CN109394768A - A kind of drug and preparation method thereof for treating eczema - Google Patents

A kind of drug and preparation method thereof for treating eczema Download PDF

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Publication number
CN109394768A
CN109394768A CN201811505153.6A CN201811505153A CN109394768A CN 109394768 A CN109394768 A CN 109394768A CN 201811505153 A CN201811505153 A CN 201811505153A CN 109394768 A CN109394768 A CN 109394768A
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compound
glycerol
drug
carbomer
gel
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CN109394768B (en
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刘晶莹
赵丹
刘洋
武晓萌
教传华
董文杰
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Mudanjiang Medical University
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Mudanjiang Medical University
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/351Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom not condensed with another ring
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders

Abstract

The present invention relates to a kind of drugs and preparation method thereof for treating eczema.Specifically, the drug is with 1- phenyl-8- (7H- simultaneously [2,3-d] pyrimidine-4-yl)-1,3, tri- aza-spiro of 8- [4.5]-decyl- 4- ketone, 3- [3- methyl-1-(1H- pyrrolo- [2,3-b] pyridin-4-yl)-1H- pyrazoles-4- base]-cyclohexanol and deoxyarbutin three are as active pharmaceutical ingredient, and wherein the weight proportion between three of the above active pharmaceutical ingredient is 5~10:2~6:0.5~2.The drug is particularly effective in the treatment of eczema.

Description

A kind of drug and preparation method thereof for treating eczema
Technical field
The present invention relates to pharmaceutical technology fields, and in particular to a kind of drug and preparation method thereof for treating eczema.
Background technique
Eczema (eczema) is a series of a kind of clinically common anaphylaxis dermatosis characterized by fash, clinical table Now based on red and swollen, dry and itch, and can with get blister, chap, oozing of blood, incrustation, the symptoms such as peeling.Eczema is often repeatedly Breaking-out, does not recover for a long time, and brings greatly puzzlement and inconvenience to the daily life of patient.
The pathogenesis of eczema is more complicated, and is not yet completely understood so far.Generally, it is considered that eczema and inherent cause, interior Secretion factor, blood circulation factor, environmental factor, dietary factor, infective agent, drug factors are all relevant.Currently, eczema Treatment means include using antiallergic such as antihistaminic, glucocorticoids preparation, antibiotic formulations etc..The cause of disease still not Under the premise of specific, clinical application often can only symptomatic treatment, be but limited to limited effect and biggish side effect and cannot It is enough satisfactory.
Inventor has found that the prior art disclosed in the drug therapy field of eczema is mainly with Chinese medicine at present by retrieval Based on composition.For example, Chinese patent application 201510798118.8 discloses a kind of composition for treating eczema, mainly by ground Skin 8g, frutus cnidii 12g, maple leaf 6g, Golden Larch Bark 9g, yellow lead 6g, half 8g of summer, agalloch eaglewood 13g and tuber of stemona 5g are formulated.It is said that should The composition of invention has the effect of clearing heat and detoxicating, convergence running sore, has unique curative effect and non-relapse after healing to eczema.
Furthermore Chinese patent application 201410280550.3 discloses the drug that eczema is controlled outside one kind, by following Chinese medicine Composition composition: 55~65 grams of raw hawthorn, 45~50 grams of raw rhubarb, 35~45 grams of big maple, 25~30 grams of frutus cnidii, the fruit of summer cypress 25 ~35 grams, 50~65 grams of kuh-seng, 15~25 grams of cicada slough, 55~60 grams of alum, also disclose the production for furthermore controlling the drug of eczema Method.It is said that the medicine effect of the invention is good, short treating period.
