CN118021984A - Compound external preparation, preparation method and application thereof - Google Patents
Compound external preparation, preparation method and application thereof Download PDFInfo
- Publication number
- CN118021984A CN118021984A CN202410138167.8A CN202410138167A CN118021984A CN 118021984 A CN118021984 A CN 118021984A CN 202410138167 A CN202410138167 A CN 202410138167A CN 118021984 A CN118021984 A CN 118021984A
- Authority
- CN
- China
- Prior art keywords
- hydrochloride
- external preparation
- ointment
- compound external
- cream
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 238000002360 preparation method Methods 0.000 title claims abstract description 72
- 150000001875 compounds Chemical class 0.000 title claims abstract description 35
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- OETHQSJEHLVLGH-UHFFFAOYSA-N metformin hydrochloride Chemical compound Cl.CN(C)C(=N)N=C(N)N OETHQSJEHLVLGH-UHFFFAOYSA-N 0.000 claims abstract description 50
- 239000000739 antihistaminic agent Substances 0.000 claims abstract description 26
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- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 64
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- ZKLPARSLTMPFCP-OAQYLSRUSA-N 2-[2-[4-[(R)-(4-chlorophenyl)-phenylmethyl]-1-piperazinyl]ethoxy]acetic acid Chemical compound C1CN(CCOCC(=O)O)CCN1[C@@H](C=1C=CC(Cl)=CC=1)C1=CC=CC=C1 ZKLPARSLTMPFCP-OAQYLSRUSA-N 0.000 claims description 2
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- ZKLPARSLTMPFCP-UHFFFAOYSA-N Cetirizine Chemical compound C1CN(CCOCC(=O)O)CCN1C(C=1C=CC(Cl)=CC=1)C1=CC=CC=C1 ZKLPARSLTMPFCP-UHFFFAOYSA-N 0.000 claims description 2
- MHNSPTUQQIYJOT-SJDTYFKWSA-N Doxepin Hydrochloride Chemical compound Cl.C1OC2=CC=CC=C2C(=C/CCN(C)C)/C2=CC=CC=C21 MHNSPTUQQIYJOT-SJDTYFKWSA-N 0.000 claims description 2
- RRJFVPUCXDGFJB-UHFFFAOYSA-N Fexofenadine hydrochloride Chemical compound Cl.C1=CC(C(C)(C(O)=O)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 RRJFVPUCXDGFJB-UHFFFAOYSA-N 0.000 claims description 2
- HOKDBMAJZXIPGC-UHFFFAOYSA-N Mequitazine Chemical compound C12=CC=CC=C2SC2=CC=CC=C2N1CC1C(CC2)CCN2C1 HOKDBMAJZXIPGC-UHFFFAOYSA-N 0.000 claims description 2
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Abstract
The invention discloses a compound external preparation, a preparation method and application thereof, wherein the compound external preparation comprises two active ingredients of metformin hydrochloride and an H1 antihistamine drug. The compound external preparation disclosed by the invention has good treatment effects on eczema, atopic dermatitis, psoriasis and neurodermatitis.
Description
Technical Field
The invention relates to the technical field of pharmaceutical preparations, in particular to a compound external preparation, a preparation method and application thereof.
Background
More than 20 diseases such as contact dermatitis, atopic dermatitis, neurodermatitis and the like are included in the section of dermatitis and eczema in the tenth edition (ICD-10) of the International Classification of diseases. Currently, dermatitis and eczema are collectively known by scholars as atopic dermatitis (atopic dermatitis, AD), which is a chronic, recurrent, inflammatory skin disease. About 2.3 million people worldwide suffer from AD, which includes 20% children and 1% to 3% adults, characterized by itching, inflammatory lesions, and defects in the skin barrier. Repeated scratching can cause itching-scratching cycles, severely affecting the quality of life of the patient. Thus, controlling itch is one of its therapeutic goals. The disease mechanism of AD is related to genetic factors, environmental factors, skin barriers, immunity factors and other factors, while Th2 type inflammation is a basic characteristic of AD, the inflammation of AD at different age stages is different, the childhood mainly shows Th2 type inflammation, the adult is Th2/Th22 type mixed inflammation, and the asian is mainly Th2/Th17 mixed inflammation; psoriasis, however, is a common immune-mediated chronic inflammatory skin disease that can severely compromise the physical and mental health of a patient as it can involve the patient's skin, nails, mucous membranes and joints. The exact pathogenesis of psoriasis has not been fully elucidated. Psoriasis is considered to be polygenic hereditary disease of multiple factor interaction such as hereditary factor and environmental factor at present, the common pathway mediated by immunity causes unbalance of human immune system, nervous system and inflammatory medium, causes inherent immunity mediated by antigen presenting cells and natural killer cells and acquired immunity mediated by T cells to generate disorder, under the synergistic effect of the two, generates multiple cytokines, promotes inflammatory cell infiltration and gradual amplification of inflammatory network at the skin injury part, and finally leads to the peculiar proliferative skin injury of psoriasis.
