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Tamoxifen citrate tablets

A technology of tamoxifen and citric acid, applied in the directions of organic active ingredients, non-active ingredients of polymer compounds, pharmaceutical formulations, etc., can solve problems such as 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 tablet

Method used

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Example 1 Prescription

[0034] Tamoxifen citrate inclusion compound: Tamoxifen citrate:α-cyclodextrin is 1:2

[0035] Tamoxifen citrate inclusion compound 20.5 parts

[0036] Composition of starch and microcrystalline cellulose (the weight ratio of the two is 5.1:2.9) 18.5 parts

[0037] 11 parts of 3% polyvinylpyrrolidone 95% ethanol solution

[0038] 8 parts of sodium alginate

[0039] Composition of croscarmellose sodium and sodium carboxymethyl starch

[0040] (The weight ratio between the two is 3.3:4.7) 27 parts

[0041] Micro powder silica gel 4.6 parts

[0042] Preparation:

[0043] 1. Prepare the tamoxifen citrate inclusion compound according to the following method:

[0044] (1) React tamoxifen citrate with α-cyclodextrin in a water or water-containing ethanol medium in a certain proportion, and filter the resulting solution through a microporous membrane until it is clear, and separate the inclusion compound from the mixture Thing; or

[0045] (2) Reacting tamoxifen citrate...

Embodiment 2

[0049] The tamoxifen citrate and α-cyclodextrin described in Example 1 were fully ground in 50% ethanol to form a uniform paste. After vacuum drying, a white powder was obtained. The solubility of the powder in water is relatively low. The tamoxifen citrate increased by 12 times.

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Abstract

The invention relates to tamoxifen citrate tablets which are prepared by the following steps: firstly, preparing tamoxifen citrate to inclusion compounds; and then, preparing the tablets.

Description

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

Claims

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Application Information

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IPC IPC(8): A61K9/36A61K31/138A61K47/40A61P35/00
Inventor 李申李春涛邱俊
Owner NANTONG GUANGTAI BIOCHEM PROD