Preparation and in-vitro drug release of Baizhu Huanglian pellets containing colon-targeting capsules / 药学实践杂志

Objective Colon-targeting capsules based on gastric pellets and enteric pellets were prepared from Baizhu Huanglian prescription. The formulation composition and preparation process were optimized and the in-vitro release characteristics were investigated. Methods Optimum formulation composition and process parameters of Baizhu Huanglian pellets were screened out by single factor experiment and orthogonal design. The pellets core were prepared by extrusion-spheronization technique and coated in the fluid bed using bottom spray coating technique. To investigate the effect of coating level of the isolation layer, the proportion of polymer, the amount of plasticizer and weight gain of enteric coating on the release behavior of the enteric pellets. The pellets release behavior was fitted by model as well. Results The prescription of gastric pellets was drug loading 50%, PVPP 5%, MCC to lactose 1∶2 and wetting agent 40%. The process parameters were extrusion frequency 20 Hz, rounding speed 500 r/min and rounding time 5 min. The prescription of enteric pellets was drug loading 27%, PVPP 5%, MCC to lactose 5∶2, wetting agent 30% and adhesive 20%. The process parameters were extrusion frequency 20 Hz, rounding speed 700 r/min and rounding time 7 min. For enteric coating layer, the coating mixture of EUDRAGIT®L30D-55 to EUDRAGIT® FS30D was 1∶2. The amount of plasticizer was 10%. The increased weight of coating layer was 15%. The release time of enteric pellets in-vitro was up to 24 hours. The release behavior of the pellets conforms to the Higuchi model. Conclusion The colon targeting capsule of Baizhu Huanglian pellets were successfully prepared and showed the characteristics of sustained release and colon targeting.

Improvement on the tableting properties of traditional Chinese medicine extracts by fluid-bed coating and pore forming / 药学学报

This paper aimed to study the effect of combined co-processing of coating and pore forming on the tableting and tablet properties of traditional Chinese medicine (TCM) extracts together with its applicability. Four TCM extracts were co-processed using fluid bed with hydroxypropyl methyl cellulose (HPMC) as coating agent and ammonium bicarbonate (NH4HCO3) as pore-forming agent. Powder properties (such as particle size and size distribution, bulk density, tap density, moisture content) and tablet properties (including tensile strength, compaction ratio, fast elastic stretch, and disintegration time) were measured and compared among the powders. Scanning electron microscopy (SEM) was applied to characterize the surface of particles and tablets. Results showed that the particle size, flowability, and compactibility of the composite particles with HPMC were superior to the parent powders of TCM extracts. These properties of the porous particles with HPMC and NH4HCO3 showed further improvements. In addition, the addition of HPMC prolonged the disintegration time of tablets, whereas the pore-forming effect of NH4HCO3 could shorten the disintegration time. SEM revealed the changes in the morphology of the composite particles and the pores on the surface of the porous particles and tablets. In conclusion, co-processing with HPMC and NH4HCO3 could improve the powder and tablet properties of TCM extract powders, and this method shows certain applicability, which provides a feasible choice for improving the tableting properties of some TCM extract powders.

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 and in vtro Release of Dexketoprofen Enteric-coated Pellets / 中国药师

Objective:To prepare dexketoprofen enteric-coated pellets and explore the drug release rate respectively in 0. 1 mol· L-1 hydrochloric acid and phosphate buffered saline(PBS,pH 6. 8). Methods:Dexketoprofen enteric-coated pellets were prepared u-sing fluid-bed coating technology, the blank sugar pellets were coated with drug layer, isolation layer and enteric layer in order. Drug-loading rate as the index, the optimal concentrations of HPMC and drug were screened. Such indicators as adhesion, pellet uniform and surface color as the indices, the coating process was optimized by orthogonal experiment. Drug release in PBS of the enteric-coated pel-lets and the common enteric-coated tablets were compared. Results:The prepared pellets showed the properties of uniform drug load-ing, high drug-loading rate, complete round shape and lustrous appearance. The concentration of HPMC and drug was 5% and 15%, respectively. The optimal coating process was as follows:the material temperature was 36℃, the atomization pressure was 1. 0 bar and the airbrush rate was 0. 8 ml·min-1 . The drug release of the pellets in hydrochloric acid was below 10% in 2 hours, while the release in PBS was greater than that of the common enteric-coated tablets. Conclusion: The prepared enteric-coated pellets are feasible in technology, and exhibit satisfactory acid endurance and drug release in vitro.

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.