Trans-scleral diffusion of triamcinolone acetonide

被引:20
作者
Mora, P
Eperon, S
Felt-Baeyens, O
Gurny, R
Sagodira, S
Breton, P
Guex-Crosier, Y
机构
[1] Univ Lausanne, Jules Gonin Eye Hosp, CH-1000 Lausanne, Switzerland
[2] Univ Parma, Inst Ophthalmol, I-43100 Parma, Italy
[3] Univ Geneva, Dept Pharmaceut & Biopharmaceut, Geneva, Switzerland
[4] Virsol, Paris, France
[5] Societe FIST SA, Paris, France
[6] Immunodesigned Mol, Paris, France
关键词
human; permeability coefficient; scleral diffusion; triamcinolone;
D O I
10.1080/02713680590934094
中图分类号
R77 [眼科学];
学科分类号
100212 ;
摘要
Purpose: To assess ex vivo human scleral permeability to triamcinolone acetonide ( TA). Methods: The experiments were carried out using scleral samples and a Franz-type vertical diffusion cell. A suspension containing TA was prepared and placed in the donor chamber. The concentration of TA in the receptor chamber was measured by high-performance liquid chromatography ( HPLC) assay and expressed as a percentage relative to TA concentration dissolved in the donor chamber. Control experiments using a commercial TA suspension were performed. Results: TA (+/- SEM) dissolved in the donor suspension was 10.69 +/- 1.28 mu g/ml. The diffusion rate of TA varied from 30% after 1 day to 72% after 4 days, after which equilibrium was reached. The human scleral permeability coefficient (P-s +/- SEM) was 1.47 +/- 0.17 x 10(-5) cm/s. Conclusions: TA crossed human sclera. The mean amount of drug retained in the sclera increased with time, 4 days being necessary to equilibrate the unidirectional flux. The TA permeability coefficient was comparable to that of other corticosteroids.
引用
收藏
页码:355 / 361
页数:7
相关论文
共 31 条
[1]   PHYSICOCHEMICAL DETERMINANTS OF DRUG DIFFUSION ACROSS THE CONJUNCTIVA, SCLERA, AND CORNEA [J].
AHMED, I ;
GOKHALE, RD ;
SHAH, MV ;
PATTON, TF .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1987, 76 (08) :583-586
[2]   The effect of TNF-alpha and IL-6 on the permeability of the rat blood-retinal barrier in vivo [J].
Bamforth, SD ;
Lightman, S ;
Greenwood, J .
ACTA NEUROPATHOLOGICA, 1996, 91 (06) :624-632
[3]   REGIONAL DIFFERENCES IN OCULAR CONCENTRATION OF GENTAMICIN AFTER SUBCONJUNCTIVAL AND RETROBULBAR INJECTION IN RABBIT [J].
BARZA, M ;
KANE, A ;
BAUM, JL .
AMERICAN JOURNAL OF OPHTHALMOLOGY, 1977, 83 (03) :407-413
[4]   INTRAOCULAR PENETRATION OF GENTAMICIN AFTER SUB-CONJUNCTIVAL AND RETROBULBAR INJECTION [J].
BARZA, M ;
KANE, A ;
BAUM, J .
AMERICAN JOURNAL OF OPHTHALMOLOGY, 1978, 85 (04) :541-547
[5]  
BILL A, 1965, ARCH OPHTHALMOL-CHIC, V74, P248
[6]   CORNEAL AND CONJUNCTIVAL SCLERAL PENETRATION OF PARA-AMINOCLONIDINE, AGN-190342, AND CLONIDINE IN RABBIT EYES [J].
CHIEN, DS ;
HOMSY, JJ ;
GLUCHOWSKI, C ;
TANGLIU, DDS .
CURRENT EYE RESEARCH, 1990, 9 (11) :1051-1059
[7]   Inhibition of preretinal and optic nerve head neovascularization in pigs by intravitreal triamcinolone acetonide [J].
Danis, RP ;
Bingaman, DP ;
Yang, YS ;
Ladd, B .
OPHTHALMOLOGY, 1996, 103 (12) :2099-2104
[8]   PENETRATION ROUTES OF TOPICALLY APPLIED EYE MEDICATIONS [J].
DOANE, MG ;
JENSEN, AD ;
DOHLMAN, CH .
AMERICAN JOURNAL OF OPHTHALMOLOGY, 1978, 85 (03) :383-386
[9]  
EDELHAUSER HF, 1988, ARCH OPHTHALMOL-CHIC, V106, P1110
[10]   ON DIFFUSION OF TRITIATED WATER THROUGH SKIN [J].
FRANZ, TJ ;
DOWNES, AM ;
SWEENEY, TM ;
MATOLTSY, AG .
JOURNAL OF INVESTIGATIVE DERMATOLOGY, 1968, 50 (03) :260-&