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Tamoxifen citrate particles

A technology of tamoxifen and citric acid, applied in the field of granules, can solve the problem of low bioavailability

Active Publication Date: 2013-11-20
NANTONG GUANGTAI BIOCHEM PROD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In order to solve the shortcoming of low bioavailability of existing tamoxifen citrate preparations, the present invention has invented tamoxifen citrate inclusion compound granules

Method used

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  • Tamoxifen citrate particles
  • Tamoxifen citrate particles
  • Tamoxifen citrate particles

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Example 1 Prescription

[0029] Tamoxifen citrate inclusion compound: Tamoxifen citrate: α-cyclodextrin ratio is 1:2

[0030] Tamoxifen citrate inclusion compound 36.2 parts

[0031] The composition of microcrystalline cellulose and sucrose (the weight ratio of the two is 6.2:2.7) 31 parts

[0032] Composition of crospovidone and croscarmellose sodium (the weight ratio of the two is 2:5.7) 22.6 parts

[0033] 5 parts aspartame

[0034] Preparation:

[0035] 1. Prepare tamoxifen citrate inclusion compound according to the following method:

[0036] (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

[0037] (2) In solid form, reacting tamoxifen citrate with alpha-cyclodextrin; or

[0038] (3) Tamoxifen citrate reacts with α-cyclodextrin for high-energy grinding.

[003...

Embodiment 2

[0041] 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 particles which are prepared by the following steps: firstly, preparing tamoxifen citrate into inclusion compounds; and then, preparing the particles.

Description

technical field [0001] The present application relates to a granule, specifically, tamoxifen citrate inclusion complex granules. 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 estrogen receptor (ER) i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/138A61K47/40A61P35/00
Inventor 李春涛李申邱俊
Owner NANTONG GUANGTAI BIOCHEM PROD
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