Okafor I S, Ofoefule S I, Udeala O K
Dept. of Pharmaceutics and Pharmaceutical Technology, University of Jos, Nigeria.
Boll Chim Farm. 2000 Nov-Dec;139(6):252-5.
Some in vitro properties of chloroquine phosphate tablets formulated with four modified starches were investigated. The drug was formulated as tablets containing 250 mg of chloroquine phosphate and produced by the direct compression technique. The starches were isolated from maize, zea mays, rice, Oryza sativa, cassava, Manihot esculenta and cocoyam, Zanthosoma sagittifolium. They were modified through physicochemical process, Sta-Rx 1500, a directly compressible starch was used as basis for comparison. The hardness of the chloroquine tablets generally decreased to a minimum with all the modified starches at concentration level of 40% and with maximum hardness obtained when their concentrations were increased to 80%. The least hardness values were obtained with modified cocoa yam starch while the highest hardness values were obtained with modified rice starch. Modified rice and cassava starches produced chloroquine tablets that exhibited higher mechanical properties than those of modified maize starch, cocoayam starch and Sta-Rx 1500. On the basis of dissolution profile of chloroquine phosphate tablets, the modified starch samples were ranked in order of increasing dissolution as modified cocoayam maize Sta-Rx 1500 cassava rice starch sample. The release rate of chloroquine was found to be dependent on the physico-chemical properties of the individual modified starch granules such as particle size and degree of gelatinization.
研究了用四种变性淀粉制备的磷酸氯喹片的一些体外性质。该药物被制成含250毫克磷酸氯喹的片剂，并采用直接压片技术生产。这些淀粉分别从玉米（Zea mays）、水稻（Oryza sativa）、木薯（Manihot esculenta）和芋艿（Zanthosoma sagittifolium）中分离得到。它们通过物理化学方法进行改性，以可直接压片的淀粉Sta-Rx 1500作为比较基准。当所有变性淀粉浓度为40%时，磷酸氯喹片的硬度普遍降至最低，而当浓度增至80%时，硬度达到最高。改性芋艿淀粉的硬度值最低，而改性水稻淀粉的硬度值最高。改性水稻淀粉和木薯淀粉制成的磷酸氯喹片比改性玉米淀粉、芋艿淀粉和Sta-Rx 1500具有更高的机械性能。根据磷酸氯喹片的溶出曲线，改性淀粉样品按溶出度增加的顺序排列为：改性芋艿淀粉、玉米淀粉、Sta-Rx 1500、木薯淀粉、水稻淀粉样品。发现氯喹的释放速率取决于各个改性淀粉颗粒的物理化学性质，如粒径和糊化程度。
