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控释给药系统中的微孔表面:使用非离子表面活性剂作为致孔剂设计和评价盐酸地尔硫卓控释渗透泵。

Micro-porous surfaces in controlled drug delivery systems: design and evaluation of diltiazem hydrochloride controlled porosity osmotic pump using non-ionic surfactants as pore-former.

机构信息

Drug Applied Research Center .

出版信息

Pharm Dev Technol. 2014 Jun;19(4):507-12. doi: 10.3109/10837450.2013.805774. Epub 2013 Jun 13.

Abstract

The major problem associated with conventional drug delivery systems is unpredictable plasma concentrations. The aim of this study was to design a controlled porosity osmotic pump (CPOP) of diltiazem hydrochloride to deliver the drug in a controlled manner. CPOP tablets were prepared by incorporation of drug in the core and subsequent coating with cellulose acetate as semi-permeable membrane. Non-ionic surfactants were applied as pore-formers as well. The effect of pore-formers concentration on the in vitro release of diltiazem was also studied. The formulations were compared based on four comparative parameters, namely, total drug released after 24 h (D24 h), lag-time (tL), squared correlation coefficient of zero order equation (RSQzero) and mean percent deviation from zero order kinetic (MPDzero). Results of scanning electron microscopy studies exhibited formation of pores in the membrane from where the drug release occurred. It was revealed that drug release rate was directly proportional to the concentration of the pore-formers. The value of D24 h in the formulations containing Tween 80 (10%) and Brij 35 (5%) were found to be more than 94.9%, and drug release followed zero order kinetic (RSQzero > 0.99 and MPDzero < 8%) with acceptable tL (lower than 1 h).

摘要

与传统药物传递系统相关的主要问题是不可预测的血浆浓度。本研究旨在设计一种盐酸地尔硫卓的控释渗透泵(CPOP),以控制方式输送药物。CPOP 片剂通过将药物掺入芯部并用醋酸纤维素作为半渗透膜进行后续包衣来制备。非离子表面活性剂也用作造孔剂。还研究了造孔剂浓度对盐酸地尔硫卓体外释放的影响。根据四个比较参数,即 24 小时后释放的总药物(D24h)、滞后时间(tL)、零级方程的平方相关系数(RSQzero)和零级动力学的平均百分比偏差(MPDzero)对配方进行了比较。扫描电子显微镜研究的结果表明,在膜中形成了从其中释放药物的孔。结果表明,药物释放速率与造孔剂的浓度成正比。含有吐温 80(10%)和 Brij 35(5%)的制剂中 D24h 的值超过 94.9%,并且药物释放遵循零级动力学(RSQzero>0.99 和 MPDzero<8%),具有可接受的 tL(低于 1 小时)。

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