In addition, Chinese patent application 201810756589.6 discloses a kind of drug for treating eczema, it is by following heavy The component of amount part is made: 6~8 parts of Bunge Corydalis Herb, 16~18 parts of field pennycress, 6~8 parts of Fructus Forsythiae, 5~7 parts of tuber fleeceflower stem, cimicifugae foetidae 22~24 Part, 12~14 parts of calamine, 3~5 parts of shrub althea flower, 2~4 parts of Chinese prickly ash, 3~5 parts of radix scutellariae, 8~10 parts of lotus leaf, 3~5 parts of the root of Dahurain angelica, 5~7 parts of acalypha copperleaf, 5~7 parts of Radix zanthoxyli, 8~10 parts of Caulis Spatholobi.It is said that the invention has treatment eczema by all medicines share Fabulous curative effect.
The raw material type of these Chinese medicine compositions is various, quality is not easy to control and preparation process is complicated, limits it and is facing Purposes in bed.Therefore, there is the unsatisfied demand to the drug with efficient eczema treatment effect in this field.
Summary of the invention
The technical problem to be solved by the present invention is to overcome the deficiencies of the prior art and provide a kind of medicine of effectively treatment eczema Object and preparation method thereof.
The drug for the treatment of eczema of the invention is with 1- phenyl -8- (7H- pyrrolo- [2,3-d] pyrimidine-4-yl) -1,3,8- three Aza-spiro [4.5]-decyl- 4- ketone, 3- [3- methyl-1-(1H- pyrrolo- [2,3-b] pyridin-4-yl)-1H- pyrazoles-4- base]-ring Hexanol and deoxyarbutin three are as active pharmaceutical ingredient, the wherein weight proportion between three of the above active pharmaceutical ingredient 5~10:2~6:0.5~2.The drug is particularly effective in the treatment of eczema.
Specifically, the present invention provides a kind of drug for treating eczema, the drug includes:
1) three aza-spiro [4.5] of 1- phenyl -8- (7H- pyrrolo- [2,3-d] pyrimidine-4-yl) -1,3,8--decyl- 4- ketone (hereinafter referred to as compound A);
2) 3- [3- methyl-1-(1H- pyrrolo- [2,3-b] pyridin-4-yl)-1H- pyrazoles-4- base]-cyclohexanol (following letter Claim compound B);
3) deoxyarbutin (hereinafter referred to as compound C);With
4) pharmaceutically acceptable carrier, wherein the weight proportion between compound A, B and C be 5~10:2~6:0.5~ 2。
In one embodiment, the weight proportion between compound A, B and C is 7~9:3~5:1~2.
In one embodiment, the weight proportion between compound A, B and C is 8:4:1.5.
In one embodiment, the drug is topical formulations.
In one embodiment, the topical formulations are ointment, cream, gelling agent, paste or film.
In one embodiment, the topical formulations are gelling agents, and the pharmaceutically acceptable carrier is by card Wave nurse, polyvinylpyrrolidone, sodium alginate, sodium ethylene diamine tetracetate, benzalkonium chloride, glycerol and water composition, wherein carbomer, Weight proportion between polyvinylpyrrolidone and sodium alginate is 10~30:10~20:5~15.
In one embodiment, the weight proportion between carbomer, polyvinylpyrrolidone and sodium alginate be 15~ 25:12~18:7~12.
In one embodiment, the weight proportion between carbomer, polyvinylpyrrolidone and sodium alginate is 20: 15:9。
The present invention also provides the preparation methods of the drug, and described method includes following steps: 1) by compound A, B and C It is uniformly mixed, wherein the weight proportion between compound A, B and C is 5~10:2~6:0.5~2;2) step 1) is obtained mixed It closes object and is prepared into any pharmaceutically acceptable preparation.
In one embodiment, described method includes following steps: 1) being uniformly mixed compound A, B and C, wherein changing The weight proportion closed between object A, B and C is 5~10:2~6:0.5~2;2) mixture for obtaining step 1) is with by accounting for glycerol The mixing medium of 10~30% water composition of 10~30% glycerol and Zhan Shui total weight of total weight is finely ground, disperses;3) By carbomer, polyvinylpyrrolidone, sodium alginate, sodium ethylene diamine tetracetate, benzalkonium chloride, the glycerol of surplus and surplus Water heating stirring obtain gel-type vehicle;4) mixture for obtaining step 2) is added in the gel-type vehicle that step 3) obtains, It stirs and evenly mixs to obtain gel.
