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目的制备以泊洛沙姆407(P407)为基本材料的注射用粉防己碱温敏型缓释原位凝胶,并考察其体外溶出行为。方法采用冷溶法制备凝胶,以胶凝温度为指标,考察单独使用P407和加入其他辅料F188、PEG1500、HPMC、MC对胶凝温度的影响;采用无膜溶出法考察凝胶的体外溶蚀和释放行为,并采用HPLC测定溶出液中药物的含量,筛选较优处方。结果胶凝温度随P407浓度的增大而降低;且当P407浓度低于15%时不发生相转变,辅料F188、PEG1500、MC的加入不能制备出符合要求的凝胶;8.0%、8.5%、9.0%HPMC分别与8.0%P407混合制备凝胶的胶凝温度符合要求;HPMC浓度越高,药物释放越快,8.0%HPMC和8.0%P407混合后,胶凝温度和缓释效果均符合实验要求。结论筛选出的处方中大大降低了P407的浓度,同时胶凝温度和缓释效果均符合实验要求,该温敏性凝胶具有良好的温度敏感性,制备方法简单可行。
OBJECTIVE To prepare polodimethamine-sensitive sustained-release in situ gels with poloxamer 407 (P407) as the basic material and investigate its in vitro dissolution behavior. Methods The gel was prepared by cold-solution method. The gelation temperature was used as an index to investigate the influence of P407 and other adjuvants F188, PEG1500, HPMC and MC on the gelation temperature. Release behavior, and determination of drug content in the dissolution solution by HPLC to screen better prescription. As a result, the gelation temperature decreased with the increase of P407 concentration. When the concentration of P407 was less than 15%, the phase transition did not occur. The addition of F188, PEG1500 and MC could not produce the desired gels. 8.0%, 8.5% The gelling temperature of 9.0% HPMC mixed with 8.0% P407 respectively meets the requirements. The higher the concentration of HPMC, the faster the drug release. After the mixture of 8.0% HPMC and 8.0% P407, the gelation temperature and sustained release effect meet the experimental requirements . Conclusions The concentration of P407 was greatly reduced in the prescriptions, and the gelation temperature and sustained-release effect were in line with the experimental requirements. The temperature-sensitive gel has good temperature sensitivity and the preparation method is simple and feasible.