Hair growth microneedle patch containing androgen receptor protein targeted complex as well as preparation method and application of hair growth microneedle patch
An androgen receptor and protein target technology, applied in the field of biomedical materials, can solve the problems of needle tip dermal tissue blockage, inability to accurately control drug dosage, lack of drug loading capacity, etc., to induce hair regeneration, accelerate the growth period, and safe effect
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Embodiment 1
[0051]
[0052] The present embodiment provides a preparation method of a soluble hair growth microneedle patch, comprising:
[0053] 1. Preparation of androgen receptor protein targeting complex:
[0054] Compound 2 (2.0g, 1.0eq.) was dissolved in 20mL N,N-dimethylformamide, ice bath, sodium hydride (60%, 0.56g, 1.5eq.) was added, stirred for 0.5h, compound 1 ( 1.45g, 1.0eq.) was dissolved in 10mL N,N-dimethylformamide, dropped into the above reaction solution, reacted at room temperature until the reaction of the raw materials was complete, the reaction solution was concentrated, and purified by column chromatography (V 石油醚 / V 乙酸乙酯 =6 / 1) to obtain 3.1 g of white solid, yield 95%, UPLC-MS: m / z 351.15 [M+H] + ;
[0055] Compound 3 (1.0 g, 1.0 eq.) was dissolved in 12 mL of dichloromethane, 4 mL of trifluoroacetic acid was added, under argon protection, the reaction was performed at room temperature until the reaction of the raw materials was complete, the pH was adjusted...
Embodiment 2
[0069]
[0070] The present embodiment provides a preparation method of a soluble hair growth microneedle patch, comprising:
[0071] 1. Preparation of androgen receptor protein targeting complex:
[0072] Compound 2 (2.0g, 1.0eq.) was dissolved in 20mL N,N-dimethylformamide, ice bath, sodium hydride (60%, 0.56g, 1.5eq.) was added, stirred for 0.5h, compound 1 ( 1.45g, 1.0eq.) was dissolved in 10mL N,N-dimethylformamide, dropped into the above reaction solution, reacted at room temperature until the reaction of the raw materials was complete, the reaction solution was concentrated, and purified by column chromatography (V 石油醚 / V 乙酸乙酯 =6 / 1) to obtain 3.1 g of a white solid with a yield of 95%. UPLC-MS: m / z 351.15 [M+H] + ;
[0073] Compound 3 (1.0 g, 1.0 eq.) was dissolved in 12 mL of dichloromethane, 4 mL of trifluoroacetic acid was added, under argon protection, the reaction was performed at room temperature until the reaction of the raw materials was complete, the pH ...
Embodiment 3
[0084] This embodiment provides a method for preparing a soluble microneedle patch. The difference between this embodiment and Embodiment 1 is that step 1 in this embodiment is to synthesize the salt of the androgen receptor protein targeting complex.
[0085] In this embodiment, a solid-state soluble microneedle patch is finally obtained by mixing the androgen receptor protein targeting complex with the polymer solution. The solid-state soluble microneedle patch has a mild preparation process, does not require extreme conditions, is simple to prepare, and can be stored at room temperature in a dry environment, thereby effectively realizing the transdermal delivery of the androgen receptor protein targeting complex.
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