The Study Of Xiatianwu Alkalods Microporosity Osmotic Pump Tablets

The total alkaloids is the main active substance of Xiatianwu. It includes more than20kinds of tertiary amines and quaternary ammonium alkaloids, such as protopine and tetrahydropalmatine. Pharmacological studies show that Corydalis total alkaloids has the effects of inhibition of thrombosis, platelet aggregation, dilation of cerebral blood vessels and lower extremity vascular, analgesic, anti-inflammatory, anti-cholinesterase activity.It can be clinically used to treatment stroke hemiplegia caused by Hypertension and cerebral vascular disease. And it also has good effects on rheumatoid arthritis, sciatica and sequelae of infantile paralysis. Now there has been ordinary tablet of Xiatianwu listed. But its bioavailability is low, the patient should be frequent dosing, and prone to "peak and valley" phenomena. Therefore, the subject uses homemade total alkaloids to develop into microporosity osmotic pump tablet, which is in order to reduce the "peak an valley" phenomenon, and improve drug safety, effectiveness, applicability and controllability.This experiment used the acid dye colorimetry as the total alkaloids determination method. This method is specific, accurate and reliable, convenient, and can well satisfy the requirements in the analysis of experimental study.To meet the demand of raw material preparation, total alkaloids and protopine were taken as the index.We adopt the orthogonal experimental design to optimize the extraction process.Then we chose a suitable macroporous resin for separation and purification of total alkaloids from Xiatianwu, and studied its process conditions. The experimental results showed that the screening process is simple and feasible. In addition, we set up the quality standard of total alkaloids extract which can satisfy the osmotic pump controlled release tablet production demand.This paper used single-factor test method to investigate the types of filler, the dosage of penetration enhancer, the variety and dosage of retardant, the dosage of solubility regulator, the dosage of plasticizer DBP, the dosage of PEG400, and the coating thickness, which have effect on of the drug release. In addition, the subject adopt f2similar factor method to evaluate the in vitro release behavior of the osmotic pump tablets. Though this, we found the main factors of influence on drug release, which were NaCl’s dosage, the dosage of PEG400and coating agent thickness. Then, we took the cumulative release percent in2,6,12h and the linear correlation coefficient of0to12h cumulative release curve as evaluation index, and used the CCD-RSM for selecting the optimal prescription. Through the comparison of predicted and measured, it indicated that the model has good prediction. By model fitting, the release of optimization prescription was proved to follow zero-order release kinetics.