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A kind of total bufolide solid lipid nanoparticle drug delivery system for injection and its preparation method

A technology of solid lipid nanometer and total bufolide, which is applied to the digestive system, pharmaceutical formulas, medical preparations of non-active ingredients, etc., can solve the problems of redness and swelling at the infusion site, poor intravenous infusion, etc., and achieve the reduction of vascular Stimulant, bioavailability-enhancing, tolerability-enhancing effects

Active Publication Date: 2018-08-21
HEFEI HUAFANG PHARMA SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in the course of clinical application, vascular irritation adverse reactions such as poor intravenous infusion, redness and swelling at the infusion site, and pain in the vein often occur.

Method used

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  • A kind of total bufolide solid lipid nanoparticle drug delivery system for injection and its preparation method
  • A kind of total bufolide solid lipid nanoparticle drug delivery system for injection and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1～10

[0065] Examples 1-10 This example mainly describes the hot high-pressure emulsion homogenization method. The components specified in Table 1 were prepared according to the following steps to obtain bufogenin solid lipid nanoparticles of different examples.

[0066] (1) Heat the total bufatoxin extract, lipid material and fat-soluble emulsifier at the temperature shown in Table 2 to melt to dissolve or disperse in the lipid to prepare the melt as the oil phase;

[0067] (2) Disperse water-soluble emulsifier, antioxidant, and glucose in 100ml water for injection to form a uniform water phase;

[0068] (3) Mix and stir the oil phase obtained in (1) and the water phase obtained in (2) at the temperature and speed shown in Table 2 until uniform colostrum is formed;

[0069] (4) Transfer the colostrum prepared in (3) to a milk homogenizer, homogenize in a high-pressure milk homogenizer, and quickly cool to room temperature or below to prepare total bufogenin solid lipid nanometer grain.

[...

Embodiment 11

[0078] The solid lipid nanoparticles of total bufogenin prepared as described in the above Examples 1-10 were used for physical and chemical properties study.

[0079] Take an appropriate amount of the total bufatoxin solid lipid nanoparticle suspension, dilute it with water, and then drop it on a copper mesh covered with a carbon film, stain it with a 2.0% sodium phosphotungstate negative staining solution, and observe the nanoparticles under a transmission electron microscope Shape and take photos.

[0080] As a result, the nanoparticles were observed under the electron microscope as quasi-spherical solid particles with uniform particle size and no aggregation and adhesion.

Embodiment 12

[0082] The total bufolide solid lipid nanoparticles in Examples 1-10 were taken to determine the encapsulation efficiency and drug loading.

[0083] Sephadex glucose gel column chromatography was used to separate the total bufogenin solid lipid nanoparticles and free drugs, and determine the encapsulation efficiency. Take 1 ml of nanoparticle suspension and apply it to the column, and use distilled water as the elution medium for elution. Collect the eluate with the opalescent part, quantify the part of the eluate, add methanol to dissolve the nanoparticles; take another 1 ml of the nanoparticle suspension and add methanol to dissolve. The encapsulation efficiency and drug loading were determined by HPLC.

[0084] The particle size, encapsulation efficiency and drug loading of the total bufogenin solid lipid nanoparticles measured in Examples 11-12 are shown in the following table:

[0085] table 3

[0086] Example

[0087] The above examples are described with 100ml total bufoge...

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Abstract

The invention belongs to the field of pharmaceutical preparation, and relates to a total bufadienolides solid lipid nanoparticle drug delivery system for injection and a preparation method thereof. Total bufadienolides solid lipid nanoparticles are composed of the components in parts by weight: 0.1-2 parts of total bufadienolides with therapeutically effective amount, 0.5-20 parts of a lipid material, 0.5-15 parts of a lipid soluble emulsifier, 0.5-10 parts of a water soluble emulsifier, 0.002-2.5 part of an antioxidant, 0.1-25 parts of sugar and a proper amount of water for injection. The total bufadienolides solid lipid nanoparticles for injection allow the total bufadienolides to be wrapped in a lipoid nucleus, increase the solubility of the total bufadienolides, reduce the irritation, avoid degradation or leakage of the drug, can achieve targeting effect, controlled release and other effects, and have the advantages of stable physical and chemical properties and the like.

Description

Technical field [0001] The invention relates to a total bufolinone nano-preparation, in particular to a total bufolinone solid lipid nanoparticle drug delivery system for injection and a preparation method thereof, belonging to the field of pharmaceutical preparations. Background technique [0002] The total bufanolide compounds are a type of C-24 steroids or their glycosides with α-pyrone ring (αpyrone) attached to the C-17β position. They are a class of fat-soluble compounds and are used in traditional Chinese medicine dried toad skin. The main medicinal ingredient of anti-cancer activity. The total bufogenin mainly contains bufogenin (resibufogenin), cinobufagin (cinobufagin), bufalin (bufalin), bufafalin (Bufotalin), bufafalin-3-hemsuberic acid Ester (Gamabufotalin-3-hydrogen Suberate), Bufalin-3-succinyl arginine, Cinobufotalin-3-succinyl arginine and other lactones. Studies have shown that total bufogenin has obvious anti-tumor effects, and can also transform tumor cells ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/51A61K35/65A61K47/14A61P35/00A61P1/16A61P31/20
Inventor 何勇方宗华于艳英高永好吴宗好
Owner HEFEI HUAFANG PHARMA SCI & TECH
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