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Use of calcium sulfate whiskers or its composition in the preparation of skin penetration enhancer

A technology of calcium sulfate whisker and skin penetration enhancer, applied in the field of skin penetration enhancer, can solve problems such as difficulty in playing a role, reducing patient medication compliance, increasing skin irritation, etc.

Active Publication Date: 2020-11-10
XIAMEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, due to the elasticity of the skin itself, the microchannels formed by the microneedles on the skin surface usually close automatically within 10-20 minutes, resulting in a very limited effective penetration time for drugs, cosmetic active ingredients or nanocarrier particles
At present, microneedle technology is mainly administered in the form of microneedle patches. Long-term use may cause skin allergies. At the same time, the area of ​​administration of microneedle patches is fixed and relatively limited. Although expanding the area of ​​​​administration can increase the degree of drug penetration , but it will also increase skin irritation and reduce patient compliance
Therefore, it is generally only suitable for the delivery of drugs with small doses and strong activity, such as insulin or vaccine products
In addition, the sharpness of the end of the microneedles and the density of the arrangement of the microneedles depend on its production and etching process, which requires high requirements for its preparation material, preparation process and industrialization, and the microneedles are usually arranged in an array. It is difficult to function in non-flat areas such as

Method used

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  • Use of calcium sulfate whiskers or its composition in the preparation of skin penetration enhancer
  • Use of calcium sulfate whiskers or its composition in the preparation of skin penetration enhancer
  • Use of calcium sulfate whiskers or its composition in the preparation of skin penetration enhancer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Embodiment 1: Calcium sulfate whisker transdermal experiment

[0040] experimental method:

[0041] (1) Pre-treatment of pigskin: take fresh pigskin, remove the subcutaneous fat layer, shave the pig hair to a length no longer than 2mm, and use it immediately or freeze it at -20°C to -80°C for later use.

[0042] (2) In vitro transdermal test: Pig skin with the same diameter was drilled with a φ40mm circular punch, installed on the Franz diffusion transdermal device, and the skin conductance change was measured by the isolated skin percutaneous resistance test.

[0043] Apply calcium sulfate whiskers on the surface of pigskin, 10mg per piece of pigskin, and massage for 2 minutes. After massage with calcium sulfate whiskers, the average conductance of pigskin increased by more than 70 μA (Table 4), indicating that the skin stratum corneum barrier was damaged by calcium sulfate whiskers.

[0044] Then smear FITC-Dextran (dextran) (MW=10K) and FITC-Dextran (MW=4K) on the su...

Embodiment 2

[0054] Embodiment 2: the irritation test of calcium sulfate whisker massage

[0055] experimental method:

[0056] Shave the guinea pigs, take 10 mg of calcium sulfate whiskers and massage the back of the guinea pigs for two minutes. The control group does not use calcium sulfate whiskers, only massages, and after the massage, 24h, 48h, and 72h were photographed and recorded. The results are shown in Table 2 and Figure 6 .

[0057] Table 2 Irritation test results of calcium sulfate whisker massage

[0058]

[0059] Skin irritation index (Primary Irritation Index, P.I.I), the formula is as follows:

[0060] P.I.I=(sum of erythema and edema scores at 1h, 24h and 72h) / (number of animals*administration site*number of observations)

[0061] Calculated according to Table 2, P.I.I (experimental group)=3 / (3*1*4)=0.25

[0062] Table 3 Classification of stimulus intensity

[0063] P.I.I. Classification 0.0-0.4 no stimulation 0.5-1.9 slight irritation ...

Embodiment 3

[0065] Embodiment 3: Conductance variation and its length and diameter before and after different whisker massages

[0066] experimental method:

[0067] The morphology of calcium sulfate whiskers, silicon nitride whiskers, aluminum borate whiskers, potassium titanate whiskers, silicon carbide whiskers, magnesium oxide whiskers, and zinc oxide whiskers under the microscope is shown in Figure 7. Referring to the method of Example 1, the change of skin conductance before and after the action of different types of whiskers was investigated. Use 10 mg of whiskers for each piece of pigskin, massage for 2 minutes, wash off the whiskers on the surface of the pigskin, and then measure the change in conductance before and after massage (the medium is 0.2M PBS). The results are shown in Table 4.

[0068] Table 4 The conductance change and the length and diameter of each whisker before and after massage with different whiskers

[0069]

[0070] Combining Table 4 and Figure 8 It ca...

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PUM

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Abstract

The invention discloses a purpose of calcium sulphate crystal whiskers or a composition thereof to preparation of a skin penetration promoting agent. The calcium sulphate crystal whiskers can overcomethe stratum corneum protective screen of skin, can promote skin absorption of percutaneous absorption of medicines and cosmetic active components, and can be used for local medicine delivery or systematic medicine delivery of the skin.

Description

technical field [0001] The invention belongs to the technical field of skin penetration enhancers, and in particular relates to the application of calcium sulfate whiskers or a composition thereof in the preparation of skin penetration enhancers. Background technique [0002] The skin is the largest organ in the human body and the most direct route of drug delivery. Compared with other routes of administration (such as: oral administration, injection, etc.), skin administration has many unique advantages, including avoiding the first-pass effect of the liver, damage to the gastrointestinal tract, and infection and infection caused by injection. Pain, etc.; at the same time, it can also directly act on local skin lesions, and can be administered in a sustained or controlled manner. There are few adverse drug reactions and the administration can be terminated at any time, which greatly improves the convenience and compliance of patients' treatment, etc. . [0003] However, t...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/02A61K8/23A61Q19/00
CPCA61K8/23A61K47/02A61K2800/10A61K2800/882A61K2800/884A61Q19/00
Inventor 陈铭梁雪娇张赛曼张驰
Owner XIAMEN UNIV
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