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.
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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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