The current drugs for the treatment of atopic dermatitis and psoriasis are of various kinds, wherein specific drug biologicals (antibody preparations) are expensive, topical glucocorticoids (TCS) are liable to cause drug resistance, skin pigmentation, topical calcium-regulated neurotransmission inhibitors (TCI) may cause an increased risk of viral, bacterial, fungal and/or protozoal infections, and topical use may cause skin burning (burning, stinging, pain) or itching; the medicine for treating atopic dermatitis and psoriasis also comprises vitamin D3 derivatives, retinoids, moisturizers and the like, but has poor effect or slow effect. Thus, there is an urgent need for a pharmaceutical preparation for treating atopic dermatitis and psoriasis to solve the above-mentioned problems.
Metformin hydrochloride is an oral hypoglycemic drug widely used clinically, and is recommended internationally as a first-line therapeutic drug for type 2 diabetes (T2 MD); the research shows that the metformin hydrochloride can obviously inhibit the growth of tumors under the fasted state, and the PP2A-GSK3 beta-MCL-1 pathway is proposed to be a new target point for tumor treatment.
Histamine is a monoamine neurotransmitter and active signaling molecule that plays an important role in a variety of physiological and pathological processes by binding to histamine receptors. There are 4 types of histamine receptors known at present, H1-4, all belonging to the G protein-coupled receptor family. Histamine receptors are widely expressed in the central nervous system and peripheral tissues and are involved in the regulation of allergic reactions, gastric acid secretion, inflammatory reactions, central nervous system excitability, and the like. The medicine with histamine receptor as acting target is used for resisting anaphylaxis, gastric acid, dizziness, vomiting and sedation.
Disclosure of Invention
The present invention aims to solve at least one of the above technical problems in the prior art. Therefore, the invention aims to provide a compound external preparation which simultaneously comprises two active ingredients of metformin hydrochloride and an H1 antihistamine drug; the compound external preparation has good treatment effect on skin diseases, especially eczema, atopic dermatitis, psoriasis and neurodermatitis.
Meanwhile, the invention also provides a preparation method and application of the compound external preparation.
Specifically, the invention adopts the following technical scheme:
in a first aspect of the present invention, there is provided a compound external preparation comprising metformin hydrochloride and an H1 antihistamine.
In some embodiments of the invention, the H1 antihistamine comprises chloromastine fumarate, terfenadine, astemizole, diphenhydramine hydrochloride, diphenhydramine, loratadine, desloratadine citrate, doxepin hydrochloride, promethazine hydrochloride, perphenazine, chlorphenamine, fexofenadine hydrochloride, cetirizine hydrochloride, levocetirizine, pramine maleate, hydroxyzine hydrochloride, meclozine hydrochloride, mirtazapine, ebastine hydrochloride, azelastine fumarate, rupatadine fumarate, clopenthizot, clopenthizome hydrochloride, opamine hydrochloride, clemastine hydrochloride, clemizole, pemetrexed potassium, asenapine, mehydramine hydrochloride, bepotastine, mequitazine, thioethylpiperazine dimaleate, carbocisteine, dihydroxynapthalene, brompheniramine maleate, emetine, thiomerone, at least one of epinastine hydrochloride, nipradine hydrochloride, pyrilamine hydrochloride, bispyrilamine hydrochloride, mizolastine dihydrochloride, alcaftadine, bilastine, epinastine, fenspirits hydrochloride, chlorocirizine hydrochloride, triprolidine hydrochloride, rupatadine, decclodrozine, betosetin besylate, hydroxyzine, decclodrozine hydrochloride, chloro Ma Siding, mehai Qu Linnai disulfonate, benazine hydrochloride, qu Bi na-sensitive citrate, clopyraramide, triprolidine hydrochloride, pyrrolimidazole, fenspiride, chlorocirizine, fexofenadine, azelastine, rocarubide, cinnarizine, flunarizine hydrochloride, and terfenadine; more preferably, the H1 antihistamine comprises at least one of chlorphenamine, desloratadine citrate, rupatadine fumarate, azelastine hydrochloride, cinnarizine, and flunarizine hydrochloride.
In some embodiments of the invention, the H1 antihistamine is an organic acid salt or an inorganic acid salt; the organic acid salt or the inorganic acid salt of the H1 antihistamine is easy to dissolve in water, and is beneficial to skin absorption.
