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Preparation method and application of crisaborole topical slow-release liposome

A technology of crisborole and liposome, which is applied in the direction of liposome delivery, medical preparations of non-active ingredients, active ingredients of boron compounds, etc., can solve the problem of inability to get the best of both worlds between the amount of application and the actual curative effect, and the amount of drug transdermal High, loss of active ingredients and other issues, to achieve a stable and controllable release curve, good penetration-promoting effect, and improve stability

Inactive Publication Date: 2018-06-29
苏州尚宜佳生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the traditional ointment contains a large amount of Vaseline, which has a strong greasy feeling during use, easily stains clothes, and loses a considerable part of the active ingredients.

Method used

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  • Preparation method and application of crisaborole topical slow-release liposome

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Dissolve 150mg of egg yolk lecithin, 50mg of cholesterol and 20mg of crisborole in 4ml of ethanol to form an organic phase. Add 70 mg of polyvinyl alcohol to 10 ml of water to swell overnight as the water phase. Inject the organic phase into the water phase, and homogenize under 800Mpa high pressure for 3-5 times to obtain crisborole liposomes, add 0.1% antioxidant BHT, and fill it in a special spray bottle.

Embodiment 2

[0024] Dissolve 250mg of egg yolk lecithin, 50mg of cholesterol and 20mg of crisborole in 4ml of ethanol to form an organic phase. Add 200mg PEG300 into 10ml water to dissolve, and add 100mg copovidone to swell overnight, as the water phase. Inject the organic phase into the water phase, and homogenize under 800Mpa high pressure for 3-5 times to obtain crisborole liposomes, add 0.1% antioxidant BHT, and fill it in a special spray bottle.

Embodiment 3

[0026] Dissolve 200mg of egg yolk lecithin, 50mg of cholesterol and 20mg of crisborole in 4ml of ethanol to form an organic phase. 200 mg of propylene glycol was added into 10 ml of water to dissolve, and 100 mg of copovidone was added to swell overnight as the water phase. Inject the organic phase into the water phase, and homogenize under 400Mpa high pressure for 3-5 times to obtain crisborole liposomes, add 0.1% vitamin E, and fill it in a special spray bottle.

[0027] Such as figure 1 Shown is the in vitro release curve of the local sustained-release liposome prepared by the present invention in a dialysis bag, pH7.4PBS, 500ml, 37°C, and 100rpm / min.

[0028] The application of the treatment method and multiple application methods of the present invention has outstanding substantive features and remarkable progress: by selecting an ionic active agent with a suitable length and controlling the ultrasonic intensity, a uniform particle size dispersion and a stable and contro...

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Abstract

The invention discloses a preparation method of a crisaborole topical slow-release liposome and application of the crisaborole topical slow-release liposome in skin topical administration by a spray mode. A liposome preparation is characterized in that phospholipid and cholesterol are used as liposome raw materials; polyethylene glycol and polyvinyl alcohol are selected as a stabilizer and a film-forming agent corresponding to the liposome; the materials are subjected to high pressure homogenization to obtain the liposome with uniformly-dispersed particle size and a stable and controllable release curve; the liposome has a good permeation enhancing effect on topically-applied drugs; the amount of the liposome entering blood is low, the liposome shows relative targeting for skin tissues, and thereby the retention volume of the drug in skin tissues is increased. Meanwhile, by taking the liposome as a drug carrier for the skin topical administration, drug reservoirs can be formed on epidermis and dermis, and slowly release the drugs for persistently taking effect on diseased regions; the liposome is particularly suitable for certain recrudescent chronic skin diseases.

Description

technical field [0001] The invention relates to a sustained-release method of a novel drug, in particular to a drug sustained-release method targeting skin diseases and psoriasis and its application. Background technique [0002] Among many diseases, skin diseases such as psoriasis, local ulcers and other minor symptoms often do not cause people's extensive attention, so in most cases, it will develop until it is difficult to deal with it. The reason is that it is not easy to detect in the early stage of the disease, and there is a lack of targeted treatment. Patients often have the trouble of dreading the process of seeking medical care. [0003] Under normal circumstances, sprains and bumps can be treated by wiping or spraying Yunnan Baiyao, and small incisions can be treated with band-aids. For this reason, it is particularly important to seek a simple and targeted rapid treatment method for the above-mentioned dermatological hidden diseases. [0004] In recent years, ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K9/70A61K47/32A61K31/69A61P17/00A61P37/08
CPCA61K9/127A61K9/7015A61K31/69A61K47/32
Inventor 付任重李建民陈航平肖海英马义成杨博
Owner 苏州尚宜佳生物科技有限公司
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