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Medicinal gel, preparation method thereof and application of medicinal gel

A gel and drug technology, applied in the field of drug gel and its preparation, can solve the problems of strong drug resistance, limited dosage, easy relapse, etc., achieve good sustained release effect, reduce release speed, and prevent drug leakage. seepage effect

Inactive Publication Date: 2021-02-19
WUHAN POLYTECHNIC UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, it is mostly believed that its onset is caused by delayed-type allergic reaction mediated by T lymphocytes. Topical application of glucocorticoids on the skin has a certain therapeutic effect, but the side effects are large and drug resistance is strong, and it is easy to relapse or even aggravate the disease. Treatment is difficult and has a great impact on the patient's physical and mental health
There is a significant unmet medical need in this area as there is currently a lack of safe and effective topical treatments for the large mild to moderate allergic dermatitis population
Criborole is a non-hormonal anti-inflammatory drug, its clinical data in the treatment of eczema is very competitive, it may become the first-line therapy for this patient group, and it has high clinical application value, diphenylheptane A (Diphenylheptane A, structural formula shown in formula I) is one of the main components of Alpinia galanga, which can inhibit the expression of inducible nitric oxide synthase iNOS by inhibiting the activity of NF-KB), cyclooxygenase 2 The expression of (COX-2) plays an anti-inflammatory and analgesic effect. The inventor found that after adding Diphenylheptane A to crisborole, it can produce a significant anti-inflammatory synergistic effect, but Diphenylheptane A itself has certain irritation, which limits added amount

Method used

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  • Medicinal gel, preparation method thereof and application of medicinal gel
  • Medicinal gel, preparation method thereof and application of medicinal gel
  • Medicinal gel, preparation method thereof and application of medicinal gel

Examples

Experimental program
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preparation example Construction

[0030] The second aspect of the present invention provides the preparation method of the above-mentioned pharmaceutical gel, the preparation method comprising:

[0031] (1) Mix and swell the poloxamer 407, poloxamer 188, hydroxypropyl cellulose and water, then add the diphenylheptane A hydroxypropyl-β-cyclodextrin under stirring clathrate and glycerol to obtain the first solution;

[0032] (2) mixing the crisborole, ethylparaben and propylene glycol to obtain a second solution;

[0033] (3) Mixing the first solution and the second solution uniformly to obtain the drug gel.

[0034] According to the present invention, preferably, in step (1), the poloxamer 407, poloxamer 188, and hydroxypropyl cellulose are spread on the surface of water, and then left to swell.

[0035] According to the present invention, preferably, the swelling temperature is 4-8° C., and the swelling time is not less than 24 hours.

[0036] The third aspect of the present invention provides the applicati...

Embodiment 1

[0039] The present embodiment provides a pharmaceutical gel, the specific formulation is shown in Table 1, and the specific preparation method is as follows:

[0040] (1) Spread poloxamer 407, poloxamer 188, and hydroxypropyl cellulose on the surface of purified water, let it swell at 4°C for 24 hours to obtain a homogeneous solvent, and then add diphenylheptane A hydroxyl Propyl-beta-cyclodextrin inclusion complex and glycerin to obtain the first solution;

[0041] (2) Criborole, ethylparaben and propylene glycol are mixed to obtain a second solution;

[0042] (3) Add the second solution into the first solution under stirring, and stir evenly to obtain the drug gel;

[0043] Wherein, the diphenylheptane A hydroxypropyl-β-cyclodextrin inclusion compound is prepared by the following method:

[0044] (1) Weigh 10g of diphenylheptane A, add 10ml of ethanol to dissolve, and obtain diphenylheptane A ethanol solution;

[0045] (2) Mix 50 g of hydroxypropyl-β-cyclodextrin with 200...

Embodiment 2

[0051] This embodiment provides a drug gel, and the specific formula is shown in Table 2;

[0052] The dosage and preparation method of each raw material for preparing diphenylheptane A hydroxypropyl-β-cyclodextrin inclusion complex and the preparation method of the drug gel are the same as in Example 1.

[0053] Table 2

[0054]

[0055]

[0056] The mass ratio of crisborole to diphenylheptane A contained in the drug gel prepared in this example is 7.5:1. The phase transition temperature of the pharmaceutical gel prepared in this example is 29°C.

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Abstract

The invention discloses a medicine gel, a preparation method thereof and application of the medicine gel. The medicine gel is prepared from the following components: 1-2 wt% of crisaborole, 1.2-2.4 wt% of diphenylheptane A hydroxypropyl-beta-cyclodextrin inclusion compound, 18-20 wt% of poloxamer 407, 1-3 wt% of poloxamer 188, 0.1-0.2 wt% of hydroxypropyl cellulose, 8-10 wt% of propylene glycol, 5-10 wt% of glycerol, 0.1-0.2 wt% of ethylparaben and 51.6-64.9 wt% of water. The medicinal gel disclosed by the invention can realize long-term drug release; By employing a percutaneous drug deliveryway, the drug can play a very good slow-release role in a human body, and the drug can be prevented from extravasation, and is released for a long time.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and more specifically relates to a pharmaceutical gel and its preparation method and application. Background technique [0002] Eczema is an allergic inflammatory skin disease caused by a variety of internal and external factors. It is characterized by symmetrical distribution of skin lesions, polymorphic lesions, severe itching, tendency to exudate, and repeated attacks. At present, it is mostly believed that its onset is caused by delayed-type allergic reaction mediated by T lymphocytes. Topical application of glucocorticoids on the skin has a certain therapeutic effect, but the side effects are large and drug resistance is strong, and it is easy to relapse or even aggravate the disease. Treatment is difficult and has a great impact on the physical and mental health of patients. Currently, there is a significant unmet medical need in this area for the large mild-to-moderate...

Claims

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Application Information

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IPC IPC(8): A61K9/06A61K31/12A61K47/69A61P17/00A61P37/08
CPCA61K9/0014A61K9/06A61K31/12A61K47/6951A61P17/00A61P37/08
Inventor 徐晨星赵玲李心怡杨博
Owner WUHAN POLYTECHNIC UNIVERSITY
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