Effect of additives on dissolution and swelling of soybean lecithin microcapsules prepared using the Wurster process.
Microcapsules whose membranes contained soybean lecithin (SL), cholesterol (CH), stearic acid (SA) and polyvinylpyrrolidone (PVP) at various compositions were prepared. Then, dissolution and swelling behaviors of the microcapsules in a 0.9% saline solution were studied to be related to the phase diagram of three components containing 42% of PVP in anhydrous state. In the aqueous solution, when an anhydrous microcapsule membrane was composed of SL not saturated with both CH and SA, the microcapsules showed rapid release of carbazochrome sodium sulfonate (CCSS, a model drug), poor particle-swelling and spouting of droplets containing CCSS. Long-delayed release of CCSS and drastic particle-swelling with no spouting of droplets were observed when the anhydrous membrane was composed of SL saturated with both CH and SA and the composition was not close to the two-component line, CH-SA, or to the saturation line. The spouting of droplets would be attributable to the CH and/or SA-poor SL phase and to the SL phase which dissolved CH and SA, but contained either CH or SA only in a small amount, and the delayed release would be due to the CH and SA-rich SL phase dissolving a great amount of CH and SA formed by hydration. The degree of release suppression and particle-swelling depended on the SL content. At 20-45% of SL content, the prolonged-release, great particle-swelling and no spouting of droplets at the early stage were observed only when the CH and SA-rich SL phase formed by hydration contained a high content of CH and SA.
Jono
K
K
Faculty of Pharmaceutical Sciences, Kobe Gakuin University, Japan.
Ichikawa
H
H
Fukumori
Y
Y
Kanamori
R
R
Tsutsumi
Y
Y
Murata
K
K
Morimoto
A
A
Nakamura
K
K
D000323:Adrenochrome / Q000031:analogs & derivatives* / Q000737:chemistry; D002214:Capsules; D002784:Cholesterol / Q000737:chemistry*; D003692:Delayed-Action Preparations; D004339:Drug Compounding; D016503:Drug Delivery Systems; D006490:Hemostatics / Q000737:chemistry; D010316:Particle Size; D010713:Phosphatidylcholines / Q000737:chemistry*; D011205:Povidone / Q000737:chemistry*; D012995:Solubility; D013025:Glycine max; D013229:Stearic Acids / Q000737:chemistry*
D002214:Capsules; D003692:Delayed-Action Preparations; D006490:Hemostatics; D010713:Phosphatidylcholines; D013229:Stearic Acids; C031183:stearic acid; D000323:Adrenochrome; C073338:carbazochrome; D002784:Cholesterol; D011205:Povidone