Preparation of sustained-release nitrendipine microspheres with Eudragit RS and Aerosil using quasi-emulsion solvent diffusion method
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Preparation of sustained-release nitrendipine microspheres with Eudragit RS and Aerosil using quasi-emulsion solvent diffusion method. / Yang, Mingshi; Cui, Fu de; You, Ben gang; Fan, Yu ling; Wang, Liang; Yue, Peng; Yang, He.
In: International Journal of Pharmaceutics, Vol. 259, No. 1-2, 2003, p. 103-13.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - Preparation of sustained-release nitrendipine microspheres with Eudragit RS and Aerosil using quasi-emulsion solvent diffusion method
AU - Yang, Mingshi
AU - Cui, Fu de
AU - You, Ben gang
AU - Fan, Yu ling
AU - Wang, Liang
AU - Yue, Peng
AU - Yang, He
PY - 2003
Y1 - 2003
N2 - 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.
AB - 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.
KW - Acetone
KW - Acrylic Resins
KW - Crystallization
KW - Delayed-Action Preparations
KW - Emulsions
KW - Excipients
KW - Kinetics
KW - Methylene Chloride
KW - Microscopy, Electron, Scanning
KW - Microspheres
KW - Nitrendipine
KW - Particle Size
KW - Silicon Dioxide
KW - Sodium Dodecyl Sulfate
KW - Solubility
KW - Temperature
KW - X-Ray Diffraction
M3 - Journal article
C2 - 12787640
VL - 259
SP - 103
EP - 113
JO - International Journal of Pharmaceutics
JF - International Journal of Pharmaceutics
SN - 0378-5173
IS - 1-2
ER -
ID: 44057254