Study On Application Of Moisture-proof Excipients To Traditional Chinese Solid Preparations

Traditional Chinese solid preparations are the main form of modern Chinese medicine preparations. Traditional Chinese medicine (TCM) pure extract preparations of extraction and separation exist easy moisture absorption. The moisture absorption results in the solid drugs soften, the change of chemical composition and mold, which affects the quality and effect of drugs and brings difficulties to the production and storage. The moisture absorption has always been a general difficulty. In the actual production, for extraction and refining process of preparation change inconveniently,it is particularly important to screen the kinds and amount of the excipients for reducing hygroscopicity.This thesis focused on moisture-proof excipients. Effective component was choosed as a model drug to explore the suitability of hygroscopic TCM.In early experiments, hygroscopicity of polysaccharides and saponins from astragalus, bupleurum, ginseng were compared respectively.The result was that polysaccharides were more hygroscopic than saponins. Astragalus polysaccharide (APS) which was the most serious hygroscopicity was selected as a model drug.By consulting related literature and previous experimental experiece, this thesis investigated the moisture-proof function of 14 kinds of excipients. Pure excipients and the powders mixed with APS were at 75% relative humidity and 25℃for 7 days,to measure relative humidity of every mixture, then draw the moisture absorption curve and extract characteristic parameters.Preliminarily screen excipients and determine ratio between drug and excipients. The result was lactose,β-CD, CaHPO4, mannitol, MCC by 1:1 ratio with APS. Adopting mixture design with Design Expert optimized the most excellent combination of excipients. There were the better ratio of 11 groups.The best one was lactose, MCC and CaHPO4 by 0.297:0.503:0.200 ratio.Forming excipient of ordinary granule was dextrin. The moisture-proof excipients of effective component were applied to astragalus and Dangguibuxue prescription which were made of granules. Adjustment process was for the appropriate moisture-proof excipients by hygroscopicity, formability and appearance. Moisture absorption characteristics of ordinary granule, moisture-proof granule,the powers of different formula and different preparation. The result showed that drug added moisture-proof excipients could effectively reduce the moisture absorption and improve the appearance, compared with drug added ordinary excipients. The thesis summarized the suitability of Single herb and TCM preparation adopting effective component's moisture-proof excipients.