Abstract
Preparation and in vitro and in vivo evaluation of vinpocetine (VIN) elementary osmotic pump (EOP) formulations were investigated. A method for the preparation of VIN elementary osmotic pump tablet was obtained by adding organic acid additives to increase VIN solubility. VIN was used as the active pharmaceutical ingredient, lactose and mannitol as osmotic agent. Citric acid was used as increasing API solubility and without resulting in the API degradation. It is found that the VIN release rate was increasing with the citric acid amount at a constant range. Cellulose acetate 398-3 was employed as semipermeable membrane containing polyethylene glycol 6000 and diethyl-o-phthalate as pore-forming agent and plasticizer for controlling membrane permeability. In addition, a clear difference between the pharmacokinetic patterns of VIN immediate release and VIN elementary osmotic pump formulations was revealed. The area under the plasma concentration-time curve after oral administration of elementary osmotic pump formulations was equivalent to VIN immediate release formulation. Furthermore, significant differences found for mean residence time, elimination half-life, and elimination rate constant values corroborated prolonged release of VIN from elementary osmotic pump formulations. These results suggest that the VIN osmotic pump controlled release tablets have marked controlled release characters and the VIN osmotic pump controlled release tablets and the normal tablets were bioequivalent.
Highlights
Vinpocetine (VIN) is a vasoactive vinca alkaloid and a synthetic derivative of apovincamine which has been used in clinical practice in Europe for 30 years for the treatment of disorders arising from cerebrovascular and cerebral degenerative diseases [1, 2]
Conventional preparation will lead to large fluctuation in drug plasma concentration and side effect on human body
In order to study the influence of citric acid amount on drug dissolution, core tablets with various molar ratios of VIN and citric acid formulations in Table 1 were prepared and were investigated
Summary
Vinpocetine (VIN) is a vasoactive vinca alkaloid and a synthetic derivative of apovincamine which has been used in clinical practice in Europe for 30 years for the treatment of disorders arising from cerebrovascular and cerebral degenerative diseases [1, 2]. It was reported that a method for the preparation of water-soluble drug was obtained by adding acid additives to increase dissolution and improve the release profile [13, 14].
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