In one embodiment, the present invention provides a kind of drug for treating eczema, and the drug includes: 1) compound A; 2) compound B;3) compound C;With 4) pharmaceutically acceptable carrier, wherein the weight proportion between compound A, B and C is 5 ~10:2~6:0.5~2, wherein the drug is gelling agent, the pharmaceutically acceptable carrier is by carbomer, polyethylene pyrrole Pyrrolidone, sodium alginate, sodium ethylene diamine tetracetate, benzalkonium chloride, glycerol and water form, wherein carbomer, polyvinylpyrrolidine Weight proportion between ketone and sodium alginate is 10~30:10~20:5~15, and the drug is by including the following steps Method is made: 1) compound A, B and C is uniformly mixed, wherein the weight proportion between compound A, B and C is 5~10:2~6: 0.5~2;2) by mixture that step 1) obtains with by the 10 of 10~30% glycerol and Zhan Shui total weight that account for glycerol total weight The mixing medium of~30% water composition is finely ground, disperses;3) by carbomer, polyvinylpyrrolidone, sodium alginate, ethylenediamine Tetraacethyl sodium, benzalkonium chloride, the glycerol of surplus and surplus water heating stirring obtain gel-type vehicle;4) step 2) is obtained Mixture be added in the gel-type vehicle that step 3) obtains, stir and evenly mix to obtain gel.
Compound A is previously described in patent document CN1305479A, and can be according to 9 reference of embodiment of the patent document Similar to the method preparation of embodiment 1.It is believed that the compound can be used as immunosuppressor for treating rheumatoid arthritis, wolf The diseases such as sore, multiple sclerosis.
Compound B can be prepared according to the embodiment 25 of patent document CN103214484A.It is believed that the compound can be used as and exempt from Epidemic disease inhibitor is for treating the diseases such as autoimmune disease, cancer, inflammatory disease.
Compound C, that is, deoxyarbutin is a kind of competitive tyrosinase inhibitor, can adjust the generation of melanin, gram Pigmentation is taken, skin black splotch is desalinated, there is rapid and lasting skin-whitening effect.
Inventor is it was unexpectedly observed that match existing compound A, B and C in the treatment of eczema with specified weight in the drug It can produce unexpected excellent effect in the process.Particularly, inventors have found that working as compound A, B and C with 5~10:2 It is right with compound A, B and C and the positive of exclusive use when treatment eczema is applied in combination in the specific weight proportion of~6:0.5~2 It is compared according to momestasone furoate, there is significant better therapeutic effect.This illustrates the change of the invention using specific weight proportion Close object A, B and C and as the drug of active constituent be capable of providing significant eczema treatment effect, so can satisfy it is right in this field The demand of drug with efficient eczema treatment effect.
In order to be further understood essence and spirit of the invention, combined with specific embodiments below to of the invention excellent Embodiment and its effect is selected to be described.It is understood, however, that these descriptions are only intended to further illustrate spy of the invention It seeks peace advantage, and any restrictions is constituted to claim of the invention absolutely not.
Specific embodiment
The source of all raw materials used in the preparation of described pharmaceutical composition is not particularly limited in the present invention, in city It is being bought on field or according to conventional method well known to those skilled in the art preparation.
