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Crisaborole sustained-release film with good paste effect and preparation method thereof

A technology of criborole and sustained-release film, which is applied in the field of biomedical materials, can solve the problems of not being able to be retained for a long time and being easily wiped, and achieve the effect of good sustained-release treatment effect and strong binding force.

Inactive Publication Date: 2018-12-04
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

At present, most of the crisborole preparations are ointments, which do not involve sustained release, need fixed-point administration, and are easy to be wiped off, so they cannot be kept for a long time

Method used

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  • Crisaborole sustained-release film with good paste effect and preparation method thereof
  • Crisaborole sustained-release film with good paste effect and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] A, the first layer of sustained-release film preparation: with crisborole 20%, glycerin 25%, microcrystalline cellulose 25%, propylene glycol 7%, carrageenan 8%, adhesive agent 15% (by polyvinylpyrrolidone 60%, 10% polycarbophil, 10% rosin, 10% polyvinyl alcohol and 10% cornstarch) mixed fully, melted, extruded film-forming agent with extruder;

[0028] B, the second layer of delayed-release film preparation: with 20% of crisborole, 25% of propylene alcohol, 25% of sorbitol, 7% of polysorbate, 8% of guar gum, 15% of binding agent (by polyvinylpyrrolidone 60%, polycarbophil 10%, rosin 10%, polyvinyl alcohol 10% and cornstarch 10%) mixed fully, add appropriate amount of water to dissolve, stir evenly, apply it evenly on the above slow-release film, dry Machine drying until there is no obvious moisture, and the drying temperature is 60°C;

[0029] C. Cut and get.

Embodiment 2

[0031] A, the preparation of the first layer of slow-release film: with crisborole 25%, polyethylene glycol 23%, modified starch 22%, menthol 8%, sodium carboxymethyl cellulose 7%, binding agent 15% (by 60% polyvinylpyrrolidone, 10% polycarbophil, 10% rosin, 10% polyvinyl alcohol and 10% cornstarch) are fully mixed, melted, and extruded film-forming agent with an extruder;

[0032] B, the preparation of the second layer of delayed-release film: with crisborole 25%, glyceryl triacetate 23%, dextrin 22%, menthol 8%, sodium carboxymethyl cellulose 7%, binding agent 15% (by 60% polyvinylpyrrolidone, 10% polycarbophil, 10% rosin, 10% polyvinyl alcohol and 10% cornstarch) mixed well, add appropriate amount of water to dissolve, stir evenly, and spread it evenly on the above slow-release film , the dryer is dried until there is no obvious moisture, and the drying temperature is 60°C;

[0033] C. Cut and get.

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Abstract

The invention discloses a Crisaborole sustained-release film with good paste effect and a preparation method thereof. The film is prepared by the following raw materials: active ingredients, a plasticizer, a filler, an absorption enhancer, a suspending agent, and an adhesive. The film solves the problem that the frequency of drug use is too high and a longer skin retention time and a reduced number of administrations can be provided, a film preparation is prepared by using a variety of film-forming auxiliary materials, which complement each other and indispensable, the plasticizer and the filler enhance film formation, the absorption enhancer enhances drug penetration capability, and the suspending agent ensures the dispersibility of the raw materials in a liquid state, and the adhesive enhances the adhesion of the film to the skin.

Description

technical field [0001] The invention relates to a crisborole slow-release film with good sticking effect and a preparation method thereof, belonging to the field of biomedical materials. Background technique [0002] Crisaborole, an inhibitor of phosphodiesterase 4 (PDE4), which results in increased intracellular levels of cyclic adenosine monophosphate (cAMP), is used in the treatment of fungal infections, more specifically Onychomycosis and / or fungal skin infections. The drug was approved for marketing by the U.S. Food and Drug Administration (FDA) in December 2016. It was developed by Anacor Pharmaceuticals and is responsible for marketing in the United States. The trade name is Crisaborole and its chemical name is 5-(4-cyanophenoxy )-1,3-dihydro-1-hydroxy-2,1-benzoxaborole, the English name is 4-((1-hydroxy-1,3-dihydrobenzo[c][1, 2] oxaborol-5-yl)oxy)benzonitrile, the chemical structural formula is as shown in formula (I): [0003] [0004] The characteristic of dr...

Claims

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Application Information

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IPC IPC(8): A61K9/70A61K47/46A61K47/10A61K47/38A61K47/36A61K47/26A61K47/14A61K31/69A61P17/00A61P31/10
CPCA61K9/7007A61K31/69A61K47/10A61K47/14A61K47/26A61K47/36A61K47/38A61K47/46A61P17/00A61P31/10
Inventor 付任重李建民马义成肖海英
Owner 苏州尚宜佳生物科技有限公司
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