CN1857278A - Externally applied compound gel and its preparing method - Google Patents

Abstract

The present invention relates to a compound external gel and its preparation method. The external gel and the preparation method thereof can be used for treating ringworm (tinea corporis, tinea cruris, tinea manus, tinea capitis, etc.), skin yeast infection caused by candida, and onychomycosis caused by fungus. The invention is convenient to use and has a high cure rate, and is suitable for skin disease patients.

Description

A kind of compound gel for external use and preparation method thereof

technical field

The invention relates to a new type of pharmaceutical dosage form, in particular to a treatment for ringworm (tinea corporis, jock itch, tinea manuum, tinea capitis, etc.), skin yeast infection caused by Candida, and onychomycosis caused by moldy fungus and other diseases Compound gel for external use and preparation method thereof.

Background technique

Terbinafine Hydrochloride (TER-HCL) has the effect of specifically inhibiting squalene cyclooxygenase. Fungal cells continuously ingest squalene, resulting in cell membrane damage and fungal cell death. This is its bactericidal effect. In addition, squalene epoxidase is the key enzyme for the formation of ergosterol. Since squalene cannot be epoxidized, the synthesis of ergosterol, the main component of the sensitive fungal cell membrane, is reduced, thereby inhibiting the activity of fungal cells. This is its Antibacterial effect. Therefore, the mechanism of action of terbinafine hydrochloride is to selectively inhibit the necessary oxidase in the process of fungal synthesis and reproduction, so as to achieve the dual effects of bactericidal and fungal inhibition, and it also has a broad-spectrum antifungal effect.

Clobetasol propionate (Clobetasol Propionate, CBT) is an adrenal cortex hormone drug, which has strong anti-inflammatory, anti-itching and vasoconstrictive effects, and is clinically used to treat neurodermatitis, contact dermatitis, seborrheic dermatitis, etc. disease.

The aqueous gel matrix involved in the present invention has the functions of being easy to spread, easy to wash and remove, no greasy feeling, and capable of absorbing tissue exudate without hindering the normal function of the skin. At the same time, due to the low viscosity of the matrix, it has Facilitate rapid drug release.

The compound gel for external use is made of terbinafine hydrochloride and clobetasol propionate as the main ingredients, which can effectively sterilize bacteria, and is convenient and comfortable to apply without irritation. It is suitable for people with ringworm and skin yeast infection. And patients with diseases such as onychomycosis.

But there is still a lack of a kind of external compound condensate that can treat ringworm (tinea corporis, jock itch, tinea manuum and tinea capitis, etc.), skin yeast infection caused by Candida, and diseases such as onychomycosis caused by moldy fungi at present. glue.

Contents of the invention

The object of the present invention is to provide a kind of compound gel for external use for the treatment of ringworm (tinea corporis, jock itch, tinea manuum and tinea capitis, etc.), skin yeast infection caused by candida, and onychomycosis caused by moldy fungus and its preparation method.

The invention relates to a compound gel for external use, which is characterized in that the main ingredients of the prescription are terbinafine hydrochloride (0.01-20)%, clobetasol propionate (0.01-10)%, and other ingredients include: carbomer (0.1～5)%, hydroxypropyl methylcellulose (0～20)%, pH adjuster (0.5～10)%, humectant (5～30)%, solvent (10～80)%, preservative ( 0.01～1.5)%.

Wherein: the pH regulator includes but not limited to disodium hydrogen phosphate, sodium dihydrogen phosphate, triethanolamine, ethylenediamine, laurylamine, sodium bicarbonate, sodium hydroxide, etc., which can be used alone or in combination.

The humectants include but are not limited to glycerin, propylene glycol, sorbitol, diethylene glycol, xylitol, etc., which can be used alone or in combination.

The solvents include but are not limited to propylene glycol, ethanol, purified water, distilled water, water for injection, etc., and can be used alone or in combination.

The preservatives include but are not limited to benzyl alcohol, methylparaben, propylparaben, butylparaben, etc., which can be used alone or in combination.