Prepare embodiment 1
The each component of the drug for the treatment of eczema and its dosage are as shown in following table described in the present embodiment:
Preparation method are as follows: 1) be uniformly mixed compound A, B and C;2) by mixture that step 1) obtains with sweet by accounting for The mixing medium of the 20% water composition of 20% glycerol and Zhan Shui total weight of oily total weight is finely ground, disperses;3) by card wave Nurse, polyvinylpyrrolidone, sodium alginate, sodium ethylene diamine tetracetate, benzalkonium chloride, the glycerol of surplus and surplus water add Thermal agitation obtains gel-type vehicle;4) mixture for obtaining step 2) is added in the gel-type vehicle that step 3) obtains, and stirring is mixed It is even to obtain gel.
Prepare embodiment 2
The each component of the drug for the treatment of eczema and its dosage are as shown in following table described in the present embodiment:
Component Dosage
Compound A 8g
Compound B 4g
Compound C 1.5g
Carbomer 20g
Polyvinylpyrrolidone 15g
Sodium alginate 9g
Sodium ethylene diamine tetracetate 1g
Benzalkonium chloride 1g
Glycerol 100g
Water 1000g
Preparation method are as follows: 1) be uniformly mixed compound A, B and C;2) by mixture that step 1) obtains with sweet by accounting for The mixing medium of the 20% water composition of 20% glycerol and Zhan Shui total weight of oily total weight is finely ground, disperses;3) by card wave Nurse, polyvinylpyrrolidone, sodium alginate, sodium ethylene diamine tetracetate, benzalkonium chloride, the glycerol of surplus and surplus water add Thermal agitation obtains gel-type vehicle;4) mixture for obtaining step 2) is added in the gel-type vehicle that step 3) obtains, and stirring is mixed It is even to obtain gel.
Prepare embodiment 3
The each component of the drug for the treatment of eczema and its dosage are as shown in following table described in the present embodiment:
Component Dosage
Compound A 10g
Compound B 6g
Compound C 2g
Carbomer 20g
Polyvinylpyrrolidone 15g
Sodium alginate 9g
Sodium ethylene diamine tetracetate 1g
Benzalkonium chloride 1g
Glycerol 100g
Water 1000g
Preparation method are as follows: 1) be uniformly mixed compound A, B and C;2) by mixture that step 1) obtains with sweet by accounting for The mixing medium of the 20% water composition of 20% glycerol and Zhan Shui total weight of oily total weight is finely ground, disperses;3) by card wave Nurse, polyvinylpyrrolidone, sodium alginate, sodium ethylene diamine tetracetate, benzalkonium chloride, the glycerol of surplus and surplus water add Thermal agitation obtains gel-type vehicle;4) mixture for obtaining step 2) is added in the gel-type vehicle that step 3) obtains, and stirring is mixed It is even to obtain gel.
Comparative example 1
The each component of the drug for the treatment of eczema and its dosage are as shown in following table described in the present embodiment:
Preparation method are as follows: 1) weigh the momestasone furoate of formula ratio;2) by momestasone furoate with by accounting for glycerol total weight 20% glycerol and Zhan Shui total weight 20% water composition mixing medium it is finely ground, dispersion;3) by carbomer, polyethylene Pyrrolidones, sodium alginate, sodium ethylene diamine tetracetate, benzalkonium chloride, the glycerol of surplus and surplus water heating stirring obtain To gel-type vehicle;4) mixture for obtaining step 2) is added in the gel-type vehicle that step 3) obtains, and is stirred and evenly mixed and is coagulated Glue.
Comparative example 2
The each component of the drug for the treatment of eczema and its dosage are as shown in following table described in the present embodiment:
Preparation method are as follows: 1) weigh the compound A of formula ratio;2) by 20% of compound A by accounting for glycerol total weight Glycerol and Zhan Shui total weight 20% water composition mixing medium it is finely ground, dispersion;3) by carbomer, polyvinylpyrrolidine Ketone, sodium alginate, sodium ethylene diamine tetracetate, benzalkonium chloride, the glycerol of surplus and surplus water heating stirring obtain gel Matrix;4) mixture for obtaining step 2) is added in the gel-type vehicle that step 3) obtains, and stirs and evenly mixs to obtain gel.
