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Topical pharmaceutical composition of phosphodiesterase-4 inhibitor and preparation method thereof

A phosphodiesterase and local drug technology, applied in the field of medicine, can solve the problems of easy recurrence, easy recurrence after recovery, low cure rate, etc., and achieve the effects of reducing discomfort and trouble, clear mechanism of action, and good patient tolerance

Inactive Publication Date: 2018-07-17
ZHAOKE PHARMA GUANGZHOU
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, the treatment drugs for eczema are mainly hormone creams, and antihistamines are used together to relieve itching. For generalized eczema, glucocorticoids can be taken orally or injected. For subacute and chronic eczema, suitable glucocorticoid creams, Tar-based preparations or immunomodulators, such as tacrolimus ointment and pimecrolimus ointment, are more effective in hormone therapy, but long-term use of hormone cream drugs may cause side effects of skin atrophy, and it is easy to relapse after healing, etc. Disadvantages: Add antibiotic preparations for secondary infections, and use more irritating drugs containing antibiotics, biological agents, etc., which are more harmful to the human body
In addition, there are currently researches on traditional Chinese medicine formulas for the treatment of eczema in China. The conventional external medicine is Indigo sativa powder, which is black and greasy and unhygienic. Welcome, leading to insignificant treatment effect and low cure rate
Therefore, prior art treatment of eczema has disadvantages such as relatively large side effects, high irritation, inconspicuous curative effect, and easy recurrence after healing. A kind of curative effect can replace existing therapeutic drugs with little or no side effects for the treatment of eczema. has great practical significance

Method used

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  • Topical pharmaceutical composition of phosphodiesterase-4 inhibitor and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] Table 1 Aqueous base ointments

[0052] prescription composition

%(w / w)

Apster

0.5

Vitamin C

0.05

PEG4000

30

PEG400

60

Propylene Glycol

6.2

distilled water

2

Dimethylsulfoxide (DMSO)

1

Anhydrous sodium sulfite

0.05

hydrochloric acid / sodium hydroxide

Adjust pH to 5.0~6.0

[0053] Preparation Process:

[0054] a) Add DMSO into a stainless steel container, and gradually add Apremilast and mix until completely dissolved, then add propylene glycol and stir continuously with a spiral stirrer, set aside;

[0055] b) Dissolve anhydrous sodium sulfite in distilled water in addition, and set aside;

[0056] c) Heat PEG4000 and PEG400 on a water bath to 85°C to melt, and when cooled to below 40°C, add the solutions of a) and b) and stir well.

[0057] d) Adjust the pH to 5.0-6.0 with hydrochloric acid / sodium hydroxide to obtain the aqueous matrix apremilast ointment.

Embodiment 2

[0059] Table 2 Oily base ointments

[0060] prescription composition

Proportion in prescription (%)

Apster

0.5

DMSO

1.5

vegetable oil

25

liquid paraffin

30

White Vaseline

30

lanolin

3

Propylene Glycol

10

[0061] Preparation Process:

[0062] a) Heat liquid paraffin, white vaseline and lanolin on a water bath to 85°C to melt to remove moisture, filter, and let cool to 70°C.

[0063] b) Dissolve Apremilast in DMSO, add vegetable oil and propylene glycol and stir evenly.

[0064] c) Add b) to a) and stir, and mix evenly to obtain an oily matrix apremilast ointment.

Embodiment 3

[0066] Table 3 cream (O / W type)

[0067] prescription composition

Proportion in prescription (%)

Apster

0.5

DMSO

25

stearyl alcohol

24

White Vaseline

24

Sodium dodecyl sulfate

0.1

Propylene Glycol

10.39

Methylparaben

0.01

distilled water

15.16

[0068] Preparation Process:

[0069] a) Weigh stearyl alcohol and white petrolatum into a stainless steel container, heat to 75°C on a water bath to melt, stir with a spiral stirring paddle, gradually add DMSO and apremilast mixture, and mix evenly (oil phase);

[0070] b) Separately weigh methylparaben and sodium lauryl sulfate into a stainless steel container, add distilled water to dissolve, and heat to 75° C. (water phase) on a water bath;

[0071] c) Gradually add the water phase to the oil phase, and stir while adding, so as to disperse evenly until it condenses, and then the O / W type apremilast cream is obtained.

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PUM

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Abstract

The invention discloses a topical pharmaceutical composition of a phosphodiesterase-4 inhibitor and a preparation method thereof, wherein the topical pharmaceutical composition comprises 0.5 to 10% bymass of apremilast active ingredient, 0.2 to 25% by mass of dimethyl sulfoxide and 65 to 99.3% by mass of a topical pharmaceutical acceptable carrier. The dosage forms of the topical pharmaceutical composition are ointments, creams, gels, coatings, lotions, tinctures, powders and liniments. The invention also discloses the preparation method of the topical pharmaceutical composition and use of the topical pharmaceutical composition. The pharmaceutical composition is not like hormonal drugs which have the side effects to cause adermotrophia after long time of use, and the pharmaceutical composition has no disadvantages such as recurrence after curing, has desired pharmacological activity and less side effects, is stable in quality and convenient to use, is safe and effective in treatment of eczema, and has strong practical application value.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a local pharmaceutical composition of phosphodiesterase-4 inhibitor and a preparation method thereof. Background technique [0002] Atopic dermatitis is one of the most common, chronic, non-infectious skin diseases, commonly known as "eczema", with the highest incidence rate among all skin diseases, and it is the number one disease in dermatology. From the perspective of pathogenesis, eczema is a kind of skin inflammatory reaction with severe itching caused by various internal and external factors, which belongs to type IV allergy, and is mainly immune injury mediated by T cells. [0003] In recent years, the incidence of eczema has been on the rise, which may be related to changes in climate and environment, the application of a large number of chemicals in life, mental stress, accelerated pace of life, and changes in dietary structure. The etiology of eczema is complicated,...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K31/4035A61K47/20A61P17/00
CPCA61K9/0014A61K9/06A61K31/4035A61K47/20
Inventor 丁领振李小羿戴向荣殷雷凌娟
Owner ZHAOKE PHARMA GUANGZHOU
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