| Osteoarthritis is a common disease,brings unbearable pain and heavy economic burden to the patients.When use drugs to treat the type of disease,the drugs by oral often shows strong toxicity to the gastrointestinal tract and renal.In recent years,transdermal patches rise gradually because the drugs in the patch are absorbed directly into the circulation system through skin capillaries,which can avoid the first-pass effects of drugs in liver and intestine in the absorption process and greatly reduce the side effect and the damage to human body.Zushima has anti-inflammatory and analgesic effect and commonly used in the treatment of arthritis in clinical.Related studies showed that coumarins were the active ingredients.In this paper,active ingredients in Zushima herbs were extracted with different solvents and then the raw extracts were separated by using silica gel column chromatography,thin layer chromatography,liquid chromatography and other modern separation techniques.High Performance Liquid Chromatography(HPLC),Ultraviolet chromatography(UV),Liquid Chromatography and Mass Spectrometry(LC-MS)and Nuclear Magnetic Resonance Spectroscopy(NMR)were used to determine the structure of the obtained compounds.A few compounds were obtained and mainly of them were coumarins,such as daphnetin,daphnin,daphnetin-8-O-?-Dglucoside.The three components obtained were pure enough to be used as standard matreials in the subsequent studies.Orthogonal experiment was designed and used to optimize the preparation process of Zushima patch.The optimum process was determined as follows: 20 g of sodium polyacrylate,10 g gelatin and 2 g aerosil were mixed and 30 g glycerin was added give the A phase;extracts of Zushima was suspended in water to give the B phase;the B phase was then poured into the A phase,the traditional Chinese molding machine to used to suppress experimental drug mixture to give a flat patch,divided the patch into small ones of 8cm×10cm.In vitro drug release behavior of the Zushima patch was studied in order to investigate the drug bioavailability of the patch and control the drug quality.Twomethods were adopted to study the release pattern: one is determining the drug release of three index components of patch(daphnetin,daphnin,daphnetin-8-O-?-D-glucoside)by using HPLC.The second method is measuring the amount of total coumarin constituents that released from the patch with UV analytical method.In both cases,the type of release media and speed were screened to optimize the process.Saline was found to be the suitable release medium and the best volume is 900 ml with a speed of100r/min.Results showed that the first method is much better than the second one in view of specificity and stability,sensitivity and repeatability.The reproducibility and recovery of the first method was found to be conformed with the requirements of the Pharmacopoeia and can be used to study the drug release pattern of the patch.The second method of using ultraviolet spectrophotometry to study the release of total coumarin of patch is easy to operate.The reproducy,reproducibility and recovery of the method can meet the requirements of the pharmacopoeia but the stability and precision are not as good as the HPLC method.Therefore,the HPLC method was selected to be the analytical method to determine the release behavior of Zushima total coumarin from the patch,which can also be used for the quality control of the patch. |
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