The specific preparation method of this dosage form is as follows:

The first step is to take carbomer, add a moisturizer to grind and moisten it, then add an appropriate amount of water to fully swell the carbomer to obtain a carbomer matrix;

The second step is to take hydroxypropyl methylcellulose, add an appropriate amount of water at 90°C and stir quickly to obtain a uniform white hydroxypropyl methylcellulose solution, add it to the carbomer matrix and mix well for later use;

The third step is to take terbinafine hydrochloride and clobetasol propionate, dissolve them in ethanol, and slowly add them to the matrix obtained in the second step while stirring;

The fourth step is to add the pH regulator solution and preservative to the mixture obtained in the third step, and then add water to the full amount, and stir evenly;

The fifth step is to carry out primary filtration and fine filtration of the above liquid, and then fill it to obtain the compound gel for external use of the present invention.

The invention is a water-based gel, which has no greasy feeling, can absorb tissue exudate without hindering the normal function of the skin, and at the same time, because the viscosity of the matrix is small, it is beneficial to the rapid release of drugs. At the same time, after the preparation is administered, it is easy to spread and wash off, and is easy to be accepted by patients, which helps to improve the medication compliance of patients, and is an effective new clinical anti-infection preparation.

Detailed ways

The compound gel for external use of the present invention comprises main components terbinafine hydrochloride and clobetasol propionate, and carbomer, hypromellose, pH regulator, humectant, solvent, preservative, etc., after Prepared by a specific method. For a better description of the preparation method of the external compound gel of the present invention, special examples are as follows:

Embodiment 1. The preparation of compound gel for external use

Prescription: Terbinafine Hydrochloride 1.0g

                                                                                             

Carbomer 941 0.5g

                                                                                                           

                                              

Glycerin 15.0g

Propylene Glycol 10.0g

Ethanol 10.0ml

Benzyl alcohol 0.5g

                                                                                                                                                                     

Preparation:

1. Take carbomer, grind it with glycerin, add 10ml of purified water to fully swell the carbomer, and obtain the carbomer matrix;

2. Take hydroxypropyl methylcellulose, add 15ml of 90°C water and stir quickly to obtain a uniform white hydroxypropyl methylcellulose solution, add it to the carbomer matrix and mix well for later use;

3. Take terbinafine hydrochloride and clobetasol propionate, dissolve them in ethanol, and slowly add them to the carbomer matrix under stirring;

4. Slowly add propylene glycol to the mixture obtained in the previous step, and stir evenly;

5. Add triethanolamine and benzyl alcohol dropwise to the mixture obtained in the previous step, then add purified water to the full amount, and stir evenly;

6. The above-mentioned liquid is subjected to initial filtration and fine filtration, and then filled to obtain the compound gel for external use of the present invention. The total amount is 100g, divided into 10 sticks, each stick is 10g, and the content of terbinafine hydrochloride is 0.1g/10g.

Embodiment 2. The preparation of compound gel for external use

Prescription: Terbinafine Hydrochloride 1.0g

                                                                                             

Carbomer 941 1.5g

                                            

Glycerin 10.0g

Diethylene glycol 10.0g

Ethanol 10.0ml

Benzyl alcohol 0.5g

Distilled water Add up to 100g

Preparation:

1. Take carbomer, add glycerin to grind and moisten it, add 20ml of distilled water to fully swell the carbomer, and obtain the carbomer matrix;

2. Take terbinafine hydrochloride and clobetasol propionate, dissolve them in ethanol, and slowly add them to the carbomer matrix under stirring;

3. Slowly add diethylene glycol to the mixture obtained in the previous step, and stir evenly;

4. Add triethanolamine and benzyl alcohol dropwise to the mixture obtained in the previous step, then add distilled water to the full amount, and stir evenly;

5. The above-mentioned liquid is subjected to primary filtration and fine filtration, and then filled to obtain the compound gel for external use of the present invention. The total amount is 100g, divided into 10 sticks, each stick is 10g, and the content of terbinafine hydrochloride is 0.1g/10g.

