Studies On Lansoprazole Tablets

Lansoprazole is a second proton pump inhibitors(PPI),it has already widely used in the digestive function disorder diseases relevant to acid secretory arround abroad.To prepare Lansoprazole as pattern drug in this paper, on the basis of investigating the characters of Lansoprazole and various ingredients,it was used Mannitol、Microcrystalline cellulose for filler;Meglumine、Poloxamer for solubilizing agent;Sodium sulfite、Sodium carbonate for stabilizing agent;Carboxymethylstarch sodium for disintegrant;8% Opadry solution for isolation gown;Eudragit L30D-55、Tween 80、Glycerin monostearate and Polyethylene glycol 6000(PEG 6000) for coating material;water for coating solution,made of Lansoprazole enteric-coated tablets.The effect of filler、stabilizing agent、disintegrant layer on drug release in the pH6.8 phosphate damping fluid were researched. And the effect of different weight addition of isolation gown layer on the related substance of Lansoprazole enteric-coated tablets were investigated. And the effect of different weight addition of enteric coated layer on drug release in the O.1mol·L-1 HCl and the pH6.8 phosphate damping fluid were also investigated. It was shown that the release and stability of the drug was selected to estimate index in the pH6.8 phosphate damping fluid, optimize and screening the best formula technology of tablet core and coating solution were obtained finally.The effect of different solubilizing agents layer on drug dissolution were researched in the paper, and the effect of different disintegrants layer on drug dissolution and stability were investigation;It was shown that Meglumine and Poloxamer could obviously raise drug dissolution; and CMS-Na could obviously raise drug dissolution and disintegrant.Meanwhile,as it was instability in the acidity surrounding,some organism amines substance could obviously raise the stability in the formula,so add Sodium carbonate can obviously raise drug dissolution and stability.Base on the formula of Lansoprazole tablets core, determine the best formula of isolation gown and enteric coated by investigation coating material and coating weight addition,made the preparation releasing 2.2% in 2 hours in acid liquor and releasing 92.6% in pH6.8 phosphate damping fluid.The result of stability study show that Lansoprazole enteric tablets is well of stability at conditions of high temperature% moist and light.Accelerate and long-term test show Lansoprazole can placement long-term.Consideration the stability of self-made and market Lansoprazole tablets, test result show the stability of self-made Lansoprazole is better than market.With the commercial Lansoprazole tablets as the reference, the in vivo pharmacokinetics of self-prepared Lansoprazole tablets was studied with 18 people. Double-cycle and double-crossover tests was designed and LC-MS/MS method was employed to detect the blood drug level in people administered with single dose. Compared to the commercial Lansoprazole tablets, the relative bioavailability of the self-prepared Lansoprazole tablets is (108.4±40.3)%.