In some embodiments of the invention, the weight percentage of the metformin hydrochloride in the compound external preparation is 0.5-20%, and the weight percentage of the H1 antihistamine in the compound external preparation is 0.5-10%; more preferably, the mass percentage of the metformin hydrochloride in the compound external preparation is 1-10%.
In some embodiments of the invention, the dosage form of the formulation includes ointments, creams, gels, topical solutions, mucilage, patches, plasters, tinctures, lotions, paints, powders, lyophilized powders, aerosols and foams.
In some embodiments of the invention, the formulations are preferably ointments and creams.
In some embodiments of the invention, the compound external preparation further comprises an auxiliary agent, wherein the auxiliary agent comprises an ointment base, a solubilizer, a thickener, an ion complexing agent, a preservative, a consistency regulator, a oleaginous base, an oil phase emulsifier, an aqueous phase emulsifier, a humectant, a preservative, an ion complexing agent and a softener.
In some embodiments of the present invention, the compound external preparation is an ointment, and the ointment comprises the following components in percentage by mass: 50% -80% of ointment matrix, 10% -20% of solubilizer, 2% -8% of thickener, 0.1% -0.5% of ion complexing agent, 0.5% -20% of metformin hydrochloride and 0.5% -10% of H1 antihistamine drug; preferably, the ointment further comprises 0.1% -0.5% of a preservative.
In some embodiments of the present invention, the compound external preparation further comprises a diluent, wherein the diluent is deionized water.
In some embodiments of the invention, the ointment comprises the following components in percentage by mass: 2% of metformin hydrochloride, 1% of H1 antihistamine, 15% of solubilizer, 0.1% of ion complexing agent, 0.1% of preservative, 5% of thickener, 72% of ointment base and 5% of deionized water; preferably, the H1 antihistamine is chlorphenamine.
In some embodiments of the invention, the ointment base of the ointment comprises at least one of vaseline, paraffin, liquid paraffin, silicone oil, beeswax, stearic acid, lanolin.
In some embodiments of the invention, the ester thickening agent of the ointment comprises glyceryl monostearate, EG-80 glyceryl tallow, PEC-8PPG (polypropylene glycol) -3 diisostearate, PEG-200 hydrogenated glyceryl palmitate, PEG-n (n=6, 8, 12) beeswax, PEG-4 isostearate, PEG-n (n=3, 4, 8, 150) distearate, PEG-18 glyceryl oleate/cocoate, PEG-8 dioleate, PEG-200 glyceryl stearate, PEG-n (n=28, 200) glyceryl tallow, PEG-7 hydrogenated castor oil, PEG-40 jojoba oil, PEG-2 laurate, PEG-120 methyl glucose dioleate, PEG-150 quaternary amyl tetrastearate, PEG-55 propylene glycol oleate, PEG-160 sorbitan triisostearate, PEG-n (n=8, 75, 100) stearate, PEG-150/decyl/di copolymer (polyethylene glycol-150/decyl/methacrylate copolymer), PEG-150/di copolymer, PEG-90. Isostearate, PEG-8PPG-3 dilaurate, cetyl myristate, cetyl palmitate, ethylene glycol C18-36, pentaerythritol tetrastearate, pentaerythritol tetrasulfame ate, propylene glycol stearate, behenate, cetyl esters, glyceryl tribehenate, glyceryl trihydroxystearate, and the like; fatty alcohols and fatty acid thickeners include lauryl alcohol, myristyl alcohol, C12-15 alcohol, C12-16 alcohol, decyl alcohol, hexanol, octanol, cetyl alcohol, stearyl alcohol, behenyl alcohol, lauric acid, C18-36 acid, linoleic acid, linolenic acid, myristic acid, stearic acid, behenic acid, and the like; alkanolamide thickeners include cocodiethanolamide, cocomonoethanolamide, cocomonoisopropanolamide, cocoamide, lauroyl-linoleoyl diethanolamide, lauroyl-myristoyl diethanolamide, isostearoyl diethanolamide, linoleoyl diethanolamide, myristoyl monoethanolamide, oleamide, palmitomonoethanolamide, castor oil monoethanolamide, sesamodiethanolamide, soy diethanolamide, stearoyl monoethanolamide stearate, stearoyl diethanolamide, PEG (polyethylene glycol) -3 lauroyl amide, PEG-4 oleamide, PEG-50 tallow amide, and the like; the ether thickener includes cetyl alcohol polyoxyethylene (3) ether, isocetyl alcohol polyoxyethylene (10) ether, laureth alcohol polyoxyethylene (3) ether, laureth alcohol polyoxyethylene (10) ether, poloxamer-n (ethoxylated polyoxypropylene ether) (n=105, 124, 185, 237, 238, 338, 407) and the like; the polyacrylic thickener comprises at least one of an acrylate/C10-30 alkyl acrylate cross-linked polymer, an acrylate/hexadecylethoxy (20) itaconate copolymer, an acrylate/hexadecylethoxy (20) methacrylate copolymer, an acrylate/tetradecylethoxy (25) acrylate copolymer, an acrylate/octadecyl ethoxy (20) itaconate copolymer, an acrylate/octadecyl ethoxy (20) methacrylate copolymer, an acrylate/octadecyl ethoxy (50) acrylate copolymer, an acrylate/VA cross-linked polymer, PAA (polyacrylic acid), a sodium acrylate/ethylene isodecanoate cross-linked polymer, carbomer (polyacrylic acid) and sodium salts thereof.
