Pharmaceutical composition with improved dissolution properties and apparent solubility and preparation method thereof

A technology for insoluble drugs and solubility, which is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, etc. It can solve the problems of low bioavailability, many restrictions, and poor solubility, and achieve easy Industrialized production, wide range of options, stable solubilization effect

Active Publication Date: 2021-11-02
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Poor solubility and the resulting low bioavailability have been one of the key factors limiting the drug development of a large number of poorly soluble drug candidates with biological activity
CN111560018A discloses the solubilization mode of dissolving insoluble drug components in organic solvents, dispersing in aqueous solutions containing stabilizers, emulsifying, and volatilizing organic solvents to prepare insoluble drug particles, but the solubilizing effect of this method is not obvious. Drugs that are insoluble in solvents are not suitable, and the storage stability of pharmaceutical compositions in solvent environments cannot be guaranteed, which is not conducive to stable solubilization
CN105640890A discloses a method of dissolving acidic or basic drugs and polymers in alkaline or acidic solutions, and then adjusting the pH to prepare insoluble drug particles, but it does not investigate the degree of solubilization, and the drug precipitation process in this method is adjusted by pH Do not apply to unstable drugs
[0006] Therefore, for insoluble pharmaceutical ingredients, it is necessary to find a method with wide application range, good solubilization effect, high drug universality, and fast curing process to solve the problem of poor solubilization effect and many limitations.

Method used

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  • Pharmaceutical composition with improved dissolution properties and apparent solubility and preparation method thereof
  • Pharmaceutical composition with improved dissolution properties and apparent solubility and preparation method thereof
  • Pharmaceutical composition with improved dissolution properties and apparent solubility and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0271] In this example, the ursolic acid composition coated with L-grade hypromellose acetate succinate was prepared by drying by rotary evaporation.

[0272] Ursolic acid (5 mg / mL) and L-grade hypromellose acetate succinate (10 mg / mL) were dissolved in ethyl acetate containing 5% methanol and subjected to rotary evaporation. The vacuum degree is 10mbar, the temperature of the water bath is 25°C, and the rotation speed is 200rpm. A film-like composition was obtained.

Embodiment 2

[0274] In this example, the ursolic acid composition coated with L-grade hypromellose acetate succinate was prepared by spray drying.

[0275] Ursolic acid (5 mg / mL) and L-grade hypromellose acetate succinate (10 mg / mL) were dissolved in ethyl acetate containing 5% methanol and spray dried. The inlet temperature was 95°C, the outlet temperature was 60°C, and the injection rate was 10mL / h. Obtain powder composition ( figure 1 ).

Embodiment 3

[0277] In this example, an ursolic acid composition coated with L-grade hypromellose acetate succinate was prepared by drying by electrospinning.

[0278] Ursolic acid (5 mg / mL) and L-grade hypromellose acetate succinate (100 mg / mL) were dissolved in ethanol: dichloromethane 1:1 mixed solvent for electrospinning. The positive pressure is 20.0kV, the negative pressure is -1.0kV, and the flow rate is 2mL / h. Obtain fibrous composition ( figure 2 ).

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Abstract

The invention discloses a pharmaceutical composition capable of improving the dissolution property and apparent solubility of insoluble drugs. The pharmaceutical composition comprises insoluble pharmaceutical ingredient particles and a stabilizer, wherein the mass of the insoluble drug component accounts for 0.1-95% of the mass of the whole pharmaceutical composition; and the particle size of the insoluble drug component particles is 10 to 2000 nm. The apparent solubility of the medicine can be remarkably improved through the interaction of the medicine colloid particles and the stabilizer. In addition, the pharmaceutical composition can be directly used as a medicine or used as a medicine intermediate for preparing other medicine dosage forms, such as capsules, tablets, suspensions, granules, inhalants, emulsions, ointments and the like. The invention also discloses a preparation method of the pharmaceutical composition with improved dissolution property and solubility.

Description

technical field [0001] The invention relates to a pharmaceutical composition with improved drug dissolution properties and apparent drug solubility, belonging to the technical field of pharmaceutical preparations. Background technique [0002] With the application of high-throughput screening and combinatorial chemistry in drug development, poorly soluble drug candidates are increasing. 80% of candidate drugs in the R&D stage are poorly soluble drugs, and the proportion of poorly soluble drugs in marketed drugs is as high as 40% [1] . Poor solubility and the resulting low bioavailability have been one of the key factors limiting the drug development of a large number of poorly soluble drug candidates with biological activity. [0003] To increase the solubility of poorly soluble drugs, including salt formation, liposomes [2] , cyclodextrin inclusion [3] strategies are widely used. Although these strategies can increase the bioavailability of poorly soluble drugs to a ce...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K47/32A61K47/38A61K47/34A61K47/36A61K47/10A61K45/00A61K31/56A61K31/519A61K31/506A61K31/4535
CPCA61K9/1682A61K9/1635A61K9/1652A61K9/1641A61K45/00A61K31/56A61K31/519A61K31/506A61K31/4535Y02A50/30
Inventor 刘东飞张子帆冯国兵
Owner CHINA PHARM UNIV
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