CN1092651A - Cortical hormone compound preparation for external use - Google Patents

Cortical hormone compound preparation for external use Download PDF

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Publication number
CN1092651A
CN1092651A CN 93120481 CN93120481A CN1092651A CN 1092651 A CN1092651 A CN 1092651A CN 93120481 CN93120481 CN 93120481 CN 93120481 A CN93120481 A CN 93120481A CN 1092651 A CN1092651 A CN 1092651A
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acetate
external
dehydrocorticosterone
hydroxy
exfoliator
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CN 93120481
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CN1042896C (en
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王宗锐
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Guangdong Medical University
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Guangdong Medical University
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Abstract

The present invention relates to a kind of compound corticoid preparation of external preparation for skin.It is by the external 17-hydroxy-11-dehydrocorticosterone, transdermal enhancer and exfoliator are formed, the external 17-hydroxy-11-dehydrocorticosterone can be hydrocortisone acetate (0.5~1%), Triamcinolone acetonide acetate (0.025~0.2%) etc., and transdermal enhancer can be azacyclo--2-ketone (as a laurocapram 0.3~15%); Dimethyl sulfoxine 15~50%, propylene glycol 15~50% etc., exfoliator is salicylic acid (0.3~6%); Make solution, Emulsion, ointment, aerosol, gel, liposome by the difference that adds organic solvent, substrate and adjuvant.This product has improved transdermal absorption factor and has strengthened antiinflammatory action, thereby improves clinical efficacy, reduces cost.

Description

Cortical hormone compound preparation for external use
The present invention relates to a kind of compound corticoid preparation of external preparation for skin.
The present cortical hormone compound preparation for external use of using, generally be that 17-hydroxy-11-dehydrocorticosterone is dissolved in some organic solvents such as the ethanol, perhaps with mixings such as ointment base such as vaseline, sometimes in preparation, add antibiotic and antifungal agent, compound preparation is had also have antibiotic, antifungic action outside the antiinflammatory action, but because the barrier action of keratodermatitis, the Transdermal absorption of such preparation of Chinese medicine is affected, thereby the drug level minimizing of arrival site of action, this type of external 17-hydroxy-11-dehydrocorticosterone transdermal bioavailability is low.
The object of the present invention is to provide a kind of transdermal absorption factor height, cortical hormone compound preparation for external use that curative effect is high.
The present invention is by the external 17-hydroxy-11-dehydrocorticosterone, transdermal enhancer and exfoliator are formed, the external 17-hydroxy-11-dehydrocorticosterone can be hydrocortisone acetate (0.5~1%), hydroprednisone acetate (prednisolone) (0.05~0.2%), dexamethasone acetate (0.05~0.3%), dexamethasone pivalate (0.03~0.2%), acetic acid Beta-corlan (0.03~0.2%), betamethasone valerate (0.03~0.2%), Triamcinolone acetonide acetate (0.025~0.2%), fluocinonide (0.01~0.2%), halcinonidedcorten (0.025~0.1%), triamcinolone (0.05~0.2%), halcinonidedcorten (0.05~0.1%), dipropionic acid Clobetasol (0.03~0.1%), fludrocortisone acetate (0.05~0.25%); Transdermal enhancer can be that azacyclo--2-ketone is (as Laurel nitrogen
Figure 93120481X_IMG3
Ketone (0.3~15%), 2-Pyrrolidone class (as N-N-methyl-2-2-pyrrolidone N-0.3~15%), dimethyl sulfoxine 15~50%, urea 3~15%, propylene glycol 15~50%, oleic acid 1~10%, terpenes (as Borneolum Syntheticum 0.3~10%); Exfoliator is salicylic acid (0.3~6%); Make solution, Emulsion, ointment (Sorbidon Hydrate, oil-in-water ointment), aerosol, gel, liposome by the difference that adds organic solvent, substrate and adjuvant.
Below in conjunction with embodiment the present invention is described in detail.
Embodiment one: hydrocortisone acetate 10g, salicylic acid 30g, Laurel nitrogen
Figure 93120481X_IMG4
Ketone 20ml, ointment base add to 1000g, abundant grinding, mixing.
Embodiment two: Triamcinolone acetonide acetate 1g, salicylic acid 20g, Laurel nitrogen
Figure 93120481X_IMG5
Ketone 20ml, propylene glycol 300ml, ethanol add to 1000ml, dissolving.
Embodiment three: Triamcinolone acetonide acetate 1g, salicylic acid 30g, Laurel nitrogen
Figure 93120481X_IMG6
Ketone 50ml, ointment base adds to 1000g, the grinding mixing.
Embodiment four: halcinonidedcorten 1g, salicylic acid 10g, Laurel nitrogen
Figure 93120481X_IMG7
Ketone 10ml, ointment base adds to 1000ml, the grinding mixing.
Embodiment five: halcinonidedcorten 1g, salicylic acid 30g, dimethyl sulfoxine 500ml, ethanol adds to 1000ml.
Embodiment six: dipropionic acid Clobetasol 0.5g, salicylic acid 30g, Borneolum Syntheticum 20g, ointment base adds to 1000g, fully grinds mixing.
This product is because of containing transdermal enhancer, external 17-hydroxy-11-dehydrocorticosterone, salicylic acid, antibiotic transdermal absorption factor (table 1,2,3) have been improved, owing to contain salicylic acid, make this product have exfoliation effect (table 4), salicylic acid has strengthened the antiinflammatory action (table 5) of external 17-hydroxy-11-dehydrocorticosterone as NSAID (non-steroidal anti-inflammatory drug), thereby can improve clinical efficacy, reduce cost.
Table 1.
Laurel nitrogen
Figure 93120481X_IMG8
Ketone increases the contraction of Triamcinolone acetonide acetate to normal person's forearm inside skin blood vessel
Palor reaction score value
The drug test number (X ± SD)
1 * 10 -5Triamcinolone acetonide acetate ethanol liquid 13 19 ± 4.4
Add 2% Laurel nitrogen chlorine
Figure 93120481X_IMG9
Ketone
1 * 10 -5Triamcinolone acetonide acetate ethanol liquid 13 29 ± 3.2
With 1 * 10 -5Triamcinolone acetonide acetate ethanol liquor ratio.P<0.05
Table 2. Laurel nitrogen
Figure 93120481X_IMG10
Ketone is in the influence of nude mice isolated skin to the salicylic acid transdermal absorption factor
Drug study skin is counted transdermal percentage rate (12h) (% X ± SD)
2% salicylic acid alcoholic solution 7 14 ± 2.1
Add 2% Laurel nitrogen
Figure 93120481X_IMG11
Ketone
2% salicylic acid alcoholic solution 7 25 ± 3.8
Compare with 2% salicylic acid alcoholic solution.P<0.01
Table 3. Laurel nitrogen
Figure 93120481X_IMG12
Ketone is in the influence of nude mice isolated skin to the rifampicin transdermal absorption factor
Drug study number of times transdermal percentage rate (12h) (% X ± SD)
0.5% rifampicin alcoholic solution 20 4.2 ± 1.6
Add 2% Laurel nitrogen
Figure 93120481X_IMG13
Ketone
0.5% rifampicin alcoholic solution 20 17.1 ± 3.8
Compare with 0.5% rifampicin alcoholic solution.P<0.01
Table 4. saligenin in compound recipe Triamcinolone acetonide acetate solution to the exfoliation effect of normal person's forearm inside skin
Pharmaceutical samples is counted keratodermatitis labelling mottle and is disappeared
Required natural law X ± SD (day)
Compound recipe Triamcinolone acetonide acetate solution 8 8.8 ± 0.71
(containing 2% salicylic acid)
2% salicylic acid alcoholic solution 8 9.4 ± 0.74
Lack salicylic " compound recipe acetic acid 8 14.5 ± 1.20
Triamcinolone acetonide solution "
Compare with scarce salicylic " compound recipe Triamcinolone acetonide acetate solution ".P<0.01
Table 5. salicylic acid and Triamcinolone acetonide acetate are worked in coordination with anti-U.V. erythema effect
Medicine number of animals rat skin U.V. erythematous response score value
X±SD
Blank 8 1.0 ± 0
0.1% Triamcinolone acetonide acetate alcoholic solution 8 0.69 ± 0.16
0.1% Triamcinolone acetonide acetate
+ 2% salicylic acid alcoholic solution 8 0.31 ± 0.12
Compare with 0.1% Triamcinolone acetonide acetate alcoholic solution.P<0.05。

