Preparation method for nano-granular solid dispersion of hydrophobic drug by high-voltage electrostatic spraying

A technology of high-voltage electrostatic spraying and hydrophobic drugs, which is applied in the direction of making drugs into special physical or ingestible devices, etc., which can solve the problem that the degree of entanglement of polymer molecules cannot be guaranteed, the stability of solid dispersions is not good, and it should not be too high Problems such as clogging of the spinning head, etc., achieve the effect of low cost, fast drying and convenient operation

Inactive Publication Date: 2011-10-19
UNIV OF SHANGHAI FOR SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The existing solid dispersion preparation technology has developed from the initial melting method to more than 10 methods including various solvent volatilization methods. Among them, the main problems of the traditional solvent volatilization method for preparing solid dispersions are: (1) the prepared Solid dispersions often need to be sieved and pulverized, and then compressed into tablets for dosage form conversion; (2) Solid dispersions have poor stability, drug recrystallization, and agglomeration are serious; (3) During the preparation process, as the drying progresses, Co-precipitates become increasingly viscous, making it difficult to remove organic solvents quickly and efficien

Method used

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  • Preparation method for nano-granular solid dispersion of hydrophobic drug by high-voltage electrostatic spraying
  • Preparation method for nano-granular solid dispersion of hydrophobic drug by high-voltage electrostatic spraying
  • Preparation method for nano-granular solid dispersion of hydrophobic drug by high-voltage electrostatic spraying

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Effect test

Embodiment 1

[0050] High-voltage electrostatic spraying prepares hydrophobic drug nanoparticles--the method for paracetamol solid dispersion, comprising the steps:

[0051] (1) Preparation of paracetamol and polymer spinning solution

[0052] Polyvinylpyrrolidone (PVP K25) is used as the drug-loaded polymer substrate, and ethanol is used as the solvent to add paracetamol and the drug-loaded polymer substrate according to the mass ratio, that is, the ratio of paracetamol: drug-loaded polymer substrate is 1:10 Dissolve in an ethanol solvent to prepare a transparent and clear eutectic electrospray solution;

[0053] The eutectic electrospray solution is calculated by mass percentage, wherein the PVP content is 20%, the paracetamol content is 2%, and the rest are ethanol solvents;

[0054] (2), preparation of paracetamol solid dispersion

[0055] The eutectic electrospray solution obtained in step (1) was subjected to high-voltage electrostatic spraying, the flow rate of the high-voltage ele...

Embodiment 2

[0065] High-voltage electrostatic spraying prepares hydrophobic drug nanoparticles--the method for paracetamol solid dispersion, comprising the steps:

[0066] (1) Preparation of paracetamol and polymer spinning solution

[0067] Polyvinylpyrrolidone (PVP K25) is used as the drug-loaded polymer substrate, and ethanol is used as the solvent to mix paracetamol and the drug-loaded polymer substrate according to the mass ratio, that is, the ratio of paracetamol: drug-loaded polymer substrate is 5:10 Added to ethanol for dissolution to prepare a transparent and clear eutectic electrospray solution;

[0068] In the co-dissolving electrospray solution, calculated by mass percentage, the PVP content is 20%, the paracetamol content is 10%, and the rest is ethanol solvent;

[0069] (2), preparation of paracetamol solid dispersion

[0070] The co-dissolution electrospray solution obtained in step (1) was subjected to high-voltage electrostatic spraying according to the conditions of Ex...

Embodiment 3

[0072] High-voltage electrostatic spraying prepares hydrophobic drug nanoparticles--the method for paracetamol solid dispersion, comprising the steps:

[0073] (1) Preparation of paracetamol and polymer spinning solution

[0074] Polyvinylpyrrolidone (PVP K25) is used as the drug-loaded polymer substrate, and ethanol is used as the solvent to mix paracetamol and the drug-loaded polymer substrate according to the mass ratio, that is, the ratio of paracetamol: drug-loaded polymer substrate is 5:20 Add it to ethanol solvent for dissolution to prepare a transparent and clear eutectic electrospray solution;

[0075] In the co-dissolving electrospray solution, calculated by mass percentage, the PVP content is 20%, the paracetamol content is 5%, and the rest is ethanol solvent;

[0076] (2), preparation of paracetamol solid dispersion

[0077] The co-dissolution electrospray solution obtained in step (1) was subjected to high-voltage electrostatic spraying according to the conditio...

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Abstract

The invention relates to a preparation method for a nano-granular solid dispersion of a hydrophobic drug by high-voltage electrostatic spraying, which comprises the following steps of: mixing a hydrophobic drug, a drug-carrying polymer and an organic solvent at a mass ratio of (1-10): (10-20): (80-94) to prepare a consolute electric spraying solution; and then carrying out high-voltage electrostatic spraying while controlling the flow rate of the consolute electric spraying solution at 0.5-2.5 mL/h, the distance between a receiving board and a wire spraying port at 15-30cm and the voltage at 5-30kV to obtain the nano-granular solid dispersion of the hydrophobic drug. The preparation method is simple to operate, is low in cost, is environmentally-friendly and is suitable for industrial production; and the prepared solid dispersion of the hydrophobic drug not only can highly disperse a composite of a polymer and the drug into an amorphous state and has a nano-structural characteristic.

Description

technical field [0001] The invention belongs to the field of preparation of solid dispersions, in particular to a method for preparing hydrophobic drug nanoparticle solid dispersions by high-voltage electrostatic spraying. Background technique [0002] Although the application of high-throughput screening and combinatorial chemistry, as well as the rapid development of bioengineering technology, more and more active substances can be used in the treatment and protection of diseases, but more than 40% of them have solubility problems. In the existing drugs, there are also a large number of compounds with poor water solubility. Therefore, researchers in the field of pharmacy have been looking for various technologies or strategies to improve the solubility of drugs, so as to improve the bioavailability of drugs, enhance curative effect, and reduce toxicity. These technologies include micronization of drugs, modified PEGylation, saccharification, synthesis of water-soluble pro...

Claims

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Application Information

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IPC IPC(8): A61J3/02
Inventor 余灯广王霞李晓燕李颖钱微
Owner UNIV OF SHANGHAI FOR SCI & TECH
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