Takeda Chemical Industries, Inc.

Jun-ichi Kikuta

Tadashi Makino

Masayuki Yamada

Tetsuro Tabata

Hiroyoshi Koyama

Hiroshi Matoba

Hiroki Itoh

Yoshio Mizukami

Yashio Mizukami

A solid pharmaceutical preparation containing 5 to 50% by weight of ibuprofen and 0.1 to 10% by weight of phenylpropionamide or a pharmaceutically acceptable salt thereof which are stabilized. The solid pharmaceutical preparation can be produced by means of granulating with carriers at least one active ingredient, preferably both ingredients separately into the ibuprofen group and the phenylpropanolamine group, and mixing the former with the latter to enhance the stability of the active ingredients. Preferably, in the phenylpropanolamine group, the amount of any reducing sugar is minimized to such an extent as to maintain the stability of the active ingredient. The above pharmaceutical preparation is suitable for a cold remedy, which has a more excellent pharmacological activity based on ibuprofen, less decomposability of phenylpropanolamine and less change of external appearance of the preparation due to low compatibility between phenylpropanolamine and ibuprofen. Therefore, the pharmaceutical preparation has a longer period of quality assurance.

Stabilized solid pharmaceutical preparation and method of producing the

A method of producing a fast dissolving tablet comprising compression-molding a composition comprising an active ingredient, a carbohydrate and a barely sufficient amount of water to moisten the surface of particles of said carbohydrate into a tablet form and a fast dissolving tablet obtainable by the method. The active ingredient may for example be a vitamin, a gastrointestinal function conditioning agent or an antipyretic-analgesic-antiinflammatory agent. The carbohydrate includes sugar, starch sugars, lactose, honey, sugar alcohols and tetroses. The amount of water to be added is about 0.3 to 10% by weight. The above fast dissolving tablet has a porous structure with excellent disintegratability and solubility as well as adequate strength.

Fast dissolving tablet and its production

A pharmaceutical composition for oral use comprising an effective amount of a compound of the formula (I) having antagonistic action to angiotensin II ##STR1## (wherein the ring W is an optionally substituted N-containing heterocyclic residue; R.sup.3 is a group capable of forming an anion or a group convertible thereinto; X is a direct bond or a spacer having an atomic length of two or less between the phenylene group and the phenyl group; and n is an integer of 1 or 2) and an oily substance having a lower melting point, and a method for preparing a pharmaceutical composition for oral use comprising an effective amount of a compound of the formula (I) and an oily substance having a lower melting point, which comprises admixing the compound of the formula (I) with an oily substance having a lower melting point and then subjecting the mixture to molding.

Pharmaceutical compositions for oral use and method of preparing them

A method of producing a fast dissolving tablet comprising compression-molding a composition comprising an active ingredient, a carbohydrate and a barely sufficient amount of water to moisten the surface of particles of said carbohydrate into a tablet form and a fast dissolving tablet obtainable by the method. The active ingredient may, for example, be a vitamin, a gastrointestinal function conditioning agent or an antipyretic-analgesic-antiinflammatory agent. The carbohydrate includes sugar, starch sugars, lactose, honey, sugar alcohols and tetroses. The amount of water to be added is about 0.3 to 10% by weight. The above fast dissolving tablet has a porous structure with excellent disintegratability and solubility as well as adequate strength.

Heat-labile vitamin D is dispersed in a basic polymer and an excipient readily soluble in an organic solvent to provide a pharmaceutical composition. The composition exhibits reduced isomerization, decomposition, and discoloration while showing excellent stability.

Stabilized vitamin D preparation

A compression-moldable composition comprising an active ingredient, an excipient and an oily or fatty substance having a lower melting point of about 20.degree. to 90.degree. C. is compression-molded into uncoated tablets without coating to improve the abrasion resistance. The oily or fatty substance includes a higher fatty acid or a salt thereof, a wax, a fatty acid ester, a hardened oil, a polyalkylene oxide, etc., and the amount thereof is about 0.01 to 10% by weight. The composition may comprise (1) a granulated powder containing the active ingredient and the excipient, and the powdery or granular oily or fatty substance having a lower melting point, or (2) a granulated powder containing the active ingredient, the excipient and said oily or fatty substance. Compression-molding of the composition improves the abrasion resistance of the tablet and significantly inhibits the development of powder by wearing or abrasion even when the oily or fatty substance is used in a small amount of about 0.1 to 0.5% by weight.

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Suita, Japan

Jun-ichi Kikuta