In some embodiments of the invention, the solubilizing agent of the ointment comprises at least one of ethanol, propylene glycol, polyethylene glycol, glycerol.
In some embodiments of the invention, the preservative of the ointment comprises at least one of dibutyl hydroxy toluene, 1, 2-pentanediol, 1, 2-hexanediol, phenethyl alcohol, phenoxyethanol, p-hydroxyacetophenone, ethylhexyl glycerol, glyceryl decanoate, sorbitan octanoate, glyceryl undecylenate, methyl p-hydroxybenzoate, ethyl p-hydroxybenzoate (ethylparaben), propyl p-hydroxybenzoate, butyl p-hydroxybenzoate, levulinic acid, anisic acid, octanoyl hydroxamic acid.
In some embodiments of the invention, the ionic complexing agent of the ointment comprises at least one of disodium Edentate (EDTA), citric acid, tartaric acid, polyphosphates, aminocarboxylic acids, 1, 3-diketones, hydroxycarboxylic acids, polyamines. The ionic complexing agent is added into the ointment to effectively stabilize divalent metal ions such as Mg 2+、Ca2+、Mn2+、Fe2+ and the like, so that the oxidation reaction of the medicine catalyzed by the divalent metal ions is effectively prevented, and the medicine is more stable.
In some embodiments of the invention, the ointment comprises the following components in percentage by mass: metformin hydrochloride 0.5-20%, chlorphenamine 0.5-10%, propylene glycol 15%, disodium edentate 0.1%, dibutyl hydroxytoluene 0.1%, glyceryl monostearate 5%, white vaseline 71%, paraffin 1%, and deionized water 5%.
In some embodiments of the present invention, the compound external preparation is a cream, and the cream comprises the following components in percentage by mass: 0.5 to 20 percent of metformin hydrochloride, 0.5 to 10 percent of H1 antihistamine, 5 to 15 percent of consistency regulator, 5 to 12 percent of oleaginous matrix, 5 to 15 percent of oil phase emulsifier, 2 to 5 percent of water phase emulsifier, 5 to 15 percent of humectant, 0.1 to 0.5 percent of preservative and 0.1 to 0.5 percent of ion complexing agent.
In some embodiments of the invention, the cream further comprises 0.5% -5% of a softening agent.
In some embodiments of the present invention, the compound external preparation further comprises a diluent, wherein the diluent is deionized water.
In some embodiments of the invention, the oleaginous base of the cream comprises at least one of white petrolatum, paraffin wax, liquid paraffin wax, beeswax and spermaceti, lanolin, silicone, vegetable oil, hydrogenated vegetable oil.
In some embodiments of the invention, the consistency regulator of the cream comprises at least one of cetyl alcohol, stearyl alcohol, liquid paraffin, and solid paraffin.
In some embodiments of the invention, the oil phase emulsifier of the cream comprises at least one of glyceryl monostearate, croafos CES, cetyl alcohol (cetyl alcohol), stearyl alcohol, peregal O, OP.
In some embodiments of the invention, the aqueous phase emulsifier of the cream comprises at least one of tween 20, tween 21, tween 40), tween 60, tween 61), tween 80, tween 81, tween 85.
In some embodiments of the invention, the humectant of the cream comprises at least one of glycerol, butylene glycol, polyethylene glycol), propylene glycol, hexylene glycol, xylitol, polypropylene glycol, sorbitol.
In some embodiments of the invention, the preservative of the cream comprises at least one of dibutyl hydroxy toluene, 1, 2-pentanediol, 1, 2-hexanediol, phenethyl alcohol, phenoxyethanol, p-hydroxyacetophenone, ethylhexyl glycerol, glycerol decanoate, sorbitan octanoate, glycerol undecylenate, methyl parahydroxybenzoate, ethyl parahydroxybenzoate (ethylparaben), propyl parahydroxybenzoate, butyl parahydroxybenzoate, levulinic acid, anisic acid, octanoyl hydroxamic acid.
