| The total coumarins in Daphne giraldii are the main active substance of Daphne giraldii. It including daphnetin and Zushima B ect. Pharmacological studies showed that the total coumarins in Daphne giradii has the effects of anti-inflammatory and analgesic. In clinical.the preparation of Daphne giraldii has been widely used for sedation-analgesia and qufeng-desiccant.There have a lot of Daphne giraldii preparation and Daphne giraldii compound preparation been used for the treatment of rheumatoid disease, such as rheumatic arthritis, rheumatoid arthritis and rheumatism. Now there has been ordinary tablet of Daphne giraldii listed. But its bioavailability is low and frequent dosing, the patient could not adaptaby and prone to "peak and valley" phenomena. Therefore, the subject uses homemade total coumarins in Daphne giraldii to develop into microporosity osmotic pump tablet, which is in order to reduce the time of administration and avoid the "peak an valley" phenomenon, and improve the effectiveness, applicability and security of drugs..To meet the demand of raw material preparation in this experiment. Through the study of single factor test method and the orthogonal experimental to selection the best experimental conditions and macroporous for the separation and purification the total coumarins in Daphne giraldii. The experimental results showed that the screening process is simple and feasible, can satisfy the osmotic pump controlled release tablet production demand.In this experiment, established the method of determining release degrees and content of the microporosity osmotic pump tablets of total coumarins in Daphne giraldii and laid the foundation for prescription screening and preparations evaluation, the UV determination method established was Reliable and could be used as the standard for the quality determination.In this experiment used single-factor test method to investigate the compression method, tablet hardness, the variety of filler, the variety and dosage of penetration enhancer, the variety and dosage of retardant, the dosage of solubility regulator, the dosage of plasticizer DBP, the variety and dosage of pore-foaming agent, 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 proe-foaming agent and coating agent thickness. And to optimize the formulations of hawthorn leaves flavonoids microporosity osmotic pump tablets by a central composite design-response surface methodology and to fit the the optimum with the prescription0-level model, the primary model and the Higuchi model. Results show that the optimization prescription0-level model and zero-order release characteristics is significant. |