Physicochemical and release studies of naproxen in poloxamer gels

被引:75
作者
Suh, H [1 ]
Jun, HW [1 ]
机构
[1] UNIV GEORGIA,COLL PHARM,DEPT PHARMACEUT,ATHENS,GA 30602
关键词
naproxen; micellar solubilization; PF-127; membrane transport; isopropyl myristate; diffusion coefficient; PLURONIC F-127 GELS;
D O I
10.1016/0378-5173(95)04210-5
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The solubility of naproxen at pH 2 was significantly increased as a linear function of PF-127 concentration at three temperatures. Naproxen was highly entrapped by the micelles as indicated by large partition coefficients. The micellar solubilization was a spontaneous (Delta G < 0) and exothermic (Delta H < 0) process which resulted in a less orderly state (Delta S > 0). In the presence of PF-127, the release of naproxen across the membrane was significantly sustained at pH 2 and inversely proportional to the surfactant concentration. At pH 7, PF-127 had little effect on the membrane transport of naproxen. The release of naproxen from the PF-127 gel into isopropyl myristate was dependent on the medium pH. The highest release was observed at pH 6.3. The diffusion coefficients of naproxen were inversely proportional to drug loading and PF-127 concentration. The activation energy of 7.45 kcal/mol for the diffusion of naproxen in the gel was calculated using the Arrhenius equation.
引用
收藏
页码:13 / 20
页数:8
相关论文
共 19 条
[1]  
Barry B.W., 1976, J PHARM PHARM, V28, P210218
[2]  
Collet JH, 1985, P INT S CONTROL REL, V12, P28
[3]   CHEMISTRY OF NON-IONIC DETERGENTS .7. VARIATIONS OF MICELLAR STRUCTURE OF SOME SYNTHETIC NON-IONIC DETERGENTS WITH TEMPERATURE [J].
ELWORTHY, PH ;
MCDONALD, C .
KOLLOID-ZEITSCHRIFT AND ZEITSCHRIFT FUR POLYMERE, 1964, 195 (01) :16-+
[4]   MASS-TRANSPORT PHENOMENA AND MODELS - THEORETICAL CONCEPTS [J].
FLYNN, GL ;
YALKOWSKY, SH ;
ROSEMAN, TJ .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1974, 63 (04) :479-510
[5]  
HENRY RL, 1989, CRIT REV BIOCOMPAT, V5, P207
[6]   ANALYSIS OF DATA ON MEDICAMENT RELEASE FROM OINTMENTS [J].
HIGUCHI, WI .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1962, 51 (08) :802-&
[7]   EFFECT OF TEMPERATURE UPON SOLUBILIZATION BY A SERIES OF NONIONIC SURFACTANTS [J].
HUMPHREYS, KJ ;
RHODES, CT .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1968, 57 (01) :79-+
[8]   THEORY OF DIFFUSION IN GELS [J].
LAUFFER, MA .
BIOPHYSICAL JOURNAL, 1961, 1 (03) :205-&
[9]  
McBain ME., 1955, SOLUBILIZATION RELAT
[10]  
MIYAZAKI S, 1984, CHEM PHARM BULL, V32, P4205