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

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...

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 efficiently

[0009] However, the preparation of solid dispersion by high-voltage electrospinning technology must meet the following requirements: (1) There is a co-solvent solvent for the drug and the polymer; (2) In the selected solvent, the polymer must have good filament-forming properties; (3) The polymer’s The concentration is limited, it can't be too high to block the spinning head, and it can't be too low, otherwise it can't ensure enough entanglement between polymer molecules to ensure the formation of uniform drug-loaded composite fibers

Therefore, the spinnability of the polymer itself greatly limits the application of high-voltage electrospinning technology in the development of solid dispersions.

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