PLASTICIZERS AND THEIR EFFECTS ON MICROENCAPSULATION PROCESS BY SPRAY-DRYING IN AN AQUEOUS SYSTEM

被引:22
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
10.3109/02652049209021222
中图分类号
O69 [应用化学];
学科分类号
081704 ;
摘要
Microencapsulated theophylline particles were prepared by an aqueous spray-drying process using hydroxypropylmethylcellulose. The effect of different plasticizers, triethylcitrate, polyethylene glycol, propylene glycol, glycerin and citric acid, was investigated. Triethylcitrate, a water-insoluble plasticizer, produced a porous honeycomb-like microcapsule wall resulting in rapid drug release. The presence of the plasticizers also influenced crystallization of the drug. The formation of a solid drug dispersion was observed with the addition of citric acid or glycerin. Changes in the pH of liquid feed caused by the plasticizer had an effect on the product dissolution profile, but this was not a major factor. Formation of pores due to leaching of plasticizers during dissolution enhanced drug release. Flow property measurements indicated that the plasticizers also affect the cohesiveness of the spray-dried products. Compared to the microcapsules formed without any plasticizers, propylene glycol, glycerin and citric acid appeared to be beneficial to the microcapsule wall formation, with microcapsules containing citric acid having the slowest drug release.
引用
收藏
页码:53 / 62
页数:10
相关论文
共 12 条
[1]  
Aulton M.E., Abdul-Razzak M.H., The mechanical properties of hydroxypro-pylmethylcellulose films derived from aqueous systems. I. The influence of plasticizers, Drug Development and Industrial Pharmacy, 7, pp. 649-668, (1981)
[2]  
Dor P.H., Benita S., Levesque G., Cellulose hydrogen phthalate—a coating polymer in controlled release dosage forms, Pharmaceutica Acta Helvitiae, 62, 9, pp. 255-261, (1987)
[3]  
Kawashima Y., Saito M., Takenaka H., Improvement of solubility and dissolution rate of poorly water-soluble salicylic acid by a spray drying technique, Journal of Pharmacy and Pharmacology, 27, pp. 1-5, (1975)
[4]  
Li S.P., Mehta G.N., Buehler J.D., Grim W.M., Harwood J.H., Effect of film-coating additives on the in vitro dissolution rate of ethylcellulose-coated theophylline granules, Pharmaceutical Technology, pp. 48-52, (1990)
[5]  
Newton J.M., Spray drying and its applications in pharmaceuticals, Manufacturing Chemistry and Aerosol News, pp. 33-36, (1966)
[6]  
Raff A.M., Robinson M.J., Svedres E.V., Spray drying of tablet granulations I, Journal of Pharmaceutical Sciences, 50, 1, pp. 76-79, (1961)
[7]  
Samuelov Y., Donbrow M., Friedman M., Sustained release of drugs from ethylcellulose-polyethylene glycol films and kinetics of drug release, Journal of Pharmaceutical Sciences, 68, 3, pp. 325-329, (1979)
[8]  
Seagar H., Spray coating bulk drugs aids dosage form production, Manufacturing Chemistry and Aerosol News, pp. 25-35, (1977)
[9]  
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)
[10]  
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)