Embodiment 3. Preparation of compound gel for external use

Prescription: Terbinafine Hydrochloride 1.0g

                                                                                  

Carbomer 941 1.5g

Sodium bicarbonate 2.5g

Diethylene glycol 10.0g

Sorbitol 10.0g

Ethanol 10.0ml

Methylparaben 0.1g

                                                                                                                                                                     

Preparation:

1. Take carbomer, add diethylene glycol to grind and moisten it, add 20ml of purified water to fully swell the carbomer, and obtain the carbomer matrix;

2. Take terbinafine hydrochloride and clobetasol propionate, dissolve them in ethanol, and slowly add them to the carbomer matrix under stirring;

3. Slowly add propylene glycol to the mixture obtained in the second step, and stir evenly;

4. Add triethanolamine and methylparaben dropwise to the mixture obtained in the previous step, then add purified water to the full amount, and stir evenly;

5. The above-mentioned liquid is subjected to primary filtration and fine filtration, and then filled to obtain the compound gel for external use of the present invention. The total amount is 100g, divided into 10 sticks, each stick is 10g, and the content of terbinafine hydrochloride is 0.1g/10g.

Embodiment 4. Preparation of compound gel for external use

Prescription: Terbinafine Hydrochloride 1.0g

                                                                                             

Carbomer 941 1.5g

Sodium Hydroxide 2.5g

Glycerin 20.0g

Ethanol 10.0ml

                                                           

Distilled water Add up to 100g

Preparation:

1. Take carbomer, add glycerin to grind and moisten it, add 20ml of distilled water to fully swell the carbomer, and obtain the carbomer matrix;

2. Take terbinafine hydrochloride and clobetasol propionate, dissolve them in ethanol, and slowly add them to the carbomer matrix under stirring;

3. Add sodium hydroxide and propylparaben dropwise to the mixture obtained in the previous step, then add distilled water to the full amount, and stir evenly;

4. The above-mentioned liquid is subjected to initial filtration and fine filtration, and then filled to obtain the compound gel for external use of the present invention. The total amount is 100g, divided into 10 sticks, each stick is 10g, and the content of terbinafine hydrochloride is 0.1g/10g.

Claims (4)

1. externally applied compound gel agent, its component comprises TER-HCL, clobetasol propionate, carbomer, pH regulator agent, wetting agent, solvent and antiseptic, the percentage by weight of each component is in it is characterized in that writing out a prescription:

TER-HCL 0.01～20%

Clobetasol propionate 0.01～10%

Carbomer 0.1～5%

Hydroxypropyl methylcellulose 0～20%

PH regulator agent 0.5～10%

Wetting agent 5～30%

Solvent 10～80%

Antiseptic 0.01～1.5%.

2. according to the described a kind of externally applied compound gel agent of claim 1, it is characterized in that:

Described pH regulator agent comprises sodium hydrogen phosphate, sodium dihydrogen phosphate, triethanolamine, ethylenediamine, lauryl amine, sodium bicarbonate, sodium hydroxide, can be separately or combination in any use;

Described wetting agent comprises glycerol, propylene glycol, sorbitol, diethylene glycol, xylitol, can be separately or combination in any use;

Described solvent comprises propylene glycol, ethanol, purified water, distilled water, water for injection, can be separately or combination in any use;

Described antiseptic comprises benzyl alcohol, methyl hydroxybenzoate, propylparaben, butoben, can be separately or combination in any use.

3. the preparation method of a kind of externally applied compound gel agent of stating according to claim 1 or 2 is characterized in that this method comprises by following steps to form:

The first step is got carbomer, after adding wetting agent and grinding moistening, add suitable quantity of water and make carbomer be able to abundant swelling, carbomer substrate;

Second step was got hydroxypropyl methylcellulose, add an amount of 90 ℃ of water and stir fast, evenly white hydroxypropyl methylcellulose solution, it is standby that it is added in carbomer substrate mixing;

The 3rd step was got TER-HCL and clobetasol propionate, behind dissolve with ethanol, under agitation slowly added in the second step gained substrate;

The 4th step dripped pH regulator agent solution and antiseptic in the 3rd step gained mixture, add to full dose with water again, and stir;

The 5th step was carried out just filter and fine straining with aforesaid liquid, carried out fill again and promptly got externally applied compound gel of the present invention.

4. comprise the tinea of tinea corporis, tinea cruris, tinea manus and pedis and tinea capitis according to the described a kind of externally applied compound gel agent of claim 1 in treatment, by the microbial skin yeast infection of beads, and by the application of mouldy microbial tinea unguium aspect.