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Molecules 2018, 23(9), 2161; https://doi.org/10.3390/molecules23092161

Co-Amorphous Simvastatin-Nifedipine with Enhanced Solubility for Possible Use in Combination Therapy of Hypertension and Hypercholesterolemia

School of Engineering and Sciences, Department of Sciences—Chemistry and Nanotechnology, Tecnologico de Monterrey, Campus Monterrey, Av. Eugenio Garza Sada 2501 Sur. Monterrey N.L., Monterrey 64849, Mexico
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Received: 26 July 2018 / Revised: 19 August 2018 / Accepted: 20 August 2018 / Published: 28 August 2018
(This article belongs to the Collection Poorly Soluble Drugs)
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Abstract

The high index of simultaneous incidence of hypertension and hypercholesterolemia in the population of many countries demands the preparation of more efficient drugs. Therefore, there is a significant area of opportunity to provide as many alternatives as possible to treat these illnesses. Taking advantage of the solubility enhancement that can be achieved when an active pharmaceutical ingredient (API) is obtained and stabilized in its amorphous state, in the present work, new drug-drug co-amorphous formulations (Simvastatin SIM- Nifedipine NIF) with enhanced solubility and stability were prepared and characterized. Results show that the co-amorphous system (molar ratio 1:1) is more soluble than the pure commercial APIs studied separately. Aqueous dissolution profiles showed increments of solubility of 3.7 and 1.7 times for SIM and NIF, correspondingly, in the co-amorphous system. The new co-amorphous formulations, monitored in time, (molar fractions 0.3, 0.5 and 0.7 of SIM) remained stable in the amorphous state for more than one year when stored at room temperature and did not show any signs of crystallization when re-heating. Inspection on the remainder of a sample after six hours of dissolution showed no recrystallization, confirming the stability of co-amorphous system. The enhanced solubility of the co-amorphous formulations makes them promising for simultaneously targeting of hypertension and hypercholesterolemia through combination therapy. View Full-Text
Keywords: solubility; Nifedipine; Simvastatin; co-amorphous; amorphous drug; hypertension; hypercholesterolemia solubility; Nifedipine; Simvastatin; co-amorphous; amorphous drug; hypertension; hypercholesterolemia
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).
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Martínez-Jiménez, C.; Cruz-Angeles, J.; Videa, M.; Martínez, L.M. Co-Amorphous Simvastatin-Nifedipine with Enhanced Solubility for Possible Use in Combination Therapy of Hypertension and Hypercholesterolemia. Molecules 2018, 23, 2161.

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