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Houttuynin derivative lipid microsphere preparation and preparation method thereof

A technology for houttuyniacin and derivatives, which is applied in the directions of antifungal agents, pharmaceutical formulations, anhydride/acid/halide active ingredients, etc., can solve the problems of hidden safety hazards, multiple side effects, and high prices, and save time and cost. The effect of improving solubility and improving stability

Inactive Publication Date: 2011-02-09
XIAN LIBANG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Chinese patent CN1404825A describes a new Houttuyniatin Sodium Injection using Tween-80 as a cosolvent to help improve the solubility of the drug, but Tween-80 has more side effects, such as causing hemolysis, so in terms of safety There are hidden dangers
Chinese patent CN1449834A describes the application of 2-hydroxypropyl β-cyclodextrin to inclusion and solubilization of neohouttuyfonate sodium, but the high price and large amount make it limited in practical application

Method used

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  • Houttuynin derivative lipid microsphere preparation and preparation method thereof
  • Houttuynin derivative lipid microsphere preparation and preparation method thereof
  • Houttuynin derivative lipid microsphere preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] Example 1. Houttuyfotin derivative lipid microsphere preparation (0.1%):

[0057]

[0058] Preparation Process:

[0059] (1) Dissolve 12g egg yolk lecithin with 100g soybean oil for injection in a water bath at 70°C under nitrogen protection, add 1g houttuydine (I) derivative and 10g vitamin E, heat and stir to dissolve, and obtain oil phase;

[0060] (2) 22.5g glycerol and 5g EDTA were dissolved in 500ml water to obtain the water phase;

[0061] (3) Slowly add the oil phase to the water phase dropwise, at the same time under the protection of nitrogen, shear (shear speed: 10000r / min) for 20min, add water for injection to 1000ml to obtain colostrum, and use sodium hydroxide or hydrochloric acid if necessary Adjust the pH value to about 7.0;

[0062] (4) Under the pressure of 800-900 bar, the colostrum is homogenized by a high-pressure homogenizer for 5-8 times, filtered through a microporous membrane, filled with nitrogen, potted, and sterilized under high pressur...

Embodiment 2

[0063] Example 2, houttuyfonate derivative lipid microsphere preparation (4%):

[0064]

[0065]

[0066] Preparation Process:

[0067] (1) Under 70°C water bath and nitrogen protection, 24g egg yolk lecithin was completely dissolved with 300g soybean oil for injection, 40g houttuyfotin (II) type derivative and 10g vitamin E were added, heated and stirred to dissolve, and obtained oil phase;

[0068] (2) 22.5g glycerol and 5g EDTA were dissolved in 500ml water to obtain the water phase;

[0069] (3) Slowly add the oil phase to the water phase dropwise, at the same time under the protection of nitrogen, shear (shear speed: 10000r / min) for 20min, add water for injection to 1000ml to obtain colostrum, and use sodium hydroxide or hydrochloric acid if necessary Adjust the pH value to about 7.0;

[0070] (4) Under the pressure of 800-900 bar, the colostrum is homogenized by a high-pressure homogenizer for 5-8 times, filtered through a microporous membrane, filled with nitro...

Embodiment 3

[0071] Example 3. Lipid Microsphere Preparation of Medium and Long Chain Houttuyfondin Derivatives (1%):

[0072]

[0073] Preparation Process:

[0074] (1) Mix 100g of soybean oil for injection and 100g of medium-chain oil for injection in a 70°C water bath and under the protection of nitrogen, and use it to dissolve 24g of egg yolk lecithin, then add 40g of houttuyfonate (III) derivatives and 10g of vitamin E, heated and stirred to dissolve to obtain an oil phase;

[0075] (2) 22.5g glycerol and 5g EDTA were dissolved in 500ml water to obtain the water phase;

[0076] (3) Slowly add the oil phase to the water phase dropwise, at the same time under the protection of nitrogen, shear (shear speed: 10000r / min) for 20min, add water for injection to 1000ml to obtain colostrum, and use sodium hydroxide or hydrochloric acid if necessary Adjust the pH value to about 7.0;

[0077] (4) Under the pressure of 800-900 bar, the colostrum is homogenized by a high-pressure homogenizer ...

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Abstract

The invention belongs to the field of medicinal preparations and particularly relates to a preparation method of a lipid microsphere preparation of houttuynin and a houttuynin derivative. The lipid microsphere preparation contains the houttuynin or the houttuynin derivative. The preparation takes phospholipid and other surfactants as emulsifiers and takes high-purity plant oil as a solvent. Lipid microspheres are prepared by high-pressure homogenizing equipment. Compared with the conventional houttuynin injection, the lipid microsphere preparation avoids the application of latent solvents such as Tween and the like and remarkably improves the stability of a preparation.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a pharmaceutical composition and a preparation method thereof, in particular to an antibacterial drug houttuyfonate lipid microsphere preparation and a preparation method thereof. Background technique [0002] Houttuynia cordata, also known as Houttuynia cordata, is a perennial herbaceous plant of the family Sanbaiaceae, and is one of the commonly used Chinese herbal medicines. Houttuynia cordata (decanoyl acetaldehyde) is the main active ingredient in Houttuynia cordata. Houttuyfotin is a yellow oily liquid that solidifies when cooled to 6-8°C, soluble in methanol, ethanol, ether, petroleum ether and 5% NaOH solution, insoluble in water, and FeCl 3 The reaction is red and easy to polymerize. Pharmacological research and clinical application show that it has obvious inhibitory effect on Diplococcus pneumoniae, Haemophilus influenzae, Candida albicans, Bacillus typhi, Sta...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/185A61K31/22A61P31/10A61K31/255A61K31/121A61K31/20A61K31/19A61K31/662A61P31/04A61K9/107A61K31/23
Inventor 王汝涛陈涛安龙胡慧静
Owner XIAN LIBANG PHARMA
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