The Kadsura Microemulsion Oral Liquid Pharmaceutical Research

NanWeiZi is the dry ripe fruit of Magnoliaceae plant HuaZhongWuWeiZi (Schisandra sphenanthera Rehd. Et Wils. ). Pharmacological studies show that its lignans has strong capability of cutting down the concentration of aminopherase in plasma, liver protection role. But its lignans is hydrophobic,so its oral absorption bioavailability is poor,which limits its clinical application. Microemulsion delivery systems developed in recent years is a new type of drug delivery system which is a good carrier for hydrophobic drugs, to increase the solubility of hydrophobic drugs ,to enhance its oral absorption bioavailability. Based on the prescription of "WuZi capsule" in national drug standards, this project aimed at the property of the lignans part, and systematically studied the extraction, separation and preparation procedure of the microemulsion,as a result, the microemulsion oral solution with beter quality has been made.Based on "Chinese Pharmacopoeia" 2005 editon 1st part, TLC was done to distinguish NanWeiZi and the content of Schisantherin A was determined by HPLC. In addition, HPLC method has been adopted to measure the content of deoxyschizandrin, ultraviolet spectrophotometry method has been adopted to measure the content of total lignans, and the according limits have also been formulated.Taking the contents of total lignans and deoxyschizandrin as the evaluation indexes, the procedure of extraction, separation and concentration was studied with orthogonal test and mono-factorial test. The more efective technology was to decoct with 8 times amount of water, 1.5h, filtrate, abandent the filtrate, gruffs drying (60℃to 70℃), crash to extreme coarse powder, extract with 10 times amount of 70% alcohol, 1h, two times, filtrate and collect filtrate, recycle alcohol and concentrate the filtrate to extractum which 1ml contain 1g herbs, the total lignans transfer rate of 88.77%,deoxyschizandrin transfer rate of 86.53 %.In the research on the microemulsion preparation technology, the optimized formulation of the microemulsion selected by pseudo tertiary phase diagrams. The procedure of preparation is to mix the extraction of NanWuWeiZi 4.5g, RH40 220g, glycerin 110g,IPM 30g together,add water to about 1000ml, add sorbic acid 2g, add water to 1000mK mix uniform. The range of particle size is 30 to 50nm. Influencing factor test showed that the preparation has good stability on the temperature, light, salinity, pH, etc.In the research on quality evaluation study of preparation, ultraviolet spectrophotometry method has been adopted to measure the content of total lignans ,HPLC method has been adopted to measure the content of deoxyschizandrin, and to formulate corresponding limits. Meanwhile, the exterior character and particle size check of the microemulsion and other regular check related to oral solution have also been done. The results indicate that the quality of this oral solution is stable and controllable.Preliminary stability test show that the exterior character, particle size, relative density, pH, drug content of product stored at room temperature for 3 months had no significant difference, particle size...