Microemulsion-based gel pharmaceutical composition and preparation method thereof

A microemulsion gel and drug technology, applied in the field of biomedicine, can solve the problems of high irritation and no targeting effect on dermal lesions, achieve high drug retention, facilitate drug efficacy, and increase drug retention Effect

Active Publication Date: 2014-10-22
JIANGSU SEMPOLL PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Patent CN100423786C discloses a kind of acyclovir hydrogel dressing, and it adopts azone, dimethyl sulfoxide as transdermal penetra

Method used

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  • Microemulsion-based gel pharmaceutical composition and preparation method thereof
  • Microemulsion-based gel pharmaceutical composition and preparation method thereof
  • Microemulsion-based gel pharmaceutical composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Embodiment 1: the preparation of drug microemulsion solution

[0026] Table 1 Prescription table of drug microemulsion solution

[0027] name Quantity, g / 100g Aciclovir 2 Stearamide 1 medium chain fatty acid triglycerides 3 castor oil 4 Tween 80 20 Span 60 5 PEG400 10 glycerin 5 pH7.4 Phosphate Buffer 50

[0028] Preparation process: 1) Take medium-chain fatty acid triglycerides, castor oil, and stearamide in a water bath and heat to 60°C-80°C, add acyclovir, Tween 80, and Span 60 until dissolved; 2) Take another PEG400, Glycerin is added to pH 7.4 phosphate buffer solution to dissolve; 3) Under continuous stirring, add the water phase to the oil phase, and keep stirring until clear and transparent.

[0029] The encapsulation efficiency in the obtained drug microemulsion solution is 95.7%; the average particle size is 34.7nm.

Embodiment 2

[0030] Embodiment 2: the preparation of drug microemulsion solution

[0031] Table 2 Prescription table of drug microemulsion solution

[0032] name Quantity, g / 100g Aciclovir 2 Stearamide 1 medium chain fatty acid triglycerides 3 vegetable oil 4 Tween 80 20 Span 60 5 PEG400 10 glycerin 5 pH7.4 Phosphate Buffer 50

[0033] Preparation process: 1) Take medium-chain fatty acid triglycerides, vegetable oil, and stearamide in a water bath and heat to 60°C-80°C, add acyclovir, Tween 80, and Span 60 until dissolved; 2) Take another PEG400, Glycerin is added to pH 7.4 phosphate buffer solution to dissolve; 3) Under continuous stirring, add the water phase to the oil phase, and keep stirring until clear and transparent.

[0034] The encapsulation efficiency in the obtained drug microemulsion solution is 96.3%; the average particle size is 33.9nm.

Embodiment 3

[0035] Embodiment 3: the preparation of drug microemulsion solution

[0036] Table 3 Prescription table of drug microemulsion solution

[0037] name Quantity, g / 100g Aciclovir Palmitate 1 Stearamide 0.5 Isopropyl Laurate 3 Isopropyl myristate 2 Tween 80 10 Lecithin 10 ethanol 5 Propylene Glycol 5 pH6.8 Phosphate Buffer 63.5

[0038]Preparation process: 1) Take isopropyl laurate, isopropyl myristate, and stearamide in a water bath and heat to 60°C-80°C, add acyclovir palmitate, Tween 80, and lecithin until dissolved; 2 ) Add ethanol and propylene glycol to pH 6.8 phosphate buffer to dissolve; 3) Under continuous stirring, add the water phase to the oil phase, and keep stirring until it is clear and transparent.

[0039] The encapsulation efficiency in the obtained drug microemulsion solution is 86.5%; the average particle size is 43.2nm.

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Abstract

The invention provides acyclovir microemulsion-based gel. The acyclovir microemulsion-based gel is a clear and transparent O/W acyclovir microemulsion prepared from an oil phase, a water phase, a surfactant and a cosurfactant. Through use of carbomer as a hydrophilic gel matrix, the acyclovir microemulsion-based gel is prepared. The acyclovir microemulsion-based gel has surface positive charge, small and uniform particles and average granularity in 50nm, and can carry a drug into skin minimal structures such as hair follicles, sebaceous gland and sweat gland opening, keep them in the minimal structures, improve a drug retention amount of the skin and realize continuous drug release in the skin. Compared with the common gel preparations, the acyclovir microemulsion-based gel has good skin targeting effects and can be used for treating diseases related to virus infection.

Description

technical field [0001] The invention belongs to the field of biomedicine, and specifically relates to a microemulsion gel and a preparation method thereof. The microemulsion gel can carry medicine through the stratum corneum of the skin, and has the characteristics of high skin penetration and high skin drug retention. For the treatment of herpes zoster herpes simplex virus skin and mucous membrane infection and other diseases. Background technique [0002] Herpes zoster (herpes zoster) is an acute inflammatory skin disease caused by varicella-zoster virus. Its main feature is clustered vesicles distributed in clusters and bands along one peripheral nerve, accompanied by obvious neuralgia. The first infection manifests as chickenpox, and the virus can remain dormant in the dorsal root ganglia of the spinal cord for a long time later. The weakened immune function can induce the varicella zoster virus to reactivate, grow and reproduce, and spread to the skin along the peripher...

Claims

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Application Information

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IPC IPC(8): A61K9/06A61K31/522A61K47/44A61K47/34A61K47/32A61K47/24A61K47/22A61P31/22
Inventor 付劼王晶
Owner JIANGSU SEMPOLL PHARMA
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