Extended release formulation contg. venlafaxin

A continuous release and preparation technology, applied in the directions of non-active ingredient medical preparations, medical preparations containing active ingredients, and drug combinations, etc., can solve the problems of heat accumulation, difficult cylinder transformation, etc. Effect

Inactive Publication Date: 2000-12-27
AMERICAN HOME PRODUCTS CORPORATION
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Heat build-up occurs during extrusion, which dries the extrudate so much that it is difficult to convert the extruded cylinder into pellets

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] A mixture of 44.8 parts (88.4% free base) of venlafaxine hydrochloride, 74.6 parts of microcrystalline cellulose (NF) and 0.60 parts of hydroxypropylmethylcellulose 2208 (USP) was blended by adding 41.0 parts of water. The plastomer is extruded, pelletized and dried to form drug-containing uncoated pellets.

[0030] Stir 38.25 parts of ethylcellulose (NF, HG 2834) and 6.75 parts of hydroxypropylmethylcellulose 2910 (USP) in a 1:1 (v / v) mixture of dichloromethane / anhydrous methanol until coated. The membrane material is completely dissolved.

[0031] 0.667 parts of coating solution per part of uncoated pellets were applied to the fluidized bed of uncoated pellets to give sustained release coated pellets with a coating level of 3%.

[0032] The pellets were sieved to retain the coated pellets with a particle size of 0.85-1.76 mm. These coated pellets are selected and filled into hard gelatin capsules in the conventional manner.

Embodiment 2

[0034] Same as Example 1 except that 1.11 parts of coating solution was applied per part of uncoated pellets to achieve a coating level of 5%.

Embodiment 3

[0036] Same as Example 1 except that 1.33 parts of coating solution was applied per part of uncoated pellets to give a coating level of 6%.

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PUM

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Abstract

This invention relates to a 24 hour extended release dosage formulation and unit dosage form thereof of venlafaxine hydrochloride, and antidepressant, which provides better control of blood plasma levels than conventional tablet formulations which must be administered two or more times a day and further provides a lower incidence of nausea and vomiting than the conventional tablets. In its primary aspect, this invention provides an improved core of the extended release spheroids comprised of venlafaxine hydrochloride and microcrystalline cellulose, that is, without the addition of hydroxypropylmethylcellulose.

Description

Background of the invention [0001] Sustained release pharmaceutical formulations are usually made as compressed tablets using hydrogel tablet technology. To manufacture these sustained-release tablet dosage forms, the active ingredient is usually combined with a cellulose ether (such as methylcellulose, ethylcellulose or hydroxypropylmethylcellulose) with or without other excipients. element) were mixed and the resulting mixture was compressed into tablets. When these tablets are taken orally, the cellulose ether in the tablet swells when hydrated by moisture in the digestive system, thereby limiting the active ingredient's exposure to moisture. As the cellulose ether is gradually leached out by the water, which penetrates deeper into the gel matrix, the active ingredient slowly dissolves and diffuses through the gel, allowing it to be absorbed by the body. U.S. Patent 4,966,768 has analgesic / anti-inflammatory drug itodolac (Lodine  ) is an example of such a sustained rele...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K9/50A61K9/52A61K31/137A61K47/38A61P25/24
CPCA61K31/137A61K9/5047A61K9/1652A61P25/24A61K9/48
Inventor D·M·舍尔曼J·C·克拉克J·U·拉默
Owner AMERICAN HOME PRODUCTS CORPORATION
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