The Study Of Colon-targeted Tablets With Total Flavonoids From Euphorbia Humifusa (EFCTT)

Chronic nonspecific Ulcerative colitis (Ulcerative Colitis, UC) is a kind of the digestive system of common diseases and mainly damages the rectum and flexible, even can invade and other parts of the colon or the whole colon. Its clinical symptoms are the abdominal pain, diarrhea, having blood in one’s stool, and will take pus kind, defecate is not normal intestinal organs. The development of this disease is generally chromic, repeated and alternating episodes of a longer course, so it has been regarded as one of the modern hard diseases to cure by the World Health Organization (WHO).Oral Colon Targeting Drug-delivery System (OCTDS), is a kind of the systems of drug delivery technology,which the drugs does not release in the upper digestive after making drugs through the oral administration, but begins to collapse or erode and release drugs when they arrive at the ileocecum of the human, so that the drugs in the human body can play the role of local or systemic treatment.Euphorbia humifusa is a kind of euphorbiaceae plants and its effective components are the tannins and the flavonoids. By pharmacological research proves, quercetin, mountain endure element of flavonoid compounds used in such as ulcerative colitis (UC), and its function is better than HuangLianSu or some antibiotics and non-toxic side effects. If we make it into the colon drugs, it can release its active ingredients directly to the pathological parts and improve the local drug concentration, can increase the curative effect and reduce drug dose. At present, there are a lot of Chinese and western medicines to treatment the ulcerative colitis, but there is not any drugs with better orientation and medication large even the shortcomings of low and so on, so combining the actual situation of traditional Chinese medicine and western medicine preparations of existing design principle, making euphorbia humifusa into PH control and enzyme solution control colon targeted drugs of both control, so as to ensure the drug to release effectively in proper positioning.Use skeleton controlled release technology, so as to avoid colon-targeted drug’s existing problems,such as row piece or sudden release problem, even it will provide certain reference for the studying in effective components for traditional Chinese medicine colon drug delivery system.Based on the investigation of the methodology, then we referenced with the China Pharmacopoeia and established the methods of the colon-targeted tablets with Total Flavonoids from Euphorbia humifusa (EFCTT) to determinate contents and measure contents in the vitro release degrees with the index component of the quercetin from Euphorbia humifusa. The method is simple, reliable, and can be used as the preparation of standard quality determination, at the same time this method is a convenient method in evaluation for the preparation inherent quality.This paper used single-factor test method to investigate the influence factors of the heart of prescription and coating prescription, then using the digestive tract simulation of in vitro release and regard the accumulation of quercetin release degrees as an index, so that test the coating tablets in three release mediums. At last, we induced the significant influence releases of drugs were the factors of polysaccharide-pectin dosage, disintegrating agent of L-HPC dosage and the coating thickness.Then the design Expert software was used to fit multivariate linear models and quadratic multinomial models for experimental data. Finally we choose arbitrarily a prescription from the best prescription range, and make an on-the-spot investigation of the preparation in vitro release investigation by the use of three release test methods of the digestive tract simulation of preparation of in vitro release test, enzyme in vitro release of simulation test and rats content of digestive tract simulation and so on.This paper established the preparations of the preliminary quality standards and Preliminary stability results. The results show that in the6months, this preparation has been no significant change in quality, so its quality is basic stable.Finally this paper established the body of pharmacokinetic studies using high performance liquid chromatographic method, which is determined by the blood drugs concentration. We regarded the Total Flavonoids from Euphorbia humifusa ordinary tablets as the CST preparations, and then conduct the pharmacokinetic preliminary study on the homemade EFCTT in the rabbit body. The results show that the colon-targeted tablets with Total Flavonoids from Euphorbia humifusa (EFCTT) can release the drugs in the colon.