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Tamoxifen citrate dispersible tablets

A technology of tamoxifen and citric acid, applied in the field of dispersible tablets, can solve the problems of slow onset of action and low bioavailability

Active Publication Date: 2015-02-18
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 slow onset of action and low bioavailability of existing tamoxifen citrate preparations, the present invention has invented tamoxifen citrate inclusion compound dispersible tablets

Method used

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  • Tamoxifen citrate dispersible tablets
  • Tamoxifen citrate dispersible tablets
  • Tamoxifen citrate dispersible tablets

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Tamoxifen citrate inclusion complex: Tamoxifen citrate: α-cyclodextrin ratio 1:2

[0026]

[0027] Preparation:

[0028] 1. Prepare tamoxifen citrate inclusion compound according to the following method:

[0029] (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 mixture thing; or

[0030] (2) In solid form, reacting tamoxifen citrate with alpha-cyclodextrin; or

[0031] (3) Tamoxifen citrate reacts with α-cyclodextrin for high-energy grinding.

[0032] 2. Mix the prescription amount of low-substituted hydroxypropyl cellulose, sodium carboxymethyl starch, sorbitol, cyclamate and tamoxifen citrate inclusion compound according to the equal addition method, and then add stearic acid Magnesium and micropowder silica gel, mixed evenly, and compressed into tablets to obtain tamoxifen citrate ...

Embodiment 1

[0034] Tamoxifen citrate inclusion complex: Tamoxifen citrate: α-cyclodextrin ratio 1:2

[0035]

[0036] The preparation method is the same as above

Embodiment 2

[0038] Tamoxifen citrate inclusion complex: Tamoxifen citrate: α-cyclodextrin ratio 1:2

[0039]

[0040] The preparation method is the same as above

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Abstract

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

Description

technical field [0001] The present application relates to a dispersible tablet, specifically, a tamoxifen citrate inclusion compound dispersible 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 estrogen for the ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/20A61K31/138A61K47/48A61P15/14A61P35/00
Inventor 李春涛李申申峰邱俊
Owner NANTONG GUANGTAI BIOCHEM PROD
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