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Trospium chloride slow-release tablet

A chloramine and sustained-release technology, applied in the field of pharmaceutical preparations, can solve the problems of low drug release amount and inability to reach effective blood drug concentration and the like

Active Publication Date: 2011-11-23
北京化药科创医药科技发展有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] In U.S. Patent No. 7,410,978, a prescription and preparation method of a slow-release tablet are disclosed. The slow-release tablet part is to use a tablet core first, prepare a drug-containing layer tablet on the tablet core, and then pack the tablet containing the active ingredient. Coating sustained-release film coating, the film coating used is acrylic acid and ethyl methacrylate copolymer, or cellulose-based sustained-release materials such as hydroxypropyl methylcellulose. In the solution, no more than 10% of the drug ingredients will be released within 2 hours, and about 20%-30% will be released within 4 hours. Only the sustained release part can not reach the effective blood drug concentration due to the small amount of initial drug release.

Method used

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  • Trospium chloride slow-release tablet

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Embodiment 1～4

[0025] The sustained-release matrix is ​​prepared in this way: put the required xanthan gum, calcium sulfate, and PEG in water (the ratio of water is 1 to 4 times the total amount of the sustained-release matrix), stir to make it fully dissolve, and use it as a sustained-release matrix. The matrix solution is spray-dried in a spray dryer to prepare particles. The inlet temperature of the spray drying is 90°C, the outlet temperature is 80°C, the feed rate is 6ml / min, the atomizer pressure is 75kpa, and the particles are collected in the cyclone separator , get particles. The components of the sustained release matrix are listed in Table 1 below.

[0026] Table 1 Composition of Sustained Release Matrix

[0027] components

Example 1 (%)

Example 2 (%)

Example 3 (%)

Example 4 (%)

xanthan gum

50

70

60

100

Calcium sulfate

35

10

26

0

PEG2000

15

20

14

0

water* ...

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Abstract

The invention relates to a 24-hour slow-release tablet of trospium chloride or medicinal salt thereof. The slow-release tablet is a single-layer tablet, and can ensure the release of the trospium chloride or the medicinal salt thereof within at least 24 hours after taking medicine.

Description

technical field [0001] The invention relates to a sustained-release tablet of trospamine or its pharmaceutically acceptable salt, which can provide a sustained-release effect for at least 24 hours, and belongs to the field of pharmaceutical preparations. Background technique [0002] Trospium chloride is a tropic acid derivative with four ammonium groups. It is a parasympathetic blocker, and its effect is similar to that of atropine. It plays a role in reducing the tension of parasympathetic nerves and removing the smooth muscle spasm caused by parasympathetic nerves on the organs dominated by parasympathetic nerves. It also has certain effects on the gastrointestinal tract, biliary tract and urinary tract. [0003] Trospium chloride, a tetraammonium derivative of nortropinone, competes with the endogenous transmitter acetylcholine for postsynaptic binding sites. Trospium chloride binds to the surface amino acids of G protein membrane receptors, thereby inhibiting and antag...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/22A61K31/46A61K47/36A61K47/40A61K47/38A61P13/10A61P1/06A61P1/16
Inventor 关屹闫冬
Owner 北京化药科创医药科技发展有限公司
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