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本文以孕二烯酮(gestodene,GEST)为模型药物研究储库型阴道环药物释放的影响因素。采用注塑成型法制备孕二烯酮储库型阴道环药芯,加热硫化法包裹控释膜,通过单一变量法,以21天的释放行为作为标准考察影响药物释放的因素。当改变外层控释膜的厚度时,随着控释膜厚度的增加,相对突释,即第一天的释药速率与平均日释药速率的比值逐渐趋于1。当膜厚为1.25 mm时,相对突释为1.04;在一定范围内,药物的平均释放速率(Q/t)与载药量(A)呈正比关系(r=0.992 2);实验考察了C6-165和Q7-4765两种膜材对药物释放的影响,结果发现药物溶解度高的C6-165膜更易实现对药物的控释;药物的形态影响其释放行为,结晶型粉末状态的药物更能有效地实现药物的控释;在相同载药量的前提下,对含1/1、1/2和1/4药芯的阴道环进行释放考察,结果显示三者的相对突释分别为1.93、1.87和1.76,1/4嵌段型阴道环更易实现控释。以上研究结果提示,孕二烯酮储库型阴道环可通过调整控释膜厚度、载药量、控释膜材料、药物分散状态、处方添加物组成及阴道环结构来控制药物释放行为,以达到理想的药物控释。
In this paper, gestodene (gestodene, GEST) as a model drug to study the reservoir-type vaginal ring drug release factors. Geminigenin reservoir vaginal core was prepared by injection molding method, and the controlled release film was wrapped by heating and vulcanization method. The single factor method was used to investigate the factors influencing drug release by taking 21 days as the standard. When the thickness of the OTC film was changed, with the increase of the thickness of the controlled release film, the relative burst release, that is, the ratio of the drug release rate on the first day to the average daily drug release rate gradually became 1. When the thickness was 1.25 mm, the relative burst was 1.04. The average release rate (Q / t) and the drug loading (A) were proportional to the drug release rate (r = 0.992 2) within a certain range. -165 and Q7-4765 two kinds of membrane material on the drug release, the results found that high drug solubility of C6-165 membrane more easily controlled release of drugs; the shape of the drug affect its release behavior, crystalline powder state of the drug more Effectively controlled release of the drug; the release of the vaginal ring containing 1/1, 1/2 and 1/4 of the drug core under the same drug loading, the results show that the relative burst of the three were 1.93 , 1.87 and 1.76, 1/4 block type vaginal ring more easily controlled release. The above results suggest that Gestodene reservoir-type vaginal ring can control the drug release behavior by adjusting the thickness of the controlled release film, drug loading, controlled release membrane material, drug dispersion status, prescription additive composition and vaginal ring structure to Achieve the desired drug controlled release.