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Tamoxifen citrate sustained-release tablets

A technology of tamoxifen and sustained-release tablets, applied in the field of sustained-release tablets, can solve the problems of low bioavailability, prolonging biological half-life, slowing down absorption rate, etc.

Active Publication Date: 2013-10-16
NANTONG GUANGTAI BIOCHEM PROD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] In order to solve the shortcomings of the existing tamoxifen citrate preparations, which are inconvenient to take and have low bioavailability, the present invention has invented tamoxifen citrate inclusion complex sustained-release tablets, which can reduce the number of times of taking medicine, slow down the absorption rate, prolong the Biological half-life, so that the blood concentration is controlled within the effective blood concentration range, thereby reducing side effects and improving patient compliance

Method used

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  • Tamoxifen citrate sustained-release tablets
  • Tamoxifen citrate sustained-release tablets
  • Tamoxifen citrate sustained-release tablets

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Example 1 Prescription

[0037] Tamoxifen citrate inclusion compound: Tamoxifen citrate: α-cyclodextrin ratio is 1:2

[0038] Tamoxifen citrate inclusion compound 24.5 parts

[0039] The composition of mannitol and microcrystalline cellulose (the weight ratio of the two is 6:2.3) 27 parts

[0040] 4 parts of 3% polyvinylpyrrolidone 95% ethanol solution

[0041] 11 parts methylcellulose

[0042] Composition of crospovidone and sodium carboxymethyl starch (the weight ratio of the two is 4:7.5) 14 parts

[0043] Talc powder 5 parts

[0044] Sodium carboxymethyl cellulose 17 parts

[0045] 12 parts ethyl cellulose

[0046] Preparation:

[0047] 1. Prepare tamoxifen citrate inclusion compound according to the following method:

[0048] (1) In water or aqueous ethanol medium, react tamoxifen citrate with α-cyclodextrin in a certain proportion, filter the resulting solution through a microporous membrane until clarified, and separate the inclusion complex from the mixt...

Embodiment 2

[0053] Fully grind tamoxifen citrate and α-cyclodextrin described in Example 1 in 50% ethanol to form a uniform paste, and obtain a white powder after vacuum drying. Tamoxifen citrate increased 12-fold.

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Abstract

The invention relates to tamoxifen citrate sustained-release tablets, the preparation method of which comprises the steps of preparing tamoxifen citrates into clathrate compounds and further preparing the clathrate compounds into sustained-release tablets.

Description

technical field [0001] The present application relates to a sustained-release tablet, specifically, a tamoxifen citrate inclusion complex sustained-release tablet. Background technique [0002] Tamoxifen (TAM) is a non-steroidal compound approved by the US Food and Drug Administration in 1977 for the treatment of metastatic breast cancer in postmenopausal women. After nearly 30 years of application history, it is now also used to prevent the occurrence of breast cancer. TAM belongs to the first generation of selective estrogen receptor modulators (selective estrogen receptor modulators, SERMs), which have dual effects of estrogen agonism and estrogen antagonism, and this effect depends on different germlines, tissues and gene expression types, Different target organs or target cells have different effects. For example, TAM produces antagonizing estrogen in mammary gland tissue, while it produces estrogen agonizing effect in uterus and bone tissue. TAM competes with estrog...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K31/138A61K47/48A61K47/38A61P35/00
Inventor 李春涛李申申峰邱俊
Owner NANTONG GUANGTAI BIOCHEM PROD
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