In some embodiments of the invention, the ionic complexing agent of the cream comprises at least one of disodium Edentate (EDTA), citric acid, tartaric acid, polyphosphates, aminocarboxylic acids, 1, 3-diketones, hydroxycarboxylic acids, polyamines.
In a second aspect of the present invention, there is provided a method for preparing a compound external preparation, comprising the steps of:
Quantitatively weighing metformin hydrochloride and an H1 antihistamine drug, and adding deionized water, a solubilizer, an ion complexing agent and a preservative to dissolve and clarify the materials to obtain a drug solution; weighing thickener and ointment matrix, and heating to 70-80deg.C for dissolving; pouring the medicinal solution into the mixture of thickener and ointment matrix, stirring thoroughly, and standing at room temperature to obtain ointment; or (b)
1) Preparing an oil phase: weighing oleaginous matrix, consistency regulator and oil phase emulsifier, heating and stirring in water bath, controlling temperature at 75-80deg.C, and dissolving oil phase sufficiently;
2) Preparing an aqueous phase: weighing water phase emulsifier, humectant, preservative, ion complexing agent, adding proper amount of deionized water, heating and stirring in water bath, controlling temperature at 75-80deg.C, and dissolving water phase sufficiently for use;
3) Emulsification: slowly injecting the water phase into the oil phase, heating in 75-80deg.C water bath, stirring for about 30 min for emulsification, adding water solution of metformin hydrochloride and H1 antihistamine, stirring, and slowly cooling to room temperature to obtain cream.
In a third aspect of the invention, an application of a compound external preparation in preparing a medicament for treating skin diseases is provided.
In some embodiments of the invention, the skin disorder is selected from eczema, atopic dermatitis, psoriasis, and neurodermatitis.
The beneficial effects of the invention are as follows:
1. The invention discovers that the external preparation prepared by combining the metformin hydrochloride and the H1 antihistamine has good treatment effect on eczema, neurodermatitis, atopic dermatitis and psoriasis for the first time, enriches the treatment methods of the atopic dermatitis and the psoriasis, has high safety, no skin irritation and wide raw material sources, and can be widely popularized and applied.
2. According to the invention, the administration route of the clinical oral drug metformin hydrochloride and the H1 antihistamine is changed, so that the oral drug is directly externally applied to a skin focus without going through systemic circulation, thereby avoiding adverse drug reaction and having high safety, and the external application of the compound metformin hydrochloride and the H1 antihistamine shows good skin disease treatment effect.
3. In order to achieve the therapeutic effect in the application, the medicine must be a compound formed by combining metformin hydrochloride and an H1 antihistamine medicine; external preparations of metformin hydrochloride or H1 antihistamine drug alone have significantly reduced therapeutic effects on eczema, atopic dermatitis, psoriasis and neurodermatitis.
Drawings
FIG. 1 is a therapeutic effect of an ointment formulation prepared according to prescription 4 of example 1 on leg eczema; wherein A is before treatment and B is after treatment.
FIG. 2 is a therapeutic effect of the ointment formulation prepared according to prescription 4 of example 1 on leg psoriasis; wherein A is before treatment and B is after treatment.
FIG. 3 is a therapeutic effect of the ointment formulation prepared according to prescription 4 of example 1 on head psoriasis; wherein A is before treatment and B is after treatment.
FIG. 4 shows the therapeutic effect of the ointment preparation prepared according to prescription 4 of example 1 on neurodermatitis of the neck; wherein A is before treatment and B is after treatment.
Fig. 5 shows the therapeutic effect of the ointment preparation prepared according to prescription 4 of example 1 on neurodermatitis of the hand; wherein A is before treatment and B is after treatment.
Detailed Description
The present invention will be described in further detail with reference to specific examples. The starting materials, reagents or apparatus used in the examples and comparative examples were either commercially available from conventional sources or may be obtained by prior art methods unless specifically indicated. Unless otherwise indicated, assays or testing methods are routine in the art.
Example 1: preparation of ointment containing chlorphenamine and metformin hydrochloride
Ointments were prepared according to the following formulas 1 to 9 in Table 1, each 100g of ointment containing the following ingredients in mass:
TABLE 1 ointment compositions containing chlorphenamine and metformin hydrochloride
The preparation method of the ointment comprises the following steps: weighing quantitative metformin hydrochloride and chlorphenamine in the table 1 in a container; adding deionized water, propylene glycol, disodium edentate and dibutyl hydroxy toluene to dissolve and clarify the mixture for later use; weighing glyceryl monostearate, white vaseline and paraffin, and heating to 70-80deg.C for dissolving; pouring the dissolved medicine into the ointment, fully and uniformly stirring the mixture, and standing the mixture at room temperature to obtain the ointment preparation.
