CN103877086A - New application of desloratadine in pharmacy - Google Patents
New application of desloratadine in pharmacy Download PDFInfo
- Publication number
- CN103877086A CN103877086A CN201210557378.2A CN201210557378A CN103877086A CN 103877086 A CN103877086 A CN 103877086A CN 201210557378 A CN201210557378 A CN 201210557378A CN 103877086 A CN103877086 A CN 103877086A
- Authority
- CN
- China
- Prior art keywords
- desloratadine
- group
- gel
- agent
- cavia porcellus
- 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
Images
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention relates to a new application of desloratadine in pharmacy. The invention discloses the application of desloratadine in preparation of medicines for treating eczema. According to the invention, the application scope of desloratadine is enlarged, and the medication selection for eczema patients is enlarged. The invention also provides an external-use preparation of desloratadine, which solves the problem of the first pass effect generated by oral administration of desloratadine in a traditional mode, and the adverse side-effect generated due to oral administration of desloratadine is reduced.
Description
Technical field
The present invention relates to pharmaceutical preparation, relate in particular to Desloratadine, particularly the new purposes of Desloratadine in pharmacy.
Background technology
Desloratadine (desloratadine) be loratadine (1oratadine) in vivo piptonychia acetoacetic ester and active metabolite.Desloratadine be novel the 3rd generation antihistaminic, can highly selective be combined with H receptor-specific, anti-allergic effects is strong, rapid-action and effect is lasting.
Desloratadine is mainly used in treating the anaphylactic disease such as chronic idiopathic urticaria, catarrhus perennialis clinically.In addition also can alleviate, the symptom of cold urticaria.
The dosage form of Desloratadine is mainly taking tablet, syrup, dry suspension etc. as main peroral dosage form in the market.After these preparations are taken, gastrointestinal tract can produce first pass effect to medicine, and food and gastric emptying can exert an influence to the metabolism of medicine simultaneously.For the diseases such as treatment skin allergy, Desloratadine is oral after gastrointestinal absorption, is distributed in dermal tissue, thereby plays the effect for the treatment of dermatosis by blood circulation.Therefore Desloratadine adopts oral administering mode, and because the blood distribution of skin histology is relatively less, after absorbing, distributing, skin part local concentration is lower, is difficult to play treatment effectiveness.
Desloratadine is prepared into local topical preparation, by Transdermal absorption, increases the free drug concentration of local skin tissue, better bring into play its local therapeutic effects, reduce untoward reaction.Exterior-applied formulation, by gastrointestinal tract, has not been avoided first pass effect; Direct effect and affected part, onset is rapid; Can be according to affected part area and light and heavy degree selective dose and area coverage size, use, easy to carry.
Eczema is a kind of common anaphylaxis dermatosis, comprises the erythra of a series of lasting and superventions, with rubescent, edema, pruritus and dry be sign, can be with forming a scab, peel off, bubble, cracking, hemorrhage or oozing of blood.Treat at present the not only negligible amounts of document of eczema for Desloratadine, and focus mostly in drug combination.The local topical preparation of Desloratadine is also only present in document aspect, there is no any launch.And Desloratadine local topical preparation for treating eczema more has no correlational study report.
This patent by experiment, is investigated the impact of Desloratadine local topical preparation on Cavia porcellus contact eczema model, filters out suitable treatment concentration, provides foundation for evaluating the preclinical pharmacodynamic action of Desloratadine local topical preparation.
Summary of the invention
The object of the present invention is to provide the new purposes of Desloratadine in pharmacy.
In order to realize goal of the invention, the present invention adopts following technical scheme:
The purposes of Desloratadine in preparation treatment eczema medicine.
Described Desloratadine is Desloratadine external preparation.
Described Desloratadine external preparation is gel, ointment, paste, patch, spray or liniment.
