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Chuanhuning lipid freeze-dry powder agent and preparing method thereof

A technology of freeze-dried powder and shuning fat, which is applied in the field of Chuanhuning liposome freeze-dried powder preparation and preparation thereof, can solve problems such as the influence of drug stability, and achieve targeting, improved stability and improved bioavailability. Effect

Inactive Publication Date: 2009-12-02
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Traditional Chuanhuning injection needs to be sterilized by high temperature and high pressure, which is easy to degrade the drug and affect the stability of the drug

Method used

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  • Chuanhuning lipid freeze-dry powder agent and preparing method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Example 1: Preparation of Chuanhuning freeze-dried liposomes for intravenous injection

[0029] Dissolve 40mg of Chuanhuning and 400mg of soybean lecithin in an appropriate amount of acidified absolute ethanol. Large unilamellar liposomes were prepared by ethanol injection. At room temperature, inject the drug-containing ethanol solution into the buffer solution with a pH of about 3.5 under high-speed stirring. The resulting lipid solution was dried under reduced pressure at 60°C to remove ethanol and make up for evaporated water. Dissolve 50mg of Pluronic F68 in this crude liposome, and transfer to a high pressure homogenizer, under 5000Psi pressure, high pressure homogenization (Avestin) 3-8 times. The liposomes were cooled to room temperature.

[0030] Sterile filtered through a membrane filter (0.2 μm), filled into ampoules with 10% glucose as lyoprotectant, and freeze-dried.

[0031] Take the freeze-dried finished product, add appropriate amount of water for in...

Embodiment 2

[0032] Embodiment 2: the preparation of Chuanhuning liposome

[0033] Dissolve 120 mg of penicunine and 1000 mg of synthetic phospholipid (DMPC, purity>93% phosphatidylcholine) in an appropriate amount of acidified absolute ethanol. At 60°C-70°C, mix the above drug-containing ethanol solution with Na 2 HPO 4 Aqueous solutions are mixed. The liposomes were prepared by probe ultrasonic method (150w, 10s each time, 3-10 times). The resulting lipid solution was dried under reduced pressure at 60°C to remove ethanol and make up for evaporated water. The measured encapsulation efficiency is 60%-90%, and the average particle diameter is 160nm (PDI<0.2). Diluted with 0.5% glucose solution or normal saline, no precipitation occurs within 10 hours.

Embodiment 3

[0034] Embodiment 3: Determination of encapsulation efficiency

[0035] Measured by ultrafiltration. Draw 0.1ml Chuanhuning liposome respectively, add 0.4ml pH3.5 buffer solution, 5000rpm, 15min ultrafiltration. Take 10 μl of the supernatant and inject it into the sample, and calculate the peak area A of the free penetrant 1 . Take another 0.1ml of Chuanhuning liposome, dilute to 10ml with methanol, take 10μl of sample, calculate the total Chuanhuning peak area A 0 .

[0036] Encapsulation efficiency (EE%) was calculated according to the following formula:

[0037] EE%=(1-A 1 / A 0 )×100%

[0038] The calculated encapsulation efficiency is between 80% and 99.8%.

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Abstract

The invention relates to a liposome freeze-dried powder preparation containing chuanhuning and a preparation method thereof. The preparation is composed of penhuning as active ingredient, phospholipid as lipid component, emulsifier, freeze-drying protectant and auxiliary materials. Among them, the weight ratio of Chuanhuning to phospholipids is 1:1 to 200 parts, 0.0001 to 50 parts of emulsifier; 1 part of phospholipid is added with 0.1 to 30 parts of freeze-drying protective agent and appropriate amount of auxiliary materials to make a freeze-dried preparation, both The storage stability of the drug can be significantly improved, and the Chuanhuning liposome freeze-dried powder can be diluted with water for injection in any proportion and administered without precipitation and degradation products after being redispersed by adding water for injection. The encapsulation efficiency of the freeze-dried preparation is 50%-100%, and the particle size is 40nm-1000nm. The invention can be made into injections, oral preparations and pharmaceutically acceptable dosage forms, is suitable for industrial production, and has the advantages of low cost, good curative effect, few side effects, simple manufacturing process and the like.

Description

technical field [0001] The invention belongs to the pharmaceutical dosage form in the technical field of medicine, and in particular relates to a chuanhuning liposome freeze-dried powder preparation and a preparation method thereof. Background technique [0002] Potassium Dehydroandrographolide Succinate is a dehydrated andrographolide succinate monopotassium salt (C 28 h 35 KO 10 ), is a good antiviral drug, has antibacterial, antipyretic, and anti-inflammatory effects, and is commonly used in the treatment of exogenous high fever, acute infectious diseases, urinary tract infections, etc. (Yuan Shujie. Progress in the application of Chuanhuning for injection. Heilongjiang Medicine. (5), 388). [0003] However, the injections currently used clinically have many side effects reported. Among them, anaphylactic shock occurs within 2 to 4 minutes of the first medication, manifested as shortness of breath, profuse sweating, cold extremities, pale complexion, decreased blood p...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/365A61K9/127A61K47/26A61P29/00A61P31/04
Inventor 张志荣龚涛
Owner SICHUAN UNIV
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