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Pharmaceutical preparation containing copolyvidone

a technology of copolyvidone and pharmaceutical preparation, which is applied in the directions of organic chemistry, coatings, and active ingredients of heterocyclic compounds, can solve the problem of insufficient activity and achieve the effect of improving plasticity and film strength

Inactive Publication Date: 2004-01-29
TAKEDA PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0003] Tablets essentially require the addition of plasticizers in order to increase the film strength and to improve the plasticity during the process and appearance, and polyethylene glycol is generally used as plasticizers of a water-soluble coating agent.
[0326] The above-mentioned compound (I) has an excellent melatonin action and less toxicity. Further, it is safe and causes no side effects. Thus the compound can be suited for use in the preparation of the present invention.
[0330] The compound (II) has less toxicity and is also excellent in intracerebral transferability.

Problems solved by technology

However, depending on an active compound such as a pharmaceutically active ingredient, the stability of a base drug to heat or light is impaired by the addition of polyethylene glycol, thereby causing such a problem in the preparation that the activity cannot be maintained for a sufficient period even in a normal storage state in the medical field.

Method used

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Examples

Experimental program
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Effect test

reference example 2

Synthesis of Ethyl (E)-3-(2,3-Dihydrobenzofuran-5-yl)propenoate

[0336] To 2,3-dihydrobenzofuran-5-carbaldehyde obtained Reference Example 1 (832.3 mmol) / toluene solution (340 g), triethyl phosphonoacetate (205.3 g, 915.7 mmol) was added dropwise under cooling. Then, t-butoxy sodium (88.0 g, 1187.3 mmol) suspended in toluene (530 g) was added dropwise to the resultant mixture and, after stirring the mixture for one hour, acetic acid (20 g) and water (500 g) were further added dropwise thereto. The reaction mixture was raised to room temperature and partitioned. The organic layer was washed in turn with saturated sodium bicarbonate water and water and concentrated under reduced pressure until the volume is reduced to 300 mL or less. Methanol (396 g) was added and the mixture was heated to dissolve it. Water (500 g) was added dropwise thereto at room temperature and the mixture was stirred to deposit crystals. The crystals were collected by filtration and dried under reduced pressure to...

reference example 3

Synthesis of Ethyl 3-(2,3-Dihydrobenzofuran-5-yl)propionate

[0337] Ethyl (E)-3-(2,3-dihydrobenzofuran-5-yl)propionate (50.0 g, 227.3 mmol) was dissolved in acetic acid (312.0 g). After replacing the atmosphere in the system with nitrogen, 5% Pd / C (4.96 g) (as dry) was added to the solution and the system was pressurized with hydrogen up to 196 to 294 kPa. The reaction was conducted at 50.degree. C. under pressure of 196 to 294 kPa for one hour. The catalyst was removed by filtration, and then the reaction mixture was washed with acetic acid (208 g) to obtain an acetic acid solution of the title compound (yield: 569.3 g, apparent yield: 100%).

reference example 4

Synthesis of 3-(6,7-Dibromo-2,3-dihydrobenzofuran-5-yl)propionic Acid

[0338] To the PPE / acetic acid solution (569.3 g, 227.3 mmol) obtained from the process of Reference Example 3, anhydrous sodium acetate (18.6 g) was added. Bromine (221.6 g) was added dropwise to the resultant mixture over 2 hours under cooling with stirring. Then, the reaction was conducted at room temperature for 4 hours and the reaction mixture was added dropwise to a cooled aqueous 15% sodium sulfite solution (670 ml), followed by stirring for 30 minutes. Acetonitrile (118 g) was added thereto and the mixture was reacted by heating under reflux for 2 hours. The mixture was gradually cooled and stirred for one hour to deposit crystals. The crystals were collected by filtration, washed with water and then dried to obtain the title compound (yield: 63.3 g, 73.2%).

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Abstract

A stabilized preparation which comprises: a unstable drug in a polyethylene glycol-containing preparation; and a coating agent comprising a copolyvidone instead of polyethylene glycol with which the drug is coated.

Description

[0001] The present invention relates to a preparation, particularly a pharmaceutical preparation which is coated with a coating agent containing copolyvidone and is superior in storage stability, and the like.[0002] Tablets used commonly as oral preparations are formed by using various additives such as diluents, binders, lubricants, disintegrators, etc. Depending on an active compound, some tablets are less stable to light during circulation and storage and these tablets are often provided with a coating film capable of exerting a light protecting effect by film coating. It is also a useful means to form a coating film in order to prevent bitterness of a drug. This coating film is generally composed of hydroxypropylmethylcellulose (HPMC) or hydroxypropylcellulose (HPC) as water-soluble coating film agents, polyethylene glycol (PEG) as plasticizers and titanium dioxide as light-protecting agents and, if necessary, iron sesquioxide such as colorants.OBJECTS OF THE INVENTION[0003] Tab...

Claims

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Application Information

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IPC IPC(8): A61K9/28A61K9/32A61K9/36A61K31/137A61K31/343A61K31/352A61K31/36A61K31/407A61K47/32C07D307/93C07D491/048C07D491/052
CPCA61K9/284A61K9/2866A61K31/137A61K31/343C07D307/93A61K31/36A61K31/407A61K47/32A61K31/352A61K9/2813
Inventor ISHIDA, HAJIMEFUKUTA, MAKOTO
Owner TAKEDA PHARMA CO LTD
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