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Titolo:
PHYSICOCHEMICAL PROPERTIES, NMR-SPECTROSCOPY AND TOLERANCE OF INCLUSION COMPLEXES OF ANTAZOLINE AND TETRACAINE WITH HYDROXYPROPYL-BETA-CYCLODEXTRIN
Autore:
VANSANTVLIET L; CALJON K; PIETERS L; LUDWIG A;
Indirizzi:
UNIV INSTELLING ANTWERP,LAB PHARMACEUT TECHNOL & BIOPHARM,DEPT PHARMACEUT SCI,UNIV PLEIN 1 B-2610 WILRIJK BELGIUM UNIV INSTELLING ANTWERP,LAB PHARMACEUT TECHNOL & BIOPHARM,DEPT PHARMACEUT SCI B-2610 WILRIJK BELGIUM UNIV INSTELLING ANTWERP,LAB PHARMACOGNOSY,DEPT PHARMACEUT SCI B-2610 WILRIJK BELGIUM
Titolo Testata:
International journal of pharmaceutics
fascicolo: 2, volume: 171, anno: 1998,
pagine: 147 - 156
SICI:
0378-5173(1998)171:2<147:PPNATO>2.0.ZU;2-Z
Fonte:
ISI
Lingua:
ENG
Soggetto:
PILOCARPINE PRODRUG; PHARMACEUTICAL APPLICATIONS; TOLERABILITY; DRUGS; IRRITATION; IMPROVES; DELIVERY; RABBITS;
Keywords:
TETRACAINE; ANTAZOLINE; HYDROXYPROPYL-BETA-CYCLODEXTRIN; SURFACE TENSION; NMR SPECTROSCOPY; IN VIVO TOLERANCE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
24
Recensione:
Indirizzi per estratti:
Citazione:
L. Vansantvliet et al., "PHYSICOCHEMICAL PROPERTIES, NMR-SPECTROSCOPY AND TOLERANCE OF INCLUSION COMPLEXES OF ANTAZOLINE AND TETRACAINE WITH HYDROXYPROPYL-BETA-CYCLODEXTRIN", International journal of pharmaceutics, 171(2), 1998, pp. 147-156

Abstract

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.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 08/07/20 alle ore 07:42:48