| Dimenhydrinate (DMH), a histamine H1-receptor antagonist, is widely used in the treatment of giddy ,irritability,pollenosis and urticaria. It has a little side-effects.Absorbrapidly and complete after taking orally.The result from 1516 minutes,function can last36 hours.The elimination half-life of orally administered dimenhydrinate is between 4and 6 hours. Protein binding is relatively high .The medicine is in the liver supersession mainly.Dimenhydrinate was chosen as a model drug, and was prepared of rapid disintegrated tablet in mouth. In order to avoid the disadvantages mentioned and enhance bioavailability, the dosage form of Dimenhydrinate was absorbed in mouth mucous that dissolves quickly on the tongue. Rapid disintegrated tablet in mouth without addition of water consists of little disintegration agent.The tablet was prepared by direct compression. The effects of different variables on the preparation of the tablet were studied according to the orthogonal design of experiments by the dissolution behavior of T50 and AUC0-2h. The result show that pH, stirring rate and temperature of the dissolving media could affect drug release. T50 was proportional to the percentage of microcrystalline cellulose(MCC) and disintergration agent in the carrier while other excipients were remain unchanged.A highly performance liquid chromatographic method was developed to determine DMH concentration in rabbit's and human plasma. Solid phase extraction was also employed in this experiment. Recovery and precision of this method were all excellent. The standard curve was linear in the range of 51000ng/ml of Dimenhydrinate in plasma.Pharmacokinetics and bioavailability were carried out in rabbits and in human after a single oral administration of Dimenhydrinate rapid disintergrated tablet and market tablet. In rabbits, Tpeak of rapid disintergrated tablet and market tablet were 0.90h and 2.28h respectively. The relative bioavailability of rapid disintergrated tablet against market tablet...
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