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Pharmaceutical composition for solubility enhancement of hydrophobic drugs

A hydrophobic drug and composition technology, applied in powder delivery, pill delivery, etc., can solve the problems of increasing disintegrants and carrier materials, adverse effects of tablet drug loading, etc., and achieve the effect of rapid dissolution

Inactive Publication Date: 2006-11-01
SANDOZ AG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, increasing the amount of disintegrant and carrier material can adversely affect either tablet size or tablet drug loading

Method used

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  • Pharmaceutical composition for solubility enhancement of hydrophobic drugs
  • Pharmaceutical composition for solubility enhancement of hydrophobic drugs
  • Pharmaceutical composition for solubility enhancement of hydrophobic drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0108] Preparation of Surfactant-Containing Raloxifene HCl-PEG Solid Dispersion.

[0109] 2.5 g of PEG 4500 was placed in a 50 mL beaker with a magnetic stirrer and melted to a liquid on a hot plate. 5 drops of polysorbate 80 (approximately 2%) were added to the beaker and mixed. The mixture was stirred vigorously and 2.5 g of Raloxifene HCl was added to the mixture to form a dispersion. Homogeneous mixing was performed at room temperature, and the mixture was then cooled. The resulting solid was triturated and dried under vacuum at room temperature overnight.

Embodiment 2

[0111] Preparation of Surfactant-Containing Raloxifene HCl-PEG Solid Dispersion.

[0112] Follow the steps described in Example 1, except that PEG 8000 is used instead of PEG4500, the amount of PEG 8000:raloxifene HCl is 0.2:1 to 5:1, and the amount of polysorbate 80 is 1-5% .

Embodiment 3

[0114] Preparation of Surfactant-Free Raloxifene HCl-PEG Solid Dispersion.

[0115] 2.5 g of PEG 4500 was placed in a 50 mL beaker with a magnetic stirrer and melted to a liquid on a hot plate. 5 mL of isopropanol was added to the beaker and mixed. The mixture was vigorously stirred and 2.5 g of Raloxifene HCl was dispersed therein. Homogeneous mixing was performed at room temperature, and the mixture was then cooled. The resulting solid was triturated and dried under vacuum at room temperature overnight.

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Abstract

The present invention provides a pharmaceutical composition comprising a drug and polyethylene glycol, wherein the ratio of polyethylene glycol to drug by weight is from about 0.2:1 to about 10:1, and the polyethylene glycol has a melting point of at least 37oC. The pharmaceutical compositions of the invention exhibit rapid dissolution upon contact with physiological solvents, such as water, saliva or gastrointestinal fluids.

Description

technical field [0001] The invention provides a pharmaceutical composition comprising a drug and polyethylene glycol, wherein the weight ratio of polyethylene glycol to drug is from about 0.2:1 to about 10:1, and the polyethylene glycol has a melting point of at least 37°C. More specifically, the present invention provides pharmaceutical compositions with increased solubility. Background technique [0002] Hydrophobic drugs, ie, drugs with poor solubility in aqueous solutions, present formulation difficulties for effective administration to patients. A well-designed formulation must at least deliver a therapeutically effective amount of the hydrophobic drug in an absorbable form to the desired site of absorption. But even this minimal function is difficult for hydrophobic drugs because of their slow disintegration or dissolution. Especially in intestinal fluids, insufficiently dissolved drugs cannot enter the blood through the small intestinal wall and are simply excreted ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K9/14
CPCA61K9/146A61K9/2031
Inventor A·K·拉伊I·南迪S·帕兰尼斯韦米P·达维拉A·H·沃拉
Owner SANDOZ AG
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