Comparative example 3
The each component of the drug for the treatment of eczema and its dosage are as shown in following table described in the present embodiment:
Component Dosage
Compound B 8g
Carbomer 20g
Polyvinylpyrrolidone 15g
Sodium alginate 9g
Sodium ethylene diamine tetracetate 1g
Benzalkonium chloride 1g
Glycerol 100g
Water 1000g
Preparation method are as follows: 1) weigh the compound B of formula ratio;2) by 20% of compound B by accounting for glycerol total weight Glycerol and Zhan Shui total weight 20% water composition mixing medium it is finely ground, dispersion;3) by carbomer, polyvinylpyrrolidine Ketone, sodium alginate, sodium ethylene diamine tetracetate, benzalkonium chloride, the glycerol of surplus and surplus water heating stirring obtain gel Matrix;4) mixture for obtaining step 2) is added in the gel-type vehicle that step 3) obtains, and stirs and evenly mixs to obtain gel.
Comparative example 4
The each component of the drug for the treatment of eczema and its dosage are as shown in following table described in the present embodiment:
Component Dosage
Compound C 8g
Carbomer 20g
Polyvinylpyrrolidone 15g
Sodium alginate 9g
Sodium ethylene diamine tetracetate 1g
Benzalkonium chloride 1g
Glycerol 100g
Water 1000g
Preparation method are as follows: 1) weigh the compound C of formula ratio;2) by 20% of compound C by accounting for glycerol total weight Glycerol and Zhan Shui total weight 20% water composition mixing medium it is finely ground, dispersion;3) by carbomer, polyvinylpyrrolidine Ketone, sodium alginate, sodium ethylene diamine tetracetate, benzalkonium chloride, the glycerol of surplus and surplus water heating stirring obtain gel Matrix;4) mixture for obtaining step 2) is added in the gel-type vehicle that step 3) obtains, and stirs and evenly mixs to obtain gel.
Investigation of the experimental example drug of the invention to the therapeutic effect of eczema
The purpose of this experimental example is to investigate the drug according to made from preparation embodiment 1-3 to the therapeutic effect of eczema.
1, respondent
The volunteer that eczema is clinically diagnosed as to 175 is raised in this experiment altogether, wherein male volunteer 86, female volunteer 89, the age is between 23~47 years old.By all volunteer's mean allocations to 7 groups, every group of 25 volunteers.Through specialized medical Human assessment, each group of volunteer are comparable between the course of disease and severity of eczema.
2, experimental drug
The drug being prepared according to preparation embodiment 1-3 and comparative example 1-4.
3, experimental method
Said medicine is applied to affected area once a day to forming thin layer, dosage be equivalent to about 0.05g gel/ cm2Skin area, administration continue 12 weeks altogether.
4, standards of grading
It please model of volunteer after experimental period for the drug in terms of the therapeutic effect of eczema at 0~5 point Interior marking is enclosed, standards of grading are as follows:
Then, the score value of each embodiment is summarized, divided by the total number of persons of volunteer, obtains being averaged for its scoring Value.
5, experimental result
Group Scoring
Prepare embodiment 1 4.47±0.15
Prepare embodiment 2 4.82±0.06
Prepare embodiment 3 4.69±0.10
Comparative example 1 3.36±0.24
Comparative example 2 2.97±0.21
Comparative example 3 2.69±0.18
Comparative example 4 1.25±0.17
(as a result n=25 is expressed as means standard deviation)
By the result of upper table it is found that for compound A, B and C, no matter it is single use or is applied in combination, for Eczema all has certain therapeutic effect.But when used alone, three kinds of compounds extremely have the therapeutic effect of eczema Limit, especially compound C (comparative example 4: scoring 1.25 ± 0.17).Inventor it was unexpectedly observed that when by compound A, B and When treatment eczema is applied in combination with the specific weight proportion in 5~10:2~6:0.5~2 in C, compound A, B with exclusive use It is compared with C and positive control momestasone furoate, there is significant better therapeutic effect, almost the journey of " complete incidence graph " Degree.It is aobvious that this illustrates that compound A, B and C of the invention using specific weight proportion is capable of providing as the drug of active constituent The eczema treatment effect of work, and then can satisfy the demand in this field to the drug with efficient eczema treatment effect.
