Preparation method of lidocaine ethosome

A lidocaine and alcohol plastid technology is applied in the field of preparation of lidocaine alcohol plastids, can solve the problems of low encapsulation rate and the like, and achieves the effects of high encapsulation rate, easy industrialization and simple prescription

Inactive Publication Date: 2012-09-26
HENAN UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The encapsulation efficiency of the prepared 5% lidocaine ethosome was (52.85±0.36)%, which was low

Method used

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  • Preparation method of lidocaine ethosome
  • Preparation method of lidocaine ethosome
  • Preparation method of lidocaine ethosome

Examples

Experimental program
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Effect test

Embodiment 1

[0020] Embodiment 1: The preparation method of lidocaine ethosome of this embodiment comprises the following steps:

[0021] (1) Add 0.3 g of lecithin and 0.1 g of lidocaine into 4.5 ml of ethanol with a volume fraction of 30%, stir to make it dissolve initially, and ultrasonically induce dissolution until a uniform milky white suspension is formed;

[0022] (2) Transfer the above suspension into a round-bottomed flask, seal the mouth of the bottle, place it on a magnetic stirrer, set the temperature to 30°C, and the rotation speed to 25r / min, stir evenly under airtight conditions, and stir in a trickle while stirring. Inject 6.5ml of PBS buffer solution with pH 7.0, and then continue to stir evenly;

[0023] (3) Ultrasonic treatment for 1 min under ice bath conditions (ultrasonic power 200W, ultrasonic 5s, stop 3s), and finally filter, the filter membrane pore size is 0.40μm, and lidocaine ethosomes are obtained.

[0024] Determination of encapsulation efficiency: put 10 mL ...

Embodiment 2

[0026] Embodiment 2: The preparation method of lidocaine ethosome of this embodiment comprises the following steps:

[0027] (1) Add 0.3g lecithin and 0.1g lidocaine into 4.5ml of ethanol with a volume fraction of 40%, stir to make it dissolve initially, and ultrasonically induce dissolution until a uniform milky white suspension is formed;

[0028] (2) Transfer the above suspension into a round-bottomed flask, seal the neck of the bottle, place it on a magnetic stirrer, set the temperature to 35°C, and the rotation speed to 30r / min, stir evenly under airtight conditions, and stir in a trickle while stirring. Inject 6.5ml of PBS buffer solution with pH 7.0, and then continue to stir evenly;

[0029] (3) Ultrasonic treatment for 2 minutes under ice-bath conditions (ultrasonic power 200W, ultrasonic 5s, stop 3s), and finally filter, the filter membrane pore size is 0.45μm, to obtain lidocaine ethosome.

[0030] Measuring encapsulation efficiency: method is the same as embodimen...

Embodiment 3

[0032] Embodiment 3: The preparation method of lidocaine ethosome of this embodiment comprises the following steps:

[0033] (1) Add 0.3 g of lecithin and 0.1 g of lidocaine into 4.5 ml of ethanol with a volume fraction of 50%, stir to make it dissolve initially, and ultrasonically induce dissolution until a uniform milky white suspension is formed;

[0034] (2) Transfer the above suspension into a round-bottomed flask, seal the bottle mouth, place it on a magnetic stirrer, set the temperature to 40°C, and the rotation speed to 35r / min, stir evenly under airtight conditions, and stir in a trickle while stirring. Inject 6.5ml of PBS buffer solution with pH 7.0, and then continue to stir evenly;

[0035] (3) Ultrasonic treatment for 3 minutes under ice-bath conditions (ultrasonic power 200W, ultrasonic 5s, stop 3s), and finally filter, the pore size of the filter membrane is 0.50 μm, to obtain lidocaine ethosome.

[0036] Measuring encapsulation efficiency: method is the same a...

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Abstract

The invention discloses a preparation method of lidocaine ethosome. The method comprises the steps of: uniformly mixing lecithin, lidocaine and ethanol solution, injecting PBS (Phosphate Buffer Solution), performing ultrasonic processing and filtering and the like. The method adopts a simple prescription and stable technological conditions, is easy to industrialize and has relatively great popularization values. The lidocaine ethosome prepared by the method is stable and has high entrapment efficiency, wherein the maximal entrapment efficiency of the optimized technology can reach 80.93%. The skin irritation test proves that the lidocaine ethosome has good affinity to the skin; the medicated part does not suffer the abnormal phenomena such as erythema, edema and the like; allergic reaction is avoided; and other physiological features are normal. Moreover, the lidocaine ethosome has a strong osmosis promoting effect, can obviously improve the medicine osmosis quantity of lidocaine, and is expected to be developed into novel efficient transdermal local anesthetics for external use.

Description

technical field [0001] The invention belongs to the field of pharmacy and relates to a preparation method of lidocaine ethosome. Background technique [0002] Transdermal drug delivery system (TDDS) is a drug delivery method that is absorbed through the skin. After the drug is applied to the skin, it passes through the stratum corneum, diffuses through the skin, and is absorbed into the systemic circulation by capillaries. Ethosomes are a new type of transdermal drug delivery carrier with a vesicle structure, containing high concentrations of low molecular weight alcohols, such as ethanol, propylene glycol, and isopropanol. Etosomes are not only stable in structure, but can promote the transdermal absorption of drugs, and this type of liposome can deliver drugs to the deep layer of the skin, and can enter the blood circulation through the skin, and can even achieve intercellular delivery. It is an efficient transdermal agent. carrier. The mechanism may be that low-molecula...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/167A61P23/02
Inventor 梁菊吴文澜李梅苗娟魏学锋陈姗王芋骁
Owner HENAN UNIV OF SCI & TECH
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