Example 2: preparation of ointment containing desloratadine citrate and metformin hydrochloride
Ointments were prepared as described in formulas 1-9 of Table 2, each 100g of ointment containing the following ingredients by mass:
TABLE 2 ointment compositions containing desloratadine citrate and metformin hydrochloride
The preparation method of the ointment comprises the following steps: weighing quantitative metformin hydrochloride and desloratadine citrate in the table 2 into a container; adding deionized water and propylene glycol to dissolve and clarify the mixture for later use; weighing glyceryl monostearate, white vaseline, paraffin, disodium edentate and dibutyl hydroxy toluene, and heating to 70-80deg.C for dissolving; pouring the dissolved medicine into the ointment, fully and uniformly stirring the mixture, and standing the mixture at room temperature to obtain the ointment preparation.
Example 3: ointment preparation containing nitrogen Zhuo Siding hydrochloride and metformin hydrochloride
Ointments were prepared according to the following formulas 1 to 9 in Table 3, each 100g of ointment containing the following ingredients in mass:
TABLE 3 ointment ingredients containing N Zhuo Siding hydrochloride and metformin hydrochloride
The preparation method of the ointment comprises the following steps: weighing the quantitative metformin hydrochloride and nitrogen Zhuo Siding Yu Rongqi in the above table 3; adding deionized water and propylene glycol to dissolve and clarify the mixture for later use; weighing glyceryl monostearate, white vaseline, paraffin, disodium edentate and dibutyl hydroxy toluene, and heating to 70-80deg.C for dissolving; pouring the dissolved medicine into the ointment, fully and uniformly stirring the mixture, and standing the mixture at room temperature to obtain the ointment preparation.
Example 4: preparation of ointment containing flunarizine hydrochloride and metformin hydrochloride
Ointments were prepared according to the following formulas 1 to 9 in Table 4, each 100g of the ointment containing the following ingredients in mass:
TABLE 4 ointment compositions containing flunarizine hydrochloride and metformin hydrochloride
The preparation method of the ointment comprises the following steps: weighing quantitative metformin hydrochloride and flunarizine hydrochloride in the table 4 in a container; adding deionized water and propylene glycol to dissolve and clarify the mixture for later use; weighing glyceryl monostearate, white vaseline, paraffin, disodium edentate and dibutyl hydroxy toluene, and heating to 70-80deg.C for dissolving; pouring the dissolved medicine into the ointment, fully and uniformly stirring the mixture, and standing the mixture at room temperature to obtain the ointment preparation.
Example 5: preparation of cream containing chlorphenamine and metformin hydrochloride
The creams were prepared according to the following formulations 1-9 in Table 5, each 100g of cream containing the following ingredients in mass:
TABLE 5 cream compositions containing chlorphenamine and metformin hydrochloride
The preparation method comprises the following steps:
Oil phase part: cetyl alcohol, white vaseline, liquid paraffin and glyceryl monostearate are weighed into a container, heated and stirred in a water bath, and the temperature is controlled at 75-80 ℃ so that the oil phase is fully dissolved for standby.
Aqueous phase fraction: weighing Tween-80, propylene glycol, ethylparaben and EDTA, adding appropriate amount of deionized water, heating in water bath, stirring, controlling temperature at 75-80deg.C, and dissolving water phase completely.
Emulsification: slowly injecting the water phase into the oil phase, heating in 75-80deg.C water bath, stirring for about 30 min for emulsification, adding water solution of metformin hydrochloride and chlorphenamine prepared in the amount shown in Table 5, stirring, and slowly cooling to room temperature to obtain cream preparation.
Example 6: preparation of cream containing desloratadine citrate and metformin hydrochloride
The creams were prepared according to the following formulations 1-9 in Table 6, each 100g of cream containing the following ingredients in mass:
TABLE 6 cream compositions containing desloratadine citrate and metformin hydrochloride
The preparation method comprises the following steps:
Oil phase part: cetyl alcohol, white vaseline, liquid paraffin and glyceryl monostearate are weighed into a container, heated and stirred in a water bath, and the temperature is controlled at 75-80 ℃ so that the oil phase is fully dissolved for standby.
Aqueous phase fraction: weighing Tween-80, propylene glycol, ethylparaben and EDTA, adding appropriate amount of deionized water, heating in water bath, stirring, controlling temperature at 75-80deg.C, and dissolving water phase completely.
Emulsification: slowly injecting the water phase into the oil phase, heating and stirring in 75-80deg.C water bath for about 30min for emulsification, adding water solution of metformin hydrochloride and desloratadine citrate prepared in the amount shown in Table 6, stirring, and slowly cooling to room temperature to obtain cream preparation.