The above is only a preferred embodiment of the present invention.It should be pointed out that for the ordinary skill people of the art For member, under the premise of not departing from spirit and principles of the present invention, several improvement, modification and equivalent replacement can also be made Deng, these improve, modification and equivalent replacement after technical solution also should be regarded as falling within the scope and spirit of the invention.

Claims (10)

1. a kind of drug for treating eczema, the drug includes:
1) three aza-spiro [4.5] of compound A:1- phenyl -8- (7H- pyrrolo- [2,3-d] pyrimidine-4-yl) -1,3,8--decyl- 4- Ketone;
2) compound B:3- [3- methyl-1-(1H- pyrrolo- [2,3-b] pyridin-4-yl)-1H- pyrazoles-4- base]-cyclohexanol;
3) compound C: deoxyarbutin;With
4) pharmaceutically acceptable carrier, wherein the weight proportion between compound A, B and C is 5~10:2~6:0.5~2.
2. drug according to claim 1, wherein the drug is topical formulations, wherein the topical formulations are ointment Agent, cream, gelling agent, paste or film.
3. drug according to claim 2, wherein the topical formulations are gelling agents, and described pharmaceutically acceptable Carrier is made of carbomer, polyvinylpyrrolidone, sodium alginate, sodium ethylene diamine tetracetate, benzalkonium chloride, glycerol and water, Weight proportion between middle carbomer, polyvinylpyrrolidone and sodium alginate is 10~30:10~20:5~15.
4. drug according to claim 3, wherein the weight between carbomer, polyvinylpyrrolidone and sodium alginate is matched Than being 15~25:12~18:7~12.
5. the preparation method of drug according to claim 1, described method includes following steps: 1) by compound A, B and C It is uniformly mixed, wherein the weight proportion between compound A, B and C is 5~10:2~6:0.5~2;2) step 1) is obtained mixed It closes object and is prepared into any pharmaceutically acceptable preparation.
6. the preparation method of drug according to claim 3, described method includes following steps: 1) by compound A, B and C It is uniformly mixed, wherein the weight proportion between compound A, B and C is 5~10:2~6:0.5~2;2) step 1) is obtained mixed Close the mixing medium that object is formed with 10~30% water by 10~30% glycerol and Zhan Shui total weight that account for glycerol total weight Object is finely ground, disperses;3) by carbomer, polyvinylpyrrolidone, sodium alginate, sodium ethylene diamine tetracetate, benzalkonium chloride, surplus Glycerol and the water heating stirring of surplus obtain gel-type vehicle;4) mixture for obtaining step 2) is added to step 3) and obtains Gel-type vehicle in, stir and evenly mix to obtain gel.
7. a kind of drug for treating eczema, the drug includes: 1) (7H- pyrrolo- [2,3-d] is phonetic by compound A:1- phenyl -8- Pyridine -4- base) three aza-spiro [4.5] of -1,3,8--decyl- 4- ketone;
2) compound B:3- [3- methyl-1-(1H- pyrrolo- [2,3-b] pyridin-4-yl)-1H- pyrazoles-4- base]-cyclohexanol;
3) compound C: deoxyarbutin;With
4) pharmaceutically acceptable carrier, wherein the weight proportion between compound A, B and C is 5~10:2~6:0.5~2, Described in drug be gelling agent, the pharmaceutically acceptable carrier is by carbomer, polyvinylpyrrolidone, sodium alginate, second Sodium ethylene diamine tetracetate, benzalkonium chloride, glycerol and water composition, wherein between carbomer, polyvinylpyrrolidone and sodium alginate Weight proportion is 10~30:10~20:5~15, and the drug is made of the method including the following steps: 1) by compound A, B and C is uniformly mixed, and wherein the weight proportion between compound A, B and C is 5~10:2~6:0.5~2;2) step 1) is obtained To mixture formed with 10~30% water by 10~30% glycerol and Zhan Shui total weight that account for glycerol total weight it is mixed Conjunction medium is finely ground, disperses;3) by carbomer, polyvinylpyrrolidone, sodium alginate, sodium ethylene diamine tetracetate, benzalkonium chloride, The glycerol of surplus and the water heating stirring of surplus obtain gel-type vehicle;4) mixture for obtaining step 2) is added to step 3) it in the gel-type vehicle obtained, stirs and evenly mixs to obtain gel.
