PEG-400 和 HPMC）和水平（聚合物的 30、40 和 50%w/w）的致孔剂进行包衣来制备。
发现制剂变量（如致孔剂的类型和水平以及膜的增重百分比）会影响开发制剂的药物释放。药物释放与膜的重量成反比，但与致孔剂的水平成正比。耗尽壳的爆破强度与致孔剂的水平成反比，但直接受膜重量的影响。扫描电子显微镜（SEM）研究的结果表明，药物从膜中形成的孔中释放出来。为了建立药物释放动力学的机制，将溶解模型应用于药物释放数据。将体外释放动力学进行叠加方法处理，以预测开发制剂的体内性能。
所开发的渗透系统通过以受控方式输送两种药物，有效地用于高血压的多药物治疗。
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