Preparation and evaluation of drug release of compound aspirin and esomeprazole magnesium enteric-coated pellet capsules / 中国药学杂志

OBJECTIVE: To prepare compound aspirin and esomeprazole magnesium enteric-coated pellet capsules and evaluate the drug release in vitro/in vivo. METHODS: The aspirin pellet cores were prepared by using extrusion-spheronization method, and the esomeprazole magnesium-containing drug pellets were prepared with fluidized bed. By using fluidized bed coating method, the two kinds of drug-containing pellets were respectively coated with enteric layer to obtain enteric-coated pellets. After determining the loading capacity by measuring drug content, the two kinds of drug-containing pellets were filled into No.1 capsules. In vitro release was evaluated by measuring release percentage. The in vivo release behavior was evaluated by determination of pharmacokinetic parameters in rats. RESULTS: The cumulative release percentage of the two drugs was less than 5% in 2 h in 0.1 mol·L-1 hydrochloric acid solution. The cumulative release percentage of aspirin was more than 70% in 45 min in pH 6.8 PBS and it was more than 80% in 30 min for esomeprazole magnesium. Aspirin was metabolized to salicylic acid in plasma and its main pharmacokinetic parameters were as follows:t1/2=9.47 h, MRT0-∞=14.43 h, tmax=3.00 h, ρmax=51.34 mg·L-1, AUC0-24=703.39 mg·h·L-1, AUC0-∞=860.52 mg·h·L-1. The pharmacokinetic parameters for esomeprazole magnesium were as follows:t1/2=3.72 h, MRT0-∞=7.44 h,tmax=1.50 h, ρmax=2.71 mg·L-1, AUC0-24=11.89 mg·h·L-1, AUC0-∞=13.79 mg·h·L-1. CONCLUSION: The formulation of compound enteric-coated pellet capsules is reasonable, and the preparation technology has good reproducibility. The drug release is located in the intestinal tract, thus esomeprazole magnesium can antagonize the gastrointestinal side effects of aspirin and aspirin can produce better antithrombotic effect.

Preparation of esomeprazole magnesium enteric-coated capsules / 中国药学杂志

OBJECTIVE: To prepare and evaluate esomeprazole magnesium enteric-coated capsules which is compacted by multiple-unit pellet system (MUPS). METHODS: The esomeprazole magnesium enteric-coated pellets were prepared by fluid bed coating technology, and the effects of isolation layer, amont of core, and thickness of enteric-coated film on the quality of the product were e-valuated. RESULTS: The prepared esomeprazole magnesium enteric-coated capsules showed good release behavior in artificial gastric fluid. The dissolution in artificial intestinal fluid was rapid and complete. CONCLUSION: The established process of preparing esomeprazole magnesium enteric-coated pellets is feasible and reproducible, and the product has similar quality with the original preparation. It is expected to be used in the industrial production.

Preparation of Lansoprazole Enteric-coated Pellet Capsules / 中国药房

OBJECTIVE:To prepare lansoprazole enteric-coated pellet capsules(LECPC).METHODS:The lansoprazole enteric-coated pellets were prepared using fluid-bed coating technology through blank pellets being coated with main component layer,insulating layer and enteric layer in order.Enteric-coated pellets were encapsulated into hard gelatin capsules to obtain LECPC.Drug-loading rate and drug release in artificial intestinal fluid and artificial gastric fluid of 3 batches were investigated.RESULTS:The prepared pellets assumed complete round shape,lustrous appearance and coating well with mean drug-loading rate above 96%.The release of 3 batches in artificial intestinal fluid within 45 minutes were greater than (94.3?0.76) % while were smaller than (6.2?1.6)% in artificial gastric fluid within 2 hours.CONCLUSION:The prepared capsule is feasible in technology,reproducible and reliable in quality.It represents satisfactory release in vitro and property of resisting acid.