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Terbinafine hydrochloride gel and preparation method thereof

A technology of terbinafine hydrochloride and gel, which is applied in the field of medicine, can solve problems such as quality reduction, expiration date, and property change, and achieve the effects of improving stability, uniform content, and good stability

Inactive Publication Date: 2016-02-24
吉林修正药业新药开发有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, as an insoluble compound, terbinafine hydrochloride is easy to precipitate during daily transportation, storage and clinical long-term use, and its properties change, which reduces the quality and validity period of the drug

Method used

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  • Terbinafine hydrochloride gel and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Terbinafine hydrochloride gel, including the following components in 100g: Terbinafine hydrochloride 1g, carbomer 1.5g, propylene glycol 20g, polyethylene glycol 40010g, cetyl alcohol 5g, tert-butyl p-hydroxyanisole 0.005 g, polysorbate 808g, triethanolamine 1g, edetate disodium 0.1g, ethanol 30g, distilled water about 24g.

[0019] The preparation method of terbinafine hydrochloride gel, concrete steps are as follows:

[0020] (1) Take 80% of the prescribed amount of purified water to dissolve edetate disodium, add the prescribed amount of carbomer (stir while adding), and swell for 24 hours until the carbomer has no hard core.

[0021] (2) Stir the swollen carbomer slowly (23 rev / min), then stir rapidly (2000 rev / min), emulsify for 30 minutes, then add the prescribed amount of propylene glycol, polyethylene glycol 400, cetyl Alcohol, tert-butyl p-hydroxyanisole, emulsified for 15 minutes to form a gel matrix.

[0022] (3) Dissolve the prescribed amount of terbinafin...

Embodiment 2

[0025] Terbinafine hydrochloride gel, including the following components in 100g: Terbinafine hydrochloride 1g, carbomer 1g, propylene glycol 12g, polyethylene glycol 4006g, cetyl alcohol 4g, tert-butyl p-hydroxyanisole 0.002g , polysorbate 805g, triethanolamine 0.5g, edetate disodium 0.05g, ethanol 20g, distilled water about 50g.

[0026] The preparation method of terbinafine hydrochloride gel, concrete steps are as follows:

[0027] (1) Take 80% of the prescribed amount of purified water to dissolve edetate disodium, add the prescribed amount of carbomer (stir while adding), and swell for 24 hours until the carbomer has no hard core.

[0028] (2) Stir the swollen carbomer slowly (23 rpm), then stir rapidly (2000 rpm), emulsify for 20 minutes, add the prescribed amount of propylene glycol, polyethylene glycol 400, sixteen Alcohol, tert-butyl p-hydroxyanisole, emulsified for 10 minutes to form a gel matrix.

[0029] (3) Dissolve the prescribed amount of terbinafine hydrochlo...

Embodiment 3

[0032] Terbinafine hydrochloride gel, 100g includes the following components: Terbinafine hydrochloride 1g, carbomer 3g, propylene glycol 29g, polyethylene glycol 40015g, cetyl alcohol 6g, tert-butyl p-hydroxyanisole 0.01g , polysorbate 8010g, triethanolamine 3g, edetate disodium 0.15g, ethanol 25g, distilled water about 8g.

[0033] The preparation method of terbinafine hydrochloride gel, concrete steps are as follows:

[0034] (1) Take 80% of the prescribed amount of purified water to dissolve edetate disodium, add the prescribed amount of carbomer (stir while adding), and swell for 24 hours until the carbomer has no hard core.

[0035] (2) Stir the swollen carbomer slowly (23 rpm), then stir rapidly (2000 rpm), emulsify for 45 minutes, add the prescribed amount of propylene glycol, polyethylene glycol 400, sixteen Alcohol, tert-butyl p-hydroxyanisole, emulsified for 25 minutes to form a gel matrix.

[0036] (3) Dissolve the prescribed amount of terbinafine hydrochloride i...

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Abstract

The invention provides terbinafine hydrochloride gel and a preparation method thereof. The terbinafine hydrochloride gel is prepared from the following raw materials in parts by weight: 1 part of terbinafine hydrochloride, 1-3 part of carbomer, 10-30 parts of propylene glycol, 5-16 parts of polyethylene glycol 400, 4-6 parts of hexadecanol, 0.001-0.01 part of butylated hydroxyanisole, 4-12 parts of polysorbate 80, 0.3-3 parts of triethanolamine, 0.05-0.15 part of edetate disodium, 20-40 parts of ethanol and 8-50 parts of distilled water. The preparation method comprises the following steps: (1) swelling carbomer by adopting purified water; (2) emulsifying the swelled carbomer, and then emulsifying propylene glycol, polyethylene glycol 400, hexadecanol, and butylated hydroxyanisole to form a gel substrate; (3) dissolving terbinafine hydrochloride with ethanol, adding polysorbate 80, uniformly mixing the dissolved terbinafine hydrochloride and polysorbate 80, adding the mixed solution into the gel substrate obtained in step (2), and stirring for emulsifying; and (4) adding triethanolamine and the rest of purified water to a product in step (3), stirring for emulsifying, and uniformly mixing the obtained mixture with a gel to obtain the terbinafine hydrochloride gel. The terbinafine hydrochloride gel has the positive effects that the stability of the medicine is improved, the curative effect is high, the coating and removing by washing are easy, the irritation to the skin is eliminated, and no odor exists.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a terbinafine hydrochloride gel and a preparation process thereof. Background technique [0002] In recent years, the incidence of skin tinea caused by fungal infection, such as tinea manus, jock itch, tinea unguium, tinea capitis, etc., has become more and more frequent, and has the characteristics of easy infection, recurrence or reinfection, which brings great harm to the body and spirit of patients. caused enormous damage. The main new drugs for the treatment of antifungal diseases are: allylamine, triazoles, and imidazoles. Terbinafine hydrochloride is an allylamine drug with broad-spectrum antifungal activity. It can selectively act on the squalene cyclooxygenase in the process of ergosterol synthesis in fungal cells, prevent the production of ergosterol, destroy the lipid part in the cell membrane, so as to kill the fungus and achieve the purpose of inhibitin...

Claims

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Application Information

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IPC IPC(8): A61K9/06A61K47/34A61K47/10A61K47/08A61K31/137A61P17/00A61P31/04A61P31/10
Inventor 曹翠阎君白冰林子琦于施刘学锋
Owner 吉林修正药业新药开发有限公司
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