Membrane transport of hydrocortisone acetate from supersaturated solutions; the role of polymers

被引:96
作者
Raghavan, SL
Kiepfer, B
Davis, AF
Kazarian, SG
Hadgraft, J
机构
[1] Univ Greenwich, Medway Sci, NRI, Chatham ME4 4TB, Kent, England
[2] GlaxoSmithKline Consumer Hlth Care, Weybridge KT13 0DE, Surrey, England
[3] Univ London Imperial Coll Sci Technol & Med, Dept Chem Engn & Chem Technol, London SW7 2BY, England
基金
英国工程与自然科学研究理事会;
关键词
supersaturation; cosolvents; in vitro permeation; hydrocortisone acetate; antinucleant polymers; silicone membrane; ATR-IR spectroscopy;
D O I
10.1016/S0378-5173(01)00673-1
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Permeation of hydrocortisone acetate (HA) from supersaturated solutions was studied across a model silicone membrane. Supersaturated solutions were prepared using the cosolvent technique with propylene glycol and water (or aqueous polymer solutions) as the cosolvents. In the absence of the polymer, the flux of HA was similar at all degrees of saturation and was not significantly different from the value obtained for a saturated solution. Flux enhancement, as a result of supersaturation, was observed with all the polymers. The flux increased with increasing polymer concentration, reached a maximum and decreased at higher polymer percentages. The amount of polymer required for maximum enhancement differed for each polymer. The decrease of flux at high polymer concentrations is attributed to changes in microviscosity and a marginal increase in solubility. The infrared spectroscopic and differential scanning calorimetry data suggest that HA-polymer interactions occurred through hydrogen bonding thus explaining the proposed mechanism of the anti-nucleant properties of the polymers. (C) 2001 Elsevier Science B.V. All rights reserved.
引用
收藏
页码:95 / 105
页数:11
相关论文
共 18 条
[1]   EFFECT OF SUPERSATURATION ON MEMBRANE-TRANSPORT .1. HYDROCORTISONE ACETATE [J].
DAVIS, AF ;
HADGRAFT, J .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1991, 76 (1-2) :1-8
[2]   Membrane penetration enhancement of ibuprofen using supersaturation [J].
Iervolino, M ;
Raghavan, SL ;
Hadgraft, J .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2000, 198 (02) :229-238
[3]   Penetration enhancement of ibuprofen from supersaturated solutions through human skin [J].
Iervolino, M ;
Cappello, B ;
Raghavan, SL ;
Hadgraft, J .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2001, 212 (01) :131-141
[4]   Applications of vibrational spectroscopy to characterize poly(ethylene terephthalate) processed with supercritical CO2 [J].
Kazarian, SG ;
Brantley, NH ;
Eckert, CA .
VIBRATIONAL SPECTROSCOPY, 1999, 19 (02) :277-283
[5]   FOURIER-TRANSFORM INFRARED SPECTROSCOPIC STUDIES OF WATER-MOLECULES SORBED IN SOLID POLYMERS [J].
KUSANAGI, H ;
YUKAWA, S .
POLYMER, 1994, 35 (26) :5637-5640
[6]   Selection and use of crystallization inhibitors for matrix-type transdermal drug-delivery systems containing sex steroids [J].
Lipp, R .
JOURNAL OF PHARMACY AND PHARMACOLOGY, 1998, 50 (12) :1343-1349
[7]   Control of drug crystallization in transdermal matrix system [J].
Ma, XG ;
Taw, J ;
Chiang, CM .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1996, 142 (01) :115-119
[8]  
MEGRAB NA, 1995, J CONTROL RELEASE, V36, P205
[9]   Supersaturated solutions evaluated with an in vitro stratum corneum tape stripping technique [J].
Pellett, MA ;
Roberts, MS ;
Hadgraft, J .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1997, 151 (01) :91-98
[10]   EFFECT OF SUPERSATURATION ON MEMBRANE-TRANSPORT .2. PIROXICAM [J].
PELLETT, MA ;
DAVIS, AF ;
HADGRAFT, J .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1994, 111 (01) :1-6