Preparation of sustained-release nitrendipine microspheres with Eudragit RS and Aerosil using quasi-emulsion solvent diffusion method.
Sustained-release nitrendipine microspheres were prepared in liquid system by quasi-emulsion solvent diffusion method, in which the Aerosil was employed as an inert dispersing carrier to improve the dissolution rate of nitrendipine, and Eudragit RS as a retarding agent to control the release rate. The resultant microspheres were evaluated for the recovery, bulk density, average particle size, drug loading, and incorporation efficiency. And the factors affecting the formation of microspheres and the drug-release rate were investigated. It was observed by a scanning electron microscope (SEM) that the microspheres were finely spherical and uniform, and no entire nitrendipine crystals were observed visually. The results of X-ray diffraction indicated that nitrendipine in microspheres was disordered, suggesting that nitrendipine was highly dispersed in microspheres. The drug loading of microspheres was enhanced with increasing the ratio of drug to excipients, and the incorporation efficiency was always >90%. The formation of microspheres was mainly influenced by the amount of bridging liquid and sodium dodecyl sulfate (SDS) in poor solvent. The dissolution profiles could be modulated with adjusting the amount of retarding agent and dispersing carrier formulated.
Yang
Ming shi
Ms
Department of Pharmaceutics, School of Pharmaceutical Science, Shenyang Pharmaceutical University, No. 103, Wenhua Road, Shenyang 110016, China.
Cui
Fu de
Fd
You
Ben gang
Bg
Fan
Yu ling
Yl
Wang
Liang
L
Yue
Peng
P
Yang
He
H
D000096:Acetone / Q000737:chemistry; D000180:Acrylic Resins / Q000737:chemistry*; D003460:Crystallization; D003692:Delayed-Action Preparations; D004655:Emulsions; D005079:Excipients / Q000737:chemistry; D007700:Kinetics; D008752:Methylene Chloride / Q000737:chemistry; D008855:Microscopy, Electron, Scanning; D008863:Microspheres; D009568:Nitrendipine / Q000008:administration & dosage / Q000737:chemistry*; D010316:Particle Size; D012822:Silicon Dioxide / Q000737:chemistry*; D012967:Sodium Dodecyl Sulfate / Q000737:chemistry; D012995:Solubility; D013696:Temperature; D014961:X-Ray Diffraction
D000180:Acrylic Resins; D003692:Delayed-Action Preparations; D004655:Emulsions; D005079:Excipients; D000096:Acetone; C050528:Eudragit RS; D012967:Sodium Dodecyl Sulfate; D008752:Methylene Chloride; D012822:Silicon Dioxide; D009568:Nitrendipine