Example 7: preparation of cream containing nitrogen Zhuo Siding hydrochloride and metformin hydrochloride
The creams were prepared according to the following formulations 1-9 in Table 7, each 100g of cream containing the following ingredients in mass:
TABLE 7 cream ingredients containing nitrogen Zhuo Siding hydrochloride and metformin hydrochloride
The preparation method comprises the following steps:
Oil phase part: cetyl alcohol, white vaseline, liquid paraffin and glyceryl monostearate are weighed into a container, heated and stirred in a water bath, and the temperature is controlled at 75-80 ℃ so that the oil phase is fully dissolved for standby.
Aqueous phase fraction: weighing Tween-80, propylene glycol, ethylparaben and EDTA, adding appropriate amount of deionized water, heating in water bath, stirring, controlling temperature at 75-80deg.C, and dissolving water phase completely.
Emulsification: slowly injecting the water phase into the oil phase, heating and stirring in 75-80deg.C water bath for about 30min for emulsification, adding water solution of metformin hydrochloride and nitrogen Zhuo Siding in the amount shown in Table 7, stirring, and slowly cooling to room temperature to obtain cream preparation.
Example 8: preparation of a cream containing flunarizine hydrochloride and metformin hydrochloride (cream 1)
The creams were prepared according to the following formulations 1-9 in Table 8, each 100g of cream containing the following ingredients by mass:
Table 8. Cream ingredients containing flunarizine hydrochloride and metformin hydrochloride (cream 1)
The preparation method comprises the following steps:
Oil phase part: cetyl alcohol, white vaseline, liquid paraffin and glyceryl monostearate are weighed into a container, heated and stirred in a water bath, and the temperature is controlled at 75-80 ℃ so that the oil phase is fully dissolved for standby.
Aqueous phase fraction: weighing Tween-80, propylene glycol, ethylparaben and EDTA, adding appropriate amount of deionized water, heating in water bath, stirring, controlling temperature at 75-80deg.C, and dissolving water phase completely.
Emulsification: slowly injecting the water phase into the oil phase, heating and stirring in 75-80deg.C water bath for about 30min for emulsification, adding the water solution of metformin hydrochloride and flunarizine hydrochloride prepared in the amount shown in Table 8, stirring, and slowly cooling to room temperature to obtain cream preparation.
Example 9: preparation of a cream containing flunarizine hydrochloride and metformin hydrochloride (cream 2)
The creams were prepared according to the following formulations 1-9 in Table 9, each 100g of cream containing the following ingredients in mass:
TABLE 9 cream ingredients containing flunarizine hydrochloride and metformin hydrochloride (cream 2)
Oil phase part: weighing white vaseline, CRODAFOS CES, liquid paraffin and squalane, heating in water bath, stirring, and controlling temperature at 75-80deg.C to dissolve oil phase sufficiently.
Aqueous phase fraction: weighing Tween-80, propylene glycol, ethylparaben and EDTA, adding appropriate amount of deionized water, heating in water bath, stirring, controlling temperature at 75-80deg.C, and dissolving water phase completely.
Emulsification: slowly injecting the water phase into the oil phase, heating in 75-80deg.C water bath, stirring for about 30min for emulsification, adding water solution of metformin hydrochloride and flunarizine hydrochloride prepared in the amount shown in Table 9, stirring, and slowly cooling to room temperature to obtain cream preparation
Example 10: therapeutic effects on atopic dermatitis and psoriasis
The preparations prepared in the corresponding manner to each prescription in the above examples were applied to 10 patients with atopic dermatitis and psoriasis, respectively, and the treatment with the ointment was performed twice daily for 8 weeks, and changes in the affected area were observed.
Among them, taking prescription 4 in example 1 as an example, the effect display shows that the lesion lesions of 10 patients are cleared or controlled, and no adverse reaction or irritation reaction caused by the drug is found. Atopic dermatitis patients were controlled for skin itching in 2 weeks, and the therapeutic effects are shown in fig. 1-5. The effect of each prescription in the other embodiments is similar to the effect of the prescription 4 in the embodiment 1, and the treatment effect is achieved.
The embodiments described above are more preferred embodiments of the present invention, but the embodiments of the present invention are not limited to the embodiments described above, and any other changes, modifications, substitutions, combinations, and simplifications that do not depart from the spirit and principles of the present invention should be made in the equivalent manner, and are included in the scope of the present invention.
