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 PDFInfo
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- 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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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/35—Heterocyclic 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
- A61K31/351—Heterocyclic 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic 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
- A61K31/4353—Heterocyclic 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
- A61K31/437—Heterocyclic 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs 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
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:
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:
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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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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CN102459278A (en) * | 2009-06-16 | 2012-05-16 | 默沙东公司 | Substituted -1,3,8-triazaspiro[4.5]decane-2,4-diones |
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 |
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 |
CN108440528A (en) * | 2013-03-12 | 2018-08-24 | 艾伯维公司 | Fourth Ring Bu Luomo structural domain inhibitor |
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CN1305479A (en) * | 1998-06-19 | 2001-07-25 | 辉瑞产品公司 | Pyrrolo [2,3-d] pyrmidine compounds |
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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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