Koumine transdermal patch and preparation method thereof
A technology of transdermal patch and kombucha, which can be applied in the directions of anti-inflammatory agents, pharmaceutical formulations, non-central analgesics, etc., and can solve the problems such as the formulation of kokisu which has not yet been seen.
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Embodiment 1
[0112] Embodiment 1: the preparation of the transdermal patch of prescription 1-3
[0113] Weigh 0.92% by weight of kelezin (content in the drug storage layer), dissolve it with ethyl acetate and vortex mix. Add the ethyl acetate solution of kelezin to the pressure-sensitive adhesive DURO-TAK87-4098, DURO-TAK 87-4287 or DURO-TAK 87-2677, and stir at room temperature for 0.5h to make the drug and the pressure-sensitive adhesive Mix well, then ultrasonically degas for 2min. The obtained mixture was uniformly coated on a transparent anti-adhesive film, left to stand for 10 minutes, and then baked at 60° C. for 15 minutes. Lay it with the backing layer after letting it cool, and cut out an area of 8cm 2 , to obtain the keloid transdermal patch of prescription 1-3. In vitro transdermal experiments were carried out on the transdermal patches of prescriptions 1-3 to test their transdermal properties.
[0114] Table 1: Composition of drug reservoir layers for formulations 1-3
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Embodiment 2
[0119] Embodiment 2: the preparation of the patch of prescription 4-13
[0120] In addition to including the step of adding a penetration enhancer to the pressure-sensitive adhesive, according to the method described in Example 1, according to the composition shown in Table 2, transdermal patches (8cm 2 / paste), and in vitro transdermal experiments were carried out on the obtained transdermal patches to test their transdermal properties (Js, Q 24h and t lag ). The results are shown in figure 2 and Table 3 and Table 6.
[0121] Table 2: Composition of drug reservoir layers for formulations 4-13
[0122]
[0123]
[0124] The results showed that 15% by weight of azone as a penetration enhancer achieved the best transdermal performance (prescription 7). However, the inventors have found that the adhesive force of the patch of prescription 7 is too large (peel strength greater than 0.6kN / m), which makes it difficult to remove the release layer and is not suitable for ...
Embodiment 3
[0125] Embodiment 3: the preparation of the transdermal patch of prescription 14 and 15
[0126] By the same method as Example 1, according to the composition shown in Table 4, the transdermal patches (8cm 2 / paste), and in vitro transdermal experiments were carried out on the patches of prescriptions 2, 14 and 15 to test their transdermal properties (Js, Q 24h and t lag ). The results are shown in image 3 and Table 6.
[0127] Table 4: Composition of drug reservoirs for formulations 2, 14 and 15
[0128] prescription number pressure sensitive adhesive Penetration enhancer Gelskin content single patch dosage 2 DURO-TAK 87-4287 none 0.92% by weight 2mg 14 DURO-TAK 87-4287 none 1.83% by weight 4mg 15 DURO-TAK 87-4287 none 3.59% by weight 8mg
[0129] The results showed that the transdermal delivery effect of kelezin was basically positively correlated with its content in the drug storage layer.
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