Hydrochloric acid raloxifene dispersible tablet and preparation method thereof

A technology of raloxifene hydrochloride and dispersible tablets, which is applied in the directions of non-active ingredient medical preparations, medical preparations containing active ingredients, pharmaceutical formulas, etc., can solve the problems of low bioavailability, irritation to the body, and the like, Achieve the effect of improving bioavailability, reducing body irritation, and rapidly distributing in the body

Inactive Publication Date: 2014-06-04
崔书豪
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The present invention provides a new raloxifene hydrochloride dispersible tablet, which is based on the problems of the existing raloxifene hydrochloride ordinary tablet that the added surfactant is irritating to the body and the bioavailability is not high.

Method used

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  • Hydrochloric acid raloxifene dispersible tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Raloxifene Hydrochloride 120g

[0034] Lactose 120g

[0035] Cross-linked polyvinylpyrrolidone 25g

[0036] Carboxymethyl Starch Sodium 50g

[0037] Hypromellose 4g

[0038] Micronized silica gel 15g

[0039] Magnesium Stearate 10g

[0040] water 60g

[0041] 95% ethanol 106g

[0042] Made in 1000 pieces.

[0043] Preparation:

[0044] Step 1: Pass the pulverized raloxifene hydrochloride and pharmaceutical excipients through a 120-mesh sieve, swell the hypromellose with hot water first, stir until dissolved, and then add ethanol to make the ethanol concentration reach 70%.

[0045] Step 2: Mix raloxifene hydrochloride, 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.

[0046] 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 sieve...

Embodiment 2

[0051] Raloxifene Hydrochloride 120g

[0052] Lactose 80g

[0053] Cross-linked polyvinylpyrrolidone 14g

[0054] Carboxymethyl Starch Sodium 20g

[0055] Hypromellose 3.5g

[0056] Citric acid 100g

[0057] Micronized silica gel 15g

[0058] Magnesium Stearate 7.5g

[0059] water 60g

[0060] 95% ethanol 60g

[0061] Made in 1000 pieces.

[0062] Preparation:

[0063] Step 1: Pass the pulverized raloxifene hydrochloride and pharmaceutical excipients through a 120-mesh sieve, swell the hypromellose with hot water first, 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.

[0064] Step 2: The prescription amount of raloxifene hydrochloride and the citric acid solution in step 1 are embedded in a fluidized bed acid, and then mixed with the prescription amount of lactose, cross-linked polyvinylpyrrolidon...

Embodiment 3

[0070] Raloxifene Hydrochloride 120g

[0071] Cross-linked polyvinylpyrrolidone 40g

[0072] Carboxymethyl Starch Sodium 40g

[0073] Hypromellose 3.5g

[0074] Citric acid 100g

[0075] Micronized silica gel 15g

[0076] Magnesium Stearate 7.5g

[0077] water 80g

[0078] 95% ethanol 44g

[0079] Made in 1000 pieces.

[0080] The preparation method is the same as in Example 2.

[0081] 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 hydrochloric acid raloxifene dispersible tablet and a preparation method and an application thereof. The hydrochloric acid raloxifene dispersible tablet consists of the following components by weight percent: 5-50% of hydrochloric acid raloxifene, 10-40% of a filling agent, 10-50% of a disintegrating agent, 10-50% of an acidifying agent, 0.1-15% of an adhesive and 0.1-20% of a lubricating agent and flow aid. In comparison with the ordinary tablet, the hydrochloric acid raloxifene dispersible tablet does not contain surface active agents, is favorable in solubility, dispersibility and disintegrative, and can disintegrate completely within 1min. The hadrochloric acid raloxifene dispersible tablet prepared by the method is high in dissolution rate, good in biological availability, rapid in body distribution, stable in quality and good in mouth feeling. The preparation method is simple and feasible and suitable for industrial production.

Description

field of invention [0001] The invention relates to the field of chemical pharmacy, in particular to a raloxifene hydrochloride 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...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/4535A61K47/22A61K47/18A61K47/12A61K47/04A61P19/10A61P15/00A61P15/14A61P35/00
Inventor 崔书豪王志刚薛清佩陈洪瑜
Owner 崔书豪
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