Factors affecting the efficiency of a self-emulsifying oral delivery system

被引:83
作者
Bachynsky, MO
Shah, NH
Patel, CI
Malick, AW
机构
[1] Pharmaceutical R and D, Hoffmann-LaRoche Inc., Nutley, NJ 07110
关键词
D O I
10.3109/03639049709150551
中图分类号
R914 [药物化学];
学科分类号
100701 [药物化学];
摘要
Dosage forms containing a self-emulsifying system have shown significant promise in improving the in vitro dissolution rate and oral absorption of lipophilic drugs. In such a system, a surfactant, or a surfactant plus medium chain monoglyceride (co-emulsifier), is added to a lipophilic vehicle (oil) containing dissolved drug. In the present study, surfactants with different hydrophile-lipophile balance (HLB), fatty acid glycerides (co-emulsifiers) with varying fatty acid (C-8-C-18) chain length, and lipophilic vehicles (oils) containing different fatty acid (C-8-C-18) compositions were evaluated for their effectiveness in producing self-emulsifying systems. This investigation showed that the HLB of the surfactant, as well as the fatty acid chain length of the monoglyceride have a significant effect on the performance of the self-emulsifying system; a surfactant with an HLB in the range of 10-15 and a monoglyceride of medium chain fatty acid (C-8-C-10) were most effective. Also, there ape certain critical concentrations of surfactant and monoglyceride necessary for preparing an optimum self-emulsifying oral drug delivery system.
引用
收藏
页码:809 / 816
页数:8
相关论文
共 7 条
[1]
BACHYNSKY MO, 1990, UNPUB ORAL DELIVERY
[2]
MEDIUM-CHAIN TRIGLYCERIDES - PHYSIOLOGIC CONSIDERATIONS AND CLINICAL IMPLICATIONS [J].
GREENBERGER, NJ ;
SKILLMAN, TG .
NEW ENGLAND JOURNAL OF MEDICINE, 1969, 280 (19) :1045-+
[3]
HANE D, 1984, UNPUB ACUTE TOXICITY
[4]
POUTON CW, 1985, INT J PHARM, V27, P335, DOI 10.1016/0378-5173(85)90081-X
[5]
POUTON CW, 1987, P INT S CONTROL REL, P14
[6]
SELF-EMULSIFYING DRUG-DELIVERY SYSTEMS (SEDDS) WITH POLYGLYCOLYZED GLYCERIDES FOR IMPROVING IN-VITRO DISSOLUTION AND ORAL ABSORPTION OF LIPOPHILIC DRUGS [J].
SHAH, NH ;
CARVAJAL, MT ;
PATEL, CI ;
INFELD, MH ;
MALICK, AW .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1994, 106 (01) :15-23
[7]
STOUT SA, 1988, PHARMACEUT RES, V5, pS92