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Compressed-shaping formulation for hypnosis

A compression molding and preparation technology, which is applied in the directions of non-active ingredients medical preparations, medical preparations containing active ingredients, pill delivery, etc. Commodity value, etc.

Inactive Publication Date: 2004-04-14
SS PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, when used as an oral hypnotic, depending on the administration conditions, if the disintegration and dissolution of the preparation become slow, the effect of the hypnotic cannot be fully exhibited
[0005] On the other hand, diphenhydramine or its acid addition salts have a strong pungent bitter taste and cause discomfort when taken
But existing method is to utilize the film and matrix that contain grease and insoluble macromolecular substance to slow down the dissolving speed of diphenhydramine to cover up taste, though this method does not affect and bring into play its drug effect as antihistamine, as hypnotic Drugs have the problem of not being able to fully exert their efficacy in time
In addition, the taste masking method of mixing sweeteners or correctives has the disadvantage that the bitterness cannot be completely covered and remains on the tongue.
[0006] In addition, preparations containing diphenhydramine or its acid addition salts sometimes cause discoloration due to preparation additives such as sentencing agents mixed therein, or absorb moisture under heavy humidity conditions or cause preparations to stick to each other
In addition, diphenhydramine or its acid addition salt itself changes color when exposed to light, even if the content does not decrease, there is a disadvantage of losing commercial value

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Compression molding preparation (1):

[0033] Mix 100g diphenhydramine hydrochloride (average particle size 220μm), 100g crystalline cellulose, 728g lactose, 20g cross-carboxymethyl cellulose sodium, 48g light silicon dioxide, add 240g 10% hydroxypropyl cellulose in ethanol The solution is stirred, granulated and dried, and then passed through a 20-mesh sieve. 9.8 g of magnesium stearate and 9.8 g of talc were mixed with 1009.4 g of the granules to obtain granules for compression molding. 2 The pellets for compression molding were compressed and molded to obtain a compression molding preparation with a mass of 260 mg, a diameter of 9 mm, and a thickness of 4.2 mm.

Embodiment 2

[0035] Compression molding preparation (2):

[0036] Except that the amount of crystalline cellulose was changed to 200 g and the amount of lactose was changed to 628 g, the others were the same as in Example 1, and a compression molding preparation with a mass of 260 mg, a diameter of 9 mm and a thickness of 4.2 mm was obtained.

Embodiment 3

[0038] Compression molding preparation (3):

[0039] Except that the amount of crystalline cellulose was changed to 400g and the amount of lactose was changed to 428g, the others were the same as in Example 1, and a compression molding preparation with a mass of 260 mg, a diameter of 9 mm and a thickness of 4.2 mm was obtained.

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PUM

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Abstract

A compression molded hypnotic preparation is provided, which preparation has hypnotic / sedative actions, does not discolor, is stable, masks its bitter taste, and quickly and surely produces its effects. To provide a preparation which, while containing diphenhydramine or its acid salt as a medicinal component having hypnotic / sedative actions, does not discolor, is stable, masks its bitter taste, and quickly and surely produces its effects. The compression molded hypnotic preparation contains the diphenhydramine or its acid salt as the medicinal component having hypnotic / sedative actions, a lowly swellable polymer, and a highly swellable polymer, wherein the lowly swellable polymer is selected from crystalline cellulose, ethylcellulose and aminoalkyl methacrylate copolymer RS.

Description

Technical field [0001] The present invention relates to a compression molding preparation for hypnosis, in particular, it relates to a compression molding preparation for hypnosis that contains diphenhydramine or its acid addition salt, which is stable and does not change color, masks the bitter taste when taking it, and has a quick effect. Lamin or its acid addition salt is used as a medicinal ingredient with hypnotic and sedative effects. Background technique [0002] In the past, diphenhydramine or its acid addition salt has been used as an effective ingredient for rhinitis, skin diseases, cold medicine, and antitussive and expectorant due to its antihistamine and central effects, but its existence causes drowsiness and side effects Disadvantages. [0003] For example, it is well known that diphenhydramine hydrochloride and diphenhydramine citrate have the same hypnotic effect as mild hypnotic agents. Moreover, because it disappears quickly in the blood and does not develop to...

Claims

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Application Information

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IPC IPC(8): A61K47/30A61K9/00A61K31/135A61P25/20
CPCA61K9/2027A61K9/2054A61K31/135
Inventor 冈田実菅田晴夫神户英芳
Owner SS PHARMA CO LTD
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