Phosphodiesterase-4 inhibitor pharmaceutical composition for treatment of oral ulcer and preparation method thereof

A technology for phosphodiesterase and oral ulcers, which is applied in the direction of drug combination, drug delivery, and pharmaceutical formulations. Multiple administrations, stable and reliable quality, and fast onset of effect

Active Publication Date: 2019-11-05
ZHAOKE PHARMA GUANGZHOU
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But apremilast is practically insoluble in water, thus greatly hampering the development of its effective pharmaceutical composition
Apremilast currently on the market is a tablet. Although the dose is gradually increased from 10mg, 20mg to 30mg, due to poor water solubility, the dissolution is slow after oral administration, and the drug absorption is still not ideal.
In addition, oral administration of Apremilast tablets has low bioavailability and can easily cause adverse reactions in the gastrointestinal tract, such as diarrhea, nausea and headache
Common dosage forms currently used for oral ulcers mainly include: liquid preparations (mouthwash), semi-solid preparations (ointments, pastes) and solid preparations (powders, film preparations). The outstanding disadvantage of the above dosage forms is that the medicine is easily diluted by saliva , The time to act on the lesion is short, and the local effective drug concentration is low, so the curative effect is not good

Method used

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  • Phosphodiesterase-4 inhibitor pharmaceutical composition for treatment of oral ulcer and preparation method thereof
  • Phosphodiesterase-4 inhibitor pharmaceutical composition for treatment of oral ulcer and preparation method thereof
  • Phosphodiesterase-4 inhibitor pharmaceutical composition for treatment of oral ulcer and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Table 1 Composition of lyotropic liquid crystal drug carrier 1

[0028] prescription composition %(w / w) Apster 0.5 Glyceryl Dioleate 15 Lecithin 30 ethanol 15 Propylene Glycol 15 Tween 80 20 Menthic Acid 4.5

[0029] Preparation Process:

[0030] a) Add glyceryl dioleate into a stainless steel container, add propylene glycol and stir continuously with a spiral stirrer, mix well, and set aside;

[0031] b) Slowly add the bulk drug of Apremilast into ethanol, and add Tween 80 to fully dissolve the bulk drug, then add citric acid while stirring, mix well, and set aside;

[0032] c) adding the dissolved raw material drug into the lecithin, after stirring evenly, slowly adding the mixture of glyceryl dioleate and propylene glycol, and stirring evenly;

[0033] d) Put the above mixture in a water bath, the temperature of the water bath is 40-60°C, and the time of the water bath is 0.5-1h;

[0034] e) The mixture aft...

Embodiment 2

[0036] Table 2 Lyotropic liquid crystal drug carrier composition 2

[0037] prescription composition %(w / w) Apster 3 ethyl oleate 20 Lecithin 40 DMSO 6 glycerin 20 distilled water 5 citric acid 6

[0038] Preparation Process:

[0039] a) Ethyl oleate is added to a stainless steel container, glycerin is added and stirred continuously with a spiral agitator, mixed evenly, and set aside;

[0040] b) Dissolving the Apremilast bulk drug in DMSO, fully dissolving;

[0041] c) adding the dissolved raw drug into lecithin, stirring evenly, slowly adding a mixture of ethyl oleate and glycerin, placing it in a water bath at 50-70°C, then adding distilled water to the above mixture, fully stirring and mixing uniformly;

[0042]d) The above mixed mixture is centrifuged for 10-20 min to remove air bubbles, and then placed at 25-37° C. for a week to obtain a stable lyotropic liquid crystal drug carrier.

Embodiment 3

[0044] Table 3 oral gel composition 1

[0045] prescription composition Proportion in prescription (%) Apster 0.5 DMSO 2 Poloxamer 70 Triethanolamine 3 glycerin 20 peppermint 4.5

[0046] Preparation Process:

[0047] a) Dissolve the poloxamer in water to make it fully swell, then adjust the pH to neutral with a pH regulator, add glycerin and grind it sufficiently to make it moist;

[0048] b) After dissolving Apremilast in DMSO, slowly add it to a), grind while adding, and add an appropriate amount of distilled water to make it a gel with a suitable viscosity;

[0049] c) Add peppermint oil and triethanolamine to b), and grind to make it look like a transparent gel with a fragrant smell.

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PUM

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Abstract

The invention discloses a novel pharmaceutical composition for local drug administration with a phosphodiesterase-4 (PDE-4) inhibitor as an active component. The oral gel composition includes commonlyused additives: a gel matrix, a surfactant, a solubilizer, a pH regulator, a flavoring agent, a preservative, a solvent containing water or ethanol, and other ingredients. The composition acts directly on oral lesions, and effectively avoids the gastrointestinal adverse reactions caused by the composition. The preparation method of the local pharmaceutical composition is feasible in commercial production, and the quality of the prepared local pharmaceutical composition is stable, reliable, safe, effective, and convenient to use.

Description

technical field [0001] The invention relates to a pharmaceutical composition and a preparation method thereof, belonging to the technical field of western medicine preparations. Background technique [0002] Behcet's disease (BD), also known as Behcet's syndrome (Behcet's syndrome), was first reported by Turkish doctor Behcet in 1937. It can invade the skin, mucous membranes, joints, gastrointestinal tract, cardiovascular, urinary, reproductive, nerves, etc., among which the oral cavity, genitals, skin and eyes are most commonly involved. Behcet's disease is a recurrent chronic progressive inflammatory disease, characterized by recurrent oral ulcers, and may be accompanied by other multi-system involvement, such as genital ulcers, eye diseases, skin lesions, nervous system lesions, vasculitis and joint Inflammation and so on. Current treatment drugs include traditional drugs and biological agents, traditional drugs such as: glucocorticoids, azathioprine, cyclophosphamide, ...

Claims

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Application Information

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IPC IPC(8): A61K31/4035A61K9/06A61K9/36A61K9/127A61P1/02
CPCA61K31/4035A61K9/006A61K9/1274A61K47/44A61K47/32A61K9/2866A61P1/02
Inventor 戴向荣殷雷李灵芝李小羿
Owner ZHAOKE PHARMA GUANGZHOU
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