Improving Biopharmaceutical Properties of Vinpocetine Through Cocrystallization
| Autor: | Matteo Lusi, Miranda L. Perry, Michael J. Zaworotko, Dario Voinovich, Samuel Golob, Michele R. Chierotti, Lucia Lassiani, Iztok Grabnar |
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| Přispěvatelé: | Golob, Samuel, Perry, Miranda, Lusi, Matteo, Chierotti, Michele R., Grabnar, Iztok, Lassiani, Lucia, Voinovich, Dario, Zaworotko, Michael J. |
| Rok vydání: | 2016 |
| Předmět: |
Adult
Male Absorption (pharmacology) Stereochemistry Vasodilator Agents Cmax ionic cocrystal Administration Oral Pharmaceutical Science 02 engineering and technology vinpocetine 010402 general chemistry 01 natural sciences Cocrystal Dosage form Biopharmaceutics bioavailability boric acid pharmacokinetics Boric Acids X-Ray Diffraction Pharmacokinetics Vinpocetine medicine Humans Dissolution testing pharmacokinetic Vinca Alkaloids Chromatography Calorimetry Differential Scanning Chemistry Middle Aged 021001 nanoscience & nanotechnology 0104 chemical sciences Bioavailability Crystallization 0210 nano-technology medicine.drug |
| Zdroj: | Journal of Pharmaceutical Sciences. 105:3626-3633 |
| ISSN: | 0022-3549 |
| DOI: | 10.1016/j.xphs.2016.09.017 |
| Popis: | Vinpocetine is a poorly water soluble weakly basic drug (pKa = 7.1) used for the treatment of several cerebrovascular and cognitive disorders. Because existing formulations exhibit poor bioavailability and scarce absorption, a dosage form with improved pharmacokinetic properties is highly desirable. Cocrystallization represents a promising approach to generate diverse novel crystal forms and to improve the aqueous solubility and in turn the oral bioavailability. In this article, a novel ionic cocrystal of vinpocetine is described, using boric acid as a coformer, and fully characterized (by means of differential scanning calorimetry, solid-state nuclear magnetic resonance, powder and single-crystal X-ray diffraction, and powder dissolution test). Pharmacokinetic performance was also tested in a human pilot study. This pharmaceutical ionic cocrystal exhibits superior solubilization kinetics and modulates important pharmacokinetic values such as maximum concentration in plasma (Cmax), time to maximum concentration (tmax), and area under the plasma concentration-time curve (AUC) of the poorly soluble vinpocetine and it therefore offers an innovative approach to improve its bioavailability. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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