Diosmetin solid self-microemulsion nanoparticles prepared by electrostatic spraying method and preparation method thereof

Abstract

The invention discloses diosmetin solid self-microemulsion nanoparticles prepared by an electrostatic spraying method and a preparation method thereof, and relates to the field of nano pharmaceutical preparations. The nanoparticle is composed of diosmetin, a self-microemulsion and a solid carrier and is prepared based on an electrostatic spraying method, a medicine, an oil phase, an emulsifier and a co-emulsifier form a liquid self-microemulsion, a hydrophilic solid carrier and a spinning aid are added to form a uniform working solution, and the diosmetin solid self-microemulsion nanoparticle is prepared through a single-shaft electrostatic spraying method. According to the nano preparation, the solubility of diosmetin is remarkably increased, the in-vitro drug release speed of diosmetin is increased, and the oral bioavailability is improved. The method is simple in process and high in industrialization degree, and the prepared diosmetin solid self-microemulsion nanoparticles are uniform in particle size and stable in character and have good application prospects.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to solid self-microemulsion nanoparticles of an insoluble active ingredient diosmin and a preparation method thereof. Background technique [0002] Diosmetin, the molecular formula is C 16 h 12 o 6 , the chemical name is 3',5,7-trihydroxy-4'-methoxyflavone, which is mainly extracted from lemon, citrus, chrysanthemum, leguminous plants and olive leaves. Various pharmacological effects such as infection and anti-shock (see: Yang Y, Gong X-B, Huang L-G, et al. Diosmetin exerts anti-oxidative, anti-inflammatory and anti-apoptotic effects to protect against endotoxin-induced acute hepatic failure in mice[J] . Oncotarget. 2017, 8(19): 30723-30733). Dianophyllin is light yellow powder, odorless and tasteless, extremely insoluble in water, but soluble in organic solvents such as methanol and ethanol. In addition, studies have reported that diosmin can alleviate lipopolysaccha...

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Problems solved by technology

[0004] At present, there are few patents on the preparation of solid self-microemulsion nanoparticles, mainly including: CN 109985008 A discloses a solid self-microemulsion of astaxanthin and its preparation method, which involves physical mixing and adsorption of liquid self-microemulsion and silicon dioxide , so that the liquid self-microemulsion is stored in solid form, but the invention does not disclose the in vitro release data of the solid self-microemulsion, the determination of the plasma concentration of astaxanthin in vivo and the pharmacokinetic parameters; CN 111264860 A discloses Solid self-microemulsion microcapsules of cortex and its preparation method and application, mixing self-microemulsion containing astaxanthin and quercetin with a solid adsorbent to obtain solid self-microemulsion microcapsules, but the in vitro application of the microcapsules is not disclosed Release research and pharmacokinetic research; CN 110151730 A discloses a hesperetin solid self-microemulsion osmotic pump capsule and its preparation method, using spheroid granulation technology to prepare hesperetin solid self-microemulsion osmotic pump Controlled-release capsules, but the pharmacokinetic data has not been published and the osmotic pump capsules are prepared mainly by using the characteristics of solid self-microemulsions that are easy to transform into other dosage forms

In summary, the disclosed solid self-microemulsion mainly improves the dosage form limitation of liquid self-microemulsion, and realizes the requirement of liquid self-microemulsion solidification, but the controllability of the solid particle process is not high, while the advantage of electrostatic spray technology is that it can realize Formation of monodisperse micro-nano particles, combining self-emulsification technology with electrostatic spray forming technology to improve bioavailability of insoluble active ingredients and few reports on patents

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