Prescription of tranilast emulsifiable paste and preparation process of tranilast emulsifiable paste

A special cream and tranis technology, applied in the field of medicine, can solve the problems of insufficient blood drug concentration in local scar tissue, unfavorable patient compliance, and slow onset of effect, so as to reduce the risk of systemic adverse reactions and improve patient compliance Sexuality, the effect of avoiding liver and kidney toxicity

Inactive Publication Date: 2021-09-03
药大制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Once the scar is formed, it cannot be completely eliminated. There are many current treatment methods, but none of them can achieve a completely satisfactory effect. The prevention and treatment of scar is still an international medical problem
[0005] The oral dosage form of tranilast that has been on the market is administered systemically. The blood concentration of the local tissue of the scar is insufficient, and the onset of effect is slow. It needs to be taken for a long time. The course of treatment is long, and it is accompanied by a certain risk of liver and kidney toxicity. Liver function testing is required, which is not conducive to patient compliance

Method used

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  • Prescription of tranilast emulsifiable paste and preparation process of tranilast emulsifiable paste
  • Prescription of tranilast emulsifiable paste and preparation process of tranilast emulsifiable paste
  • Prescription of tranilast emulsifiable paste and preparation process of tranilast emulsifiable paste

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Experimental program
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Effect test

Embodiment 1

[0027] (1) Preparation of oil phase liquid: stearyl alcohol 90g, polyoxyethylene fatty alcohol ether 20g, glyceryl monostearate 20g, caprylic triglyceride 65g, butylparaben 30g, di-tert-butyl The ratio of 5g of hydroxytoluene is added to the oil phase pot in turn, and when the temperature rises to 85-90°C, turn off the heating and wait for use;

[0028] (2) Preparation of water phase liquid: Add 200g of glycerin, 500g of purified water, 1g of edetate disodium, and 1g of ethylparaben to the water phase pot in sequence. When the temperature of the water phase reaches 90-95°C, add Sodium lauryl sulfate 10g, stir until the material dissolves, turn off the stirring;

[0029] (3) Emulsification: first transfer all the oil phase substances to the vacuum emulsification pot, and then slowly transfer all the water phase substances to the emulsification pot. The cooling water starts to cool;

[0030] (4) Preparation of tranilast dispersion: disperse 10 g of tranilast and 1 g of sodium ...

Embodiment 2

[0034] (1) Preparation of oil phase liquid: stearyl alcohol 90g, polyoxyethylene fatty alcohol ether 20g, glyceryl monostearate 20g, caprylic triglyceride 65g, butylparaben 30g, di-tert-butyl The ratio of 5g of hydroxytoluene is added to the oil phase pot in turn, and when the temperature rises to 85-90°C, turn off the heating and wait for use;

[0035] (2) Preparation of water phase liquid: Add 200g of glycerin, 500g of purified water, 1g of edetate disodium, and 1g of ethylparaben to the water phase pot in sequence. When the temperature of the water phase reaches 90-95°C, add Sodium lauryl sulfate 10g, stir until the material dissolves, turn off the stirring;

[0036] (3) Emulsification: first transfer all the oil phase substances to the vacuum emulsification pot, and then slowly transfer all the water phase substances to the emulsification pot. The cooling water starts to cool;

[0037] (4) Preparation of tranilast dispersion: disperse 20 g of tranilast and 1 g of sodium ...

Embodiment 3

[0041] Production of Hypertrophic Scar Model in Rabbit Ears

[0042] After the animal was adaptively fed for 1 week, the production of the scar model referred to the literature method (Bian Huining, Li Tianzeng, Xie Julin, etc. Effect of basic fibroblast growth factor on the formation of rabbit ear hypertrophic scar. Chinese Journal of Trauma, 2004, 20(4):242-245) and improved, with 30g·L -1 Sodium pentobarbital 1.0mL·kg -1 (30mg·kg -1 ) for auricular vein anesthesia, iodophor and ethanol disinfection of the ventral skin of the rabbit ear, avoiding visible blood vessels along the long axis of the ventral middle section of the rabbit ear, and gently drilling a 1cm×1cm wound with a corneal ring, with an interval of more than 1cm between the wounds, The full-thickness skin of the rabbit ears was removed and the perichondrium was completely scraped off with a spatula. Sterile cotton balls were pressed to stop the bleeding, 4 places per ear. The postoperative wounds were exposed....

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Abstract

The invention relates to a formula and a preparation process of tranilast emulsifiable paste, relates to a treatment effect in the field of keloids and hypertrophic scars of the tranilast emulsifiable paste, and belongs to the field of medical science and technology. The formula of the tranilast cream comprises the following components in percentage by weight: 0.5%-10% of tranilast; 15%-30% of a cream matrix; 3%-5% of a thickening agent; and the balance purified water. The cream matrix comprises an oil phase liquid and a water phase liquid. The preparation process comprises the following steps: preparing the oil phase liquid; preparing the water phase liquid; and preparing emulsified tranilast dispersion liquid and the like. According to the present invention, the cream containing the tranilast component belongs to an external dosage form, and does not have untoward effects such as dependence, cytotoxicity and the like. The medicine is applied locally and permeates the scar tissue to take effect locally, and the concentration of the medicine for the scar target tissue is higher.

Description

technical field [0001] The invention relates to the technical field of medical science and technology, in particular to a prescription of tranilast cream and a preparation process thereof. Background technique [0002] Tranilast was developed and marketed by Kissei Pharmaceutical Co., Ltd. (Japan) in 1982. It is an allergic mediator blocker, which can inhibit mast cell degranulation and the release of allergic mediators caused by allergens and other stimuli. It has the function of stabilizing the cell membrane of mast cells and basophils, preventing their degranulation. Thereby inhibiting the release of histamine and 5-hydroxytryptamine allergic reaction substances, and has a significant inhibitory effect on the skin allergic reaction and experimental asthma caused by IgE antibodies, and is an etiological and therapeutic drug aimed at the occurrence mechanism of allergic diseases. [0003] In the 1990s, it was discovered that tranilast has anti-fibrosis effect, and its oral...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K31/196A61P17/02
CPCA61K9/06A61K9/0014A61K31/196A61K47/20A61P17/02
Inventor 郝静梅王鲁娟
Owner 药大制药有限公司
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