The present invention discloses a kind of Desloratadine gel, it is characterized in that comprising 1 ~ 15% Desloratadine, 2 ~ 20% solubilizing agent, 0.01 ~ 1% antioxidant, 0.01 ~ 1% metal ion chelation agent, 0.01 ~ 1% antiseptic, 0.05 ~ 5% penetrating agent, 2 ~ 20% wetting agents, 0.05 ~ 2% pH adjusting agent, 0.1 ~ 2% thickening agent, remains as solvent.
Described solubilizing agent is HP-β-CD, DM-β-CD, sulphur fourth group-beta-cyclodextrin, one or more in gamma-cyclodextrin.
Described metal ion chelation agent is one or more in EDTA, EDTA-2Na, citric acid, tartaric acid.
Described penetrating agent is one or more in Mentholum, Borneolum Syntheticum, azone, oleic acid, dimethyl sulfoxine.
The invention discloses the purposes of Desloratadine in preparation treatment eczema medicine, expand the range of application of Desloratadine, expand the selection of eczema patients medication, and the present invention also provides a kind of Desloratadine external preparation, solve that loratadine is traditionally oral and the problems such as the first pass effect that produces have reduced Desloratadine because of the oral adverse side effect producing.
Brief description of the drawings
Fig. 1 ~ Fig. 8 is that Desloratadine is to Eczema Model Cavia porcellus auris dextra Pathomorphologic figure;
Wherein Fig. 1: normal control figure; Fig. 2: model contrast figure; Fig. 3: 1 group of positive control (diphenhydramine); Fig. 4: 2 groups of positive controls (desonide); Fig. 5: blank gel group; Fig. 6: Desloratadine low dose group; Fig. 7: dosage group in Desloratadine; Fig. 8: Desloratadine high dose group;
Fig. 9 ~ Figure 16 is the affect figure of Desloratadine on NF-κ B p65 protein expression in Eczema Model Cavia porcellus auris dextra tissue;
Wherein Fig. 9: normal control figure; Figure 10: model contrast figure; Figure 11: 1 group of positive control (diphenhydramine); Figure 12: 2 groups of positive controls (desonide); Figure 13: blank gel group; Figure 14: Desloratadine low dose group; Figure 15: dosage group in Desloratadine; Figure 16: Desloratadine high dose group;
Figure 17 ~ Figure 24 is the affect detailed description of the invention of Desloratadine on COX-2 protein expression in Eczema Model Cavia porcellus auris dextra tissue;
Wherein Figure 17: normal control figure; Figure 18: model contrast figure; Figure 19: 1 group of positive control (diphenhydramine); Figure 20: 2 groups of positive controls (desonide); Figure 21: blank gel group; Figure 22: Desloratadine low dose group; Figure 23: dosage group in Desloratadine; Figure 24: Desloratadine high dose group;
Detailed description of the invention
Experiment: the therapeutical effect of Desloratadine to eczema.
test material
1.1 reagent
3.5% Desloratadine gel, 7.0% Desloratadine gel, 14.0% Desloratadine gel, blank gel; Diphenhydramine Hydrochloride Gel (specification: 2.0%, pharmaceutical Co. Ltd of Johnson & Johnson of the U.S.); Desonide emulsifiable paste (specification: 0.05%, Huabang Pharmaceutical Co., Ltd., Chongqing).
1.2 experimental animal
100 of regular grade Cavia porcelluss, 250 ~ 300 g, male and female half and half.
test method
2.1 groupings, modeling and administration
Get 100 of Cavia porcelluss, 250～300g, male and female half and half, be divided at random 10 groups (10 every group) by sex body weight, i.e. the high, medium and low dosage group of Desloratadine gel, blank gel group, 1 group of positive control (Diphenhydramine Hydrochloride Gel), 2 groups of positive controls (desonide emulsifiable paste), model control group, Normal group.Except Normal group, according to a certain method, all the other Cavia porcelluss are caused to Eczema Model.Except Eczema Model, other 8 groups are coated with Desloratadine gel, blank gel, positive control drug 1, the positive control drug 2 of high, medium and low dosage, every day 1 time, continuous 7 days respectively at Cavia porcellus auris dextra inner side.In drug withdrawal, after 1 day, anaesthetized guinea pig, gets blood, puts to death animal.
