Method for improving the aqueous solubility of poorly-soluble substances

Abstract

Provided is a method for improving the solubility of poorly-soluble substances used in pharmaceuticals, veterinary pharmaceuticals, quasi-drugs, cosmetics, food products, agricultural chemicals, and the like, without using large amounts of additives. The provided method is characterized in that fine particles of a calcium compound such as calcium phosphate or calcium carbonate are used to cover the surfaces of particles of a poorly-soluble substance used in pharmaceuticals, veterinary pharmaceuticals, quasi-drugs, cosmetics, food products, agricultural chemicals, or the like.

Description

technical field [0001] The present invention relates to a method for improving the water solubility of poorly soluble substances used in medicines, animal medicines, quasi-drugs, cosmetics, food, agricultural chemicals and the like. Background technique [0002] In the fields of medicines, animal medicines, quasi-drugs, cosmetics, food, agricultural chemicals, etc., useful substances show poor solubility in water in many cases, which limits the utilization of useful substances. Generally, as a method of increasing the solubility of a poorly soluble drug or accelerating the dissolution rate, a method of mechanically micronizing, a method of inclusion with cyclodextrin, etc., a method of improving solubility with a surfactant or a solubilizer, etc. . [0003] For the administration of pharmaceuticals, there are various administration methods such as oral administration, intravenous administration, intramuscular administration, subcutaneous administration, transdermal administ...

AI Technical Summary

Problems solved by technology

[0009] However, the method of micronizing the drug is the first technology to improve the solubility. In fact, it reaches several μm and does not help much to increase the solubility.

On the contrary, due to the micronization, the cohesion and adhesion of the drug may increase, or solidification may occur, or the dissolution rate may decrease

In addition, in the method of inclusion of a drug with cyclodextrin or the like, generally, a production method such as a freeze-drying method is used, and the production time and the number of steps increase, and it cannot be said to be an advantageous method in terms of industrialization.

In addition, in order to perform inclusion with cyclodextrin, etc., cyclodextrin is usually required in an amount equivalent to that of the drug, and only the additive part has led to an increase in the amount of the preparation

In addition, in the case of a method of amorphizing a drug, the amorphous substance is originally in an unstable state, but is easily changed to a stable state by external stimuli such as light, heat, humidity, or over time. Crystalline state, difficult to maintain amorphous

In addition, in the case of a method of improving the solubility of a poorly soluble drug with a solubilizer, an organic solvent is usually used, and there is a possibility that the organic solvent remains in the preparation, and there is a problem of safety.

In addition, from the viewpoint of environmental protection, a large amount of organic solvent needs to be safely recovered, and the production cost is high, and there are also problems from the viewpoint of the health and safety of operators.

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