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Bazedoxifene acetate dispersing tablet and preparation method thereof

A technology of bazedoxifene acetate and dispersible tablets, which is applied in the direction of active ingredients of heterocyclic compounds, pill delivery, bone diseases, etc., can solve the problems of low bioavailability and stimulation of the body, and achieve the purpose of improving bioavailability, reducing The effect of stimulating small organisms and stabilizing properties

Inactive Publication Date: 2014-06-18
王志刚
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The present invention provides a new bazedoxifene acetate dispersible tablet, which is based on the problems of the existing bazedoxifene acetate ordinary tablet that the added surfactant is irritating to the body and the bioavailability is not high.

Method used

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  • Bazedoxifene acetate dispersing tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Bazedoxifene Acetate 100g

[0033] Lactose 120g

[0034] Cross-linked polyvinylpyrrolidone 25g

[0035] Carboxymethyl starch sodium 50g

[0036] Hypromellose 4g

[0037] Micropowder silica gel 15g

[0038] Magnesium stearate 10g

[0039] 60g of water

[0040] 95% ethanol 126g

[0041] Made in 1000 pieces.

[0042] Preparation:

[0043] Step 1: Pass the pulverized bazedoxifene acetate and pharmaceutical excipients through a 120-mesh sieve, swell the hydroxypropyl methylcellulose with hot water, stir until dissolved, and then add ethanol to make the ethanol concentration reach 70%.

[0044] Step 2: Mix bazedoxifene acetate, lactose, crospovidone, and micronized silica gel evenly according to the prescription amount, and add the hypromellose solution described in step 1 to make a soft material.

[0045] Step 3: Pass the soft material prepared in step 2 through a 18-mesh sieve to granulate, dry at 50°C, the water content is 2.6%, and granulate through an 18-mesh si...

Embodiment 2

[0050] Bazedoxifene Acetate 100g

[0051] Lactose 80g

[0052] Cross-linked polyvinylpyrrolidone 14g

[0053] Carboxymethyl starch sodium 20g

[0054] Hypromellose 3.5g

[0055] Citric acid 100g

[0056] Micropowder silica gel 15g

[0057] Magnesium stearate 7.5g

[0058] 60g of water

[0059] 95% ethanol 80g

[0060] Made in 1000 pieces.

[0061] Preparation:

[0062] Step 1: Pass the pulverized bazedoxifene acetate and pharmaceutical excipients through a 120-mesh sieve, swell the hydroxypropyl methylcellulose with hot water, stir until dissolved, and then add ethanol to make the ethanol concentration reach 70%. Separately take 50 g of the above-mentioned hydroxypropyl methylcellulose solution, add 60 g of water, add citric acid and mix well.

[0063] Step 2: The prescribed amount of bazedoxifene acetate and the citric acid solution in step 1 are embedded in fluidized bed acid, and then mixed with the prescribed amount of lactose, cross-linked polyvinylpyrrolidone, ...

Embodiment 3

[0069] Bazedoxifene Acetate 100g

[0070] Cross-linked polyvinylpyrrolidone 40g

[0071] Carboxymethyl starch sodium 40g

[0072] Hypromellose 3.5g

[0073] Citric acid 100g

[0074] Micropowder silica gel 15g

[0075] Magnesium stearate 7.5g

[0076] 90g of water

[0077] 95% ethanol 54g

[0078] Made in 1000 pieces.

[0079] The preparation method is the same as in Example 2.

[0080] Implementation 3 increased the content of cross-linked polyvinylpyrrolidone and sodium starch glycolate, and the dispersibility of the dispersible tablets met the requirements of the 2010 edition of the Pharmacopoeia, and the dissolution rate was better.

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Abstract

The invention discloses a bazedoxifene acetate dispersing tablet, and a preparation method and application thereof. The bazedoxifene acetate dispersing tablet comprises the following components in percentage by weight: 5-40 percent of bazedoxifene acetate, 10-50 percent of filler, 10-50 percent of disintegrating agent, 10-50 percent of acidifying agent, 0.1-15 percent of adhesive and 0.1-20 percent of lubricant and glidant. Compared with a common tablet, the bazedoxifene acetate dispersing tablet does not contain surfactant, has excellent solubility, dispersibility and disintegration, and can be completely disintegrated in 1 minute. The bazedoxifene acetate dispersing tablet prepared by adopting the method has the advantages of high solubility, good bioavailability, quick in-vivo distribution, stable quality and good taste; the preparation method is simple and practical, and is suitable for industrial production.

Description

field of invention [0001] The invention relates to the field of chemical pharmacy, in particular to a bazedoxifene acetate dispersible tablet and a preparation method thereof. Background of the invention [0002] For more than half a century, improving the quality of life of postmenopausal women has attracted more and more attention. Hormone replacement therapy (HRT) has been widely used in perimenopausal and postmenopausal women. Although evidence from observational data has accumulated over the years, the benefits and harms of HRT in healthy postmenopausal women are still being explored. On the one hand, people are in-depth research on more scientific and reasonable HRT programs, and on the other hand, they are looking for more ideal drugs suitable for postmenopausal women. Selective estrogen receptor modulators (SERMS) are a class of synthetic drugs that play estrogen-like effects in some tissues and anti-estrogen-like effects in other tissues, and are expected to be use...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/55A61K47/12A61K47/22A61K47/18A61P19/10A61P35/00
Inventor 王志刚崔书豪陈洪瑜薛清佩
Owner 王志刚
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