Ajinomoto Co., Ltd.

Akira Yabuki

Nobutaka Ninomiya

Chisato Makino

Takahiko Ando

Masanao Ozaki

Hidetoshi Sakai

Masato Kaida

Nobuo Kato

Shigeru Shioya

Haruo Orita

Kenichi Ogawa

Hiroyuki Higuchi

Yuji Iwashita

Hirokazu Hagio

Mitsuyasu Ida

Kunikazu Suzuki

Takahiko Andou

Erika Motomura

Tomoaki Kawano

The present invention provides solid dispersions or solid dispersion pharmaceutical preparations containing a water-soluble polymeric substance(s) and a phenylalanine compound of the formula (1) or pharmaceutically acceptable salts thereof, wherein A represents the formula (2) and the like, B represent an alkoxy group and the like, E represents a hydrogen atom and the like, D represents a substituted phenyl group and the like, T, U and V represent a carbonyl group and the like, Arm represents a benzene ring and the like, R1 represents an alkyl group and the like, R2, R3, and R4 may be the same or different from one another and each represent a hydrogen atom, a substituted amino group and the like, and J and J' represent a hydrogen atom and the like; production methods thereof; and solubilized pharmaceutical preparations containing a solubilizer(s) and the compound (I) or pharmaceutically acceptable salts thereof. According to the solid dispersion pharmaceutical preparations or solubilized pharmaceutical preparations, though they contain the phenylalanine compound of the formula (1) that is a poorly-soluble drug as an active ingredient, the pharmaceutical preparations having high solubility and oral absorbability can be obtained. 

Solid dispersions or solid dispersion pharmaceutical preparations of phenylalanine derivatives

The present invention provides a small-sized preparation that is easy to take, containing 26% or more of nateglinide and 28% or more of at least one disintegrant selected from the group consisting of carmellose or salts thereof, sodium carboxymethyl starch, croscarmellose sodium, crospovidone, partly pregelatinized starch and low-substituted hydroxypropyl cellulose, based on the total mass of the preparation. The preparation of the present invention has high contents of nateglinide, which can be absorbed immediately to exhibit a hypoglycemic action.

Nateglinide-containing preparation

The present invention discloses, as a immediate-release preparation useful as an antidiabetic, a nateglinide-containing preparation comprising nateglinide as an active ingredient wherein the nateglinide is amorphous.

There is provided a single preparation which directly decreases both of the post prandial blood glucose level and the fasting blood glucose level close to normal levels, by release-sustaining a drug capable of decreasing the post prandial blood glucose level of diabetic patients close to the normal level, or mixing a controlled release drug capable of decreasing the post prandial blood glucose level close to the normal level with an immediate release drug. It is particularly preferable that the drug capable of decreasing the post prandial blood glucose level close to the normal level is nateglinide.

Antidiabetic preparation for oral administration

The problem of the present invention is to provide pharmaceutical granules containing, as active amino acid ingredients, three kinds of branched chain amino acids of isoleucine, leucine and valine, which has a smaller specific volume than conventional products, and a production method thereof. As a result of intensive studies, granules containing, as active amino acid ingredients, three kinds of branched chain amino acids of isoleucine, leucine and valine and a production method thereof have been provided, which are characterized by adding an acid to a particle mixture of three kinds of branched chain amino acids of isoleucine, leucine and valine and granulating the mixture, which has solved the above-mentioned problem.

Process for producing granules containing branched amino acids

A tablet composition containing N-(trans-4-isopropylcyclohexanecarbonyl)-D-phenylalanine and a disintegrant, selected from a low substituted hydroxypropylcellulose, sodium carboxymethyl cellulose, calcium carboxymethyl cellulose and sodium croscaramellose sodium, is disclosed. This tablet composition is rapidly disintegrated in the stomach after the administration and absorbed without being influenced by meals to inhibit the rise of the blood sugar levels of diabetics after meals.

Tablet composition

There is provided a single preparation which directly decreases both of the post prandial blood glucose level and the fasting blood glucose level close to normal levels, by release-sustaining a drug capable of decreasing the post prandial blood glucose level of diabetic patients close to the normal level, or mixing a controlled release drug capable of decreasing the post prandial blood glucose level close to the normal level with an immediate release drug. It is particularly preferable that the drug capable of decreasing the post prandial blood glucose level close to the normal level is nateglinide, repaglinide, or mitiglinide (KAD-1229).

A tablet composition containing N-(trans-4-isopropylcyclohexanecarbonyl)-D-phenylalanine and low substituted hydroxypropylcellulose is disclosed. This tablet composition is rapidly disintegrated in the stomach after the administration and absorbed without being influenced by meals to inhibit the rise of the blood sugar levels of diabetics after meals.

Tablet composition of N-(trans-4-isopropylcyclohexanecarbonyl)-D-phenylalanine

A tablet composition containing N-(trans-4-isopropylcydohexanecarbonyl)-D-phenylalanine and low substituted hydroxypropylcellulose is disclosed. This tablet composition is rapidly disintegrated in the stomach after the administration and absorbed without being influenced by meals to inhibit the rise of the blood sugar levels of diabetics after meals.

Superoxide dismutase is chemically modified with poly(alkylene oxide), the modified superoxide dismutase having a molecular structure in which both ends of a poly(alkylene oxide) molecule are attached to superoxide dismutase. The modified superoxide dismutase can be used to remove toxic substances derived from oxygen, from the blood circulation in a living body, and has a longer half life in the blood circulation as compared to superoxide dismutase which has not been modified.

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Kawasaki, Japan

Akira Yabuki