2.2 detect index
(1) ear skin irritation reaction evaluating
, during the 1st, 3,5,7 days, the tissue morphology of each group of Cavia porcellus auris dextra intact skin is carried out to macroscopy, and mark in administration.
(2) ear swelling degree is evaluated
Finish the same day in experiment, Cavia porcellus is put to death, after processing according to a certain method, calculate the weight difference that brings out rear right, left ear tissue piece.
(3) histopathological examination
Get auris dextra skin lesion place tissue, section after processing according to a certain method, respectively organizes the pathological change of auricle tissue at optical microphotograph Microscopic observation.
(4) serum cytokines detects
Detect according to a certain method the contents level of IL-2 in guinea pig serum, TNF-α, IFN-γ.
(5) analysis that auricle tissue inflammation correlation factor is expressed
Get auris dextra skin lesion place tissue, section after processing according to a certain method, and observe NF-κ B p65, COX-2 expression in damage place tissue.
statistical method
Experimental data adopts certain statistical analysis software to carry out statistical procedures, acquired results with mean ± standard deviation (± s) represent.Each group experimental data is first carried out X2 test of normality and variance analysis, if meet normal distribution and homogeneity of variance, adopts one factor analysis of variance, and multiple comparisons adopts LSD method; If heterogeneity of variance, carries out nonparametric rank test.Get P<0.05 as significant difference level.
result of the test
(1) impact on skin of pinna mode of appearance
After modeling success, after administration 1st～7 days, the basic, normal, high dosage group of Desloratadine gel, 1 group of positive control (diphenhydramine), the improvement in various degree of 2 groups of red and swollen phenomenons of (desonide) each Cavia porcellus auris dextra of positive control, and be time-effect relationship along with the prolongation for the treatment of time.
Mark according to Cavia porcellus ear tissue pathogenic site mode of appearance, result is as shown in table 1: after modeling success, Cavia porcellus auris dextra pathological score value obviously rises, and compares with Normal group, has utmost point significant difference (P<0.01); And along with the prolongation of observing time, its pathological score value is slow growth trend, it is mainly the red and swollen auris dextra tissue inner side increase of scratch and the formation of incrustation.
In drug treatment the 1st, 3,5,7 days, 1 group of Cavia porcellus auris dextra mode of appearance of positive control is observed, its pathological score value is respectively 0.30 ± 0.48,0.70 ± 0.67,0.60 ± 0.52 and 0.30 ± 0.48, compares all have significant difference (all P<0.01) with model control group; 2 groups of Cavia porcellus auris dextra mode of appearance pathological score values of positive control are respectively to 0.60 ± 0.70,0.70 ± 0.48,0.80 ± 0.42 and 0.60 ± 0.52, compare with the model control group of same time period and all there is utmost point significant difference (all P<0.01);
Desloratadine gel low dose group pathological score value is respectively 1.90 ± 0.57,2.90 ± 1.45,2.90 ± 1.45 and 2.70 ± 1.42, the difference (all P>0.05) of comparing with the model control group of same time period that there are no significant, compare with 1 group of the positive control of same time period and all there is utmost point significant difference (all P<0.01), compare and all there is utmost point significant difference (all P<0.01) with 2 groups of the positive controls of same time period.
In Desloratadine gel, dosage group pathological score value is respectively 1.80 ± 0.42,2.30 ± 0.95,2.30 ± 0.94 and 1.90 ± 0.88, the difference (all P>0.05) of comparing with the model control group of same time period that there are no significant, compare with 1 group of the positive control of same time period and all there is utmost point significant difference (all P<0.01), compare and all there is utmost point significant difference (all P<0.01) with 2 groups of the positive controls of same time period.
