Pharmaceutical composition of valsartan: beta-cyclodextrin: physico-chemical characterization and anti-hypertensive evaluation.

Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry
Carlos Eduardo de Matos JensenRubén Dario Sinisterra

Abstract

Valsartan, a water-insoluble drug, is mainly used in the treatment of hypertension albeit with reduced oral bioavailability. The aim of work was to develop a valsartan:beta-cyclodextrin (VAL:beta-CD) pharmaceutical composition in order to improve its water solubility and bioavailability. The VAL:beta-CD complexes were prepared by the kneading, solid dispersion and freeze-drying methods, of which the freeze-drying method (FDY) was found to be the best to prepare an inclusion complex. A physical mixture PM was also prepared. Complexes were characterized by thermal analysis, Fourier transformed-infrared (FTIR) spectroscopy, Powder X-ray diffractometry, intrinsic dissolution and NMR (2D-ROESY). Phase-solubility analysis showed A(L)-type diagrams with beta-cyclodextrin (beta-CD). Microcalorimetric titrations suggested the formation of 1:1 inclusion complex between VAL and beta-CD. The apparent stability constants K(1:1) calculated from phase-solubility plots were 165.4 M(-1) (298 K), 145.0 M(-1) (303 K) and 111.3 M(-1) (310 K). In vivo experiments in rats showed that reduction in arterial pressure for the FDY complex is better than with valsartan used alone. The better activity of FDY can be attributed to the higher solubility of va...Continue Reading

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Citations

May 3, 2011·Chemical & Pharmaceutical Bulletin·Mitali KakranZaher Judeh
Dec 7, 2013·Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy·C ManivannanR Renganathan
Feb 28, 2015·Drug Development and Industrial Pharmacy·Sunny ShahJayant Chavda
Jan 4, 2012·Journal of Molecular Recognition : JMR·Rajesh GhaiBrett M Collins
May 2, 2013·Journal of Microencapsulation·Durga Maheswari ParvataneniLakshmi Narasu Mangamoori
Apr 24, 2018·Drug Development and Industrial Pharmacy·Washington X De PaulaRuben D Sinisterra
Jan 1, 2013·Journal of Pharmaceutics·Jyothi SanaboinaBuchi N Nalluri
Dec 31, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Eleni ChontzopoulouThomas Mavromoustakos

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Methods Mentioned

BETA
X-ray
NMR
solubility studies

Software Mentioned

Mestre C®
Dataquest A
XWIN NMR
Microcal Origin

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