Claims (1)

1, a kind of cortical hormone compound preparation for external use, it is characterized in that it is by the external 17-hydroxy-11-dehydrocorticosterone, transdermal enhancer and exfoliator are formed, the external 17-hydroxy-11-dehydrocorticosterone can be hydrocortisone acetate (0.5~1%), hydroprednisone acetate (prednisolone) (0.05~0.2%), dexamethasone acetate (0.05~0.3%), dexamethasone pivalate (0.03~0.2%), acetic acid Beta-corlan (0.03~0.2%), betamethasone valerate (0.03~0.2%), Triamcinolone acetonide acetate (0.025~0.2%), fluocinonide (0.01~0.2%), halcinonidedcorten (0.025~0.1%), triamcinolone (0.05~0.2%), halcinonidedcorten (0.05~0.1%), dipropionic acid Clobetasol (0.03~0.1%), fludrocortisone acetate (0.05~0.25%); Transdermal enhancer can be that azacyclo--2-ketone is (as Laurel nitrogen
Figure 93120481X_IMG2
Ketone (0.3~15%), 2-Pyrrolidone class (as N-N-methyl-2-2-pyrrolidone N-0.3~15%), dimethyl sulfoxine 15~50%, urea 3~15%, propylene glycol 15~50%, oleic acid 1~10%, terpenes (as Borneolum Syntheticum 0.3~10%); Exfoliator is salicylic acid (0.3~6%); Make solution, Emulsion, ointment (Sorbidon Hydrate, oil-in-water ointment), aerosol, gel, liposome by the difference that adds organic solvent, substrate and adjuvant.
CN93120481A 1993-12-06 1993-12-06 External compound corticoid preparation Expired - Lifetime CN1042896C (en)

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Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105687207A (en) * 2016-02-26 2016-06-22 江西省皮肤病专科医院 Ointment for treating dermatitis and eczema and preparation method thereof
CN107913279A (en) * 2017-11-16 2018-04-17 钟汝华 A kind of ointment for treating multiple dermatosis
CN109602728A (en) * 2019-01-18 2019-04-12 江苏福锌雨医药科技有限公司 A kind of fludrocortisone acetate oral quick-dissolving film preparation and preparation method thereof

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES8706027A1 (en) * 1986-03-24 1987-05-16 Belda Galiana Manuel F Topical pharmaceutical compositions for treating vitiligo

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105687207A (en) * 2016-02-26 2016-06-22 江西省皮肤病专科医院 Ointment for treating dermatitis and eczema and preparation method thereof
CN105687207B (en) * 2016-02-26 2018-04-10 江西省皮肤病专科医院 A kind of paste for being used for dermatitis, eczema and preparation method thereof
CN107913279A (en) * 2017-11-16 2018-04-17 钟汝华 A kind of ointment for treating multiple dermatosis
CN109602728A (en) * 2019-01-18 2019-04-12 江苏福锌雨医药科技有限公司 A kind of fludrocortisone acetate oral quick-dissolving film preparation and preparation method thereof

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