Study On The Druggability Of Tibetan Medicine Berberis Cortex Extract

Diabetes and its complications belong to major difficult diseases. There is no confirmed drugs with the exact treatment of diabetic retinopathy so far, therefore the key to treat diabetic retinopathy is early prevention and treatment. "Jing Ni Sa Ku?diabetes?" is the characteristics dominant disease in Tibetan medicine. And diabetes specialist has been included in the key specialty of construction in 11th Five-Year of State Administration of traditional Chinese medicine. Tibetan Medicine Berberis Cortex?TMBC? is customarily used for the treatment of diabetes and its complications?such as diabetic retinopathy and other diabetic microvascular complications? in Tibetan medicine. Prevention and treatments of "Jing Ni Sa Ku?diabetes?" with TMBC were recorded in the Tibetan medicine classics, such as Yue Wang Yao Zhen, Yi Xue Si Xu, Jing Zhn Ben Cao and so on. And TMBC is also recorded in Chinese Pharmacopoeia and ministry of Public Health's Quality Standard-Tibetan medicine ?first volume? and other standards. Based on previous studies, TMBC can not only significantly reduce the blood glucose levels of model rats, but also improve the retinal vascular injury. Clinically, TMBC is always made into extract to treat eye diseases in Tibetan medicine. Research Group used the uniform design and integrated score, set the total alkaloids and the content of the total extract as the index to investigate the optimization process of extraction. This method of decoction can be available for preparation for Berberis Cortex cream in Tibetan clinical. Tt is necessary to carry out experimental research on druggability of TMBC, to play the clinical advantages and characteristics of preventing and curing "Jing Ni Sa Ku" disease in Tibetan medicine.Objectives1. Analyze previous data to lay a foundation for the researches of druggability of TMBC;2. Determinate Berbamine Hydrochloride Tablets to predict its absorption and utilization in vivo;3. Establish a content determination method of three alkaloids in TMBCC with HPLC and provide scientific basis for TMBCE in Clinically;4. Select purification process of TMBCE and provide material for preparations.Methods1. Analyze correlation based on pharmacological and chemical data of early researches;2. In order to know the physical and chemical properties of Berbamine, we determined the dissolution of Berbamine tablets bought from pharmacies and studied the n-oectanol-buffer solution systems/water partition coefficient of Berbamine.3. A good method with HPLC which is accurate and rapid was established to determine the contents of Palmatine, Jatrorrhizine and Berberine.4. Using macroporous resins to investigate the purification process of TMBCE which will for provide foundation for further studies of TMBCE.Results1. The correlation analysis shows that TMBC with the prospect of prevention and treatment of diabetic retionpathy and the mechanism of this action maybe concern with blocking the vicious circles between correlation factors ?PKC-?,HIF-1?,VEGF etc.? and DR' vasopermeability, which also provide scientific basis for Tibetan medicine clinical application and establish that alkaloids are the main components for diabetic retionpathy.2. Berbamine and Berberine has better absorption in intestinal than stomach and it is useful to improve their bioavailability to make oral dosage.3. The linear ranges for three alkaloids were 4.3886?87.7716 ?g·mL^-1 ?r=0.9997?,3.6649?73.2982 ?g·mL^-1 ?r=0.9998?,29.5994·591.9876 ?g·mL-?r=0.9999?. The average recoveries ?n=9? were 97.97% ?RSD=1.02%?,100.70% ?RSD=1.42%?,98.51%?RSD=0.86%?.The method is simple, accurate and has a good stability, can be used for the content determination in processed products of TMBC.4. The optimal purification technology was selected as type HPD100 macroporous resin, mass concentration of loading liquid is 0.3 mg·mL^-1 with loading speed of 1mL·min-1,4BV water washing first,7BV 40% ethanol solution with loading speed of 2mL·min-1, collecting the elution liquid, concentrating and drying it into powder, which is TMBCE with more than 50% alkaloids by UV and HPLC.ConclusionAlkaloids like Berberine in TMBC have a great preventive and therapeutic effect against diabetic retionpathy, which can be absorbed well in the location of intestinal. This article mainly studied on the druggability of TMBCE and provided basis for further study. The powder of TMBCE is the material for oral enteric preparation against diabetic retionpathy and provides basis for further study.