Physicochemical properties, NMR spectroscopy and tolerance of inclusion complexes of antazoline and tetracaine with hydroxypropyl-β-cyclodextrin

被引：7
|
作者：
Van Santvliet, L
Caljon, K
Pieters, L
Ludwig, A
机构：
[1] Univ Instelling Antwerp, Lab Pharmaceut Technol & Biopharm, Dept Pharmaceut Sci, B-2610 Wilrijk, Belgium
[2] Univ Instelling Antwerp, Lab Pharmacognosy, Dept Pharmaceut Sci, B-2610 Wilrijk, Belgium
来源：
INTERNATIONAL JOURNAL OF PHARMACEUTICS | 1998年 / 171卷 / 02期
关键词：
tetracaine; antazoline; hydroxypropyl-beta-cyclodextrin; surface tension; NMR spectroscopy; in vivo tolerance;
D O I：
10.1016/S0378-5173(98)00171-9
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
To improve the tolerance of antazoline and tetracaine ophthalmic solutions, inclusion complexes of the free bases of both drugs with hydroxypropyl-beta-cyclodextrin (HP-beta-CD) were prepared. The physicochemical properties of the drug:HP-beta-CD solutions were determined and the inclusion complexes were characterised by H-1 and C-13 NMR spectroscopy. The apparent complex constants were calculated from the phase-solubility diagram and were estimated at 403 M-1 and 1308 M-1 for the antazoline:HP-beta-CD complex and tetracaine:HP-beta-CD complex, respectively. H-1 and C-13 NMR analysis showed that in the 1:1 complexes the total antazoline fraction was present as an inclusion complex, whereas tetracaine was only partly included in spite of a similar phase solubility diagram. NMR spectroscopy also revealed the site of interaction of the drugs with the HP-beta-CD molecule. A solution acceptability test was carried out on volunteers. A relationship between the surface tension of the solutions and the tolerance was observed. (C) 1998 Elsevier Science B.V. All rights reserved.
引用
收藏
页码：147 / 156
页数：10
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