Claims (10)
1. A compound external preparation is characterized by comprising metformin hydrochloride and an H1 antihistamine drug.
2. The compound external preparation according to claim 1, wherein the H1 antihistamine comprises chloromastine fumarate, terfenadine, astemizole, diphenhydramine hydrochloride, diphenhydramine, loratadine, desloratadine, doxepin hydrochloride, promethazine hydrochloride, perphenazine, chlorphenamine, fexofenadine hydrochloride, cetirizine hydrochloride, levocetirizine, pralaminomaleate, hydroxyzine hydrochloride, meclozine hydrochloride, mirtapine, ebastine hydrochloride, azelastine hydrochloride, rupatadine fumarate, clopenthizothioton hydrochloride, clemastine hydrochloride, clemizole, pemetrexed potassium, asenapine, mefenamide hydrochloride, bepotastine, mequitazine, thioethyl dimaleate, carbocistin, dihydroxynaphthazine, bromelain maleate, epinastine, thiomerone, epinastine hydrochloride, nipradine hydrochloride, pyrilamine hydrochloride, bispyrine, mizolastine dihydrochloride, alcaftadine, bilastine, epinastine, fenspirits hydrochloride, chlorocirizine hydrochloride, triprolidine hydrochloride, rupatadine, decclodrozine, betosetin besylate, hydroxyzine, decclodrozine hydrochloride, chloro Ma Siding, mehai Qu Linnai disulfonate, benazine hydrochloride, qu Bi na-sensitive citrate, clopyraramide, triprolidine hydrochloride, pyrrole imidazole, fenspiride, chlorocirizine, fexofenadine, azelastine, rocarubide, cinnarizine, flunarizine hydrochloride, and terfenadine.
3. The compound external preparation according to claim 1, wherein the mass percentage of the metformin hydrochloride in the compound external preparation is 0.5-20%; the weight percentage of the H1 antihistamine drug in the compound external preparation is 0.5-10%.
4. A compound external preparation according to any one of claims 1-3, wherein the dosage form of the compound external preparation comprises an ointment, a cream, a gel, an external solution, a cement, a plaster, a tincture, a lotion, a coating, a powder, a lyophilized powder, an aerosol and a foam.
5. The compound external preparation according to claim 4, further comprising an adjuvant comprising an ointment base, a solubilizer, a thickener, an ion complexing agent, a preservative, a consistency regulator, a oleaginous base, an oil-phase emulsifier, an aqueous-phase emulsifier, a humectant, a preservative, an ion complexing agent, and a softener.
6. The compound external preparation according to claim 4, wherein the compound external preparation is an ointment, and the ointment comprises the following components in percentage by mass: 50% -80% of ointment matrix, 10% -20% of solubilizer, 2% -8% of thickener, 0.1% -0.5% of ion complexing agent, 0.5% -20% of metformin hydrochloride and 0.5% -10% of H1 antihistamine drug; preferably, the ointment further comprises 0.1% -0.5% of a preservative.
7. The compound external preparation according to claim 4, wherein the compound external preparation is a cream, and the cream comprises the following components in percentage by mass: 0.5 to 20 percent of metformin hydrochloride, 0.5 to 10 percent of H1 antihistamine drug, 5 to 15 percent of consistency regulator, 5 to 12 percent of oleaginous matrix, 5 to 15 percent of oil phase emulsifier, 2 to 5 percent of water phase emulsifier, 5 to 15 percent of humectant and 0.1 to 0.5 percent of ion complexing agent; preferably, the cream further comprises 0.1% -0.5% of a preservative; more preferably, the cream further comprises 0.5% -5% of a softening agent.
8. The method for preparing the compound external preparation according to claim 6 or 7, characterized by comprising the steps of:
Quantitatively weighing metformin hydrochloride and an H1 antihistamine drug, and adding deionized water, a solubilizer, an ion complexing agent and a preservative to dissolve and clarify the materials to obtain a drug solution; weighing thickener and ointment matrix, and heating to 70-80deg.C for dissolving; pouring the medicinal solution into the mixture of thickener and ointment matrix, stirring thoroughly, and standing at room temperature to obtain ointment; or (b)
1) Preparing an oil phase: weighing oleaginous matrix, consistency regulator and oil phase emulsifier, heating and stirring in water bath, controlling temperature at 75-80deg.C, and dissolving oil phase sufficiently;
2) Preparing an aqueous phase: weighing water phase emulsifier, humectant, preservative, ion complexing agent, adding proper amount of deionized water, heating and stirring in water bath, controlling temperature at 75-80deg.C, and dissolving water phase sufficiently for use;
3) Emulsification: slowly injecting the water phase into the oil phase, heating in 75-80deg.C water bath, stirring for about 30 min for emulsification, adding water solution of metformin hydrochloride and H1 antihistamine, stirring, and slowly cooling to room temperature to obtain cream.
9. Use of a compound external preparation according to claims 1-7 for the preparation of a medicament for the treatment of skin disorders.
10. Use according to claim 9, characterized in that the skin disease is selected from eczema, atopic dermatitis, psoriasis and neurodermatitis.
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