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Molecules 2010, 15(6), 4067-4084; doi:10.3390/molecules15064067

Pharmaceutical Composition of Valsartan: β-Cyclodextrin: Physico–Chemical Characterization and Anti-Hypertensive Evaluation

1, 2
1 Departamento de Química, ICEx, Universidade Federal de Minas Gerais, Avenida Pres. Antônio Carlos 6627, 31270-901, Belo Horizonte, Brazil 2 Departamento de Fisiologia e Biofísica, ICB, Universidade Federal de Minas Gerais, 31270-901 Belo Horizonte, Brazil 3 Campus Centro Oeste Dona Lindu, Universidade Federal de São João del Rei, R. Sebastião Gonçalves Coelho, 400, 35501-296, Divinópolis, Brazil
* Author to whom correspondence should be addressed.
Received: 17 May 2010 / Accepted: 27 May 2010 / Published: 4 June 2010
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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:β-cyclodextrin (VAL:β-CD) pharmaceutical composition in order to improve its water solubility and bioavailability. The VAL:β-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 mixtyure 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 AL-type diagrams with β-cyclodextrin (β-CD). Microcalorimetric titrations suggested the formation of 1:1 inclusion complex between VAL and β-CD. The apparent stability constants K1:1 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 valsartan after inclusion in the cyclodextrin cavity, as suggest by the intrinsic dissolution studies.
Keywords: valsartan; β-cyclodextrin; intrinsic dissolution; ROESY; anti-hypertensive evaluation valsartan; β-cyclodextrin; intrinsic dissolution; ROESY; anti-hypertensive evaluation
This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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De Matos Jensen, C.E.; Dos Santos, R.A.S.; Denadai, A.M.L.; Santos, C.F.F.; Braga, A.N.G.; Sinisterra, R.D. Pharmaceutical Composition of Valsartan: β-Cyclodextrin: Physico–Chemical Characterization and Anti-Hypertensive Evaluation. Molecules 2010, 15, 4067-4084.

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