Study And Preparation Of Lansoprazole Orally Disintegrating Tablets

Objective:Lansoprazole is an antiulcer drug that inhibits the secretion of gastric acid.For any gastric acid secretion,Lansoprazole can inhibit it and has the ability to protect and promote the healing of gastric mucosal ulcer.Lansoprazole clinically commonly used as capsules and tablets,in which the disintegrating tablet has many advantages as a new type of preparation,it is a solid preparations that can rapidly disintegrate in the mouth or rapid dissolve.The purpose of this study was to use Eudragit as enteric coating materials to prepare pellets released from the intestine,and to develop a lansoprazole oral disintegration tablets for rapid disintegration in the oral cavity sheet.Methods:1 Preparation and screening of lansoprazole orally disintegrating tablets: Blank sucrose pellets were coated with drug-containing layer,isolation layer and enteric layer by fluidized bedside spray coating to prepare the intestinal releasing pellets and pressed.The evaluation index of each coating process is the drug loading rate and release degree.Then screen the best prescription.When coat drug coating layer,we use hydroxypropyl methylcellulose as the binder,the SDS as the solubilizer.The Magnesium carbonate is the acid-base regulator and the water is the solvent.We regard the drug-holding rate as the index,screening the best proportion of three kinds of supplementary material.When coat the isolation layer coating,we use the Opadry as isolation material,water as a solvent,and regard the releasing rate as the index to screen the best weight gain.When coat the enteric layer coating,we use the isolation micropellets as the basis,fine talc as anti-sticking agent,triethyl citrate as plasticizer,Eudragit as coating material,water as solvent,and regard the release as the index to inspect the best weight gain.In the whole coating process,we continually test and determine the best inlet temperature,atomization pressure,air volume,jet speed,material temperature and other process parameters.We press in accordance with the main content of medicine and determine the best ratio.2 Ispection and construction of the method of in vitro release and content of Lansoprazole: the method of UV detection of lansoprazole orally disintegrating tablets was established.And the method of HPLC was used to determine the content and content uniformity of lansoprazole.The main contents include chromatographic conditions,detection wavelength,specificity,system suitability,linearity and range,recovery rate,precision,repeatability and stability.We also inspect the release and the content of three batches of preparations.3 The inspect of the relevant substances of lansoprazole orally disintegrating tablets: We detect the sample with high performance liquid chromatography in the dark conditions,and record the chromatogram.The stability and disintegration of lansoprazole tablets were investigated by means of accelerated test and influencing factors.The appearance,content and in vitro drug release and related substances were taken as the index of the study.The stability test of lansoprazole includes high humidity test(90%±5% and 75%±5%),high temperature test(60°C±2°C and 40°C±2°C)and high light test(4500 Lx).Accelerated test was to place the formulation in an environment at a temperature of 40°C±2°C and a relative humidity of 75%±5%,and the stability was examined after 6 months.Results:1 The best prescription for the preparation of lansoprazole tablets is as follows:Drug coating layer solution:LS 20 gHPMC 8.0 gSDS 2.0 gMgCO3 0.2 gUse purify water as solvent,put 12.5 batches.The optimum process parameters are: inlet air temperature 43-56°C,inlet air volume 115-135 m3·h-1,material temperature 34-36°C,atomization pressure 1.9-2.1 kg ·cm-2,spray rate 14-18 r·min-1.Isolation layer coating solution:Drug pellets 200 gOpadry 60 gpurified water as solvent,coating weight gain of 30%.The optimum process parameters are as follows: inlet temperature 43-56°C,inlet air volume 115-135 m3·h-1,material temperature 34-36°C,atomization pressure 1.9-2.1 kg ·cm-2,spray rate 12-16 r·min-1.Enteric layer coating solution:Isolated pellets 200 gEudragit 267 gTEC 8 gTalcum Powder 19 gPurified water as solvent,coating weight gain of 50%.The optimum process parameters are: inlet air temperature 44-57°C,inlet air volume 115-135 m3·h-1,material temperature 36-37°C,atomization pressure 1.8-2.0 kg·cm-2,spray rate 6-10 r·min-1.Tablets pressed: Calculate the drug content,mix the protective layer pills,mannitol,cross-linked povidone and magnesium fumarate for 30 minutes.Then press the tablet(the content of 30 mg / tablets).The tablets were placed in a clear,colorless,flat-bottomed glass tube(with 2 centimeter diameter)containing 3 mL of water,and allowed to stand for two minutes.Observed with the naked eyes,there should be no sample fragments larger than 2 mm.2 HPLC method was established for the determination of lansoprazole palmitutide and the method of UV detection for the release of lansoprazole palmitutide.The method was verified and found that the excipients did not interfere with the main drug,so it is suitable for the determination of dissolution of liposomal tablets.Through the inspection of three batches of preparation content and release degree,the results meet the relevant requirements.3 HPLC method was established for the determination of the related substance of Lansoprazole.The method was verified and found that the impurities did not interfere with the main drug.Through the inspection of the relevant substances,the results meet the relevant requirements.The stability of lansoprazole was analyzed.The results showed that the color of lansoprazole was increased.And the cumulative release rate was also decreased.The results of high humidity test showed that lanazolizole was inoculated with moisture.The results of strong light irradiation showed that the stability of the drug was poor.Accelerated test results showed that lansoprazole orally disintegrating tablets of the indicators are relatively stable.Conclusions:The preparation process of lansoprazole was successfully developed,and the preparation process was simple and easy to operate.The reproducibility was good,and it was consistent with the in vitro release behavior of commercial tablets.The release and content of homemade lansoprazole mouth disintegration tablet are in line with the requirements,providing a strong guarantee for the study of the lansoprazole orally disintegrating tablets quality.Through the stability test,the lansoprazole orally disintegrating tablets are not stable in high temperature,high humidity and strong light environment,so long-term storage need environment low temperature,dry and dark conditions.