Desloratadine gel high dose group pathological score value is respectively 1.60 ± 0.52, 1.40 ± 0.52, 1.50 ± 0.53 and 1.10 ± 0.57, compare with the model control group of same time period and all there is significant difference (all P<0.01), the difference (all P>0.05) of comparing with 1 group of the positive control of same time period that there are no significant, the difference (all P>0.05) of comparing with 2 groups of the positive controls of same time period that there are no significant, prompting is in this scope of experiment, Desloratadine gel high dose is to the diphenhydramine under improvement effect and the test dose of Cavia porcellus auris dextra pathology mode of appearance, the effect of desonide is suitable.
But each time period, the red and swollen phenomenon of the each Cavia porcellus auris dextra of blank gel group has no obvious improvement, the there was no significant difference (P>0.05) of comparing with model control group, point out blank gel in this laboratory observation scope without remarkable therapeutic effect, to eczema without improvement effect.
the impact (± SD, n=10) of table 1 Desloratadine gel on Eczema Model Cavia porcellus ear tissue outward appearance pathomorphism
Note: compare with model control group, a P<0.05, b P<0.01; Compare with 1 group of positive control, c P<0.05, d P<0.01; Compare with 2 groups of positive controls, e P<0.05, f P<0.01.
(2) impact on Cavia porcellus ear swelling degree
Result is as shown in table 2: Cavia porcellus auris dextra obvious tumefaction after modeling success; Compare with Normal group (left and right ear is of poor quality is 17.8 ± 7.04 mg), model control group left and right ear is of poor quality is 45.8 ± 6.29 mg, has utmost point significant difference (P<0.01).Through administration after the 7th day, the basic, normal, high dosage group of Desloratadine gel all can be improved Cavia porcellus ear swelling phenomenon to a certain extent, but Desloratadine gel low dosage, compare with model control group, there was no significant difference (P>0.05), with 1 group of positive control and 2 groups of comparisons of positive control, all there is utmost point significant difference (all P<0.01).Dosage group in Desloratadine gel, compare with model control group, there was no significant difference (P>0.05), with 1 group of positive control and 2 groups of comparisons of positive control, all there is significant difference (P<0.01, P<0.05 respectively).Desloratadine gel high dose group, compare with model control group, all there is utmost point significant difference (all P<0.01), with 1 group of positive control and 2 groups of comparisons of positive control, difference that there are no significant (all P>0.05), prompting Desloratadine gel high dose is suitable with the inhibitory action of positive control medicine (diphenhydramine and desonide) to the inhibitory action of Cavia porcellus auricle edema due to DNCB.
And blank gel group has no the improvement of each Cavia porcellus auris dextra pathological tissue mode of appearance, compare with model control group, difference that there are no significant (all P>0.05), show blank gel to the Cavia porcellus ear swelling due to DNCB all without inhibitory action significantly.
the impact (± SD, n=10) of table 2 Desloratadine gel on eczema Cavia porcellus auricle edema
Note: compare with model control group, a P<0.05, b P<0.01; Compare with 1 group of positive control, c P<0.05, d P<0.01; Compare with 2 groups of positive controls, e P<0.05, f P<0.01.
(3) impact on Eczema Model Cavia porcellus ear tissue pathological change
Choose every group of inflammatory infiltration and typically cut into slices, HE dyeing × 200.Result is as shown in Fig. 1 ~ Fig. 8, and Normal group Cavia porcellus auris dextra tissue is without erythema, edema, and histopathology has no inflammatory reaction, and cell arrangement arranges, structural integrity.Model control group Cavia porcellus auris dextra tissue presents erythema, edema, oozes out change, show as epidermis and thicken, slight hyperkeratosis, blister between epidermis cell, in intracellular edema, epidermis, epidermis, corium and subcutaneous tissue intensive inflammatory cell infiltration, telangiectasis and interstitial edema.With model control group comparison, the basic, normal, high dosage group of Desloratadine gel Cavia porcellus auris dextra histopathology symptom obviously reduces, and intracellular edema alleviates, and inflammatory cell infiltration reduces; Wherein, 1 group of Desloratadine gel high dose group and positive control, 2 groups of pathological symptoms of positive control are comparatively approaching, and the intensive inflammatory cell infiltration of epidermis, corium and subcutaneous tissue obviously reduces.And blank gel group Cavia porcellus auris dextra organizes all visible significantly epidermises to thicken, telangiectasis and interstitial edema.
