Lanzhou University Second Hospital, Lanzhou, P.R. China.
Pharm Dev Technol. 2012 Nov-Dec;17(6):666-76. doi: 10.3109/10837450.2011.565348. Epub 2011 Apr 13.
A method for the preparation of porosity osmotic pump granules was obtained by modulating carvedilol solubility with tartaric acid. Controlled porosity of the membrane was accomplished by the use of pore-forming agent in the coating. In this study, carvedilol was chosen as a model drug with an aim to develop a zero-order release system; tartaric acid was used as the solubility promoter; NaCl was used as the osmotic agent; cellulose acetate (CA) was used as the materials of semipermeable membrane; and PEG-400 was used as the pore-forming agent in the semipermeable membrane. The influence of different factors or levels on the in vitro release was studied. In order to simulate the gastrointestinal tract environments, two kinds of pH media (pH 1.5 and 6.8) on drug release were studied in this research, respectively. This porosity osmotic pump was optimized by single factor design experiments, and it was found to deliver carvedilol at a zero-order rate within 12 h and controlled release for 24 h. We drew a conclusion that the solubility-modulated porosity osmotic pump system is simple to prepare and might be used for the preparation of osmotic pump system of other poorly water-soluble drugs with alkaline or acid groups.
采用酒石酸调节卡维地洛的溶解度，得到一种制备渗透泵颗粒的方法。通过在包衣中使用成孔剂来控制膜的多孔性。在这项研究中，选择卡维地洛作为模型药物，旨在开发零级释放系统；酒石酸用作溶解度促进剂；NaCl 用作渗透压剂；醋酸纤维素（CA）用作半透膜材料；PEG-400 用作半透膜中的成孔剂。研究了不同因素或水平对体外释放的影响。为了模拟胃肠道环境，本研究分别研究了两种 pH 介质（pH1.5 和 6.8）对药物释放的影响。通过单因素设计实验对这种渗透性渗透泵进行了优化，结果发现它可以在 12 小时内以零级速率输送卡维地洛，并控制释放 24 小时。我们得出结论，该溶解度调节渗透性渗透泵系统制备简单，可用于制备具有碱性或酸性基团的其他水溶性差的药物的渗透泵系统。
