SOLVENT SYSTEM OF HARDLY SOLUBLE DRUG WITH IMPROVED DISSOLUTION RATE
First Claim
1. A pharmaceutical preparation comprising a hardly water-soluble acidic drug and a solvent system,wherein the solvent system comprises a pharmaceutically acceptable cation acceptor, 10 to 90% by weight of polyethylene glycol, 0.1 to 15% by weight of water and 0.1 to 50% by weight of a surfactant having an HLB value of 3 to 40 to improve the dissolution rate of the drug, andwherein said pharmaceutically acceptable cation acceptor is contained in an amount of 0.1 to 2 mole equivalent per mole of acidic groups in the acidic drug, and is selected from the group consisting of amines, amino acids, pharmaceutically acceptable metallic salts of weak acids having at least one of an acetate and a citrate, and mixtures thereof, and a mixture of pharmaceutically acceptable basic compounds and said pharmaceutically acceptable metallic salts of weak acids having at least one of an acetate and a citrate, amino acids or the amines.
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Accused Products
Abstract
The present invention relates to a solvent system with improved disintegration degree and dissolution ratio of a hardly soluble drug by highly concentrating the drug through partial ionization, and by establishing optimal conditions for enhancing bioavailability of the drug, such as the co-relation between the acid drug and the accompanied components, ionization degree of a solvent system, use of an appropriate cation acceptor, water content, selection of optimal mixing ratio of the respective components and use of specific surfactants, and to a pharmaceutical preparation comprising the same. The solvent system of the invention has advantages in that it can enhance bioavailability by improving the disintegration degree and dissolution ratio of a hardly soluble drug and also provide a capsule with a sufficiently small volume to permit easy swallowing.
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Citations
8 Claims
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1. A pharmaceutical preparation comprising a hardly water-soluble acidic drug and a solvent system,
wherein the solvent system comprises a pharmaceutically acceptable cation acceptor, 10 to 90% by weight of polyethylene glycol, 0.1 to 15% by weight of water and 0.1 to 50% by weight of a surfactant having an HLB value of 3 to 40 to improve the dissolution rate of the drug, and wherein said pharmaceutically acceptable cation acceptor is contained in an amount of 0.1 to 2 mole equivalent per mole of acidic groups in the acidic drug, and is selected from the group consisting of amines, amino acids, pharmaceutically acceptable metallic salts of weak acids having at least one of an acetate and a citrate, and mixtures thereof, and a mixture of pharmaceutically acceptable basic compounds and said pharmaceutically acceptable metallic salts of weak acids having at least one of an acetate and a citrate, amino acids or the amines.
Specification