(4) impact on serum cytokines
Result is as shown in table 3, and after modeling success, guinea pig serum TNF-alpha content increases, IL-2 and IFN-γ content reduce, and compares with Normal group, has utmost point significant difference (P>0.01).Through administration, after the 7th day, the basic, normal, high dosage group of Desloratadine gel all can improve guinea pig serum IL-2 content to a certain extent, compares with model control group, has utmost point significant difference (P<0.01); But aspect TNF-α and IFN-γ content, only Desloratadine gel high dose group can obviously reduce guinea pig serum TNF-α and IFN-γ content, compare with model control group, there is utmost point significant difference (P<0.01), there was no significant difference (P>0.05) of low, the middle dosage group of Desloratadine gel.The basic, normal, high dosage group of Desloratadine gel guinea pig serum IL-2 and TNF-alpha content, compare respectively with 2 groups of 1 group of positive controls, positive control, is showed no significant difference (all P<0.01); Desloratadine gel high dose group guinea pig serum IFN-γ content, compares respectively with 2 groups of 1 group of positive controls, positive control, is showed no significant difference (all P<0.01); And low, the middle dosage group of Desloratadine gel guinea pig serum IFN-γ content compares respectively with 2 groups of 1 group of positive controls, positive control, all there is significant difference (all P<0.05).Blank gel group does not make significant difference to guinea pig serum IL-2, TNF-α and IFN-γ content, compares with model control group, and there was no significant difference (P>0.01).
the impact (± SD, n=10) of table 3 Desloratadine gel on Eczema Model guinea pig serum cytokine
Note: compare with model control group, a P<0.05, b P<0.01; Compare with 1 group of positive control, c P<0.05, d P<0.01; Compare with 2 groups of positive controls, e P<0.05, f P<0.01.
(5) impact on Cavia porcellus auris dextra tissue inflammation expression of related gene proteins
Detect inflammation-related factor NF-κ B p65 and COX-2 in Cavia porcellus auris dextra tissue are carried out, under light microscopic, in cytoplasm and (or) core, occur yellow, brown particle person being positive cell.
As shown in Fig. 9 ~ Figure 16, NF-κ B p65 coloration result positive reaction product is mainly positioned at cytoplasm and reaches for master meter, positive main in subcutaneous striated muscle cell endochylema, in parts of fine karyon, in squamous cell and the visible a small amount of low expression of skin appendages.In Normal group almost without NF-κ B p65 protein positive expression, visible a large amount of NF-κ B p65 protein expressions in the subcutaneous striated muscle cell endochylema of model control group.Compare with model control group, in the basic, normal, high dosage group of Desloratadine gel, NF-κ B p65 protein expression obviously reduces.Wherein, Desloratadine gel high dose group NF-κ B p65 protein expression is suitable with 1 group of positive control.Show that Desloratadine gel high dose can pass through to suppress NF-κ B p65 protein expression, thereby improve the inflammation pathological state of tissue; And blank gel group also has great expression.
