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Huperzine A micro-emulsion type cataplasm

A technology of huperzine A and babu agent, applied in the field of medicine, can solve the problems of limited percutaneous penetration of drugs, harsh growth environment of Melaleuca tower, low bioavailability, etc., so as to improve the penetration rate of percutaneous and reduce mining. , the effect of increasing the penetration rate

Inactive Publication Date: 2013-12-25
ZHEJIANG ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the huperzine A sustained-release patch is a matrix-type transdermal drug delivery system, and the drug is evenly dispersed in the polymer adhesive matrix. Due to the influence of the stratum corneum barrier, the transdermal penetration of the drug is limited, and a considerable amount of drug needs to be added. In order to achieve effective treatment, the growth environment of Melaleuca tower is harsh, wild resources are extremely scarce, and the price is very expensive
Therefore, huperzine A sustained-release patches still have the disadvantages of low bioavailability and high cost, so it is urgent to find a better drug delivery system to improve the utilization rate of drugs and reduce the exploitation of scarce resources

Method used

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  • Huperzine A micro-emulsion type cataplasm

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Embodiment 1: Preparation of huperzine A microemulsion cataplasm

[0021] Huperzine A 0.1g

[0022] Peanut oil 10g

[0023] Polyoxyethylene hydrogenated castor oil 10g

[0024] Poloxamer 5g

[0025] Polyethylene glycol stearate 5g

[0026] Macrogol 400 5g

[0027] 1-2 propylene glycol 5g

[0028] Glycerin 5g

[0029] Laurocaprazine 7g

[0030] Carbomer U10 30g

[0031] Povidone 8g

[0032] Sodium Carboxymethyl Cellulose 20g

[0033]Aluminum glycylate 5g

[0034] Distilled water 300ml

[0035] Dissolving huperzine A into peanut oil, then adding polyoxyethylene hydrogenated castor oil, poloxamer and polyethylene glycol stearate, stirring and mixing to form the drug-containing internal phase. At room temperature, use a constant temperature magnetic stirrer to slowly add water to the drug-containing inner phase while stirring, at a rate of 300r.min -1 Stir at a constant speed until clear and transparent to prepare 100 g of transparent huperzine A microemulsion....

Embodiment 2

[0036] Embodiment 2: Preparation of huperzine A microemulsion cataplasm

[0037] Huperzine A 0.1g

[0038] Castor oil 20g

[0039] Poloxamer 10g

[0040] Lecithin 4g

[0041] Pluronic F-68 2g

[0042] Tween-80 8g

[0043] Macrogol 400 5g

[0044] Lauroazepam 10g

[0045] Oleic acid 10g

[0046] Glycerin 6g

[0047] Carbomer 934 25g

[0048] Sodium polyacrylate 15g

[0049] Tragacanth Gum 10g

[0050] Aluminum glycylate 6g

[0051] Distilled water 350ml

[0052] Stir and mix huperzine A, castor oil, poloxamer, lecithin, Tween-80, and pluronic F-68 to form a drug-containing inner phase. At room temperature, use a constant temperature magnetic stirrer to slowly add water to the drug-containing inner phase while stirring, at a rate of 300r.min -1 Stir at a constant speed until clear and transparent to prepare 150 g of transparent huperzine A microemulsion. Mix polyethylene glycol 400, laurocapram, oleic acid, and glycerin as phase A; mix carbomer 934, sodium polyacr...

Embodiment 3

[0053] Example 3: Study on the transdermal penetration rate of huperzine A microemulsion cataplasm in human isolated skin

[0054] The Franz diffusion cell was used for skin penetration test, the skin was fixed at the mouth of the diffusion cell, and the stratum corneum was facing outward, and the same dose of huperzine A microemulsion cataplasm (prescription 1) or sustained-release patch was applied to the stratum corneum On the upper layer, the receiving medium is a 40% polyethylene glycol 400 saline solution by mass, and the effective area of ​​the pool mouth is about 3.1cm 2 , with magnetic particles at 400r.min -1 Stirring at a constant speed, the diffusion tank is kept at a constant temperature of 37°C with a water bath jacket, samples are taken at the specified time, and an equal amount of receiving solution is added after sampling. The concentration of huperzine A in the permeate was determined by HPLC. The cumulative penetration Q at different times is plotted again...

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Abstract

The invention discloses huperzine A micro-emulsion type cataplasm which mainly consists of a medicament storage layer, a non-woven cloth back lining layer and an anti-adhesive layer, wherein the medicament storage layer is arranged between the non-woven cloth back lining layer and the anti-adhesive layer; and the medicament storage layer comprises huperzine A, oil, a surfactant, a cosurfactant, an absorption enhancer, a cataplasm aqueous matrix and distilled water. According to the huperzine A micro-emulsion type cataplasm, the huperzine A is uniformly dispersed in the cataplasm aqueous matrix in a micro-emulsion state and is matched with a skin penetration enhancer. Compared with a skeleton type huperzine A slow-release paster which takes polyacrylate as the matrix, the huperzine A micro-emulsion type cataplasm overcomes the following significant defects: firstly, the irritation is reduced, secondly, the toxicity is low, thirdly, the permeation rate is improved, and fourthly, the rare resource is saved; moreover, the exploration of rare plants is reduced.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a scarce resource-saving, safe and high-efficiency huperzine A microemulsion cataplasm for treating Alzheimer's disease. Background technique [0002] German doctor Alois Alzheimer first described Alzheimer's disease (AD): an age-related neurological lesion characterized by neuritic plaques, neurofibrillary tangles, and neuronal death. The main clinical manifestations are Memory impairment, cognitive impairment, personality changes, etc. [0003] At present, the world's population has entered the aging stage, and the incidence of AD is increasing day by day. There are about 20 million people in the world suffering from this disease. According to the latest statistics, the death rate of AD ranks fourth after heart disease, cancer and stroke. The incidence of the disease is positively correlated with age. According to the survey in my country, the incidence of AD is 1%-2% for 60...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/70A61K31/4748A61P25/28
Inventor 张望刚王俏俞文英汤湛陈国神
Owner ZHEJIANG ACAD OF MEDICAL SCI
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