Preparation of double-encapsulated microcapsules for mitigating drug loss and extending release.
The double-encapsulated microcapsules were prepared by the non-solvent addition, phase-separation method to form core material and, encapsulated with the O/W emulsion non-solvent addition method to increase drug loading and regulate drug release rate. The drug used was theophylline, which is water-soluble. Dichloromethane and n-hexane were used as the solvent and non-solvent, respectively. This study investigated how various core material and microcapsule EC/TH ratios affect the drug loss, particle size, surface morphology and release rate. The drug loss of the double-encapsuLated microcapsules was 12.8% less than that of microcapsules prepared by the O/W emulsion non-solvent addition method alone. The particle size of these double-encapsulated microcapsules decreased as the concentration of EC polymer was increased in the second encapsulation process. The roughness of their surface was also in proportion to the concentration of polymer solution used in the second encapsulation process. The dissolution study showed that the T20 of the double-encapsulated microcapsules ranged from 2-35.4 h, while that of the O/W emulsion non-solvent addition method microcapsules was from 2.7-7.7 h. The greater the level of EC in the polymer solution, the slower the release rate of the drug from the microcapsules when the EC was not over the critical amount.
Tsai
Y L
YL
Department of Chemical Engineering, National Central University, Chung-Li, Taiwan 320, Republic of China.
Jong
C C
CC
Chen
H
H
D002214:Capsules; D002482:Cellulose / Q000031:analogs & derivatives; D003692:Delayed-Action Preparations; D004339:Drug Compounding / Q000379:methods*; D004655:Emulsions; D006586:Hexanes; D006801:Humans; D066298:In Vitro Techniques; D008752:Methylene Chloride; D008855:Microscopy, Electron, Scanning; D010316:Particle Size; D012997:Solvents; D013499:Surface Properties; D013806:Theophylline / Q000008:administration & dosage
D002214:Capsules; D003692:Delayed-Action Preparations; D004655:Emulsions; D006586:Hexanes; D012997:Solvents; C026385:n-hexane; D008752:Methylene Chloride; C013517:ethyl cellulose; D002482:Cellulose; D013806:Theophylline