As shown in Figure 17 ~ Figure 24, COX-2 coloration result positive reaction product is mainly positioned at cytoplasm, the positive squamous cell at skin histology, and in the epithelial cell of hair follicle and sebaceous gland, part is at chondrocyte and infiltrate visible a small amount of expression in inflammatory cell.The squamous cell of each group skin histology, equal visible COX-2 protein expression in the epithelial cell of hair follicle and sebaceous gland, blood vessel also visible a small amount of expression around.But visible COX-2 albumen great expression in model control group blood vessel and infiltration inflammatory cell.Compare with model control group, in Desloratadine gel basic, normal, high dosage group blood vessel and infiltration inflammatory cell, COX-2 protein expression obviously reduces.Wherein, 1 group of Desloratadine gel high dose group COX-2 protein expression and positive control are suitable.Show that Desloratadine gel high dose can pass through to suppress COX-2 protein expression, thereby improve the inflammation pathological state of tissue; And blank gel group also has great expression.
conclusion
High, medium and low 3 dosage of Desloratadine gel all show certain therapeutical effect to Eczema Model Cavia porcellus, therefore can think that Desloratadine gel has the effect of reasonable treatment eczema.
Embodiment: prepare Desloratadine gel
Desloratadine 2g
HP-β-CD 8g
Carbomer 0.85g
Triethanolamine 0.55g
Propylene glycol 6g
Glycerol 12g
Sodium sulfite 0.1g
EDTA-2Na 0.1g
Ethylparaben 0.1g
Mentholum 0.08g
95% ethanol 45g
Water 25.22g
Make 100g
Preparation process
1, sodium sulfite, EDTA-2Na are water-soluble, add glycerol, mixed with propylene glycol even, add carbomer, are stirred to and are uniformly dispersed, and obtain A phase;
2, Desloratadine, HP-β-CD are dissolved in ethanol, stir a period of time, add ethylparaben, Mentholum, triethanolamine, stir, and obtain B phase;
3, B item is added to A item, stir, to obtain final product.
embodiment 2: Desloratadine hydrogel adhesive
Desloratadine 2g
HP-β-CD 8g
Hypromellose 1.5g
Propylene glycol 6g
Glycerol 12g
Sodium sulfite 0.1g
EDTA-2Na 0.1g
Methyl parahydroxybenzoate 0.1g
Propyl p-hydroxybenzoate 0.1g
Azone 2g
95% ethanol 20g
Water 48.2g
Make 100g
Preparation process
1, sodium sulfite, EDTA-2Na are water-soluble, add glycerol, mixed with propylene glycol even, add hypromellose, are stirred to dissolving, obtain A phase;
2, Desloratadine, HP-β-CD are dissolved in ethanol, stir a period of time, add methyl parahydroxybenzoate, ethylparaben, azone, stir, and obtain B phase;
3, B item is added to A item, stir, to obtain final product.
Solubilizing agent of the present invention has adopted derivant (comprising HP-β-CD, DM-β-CD, sulphur fourth group-beta-cyclodextrin etc.) and the gamma-cyclodextrin of beta-schardinger dextrin-.Compared with beta-schardinger dextrin-, the good water solubility of the derivant of beta-schardinger dextrin-, can greatly improve by the dissolubility of enclose medicine, rate of release and bioavailability.And internal cavity diameter (0.8nm) and the cavity volume (0.43nm of gamma-cyclodextrin
3) be all greater than internal cavity diameter (0.6nm) and the cavity volume (0.26nm of beta-schardinger dextrin-
3), the drug molecule (Mr>400) that therefore gamma-cyclodextrin is larger to number molecular weight, has better Binding ability.Taking HP-β-CD as example, its maximum solubilising power to Desloratadine is approximately 350 times of beta-schardinger dextrin-.This may be relevant much larger than beta-schardinger dextrin-(1.85%, 25 DEG C) with the water solublity of HP-β-CD (75%, 25 DEG C).
