Lidocaine hydrochloride polymeric liposome for topical anesthesia and preparation method

A technology of lidocaine hydrochloride and surface anesthesia, which is applied in the field of biomedicine, can solve the problems of poor product stability, low drug encapsulation rate, and difficult surface modification, etc. The effect of high encapsulation rate

Inactive Publication Date: 2012-04-11
STOMATOLOGICAL HOSPITAL TIANJIN MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore can consider adopting liposome to improve the penetration rate of local anesthetic as the carrier of lidocaine hydrochloride, there is the report that uses phospholipid liposome to do surface anesthetic preparation at home and abroad, but the traditional lip

Method used

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  • Lidocaine hydrochloride polymeric liposome for topical anesthesia and preparation method
  • Lidocaine hydrochloride polymeric liposome for topical anesthesia and preparation method
  • Lidocaine hydrochloride polymeric liposome for topical anesthesia and preparation method

Examples

Experimental program
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Effect test

Embodiment 1

[0038] The process of preparing lidocaine hydrochloride polymer liposomes by reverse-phase evaporation method is as follows:

[0039] (1) Accurately weigh 16 mg of OQLCS and 8 mg of cholesterol into an eggplant-shaped bottle, and dissolve in 4 ml of dichloromethane.

[0040] (2) Accurately weigh 40 mg of lidocaine hydrochloride, add it to an eggplant-shaped bottle, add 2 ml of deionized water, and dissolve completely.

[0041] (3) Add (2) to (1), and then ultrasonically disperse it with a probe-type ultrasonic generator at a power of 150 W until a translucent emulsion is formed. The above emulsion was rotary evaporated on a rotary evaporator at a rotation speed of 50 r / min at 40° C., and at the same time, a nitrogen flow was passed into the rotary evaporator for protection.

[0042] (4) After the organic solvent in the eggplant-shaped bottle is completely volatilized, the product is obtained by filtering through a 0.2 μm sterile filter membrane. The prepared lidocaine hydroc...

Embodiment 2

[0045] The process of preparing lidocaine hydrochloride polymer liposomes by reverse-phase evaporation method is as follows:

[0046] (1) Accurately weigh 48mg of OQLCS and 24mg of cholesterol into an eggplant-shaped bottle, and dissolve in 4ml of dichloromethane.

[0047] (2) Accurately weigh 80 mg of lidocaine hydrochloride, add it to an eggplant-shaped bottle, add 4 ml of deionized water, and dissolve completely.

[0048] (3) Add (2) to (1), and then ultrasonically disperse it with a probe-type ultrasonic generator at a power of 175W until a translucent emulsion is formed. The above emulsion was rotary evaporated on a rotary evaporator at a rotation speed of 50 r / min at 40° C., and at the same time, a nitrogen flow was passed into the rotary evaporator for protection.

[0049] (4) After the organic solvent in the eggplant-shaped bottle is completely volatilized, it is finally filtered through a 0.2 μm sterile filter membrane to obtain the product. The properties of the pr...

Embodiment 3

[0054] The process of preparing lidocaine hydrochloride polymer liposomes by reverse-phase evaporation method is as follows:

[0055] (1) Accurately weigh 160mg of OQLCS and 80mg of cholesterol into an eggplant-shaped bottle, and dissolve in 4ml of dichloromethane.

[0056] (2) Accurately weigh 80 mg of lidocaine hydrochloride, add it to an eggplant-shaped bottle, add 4 ml of deionized water, and dissolve completely.

[0057] (3) Add (2) to (1), and then ultrasonically disperse it with a probe-type ultrasonic generator at a power of 200 W until a translucent emulsion is formed. The above emulsion was rotary evaporated on a rotary evaporator at a rotation speed of 50 r / min at 40° C., and at the same time, a nitrogen flow was passed into the rotary evaporator for protection.

[0058] (4) After the organic solvent in the eggplant-shaped bottle is completely volatilized, the product is obtained by filtering through a 0.4 μm sterile filter membrane. The properties of the prepared...

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Abstract

The invention relates to lidocaine hydrochloride polymeric liposome for topical anesthesia and a preparation method. The preparation method comprises the following steps: dissolving OQLCS (octadecyl-quaternized lysine modified chitosan) and cholesterol in dichloromethane to form an oil phase; completely dissolving lidocaine hydrochloride in deionized water to form a water phase; performing ultrasonic treatment to the oil phase in a power range of between 150 and 200W, adding the water phase, and performing ultrasonic dispersion by using a probe type ultrasonic generator until a semitransparent emulsion is formed to form a dispersion emulsion with uniform water and oil; and performing rotary evaporation to the emulsion on a rotary evaporator at 40 DEG C at a rotating speed of 50r/min, and introducing nitrogen flow into the rotary evaporator for protecting, and filtering through a sterile filter membrane of between 0.2 and 0.4mu m after organic solvent is completely volatilized to obtain the lidocaine hydrochloride polymeric liposome. The encapsulation rate of the liposome to a medicament is between 60 and 85 percent; the grain diameter of the polymeric liposome is between 60 and 180nm, and the surface is positively charged with an electric potential of between 6 and 65mv. The lidocaine hydrochloride polymeric liposome can be directly applied to the surface of skin mucous membrane, or is further prepared to form gel or ointment.

Description

technical field [0001] The invention relates to the technical field of biomedicine, in particular to a lidocaine hydrochloride polymer liposome for topical anesthesia and a preparation method thereof. Background technique [0002] Topical anesthesia is the use of local anesthetics with strong penetrating power applied to the surface of the skin and mucous membranes, which penetrate through the skin and mucous membranes and act on the nerve endings below it, causing anesthesia in the skin and mucous membranes and the tissues below, but the onset time is long and the effect Superficial and limited. Local anesthetics that can be directly used as topical anesthesia include ester tetracaine and benzocaine, amide lidocaine, etc. In order to achieve better results, compound topical anesthetics have been greatly developed in recent years. Among them, there are reports: EMLA ointment contains 2.5% lidocaine, 2.5% prilocaine; TAC20 contains 20% lidocaine, 4% tetracaine; Oraqix conta...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/167A61K47/36A61P23/02
Inventor 张连云常津李长义王悦王汉杰李芹苏文雅
Owner STOMATOLOGICAL HOSPITAL TIANJIN MEDICAL UNIV
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