8. the drug for the treatment of eczema according to claim 7, each component and its dosage are as shown in following table:
Component Dosage Compound A 5g Compound B 2g Compound C 0.5g Carbomer 20g Polyvinylpyrrolidone 15g Sodium alginate 9g Sodium ethylene diamine tetracetate 1g Benzalkonium chloride 1g Glycerol 100g Water 1000g
Preparation method are as follows: 1) be uniformly mixed compound A, B and C;2) by mixture that step 1) obtains with total by accounting for glycerol The mixing medium of the 20% water composition of 20% glycerol and Zhan Shui total weight of weight is finely ground, disperses;3) by carbomer, poly- The water heating of vinylpyrrolidone, sodium alginate, sodium ethylene diamine tetracetate, benzalkonium chloride, the glycerol of surplus and surplus is stirred It mixes to obtain gel-type vehicle;4) mixture for obtaining step 2) is added in the gel-type vehicle that step 3) obtains, and is stirred and evenly mixed To gel.
9. the drug for the treatment of eczema according to claim 7, each component and its dosage are as shown in following table:
Component Dosage Compound A 8g Compound B 4g Compound C 1.5g Carbomer 20g Polyvinylpyrrolidone 15g Sodium alginate 9g Sodium ethylene diamine tetracetate 1g Benzalkonium chloride 1g Glycerol 100g Water 1000g
Preparation method are as follows: 1) be uniformly mixed compound A, B and C;2) by mixture that step 1) obtains with total by accounting for glycerol The mixing medium of the 20% water composition of 20% glycerol and Zhan Shui total weight of weight is finely ground, disperses;3) by carbomer, poly- The water heating of vinylpyrrolidone, sodium alginate, sodium ethylene diamine tetracetate, benzalkonium chloride, the glycerol of surplus and surplus is stirred It mixes to obtain gel-type vehicle;4) mixture for obtaining step 2) is added in the gel-type vehicle that step 3) obtains, and is stirred and evenly mixed To gel.
10. the drug for the treatment of eczema according to claim 7, each component and its dosage are as shown in following table:
Preparation method are as follows: 1) be uniformly mixed compound A, B and C;2) by mixture that step 1) obtains with total by accounting for glycerol The mixing medium of the 20% water composition of 20% glycerol and Zhan Shui total weight of weight is finely ground, disperses;3) by carbomer, poly- The water heating of vinylpyrrolidone, sodium alginate, sodium ethylene diamine tetracetate, benzalkonium chloride, the glycerol of surplus and surplus is stirred It mixes to obtain gel-type vehicle;4) mixture for obtaining step 2) is added in the gel-type vehicle that step 3) obtains, and is stirred and evenly mixed To gel.
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CN106137948A (en) * 2016-08-01 2016-11-23 中国人民解放军第三军医大学 The gel for the treatment of dermatitis and eczema and Preparation method and use
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CN103214484A (en) * 2005-12-13 2013-07-24 因塞特公司 Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors
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CN110538183A (en) * 2019-10-09 2019-12-06 吉林大学 Composition for preventing and treating infantile eczema and preparation method thereof

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