Solubilizing agent of the present invention has adopted derivant (comprising HP-β-CD, DM-β-CD, sulphur fourth group-beta-cyclodextrin etc.) and the gamma-cyclodextrin of beta-schardinger dextrin-.Compared with beta-schardinger dextrin-, the good water solubility of the derivant of beta-schardinger dextrin-, can greatly improve by the dissolubility of enclose medicine, rate of release and bioavailability.And internal cavity diameter (0.8nm) and the cavity volume (0.43nm of gamma-cyclodextrin
3) be all greater than internal cavity diameter (0.6nm) and the cavity volume (0.26nm of beta-schardinger dextrin-
3), the drug molecule (Mr>400) that therefore gamma-cyclodextrin is larger to number molecular weight, has better Binding ability.Taking HP-β-CD as example, its maximum solubilising power to Desloratadine is approximately 350 times of beta-schardinger dextrin-.This may be relevant much larger than beta-schardinger dextrin-(1.85%, 25 DEG C) with the water solublity of HP-β-CD (75%, 25 DEG C).
* note: mol ratio, lower same
Experiment also proves that HP-β-CD has good Stabilization to Desloratadine.When this may be with identical mol ratio, the envelop rate of HP-β-CD is higher than beta-schardinger dextrin-, and free Desloratadine is relatively less, so be subject to the impact of the condition such as temperature and illumination less.
Transdermal test in vitro release experiment discloses the Desloratadine gel that contains HP-β-CD simultaneously and discharges medicine faster and more.This may can improve greatly with (1) HP-β-CD the dissolubility of Desloratadine; (2) though HP-β-CD itself is difficult to see through skin, can play the effect of soften cuticle, thereby increase the permeability of medicine.
* Desloratadine concentration 2%, lower same.
As can be seen from the above table, HP-β-CD can be accelerated the release of Desloratadine; And there is certain retardation at the beta-schardinger dextrin-initial stage to the release of Desloratadine, but later stage release is accelerated gradually; Final the two total volume is all greater than independent Desloratadine gel, and the dissolubility that this may can improve with HP-β-CD and beta-schardinger dextrin-Desloratadine, makes it easily out more relevant from gel diffusion inside.
Claims (8)
1. the purposes of Desloratadine in preparation treatment eczema medicine.
2. the purposes of Desloratadine according to claim 1 in preparation treatment eczema medicine, is characterized in that described Desloratadine is Desloratadine external preparation.
3. the purposes of Desloratadine according to claim 2 in preparation treatment eczema medicine, is characterized in that described Desloratadine external preparation is gel, ointment, paste, patch, spray or liniment.
4. the purposes of Desloratadine according to claim 3 in preparation treatment eczema medicine, is characterized in that Desloratadine concentration is controlled at 1% ~ 15%.
5. a Desloratadine gel, it is characterized in that comprising 1 ~ 15% Desloratadine, 2 ~ 20% solubilizing agent, 0.01 ~ 1% antioxidant, 0.01 ~ 1% metal ion chelation agent, 0.01 ~ 1% antiseptic, 0.05 ~ 5% penetrating agent, 2 ~ 20% wetting agents, 0.05 ~ 2% pH adjusting agent, 0.1 ~ 2% thickening agent, remains as solvent.
6. Desloratadine gel according to claim 4, is characterized in that described solubilizing agent is HP-β-CD, DM-β-CD, sulphur fourth group-beta-cyclodextrin, one or more in gamma-cyclodextrin.
7. Desloratadine gel according to claim 4, is characterized in that described metal ion chelation agent is one or more in EDTA, EDTA-2Na, citric acid, tartaric acid.
