| Danhong preparation is the complex prescription of traditional Chinese medicine,which is based on medicinal herbs including Danshen and Honghua extracts,used for promoting blood circulation and removing blood stasis in general.At present,the research and clinical application of Danhong preparation is mostly about Danhong injection.But some problems are exposed gradually over the years of its use, such as the instability of its effect, prone to generate adverse reactions,such as allergic reactions,phlebitis, severe diarrhea, liver damage and so on . As the composition of traditional Chinese medicine injection is complex, its security and compliance are small,we try to change Danhong Fufang preparation from injection into oral preparations.Orally Disintegrating Tablets is a new pharmaceutical dosage form. It has great value in the development and utilization of traditional Chinese medicine,especially in the treatment of emergency.In this project,we use two water-soluble components from the principal agent, Danshensu and Safflor yellow,adopting the raw materials of high purity.On the basis of the preliminary work screening of formulation,we improved the prescription process to produce Danhong orally disintegrating tablets,and has studied on its quality. Through the determination of plasma concentration,we compare the diversifies among the different ways of administration from the perspective of pharmacokinetics .The results can provide new methods and ideas to the transformation of Chinese medicine formulations, as well as the pharmacokinetic study of traditional Chinese medicine.To promote the development of the modernization of traditional Chinese medicine.Based on the preliminary study of prescription,we determine the best prescription process of Danhong orally disintegrating tablets,using single-factor Screening and orthogonal design method to screen accessories and optimize the process , the disintegration time in vitro for the main evaluation index, combined with the appearance of molding. We use MCC and CCNa as combined disintegrants,amount of 20% mannitol as filler, 4% protein sugar as correctant, magnesium stearate as lubricant added in the end.The method of direct compression is simple,without special equipment.The feasibility of its production is good.According to the 2005 edition of Chinese Pharmacopoeia, in combination with the characteristics of Orally Disintegrating Tablets,we determine the quality standards of Danhong Orally Disintegrating Tablets,in aspect of the disintegration time,hardness,assay and so on. Groups of test results showed that ,the tablets meet the requirements of the orally disintegrating tablets .The method is simple, stable and efficient, able to control the intrinsic quality of Danhong orally disintegrating tablets effectively.The plasma concentration of Danshensu and Hydroxysafflor yellow A in rat were assayed by RP-HPLC after administration. Use DAS2.0 processing software to deal with the datas of the blood drug concentration– time,and then compare the main pharmacokinetic parameters by the use of SPSS statistical software.The result of pharmacokinetics showed that, the plasma concentration-time of Danshensu in Danfang and Danhong fang Preparations after single dose oral administration in rats fitted one-compartment model,while intravenous fitted two-compartment model. After oral administration,the total clearance and the apparent volume of distribution of Danshensu has increased apparently in Danhong fang Preparation.Its absolute bioavailability is 49.08%(Danfang) and 56.53%(Fufang). The plasma concentration-time of HSYA in Danfang and Danhong fang Preparations after single dose intravenous administration in rats fitted two-compartment model. The other pharmacokinetics parameters have not change apparently.From the perspective of the safety and bioavailability of drugs,we can preliminary judge that, it is promising to make Danshensu into oral preparation.
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