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Tetracaine hydrochloride multi-vesicular liposome freeze-dried powder and preparation method thereof

A technology of tetracaine hydrochloride and multivesicular liposome, which is applied in the field of sustained-release preparations of tetracaine hydrochloride, and can solve problems such as leakage of encapsulated substances

Active Publication Date: 2011-09-21
YOUCARE PHARMA GROUP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, liposomes may undergo many different changes during placement, such as phospholipids will be oxidized and hydrolyzed, and liposomes may also undergo physical changes such as aggregation and fusion, resulting in leakage of encapsulated substances

Method used

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  • Tetracaine hydrochloride multi-vesicular liposome freeze-dried powder and preparation method thereof
  • Tetracaine hydrochloride multi-vesicular liposome freeze-dried powder and preparation method thereof
  • Tetracaine hydrochloride multi-vesicular liposome freeze-dried powder and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] 1. Precisely weigh 60 mg of hydrogenated soybean lecithin, 30 mg of cholesterol, and 1 mg of glyceryl trilaurate and dissolve them in 2.4 ml of chloroform as the lipid phase;

[0027] 2. Preparation of Rosa Rosa extract: add 500 mg of water to 50 mg of washed Rosa Rosa fruit, ultrasonically break for 1 min, the ultrasonic frequency is 20 kHz, and centrifuge for 3 min at 10,000 rpm, take the supernatant to obtain Rosa Rosa Extraction solution;

[0028] 3. Precisely weigh 80 mg of tetracaine hydrochloride and dissolve it in water, add the Rosa rose fruit extract obtained in step 2 as the inner water phase, so that the final concentration of tetracaine hydrochloride is 40 mg / ml;

[0029] 4. Precisely weigh 99mg of glucose and dissolve it in 11ml of water, as the external water phase, the concentration of glucose is 9mg / ml;

[0030] 5. Slowly add 2ml of the inner water phase to the upper layer of 2.4ml of the lipid phase, and use a high-speed shear homogenizer to act on it...

Embodiment 2

[0036] 1. Precisely weigh 60 mg of hydrogenated soybean lecithin, 30 mg of cholesterol, and 1 mg of glyceryl trilaurate and dissolve them in 2.4 ml of chloroform as the lipid phase;

[0037] 2. Precisely weigh 80 mg of tetracaine hydrochloride and dissolve it in water as the inner water phase, so that the final concentration of tetracaine hydrochloride is 40 mg / ml;

[0038] 3. Precisely weigh 99mg of glucose and dissolve it in 11ml of water, as the external water phase, the concentration of glucose is 9mg / ml;

[0039] 4. Slowly add 2ml of the inner water phase to the upper layer of 2.4ml of the lipid phase, and use a high-speed shear homogenizer to act on it at a speed of 10,000rpm for 10min to obtain a water-in-oil emulsion;

[0040] 5. Add the above-mentioned emulsion to 11ml of the external water phase, and use a high-speed shear homogenizer to act on it at a speed of 10,000rpm for 10min to obtain a water-in-oil-in-water type double emulsion;

[0041] 6. Add the double emu...

Embodiment 3

[0045] The tetracaine hydrochloride multivesicular liposome freeze-dried powder of experimental group I is dissolved in water, and when the tetracaine hydrochloride in the liposome is all released, the concentration of tetracaine hydrochloride in the solution is 7.2mg / ml 5ml of the above-mentioned solution is taken and placed in a dialysis bag, and the corresponding concentration of tetracaine hydrochloride aqueous solution is prepared to be 7.2mg / ml, and this solution of 5ml is placed in a dialysis bag, and released simultaneously in timed release in dissolution cups with 250ml distilled water respectively, The rotation speed is 100 rpm, and the temperature is 37°C. Take samples at 20min, 40min, 60min, 90min, 150min, 240min, 360min, 480min, 540min, 720min, 960min, 1440min, 1800min respectively, and measure its concentration with HPLC (Chinese Pharmaceutical Industry Impurities, 2010, 41 (6), 453-455 ), draw the drug-time curve of tetracaine hydrochloride polyvesicular liposom...

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Abstract

The invention discloses tetracaine hydrochloride multi-vesicular liposome freeze-dried powder and a preparation method thereof, and relates to a sustained-release preparation of tetracaine hydrochloride. The invention aims to provide the tetracaine hydrochloride multi-vesicular liposome freeze-dried powder with high physical stability and medicament sustained-release effect and the preparation method thereof. The tetracaine hydrochloride multi-vesicular liposome freeze-dried powder comprises the following raw material components in part by weight: 8 parts of tetracaine hydrochloride, 6 to 6.5parts of hydrogenated soybean phosphatidylcholine, 3 parts of cholesterol, 0.1 to 0.2 part of laurin, 5 parts of rosa davurica and 9 to 11 parts of osmotic pressure regulator glucose. The invention also discloses the preparation method of the tetracaine hydrochloride multi-vesicular liposome freeze-dried powder. The freeze-dried powder can be used for preparing local anesthetics.

Description

technical field [0001] The invention relates to a slow-release preparation of tetracaine hydrochloride, in particular to a tetracaine hydrochloride polyvesicular liposome freeze-dried powder and a preparation method thereof. Background technique [0002] Many drugs need to achieve and maintain a certain blood concentration to obtain the best curative effect, but the half-life of intravenous, subcutaneous, intramuscular and other routes of administration is relatively short, usually between 1 hour and several hours. Therefore, the therapeutic concentration of the drug can only be maintained by frequent and multiple administrations, but such a treatment method not only has high cost, poor patient compliance, but also easily leads to adverse drug reactions. Tetracaine hydrochloride is a commonly used local anesthetic. It is a small molecular compound that is easily soluble in water. It is weakly alkaline in water and has a pKa value of 8.5. Tetracaine hydrochloride acts rapidl...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K31/245A61K47/46A61P23/02
Inventor 徐为公
Owner YOUCARE PHARMA GROUP
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