8. Desloratadine gel according to claim 4, is characterized in that described penetrating agent is one or more in Mentholum, Borneolum Syntheticum, azone, oleic acid, dimethyl sulfoxine.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210557378.2A CN103877086A (en) | 2012-12-20 | 2012-12-20 | New application of desloratadine in pharmacy |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210557378.2A CN103877086A (en) | 2012-12-20 | 2012-12-20 | New application of desloratadine in pharmacy |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN103877086A true CN103877086A (en) | 2014-06-25 |
Family
ID=50946425
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201210557378.2A Pending CN103877086A (en) | 2012-12-20 | 2012-12-20 | New application of desloratadine in pharmacy |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN103877086A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR101540191B1 (en) * | 2014-02-24 | 2015-07-28 | 성균관대학교산학협력단 | Composition comprising Loratadine for anti-inflammation |
| CN107233299A (en) * | 2017-06-13 | 2017-10-10 | 江苏黄河药业股份有限公司 | It is a kind of to be used to treat Loratadine paste of itch and preparation method thereof |
-
2012
- 2012-12-20 CN CN201210557378.2A patent/CN103877086A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR101540191B1 (en) * | 2014-02-24 | 2015-07-28 | 성균관대학교산학협력단 | Composition comprising Loratadine for anti-inflammation |
| CN107233299A (en) * | 2017-06-13 | 2017-10-10 | 江苏黄河药业股份有限公司 | It is a kind of to be used to treat Loratadine paste of itch and preparation method thereof |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| Luo et al. | Selenium-doped carbon quantum dots efficiently ameliorate secondary spinal cord injury via scavenging reactive oxygen species | |
| Liu et al. | Design of amphotericin B oral formulation for antifungal therapy | |
| CN111848832B (en) | Application of fluorine-containing compound modified cationic polymer as drug carrier and preparation method thereof | |
| Zeng et al. | Oral delivery of antioxidant enzymes for effective treatment of inflammatory disease | |
| CN106470702A (en) | For reducing the Cholic acids of fat and the compositionss of salt and method | |
| Wang et al. | Chitosan/hyaluronan nanogels co-delivering methotrexate and 5-aminolevulinic acid: A combined chemo-photodynamic therapy for psoriasis | |
| Zhao et al. | Flexible nano-liposomes-based transdermal hydrogel for targeted delivery of dexamethasone for rheumatoid arthritis therapy | |
| Zhang et al. | Co-hybridized composite nanovesicles for enhanced transdermal eugenol and cinnamaldehyde delivery and their potential efficacy in ulcerative colitis | |
| CN102781442B (en) | Use the method for the disease of nefopam compounds for treating cicatrix and beta-catenin mediation | |
| Khalid et al. | Macrophage targeting of nitazoxanide-loaded transethosomal gel in cutaneous leishmaniasis | |
| US20220362212A1 (en) | Sublingual or buccal administration of dim for treatment of skin diseases | |
| CN101147735A (en) | Pharmaceutical composition for injection and its medicine box | |
| CN106176758B (en) | A kind of externally-applied medicinal composition | |
| Chien et al. | Nanomicelle-generating microneedles loaded with tranilast for treatment of hypertrophic scars in a rabbit model | |
| Liu et al. | Biguanide chitosan microneedles with cell-free DNA scavenging ability for psoriasis therapy | |
| CN103877086A (en) | New application of desloratadine in pharmacy | |
| Zhou et al. | ROS-removing nano-medicine for navigating inflammatory microenvironment to enhance anti-epileptic therapy | |
| Song et al. | An inflammation-responsive double-layer microneedle patch for recurrent atopic dermatitis therapy | |
| Miao et al. | Dual-targeted colon-based integrated micelle drug delivery system for treatment of ulcerative colitis | |
| CN102525921B (en) | 2,2',6,6'-tetraisopropyl-4,4'-bigeminy phenol lipid microsphere preparation and preparation method thereof | |
| WO2015051763A1 (en) | Icotinib-containing topical skin pharmaceutical composition and use thereof | |
| CN105287612B (en) | Salinomycin Sodium and adriamycin nano liposome and the preparation method and application thereof are carried altogether | |
| CN108653296B (en) | The application of elemi eleostearic acid and the drug for the treatment of pancreatitis | |
| CN103054792B (en) | A kind of dapsone gel of steady quality and preparation method thereof | |
| CN106137948A (en) | The gel for the treatment of dermatitis and eczema and Preparation method and use |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| RJ01 | Rejection of invention patent application after publication | ||
| RJ01 | Rejection of invention patent application after publication |
Application publication date: 20140625 |