Preparation of lansoprazole biphasic release pellet capsules / 国际药学研究杂志

Objective To prepare lansoprazole biphasic release pellet capsules. Methods The pellets carrying lansoprazole were directly prepared by centrifugal making-pill method,and the pellets of enteric coating and enteric pulsatile coating were adopted by fluidized bed coating method. Then the two kinds of pellets were filled by a fixed proportion to hollow capsules. In vitro dissolution method was used for the observation of the drug release behavior. Results The optimized formulation was as follows:the magnesium carbonate level was 15%,the L-HPC level was 20%in pellets carried drug,the isolation gown level was 9%-10%,the enteric coating level was above 41%in enteric coated pellets,the swelling agent level was 50-60%,the controlled layer level was 50%,the enteric coating level was above 41%in pulsatile enteric coated pellets,and the drying time was 4 h in the end. Conclusion The method is feasible for preparation of lansoprazole biphasic release pellet capsules by encapsulating enteric-coated pellets,and able to obtain good repeatability and stable quality.

Preparation of Dexibuprofen Sustained-release Pellets and Analysis on Drug Release Behavior / 中国药房

OBJECTIVE:To prepare dexibuprofen sustained-release pellets,and to analyze the drug release behavior in vitro. METHODS:Centrifugal granulation powder layering-eudragit dispersion coating method was used to prepare dexibuprofen sus-tained-release pellets using 3%HPMC as adhesive agent. The formula of the pellets was optimized by orthogonal test with weight ra-tio of sucrose to dexibuprofen,weight ratio of HPMC to Eudragit NE30D and coating weight as factors,using 1,4 and 10 h accu-mulated release rate (Q) as index. The release of the drug from the pellets was analyzed. RESULTS:The optimized formulation was that the proportion of sucrose to drug was 1:10,the weight ratio of HPMC to Eudragit NE30D was 1.5:1,the increased weight of coating material was 8%. Q1 h,Q4 h and Q10 h of prepared pellets were 21%,57% and 89%,respectively(n=3). The co-rrelation coefficient of zero-order,one-order and Higuchi equation release model were 0.956 6,0.989 9,0.996 5. CONCLUSIONS:Prepared pellets show good sustained-release effect in vitro. Drug release of pellets is more in accordance with Higuchi equation.

Preparation of lansoprazole biphasic release pellet capsules / 国际药学研究杂志

Objective To prepare lansoprazole biphasic release pellet capsules. Methods The pellets carrying lansoprazole were directly prepared by centrifugal making-pill method, and the pellets of enteric coating and enteric pulsatile coating were adopted by fluidized bed coating method. Then the two kinds of pellets were filled by a fixed proportion to hollow capsules. In vitro dissolution method was used for the observation of the drug release behavior. Results The optimized formulation was as follows: the magnesium carbonate level was 15%, the L-HPC level was 20% in pellets carried drug, the isolation gown level was 9%-10%, the enteric coating level was above 41% in enteric coated pellets, the swelling agent level was 50-60%, the controlled layer level was 50%, the enteric coating level was above 41% in pulsatile enteric coated pellets, and the drying time was 4 h in the end. Conclusion The method is feasible for preparation of lansoprazole biphasic release pellet capsules by encapsulating enteric-coated pellets, and able to obtain good repeatability and stable quality.

Preparation of metoprolol tartrate sustained-release pellets by centrifugal granulation and the relative bioavailability in Beagle dogs / 中国药学杂志

OBJECTIVE: To prepare metoprolol tartrate sustained-release pellets and investigate the relative bioavailability in Beagle dogs. METHODS: Taking aspect ratio(AR), circularity, yield, friability, fluidity as key indexes, orthogonal design was atopted to optimize the formulation, and sustained-release pellets were prepared with Surelease. RESULTS: The optimal formulation was as follows: drug loading rate 90%, adhesive 40 mL·100 g-1, spheronization rate 30 Hz, coating weight gain 12%, and aging at 60°C for 2 h. CONCLUSION: The prepared metoprolol tartrate sustained-release pellets are bioequivalent with Betaloc in Beagle dogs.

Preparation of metformin hydrochloride pellets with centrifugal granulation technique / 西安交通大学学报(医学版)

Objective To prepare metformin hydrochloride pellets with centrifugal granulator by powder layering technique. Methods Metformin hydrochloride and MCC pellets were prepared by means of powder layering with the centrifugal granulation equipment and evaluated by yield percentage,angle of repose,bulk density,and friability. Results The preparation process parameters were optimized as follows: the ratio of metformin hydrochloride and lactose and MCC was 100∶5∶3,150 r/min rotating speed of the centrifugal granulation,20 r/min spraying serosity speed,25 r/min purveying powder speed,and the time of spheronization was 6 min.Metformin hydrochlorid pellets were prepared under the condition. Conclution The metformin hydrochloride pellets had good appearance,uniform granulation diameter,standard rigidity,good fluidity and did not have the structure of cage by means of detecting dissolubility.