K. Jono et al., EFFECT OF ADDITIVES ON DISSOLUTION AND SWELLING OF SOYBEAN LECITHIN MICROCAPSULES PREPARED USING THE WURSTER PROCESS, Chemical and Pharmaceutical Bulletin, 45(12), 1997, pp. 2061-2075
Microcapsules whose membranes contained soybean lecithin (SL), cholest
erol (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 rela
ted to the phase diagram of three components containing 42% of PVP in
anhydrous state, In the aqueous solution, when an anhydrous microcapsu
le 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 c
ontaining CCSS. Long-delayed release of CCSS and drastic particle-smel
ling with no spouting of droplets were observed when the anhydrous mem
brane was composed of SL saturated with both CH and SA and the composi
tion was not close to the two-component Line, CH-SA, or to the saturat
ion 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, bu
t contained either CH or SA only in a small amount, and the delayed re
lease would be due to the CH and SA-rich SL phase dissolving a great a
mount of CH and SA formed by hydration, The degree of release suppress
ion and particle-swelling depended on the SL content, At 20-45% of SL
content, the prolonged-release, great particle-swelling and no spoutin
g 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.