CITRIC-ACID AS A PLASTICIZER FOR SPRAY-DRIED MICROCAPSULES

被引:10
作者
WAN, LSC
HENG, PWS
CHIA, CGH
机构
[1] Department of Pharmacy, National University of Singapore, 10 Kent Ridge Crescent
关键词
D O I
10.3109/02652049309015308
中图分类号
O69 [应用化学];
学科分类号
081704 ;
摘要
An aqueous spray-drying process was used to coat theophylline particles with a cellulose polymer, sodium carboxymethylcellulose (NaCMC) or hydroxypropylmethylcellulose (HPMC). Effect of a plasticizer, citric acid, was studied. Strength of cast films have a direct relationship to the dissolution T50% values of the respective spray-dried products. With varying plasticizer concentrations, changes in interaction between plasticizer and polymer, and in size of crystallized drug crystals, were observed with HPMC films. The plasticizer content also affected the films of NaCMC by bringing about a change in the form and arrangement of the drug. X-ray diffraction analyses of the different spray-dried products revealed a possibility of the predominance of different crystal forms. Spherical spray-dried microcapsules of NaCMC were formed with a 20-30% w/w plasticizer content. With HPMC, as plasticizer concentration was increased there was a corresponding increase in mean size of the spray-dried products. In terms of drug release and formation of spherical particles, a plasticizer concentration of 30% w/w was found to be suitable for both HPMC and NaCMC.
引用
收藏
页码:11 / 23
页数:13
相关论文
共 10 条
[1]  
Borka L., Review on crystal polymorphism of substances in the European Pharmacopoeia, Pharmaceutica Acta Helvetiae, 66, 1, pp. 16-22, (1991)
[2]  
Dor P.H., Benita S., Levesque G., Cellulose hydrogen phthalate—A coating polymer in controlled release dosage forms, Pharmaceutica Acta Helvetiae, 62, 9, pp. 255-261, (1987)
[3]  
Fassihi A.R., Munday D.L., Dissolution of theophylline from film-coated slow release mini-tablets in various dissolution media, Journal of Pharmacy and Pharmacology, 41, pp. 369-372, (1989)
[4]  
Herman J., Visavarungroj N., Remon J.P., Instability of drug release from anhydrous theophylline-microcrystalline cellulose formulations, International Journal of Pharmaceutics, 55, pp. 143-146, (1989)
[5]  
Otsuka M., Kaneniwa N., Kawakami K., Umezawa O., Effect of surface characteristics of theophylline anhydrate powder on hygroscopic stability, Journal of Pharmacy and Pharmacology, 42, pp. 606-610, (1990)
[6]  
Takenaka H., Kawashima Y., Lin S.Y., Preparation of enteric coated microcapsules for tabletting by spray drying technique and in vitro simulation of drug release from the tablet in GI tract, Journal of Pharmaceutical Sciences, 69, 12, pp. 1388-1392, (1980)
[7]  
Takenaka H., Kawashima Y., Chikamatsu Y., Ando Y., Mechanical properties, dissolution behaviour and stability to oxidation of L-ascobylmonostearate microcapsules prepared by a spray drying polycondensation technique, Chemical and Pharmaceutical Bulletin, 30, 6, pp. 2189-2195, (1982)
[8]  
Takeuchi H., Handa T., Kawashima Y., Controlled release theophylline tablet with acrylic polymers prepared by spray drying technique in aqueous system, Drug Development and Industrial Pharmacy, 15, 12, pp. 1999-2016, (1989)
[9]  
Wan L.S.C., Heng P.W.S., Chia C.G.H., Plasticizers and their effects on microencapsulation process by spray drying in an aqueous system, Journal of Microencapsulation, 9, 1, pp. 53-62, (1991)
[10]  
Wan L.S.C., Heng P.W.S., Chia C.G.H., Preparation of coated particles using a spray drying process with an aqueous system, International Journal of Pharmaceutics, 77, pp. 183-191, (1991)