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Raloxifene hydrochloride phospholipid complex solid dispersion and preparation thereof

A technology of raloxifene hydrochloride and phospholipid complex, which is applied in the field of medicine, and can solve the problems of undisclosed raloxifene hydrochloride phospholipid complex solid dispersion, different physical and chemical properties, and different solubility

Active Publication Date: 2019-06-25
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to their different physical and chemical properties, different carriers have different solubility after being dispersed with the drug phospholipid complex.
[0008] There is currently no relevant literature disclosing the solid dispersion of raloxifene hydrochloride phospholipid complex

Method used

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  • Raloxifene hydrochloride phospholipid complex solid dispersion and preparation thereof
  • Raloxifene hydrochloride phospholipid complex solid dispersion and preparation thereof
  • Raloxifene hydrochloride phospholipid complex solid dispersion and preparation thereof

Examples

Experimental program
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Effect test

example 1

[0055]Example 1: The mass ratio of raloxifene hydrochloride to phospholipid is 1:3, and the reaction solvent is tetrahydrofuran.

[0056] Weigh 150 mg of raloxifene hydrochloride and 450 mg of phospholipids, and put them into a 100 mL eggplant-shaped flask. Add 30mL of tetrahydrofuran, so that the reaction concentration of the drug is 5mg / mL, and the temperature of the water bath is raised to 60°C. The system was maintained under this condition for 2 hours, the solvent was recovered, and dried to obtain the raloxifene hydrochloride phospholipid complex. The compound rate of the drug was determined to be 27.3% according to the compound rate determination method described below.

example 2

[0057] Example 2: The mass ratio of raloxifene hydrochloride to phospholipids is 1:3, and the reaction solvent is absolute ethanol.

[0058] Weigh 150 mg of raloxifene hydrochloride and 450 mg of phospholipids, and put them into a 100 mL eggplant-shaped flask. Add 30mL of absolute ethanol to make the reaction concentration of the drug 5mg / mL, and the temperature of the water bath is raised to 60°C. The system was maintained under this condition for 2 hours, the solvent was recovered, and dried to obtain the raloxifene hydrochloride phospholipid complex. The compounding rate of the drug was determined to be 71.9% according to the compounding rate determination method described below.

example 3

[0059] Example 3: The mass ratio of raloxifene hydrochloride to phospholipids is 1:3, and the reaction solvent is acetone.

[0060] Weigh 150 mg of raloxifene hydrochloride and 450 mg of phospholipids, and put them into a 100 mL eggplant-shaped flask. Add 30 mL of acetone to make the reaction concentration of the drug 5 mg / mL, and raise the temperature of the water bath to 60°C. The system was maintained under this condition for 2 hours, the solvent was recovered and dried to obtain the raloxifene hydrochloride phospholipid complex. The compound rate of the drug was determined to be 68.1% by the compound rate determination method described below.

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Abstract

The invention belongs to the technical field of a medicine, and discloses a raloxifene hydrochloride phospholipid complex solid dispersion and a preparation method thereof. The raloxifene hydrochloride phospholipid complex solid dispersion consists of raloxifene hydrochloride, phospholipid and hydroxypropyl-beta-cyclodextrin. The raloxifene hydrochloride phospholipid complex solid dispersion is prepared by the following steps: controlling the mass ratio of raloxifene hydrochloride to phospholipid to prepare a pharmaceutically acceptable raloxifene hydrochloride phospholipid complex, and takinghydroxypropyl-beta-cyclodextrin as a carrier for preparation of the solid dispersion. The dosage form not only improves the in-vitro dissolution and solubility of raloxifene hydrochloride in the phospholipid complex, but also significantly improves the bioavailability of raloxifene hydrochloride, and has certain drug-forming properties. The prepared raloxifene hydrochloride phospholipid complex solid dispersion is mixed with the pharmaceutically acceptable carrier to prepare a clinically acceptable dosage form, and the preparation process is simple and feasible, and is advantageous for industrialized large-scale production.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a raloxifene hydrochloride phospholipid complex solid dispersion and a preparation method thereof. Background technique [0002] Raloxifene hydrochloride is a second-generation selective estrogen receptor modulator, its chemical name is: [6-hydroxy-2-(4-hydroxyphenyl) benzo[b]thiophen-3-yl]- [4-[2-(1-piperidinyl)ethoxy]-phenyl]-methanone hydrochloride, the structural formula is as follows, raloxifene hydrochloride is suitable for the treatment of osteoporosis, especially for the treatment of postmenopausal osteoporosis loose active compound. Currently on the market is mainly raloxifene hydrochloride tablets produced by Jiangsu Hengrui Pharmaceutical Co., Ltd., the trade name is [0003] [0004] Raloxifene hydrochloride is mainly absorbed by the gastrointestinal tract, but raloxifene hydrochloride has the characteristics of low water solubility and high fat so...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4535A61K47/24A61K47/40A61P19/10
Inventor 张天虹何仲贵李慧新姜琪坤卢思润
Owner SHENYANG PHARMA UNIVERSITY
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