Study On Sustained-release Tablet Of 407

407 is a kind of alkaloid that was extracted from the plant by the pharmaceutical specialist of our country and its physical and chemical feature is stable. The tablet of 407 has been recorded by pharmacopoeia of China. But now that its therapeutic and lost concentration is much similar, therapeutic result of drug can only maintain about 2 hours. At the same time 407 ceases pain, it has a strong hypnotic impact. Consequently some valetudinarians are inconvenient to take it in the daytime. For many yeas, 407 has been confined to take in any degree in the hospital. Now, common tablet sale on the market, its dose is 30mg/tablet, three times one day, but takes it inconveniently. Study on sustained-release tablet of 407 might not only cease to pain in the night that was given rise to cancer, toothache, menstrual pain and so on, but also enhance their quality of sleeping, reduce valetudinarians to take drug frequently, specially take out serious phenomena of "valley". Therefore, the safety, availability and adaptation of drug might be enhanced obviously. And than the sustained-release tablet of 407 has not been reported in the national and international literature, if successfully, we may apply on the monopoly.In order to enhance drug's therapeutic effect permanently and rapidly, we develop sustained-release tablet of 407 that includes in rapid-released slice and sustained-releaseslice. In this article, the sustained-release slice were based on HPMC, the rapid-release slice were based on cross-PVP. Some factors that may affect the drug dissolution, such as particle size of 407, granule size, hardness and amount of HPMC or L (+)-Tartaric acid were studied. It was shown that particle size of HPMC and 407, granule size, hardness has little effect on drug dissolution, but the amount of HPMC and L (+)-Tartaric acid affected dramatically. On the basis of single factor test, the better formulation and preparing technique were optimized through orthogonal design and dissolution behavior was also investigated. In this study a UV spectrum method to assay the amount of 407 released from the preparation in simulated gastric fluid and distilled water was established, and established the released mode of drug in vitro. A method of HPLC detect for the quantitative analysis of 407 in beagle dog plasma was set up with codeine as internal standard. Pharmacokinetic parameters were managed using 3p87 Pharmacokinetic program.Single factors test shows that particle size of HPMC and 407, granule size, from 60 to 120 mu, hardness from 40 to 60 mu, have little effect on drug dissolution. The more amount of HPLC, the less amount of drug dissolved. The best suitable amount of L (+)-Tartaric acid is 30mg each tablet. The formulation and preparing technique were optimized through orthogonal design.In this study a UV spectrum method to assay the amount of 407 released from the preparation in simulated gastric fluid and distilled water was established. And the result indicated that the drug dissolution from the preparation was pH-independent. Sustained-released tablet of 407 of test result in vitro show:1 The amount of HPMC in the recipe has effect on discharge dramatically. The better recipe is that HPMC is forty percent, L (+)-Tartaric acid is twenty percent in the whole. The mode of drug release in vitro was suitable for Higuchi program, r=0.9921.2 The hardness and speed of basket has little effect on drug dissolution; by reason that goes into L (+)-Tartaric acid in simulated gastric fluid and distilled water, the drugdissolution from the preparation was pH-independent.3 According to our lab condition, a method of HPLC detect for the quantitative analysis of 407 in beagle dog plasma was set up with codeine as internal standard. The standard curve was linear in the range of l-250um/ml, r=0.9321,n=5.the lowest detection define is 300ng/ml, and suitable for test demand.Pharmacokinetic parameters were evaluated in vivo in 6 beagle dogs with 407 common tablets as reference standard. The data were managed using 3p87 Pharmacokinetic...