Name | Diflucortolone valerate |
Synonyms | Afusona Nerisone Nerisona Neriforte 59198-70-8 Nerisone Forte Youtolon[Tatsumi] DIFLUCORTOLONE VALERATE Diflucortolone valerate Diflucortolone 21-valerate Diflucortolone valerate (JAN) 6a,9-difluoro-11b,21-dihydroxy-16a-methylpregna-1,4-diene-3,20-dione 21-valerate (6alpha,11beta,16alpha)-6,9-Difluoro-11-hydroxy-16-methyl-3,20-dioxopregna-1,4-dien-21-yl valerate Pregna-1,4-diene-3,20-dione, 6,9-difluoro-11-hydroxy-16-methyl-21-[(1-oxopentyl)oxy]-, (6α,11β,16α)- (6alpha,11beta,16alpha)-6,9-difluoro-11-hydroxy-16-methyl-3,20-dioxopregna-1,4-dien-21-yl pentanoate pentanoic acid, (6alpha,11beta,16alpha)-6,9-difluoro-11-hydroxy-16-methyl-3,20-dioxopregna-1,4-dien-21-yl ester |
CAS | 59198-70-8 |
EINECS | 261-655-8 |
InChI | InChI=1/C27H36F2O5/c1-5-6-7-23(33)34-14-21(31)24-15(2)10-17-18-12-20(28)19-11-16(30)8-9-26(19,4)27(18,29)22(32)13-25(17,24)3/h8-9,11,15,17-18,20,22,24,32H,5-7,10,12-14H2,1-4H3/t15-,17+,18+,20+,22+,24-,25+,26+,27+/m1/s1 |
Molecular Formula | C27H36F2O5 |
Molar Mass | 478.57 |
Density | 1.1227 (estimate) |
Melting Point | 220°C |
Boling Point | 578.5±50.0 °C(Predicted) |
Specific Rotation(α) | D22 +100.8° (dioxane) |
Flash Point | 303.7°C |
Solubility | Chloroform (Slightly), Dioxane (Slightly), Methanol (Slightly) |
Vapor Presure | 8.58E-16mmHg at 25°C |
Appearance | Solid |
Color | White to Off-White |
pKa | 12.89±0.70(Predicted) |
Storage Condition | -20°C Freezer, Under inert atmosphere |
Refractive Index | 1.538 |
Use | Diflucortolone valerate is a powerful corticosteroid that can be used for the study of various skin diseases. |
In vitro study | Diflucortolone valerate is a potent corticosteroid esterified with valeric acid. Diflucortolone valerate helps reduce swelling, itching, and redness. |
In vivo study | DL 50 values are virtually non-toxic after single oral administration (mouse greater than 4 g/kg, rat ca. 3.1 g/kg, dog greater than 1 g/kg). Given s.c. (LD 50 mouse ca. 180 mg/kg, rat ca. 13 mg/kg) and i.p. (LD 50 mouse ca. 450 mg/kg, rat ca. 98 mg/kg) it is highly active and therefore produces also toxic effects. |
Toxicity | Approx LD50 in mice, rats: >4, 3.1 g/kg orally; 180, 13 mg/kg s.c.; 450, 98 mg/kg i.p. (Gunzel). |
Reference Show more | 1: Billich A, Aschauer H, Aszódi A, Stuetz A. Percutaneous absorption of drugs used in atopic eczema: pimecrolimus permeates less through skin than corticosteroids and tacrolimus. Int J Pharm. 2004 Jan 9;269(1):29-35. doi: 10.1016/j.ijpharm.2003.07.013. PMID: 14698574. 2: Henz BM, Jablonska S, van de Kerkhof PC, Stingl G, Blaszczyk M, Vandervalk PG, Veenhuizen R, Muggli R, Raederstorff D. Double-blind, multicentre analysis of the efficacy of borage oil in patients with atopic eczema. Br J Dermatol. 1999 Apr;140(4):685-8. doi: 10.1046/j.1365-2133.1999.02771.x. PMID: 10233322. 3: Täuber U, Weiss C, Matthes H. Does salicylic acid increase the percutaneous absorption of diflucortolone-21-valerate? Skin Pharmacol. 1993;6(4):276-81. doi: 10.1159/000211150. PMID: 8198813. 4: Ikoma Y, Yamashita M, Kamitani K, Nakagawa H. [Anti-inflammatory effects of methylprednisolone aceponate in animals]. Nihon Yakurigaku Zasshi. 1991 Nov;98(5):409-17. Japanese. doi: 10.1254/fpj.98.5_409. PMID: 1813371. 5: Tanaka M, Hiroshige R, Murai M, Tokunaga H, Okada S, Kimura T. [Diflucortolone-21-valerate Reference Standard (Control 871) of National Institute of Hygienic Sciences]. Eisei Shikenjo Hokoku. 1989;(107):156-9. Japanese. PMID: 2636922. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.09 ml | 10.448 ml | 20.896 ml |
5 mM | 0.418 ml | 2.09 ml | 4.179 ml |
10 mM | 0.209 ml | 1.045 ml | 2.09 ml |
5 mM | 0.042 ml | 0.209 ml | 0.418 ml |
Overview | Difluocolone valerate is a kind of steroid corticosteroid, which can inhibit inflammation and allergic skin reactions, and also inhibit the accelerated regeneration of cells Related reactions lead to symptoms, such as erythema, edema, skin thickening, loss of skin surface roughness, and relief of itching, burning sensation and pain. |
product description | difluocolone valerate external preparation is mainly 0.1% difluocolone valerate cream (trade name: GlaxoSmithKline pharmaceutical production), commercially available difluocolone valerate cream is oil-in-water cream, the formula is: about 70% of water as the water phase, the oil phase is made of hydrocarbons (white petrolatum, paraffin) polyoxyethylene (40) stearate, decanol, carbomen 934,EDTA-2Na, and methyl paraben and propyl paraben as preservatives. |
preparation method | difluocolone valerate 2.0g (crystal form I), white vaseline 150g, octaol 30g, liquid paraffin 80g, plain A- 2080g, glycerin 80g, paraben ethyl ester 1g, citric acid (C6H8O7 H2O)2g, sodium citrate (Na3C6H5O7 · 2H2O)3g of water for injection to 1000g of difluorocarbon valerate crystal type I micropowder has an average particle size of 8.1 μm and is accurately weighed according to the above ratio. The cream preparation process is as follows:(1) oil phase preparation: white petroleum jelly, 18 alcohol, liquid paraffin, plain A- 20, placed in a container, heated to melt, and kept at 90 ℃;(2) aqueous phase preparation: dissolve citric acid and sodium citrate in prescription amount of injection water, the main drug is evenly dispersed in glycerin, the aqueous solution of citric acid and sodium citrate and ethyl paraben are added, heated, and the temperature of stirring is kept at 80 ℃;(3) phase combination: the oil phase prepared in step (1) is slowly added into the aqueous phase prepared in step (2), stirred, kept at 90 ℃, stirred for 30min, cooled into paste to obtain 1000g cream with a content of 0.1%. |
biological activity | Diflucortolone valerate is a powerful corticosteroid that can be used for the study of various skin diseases. |
in vitro study | Diflucortolone valerate is a potent corticosteroid esterified with valeric acid. Diflucortolone valerate help reduce swelling, itching, and redness. |
in vivo study | DL 50 values are virtually non-toxic after single oral administration (mouse greater than 4 g/kg, rat ca. 3.1 g/kg, dog greater than 1 g/kg). Given s.c. (LD 50 mouse ca. 180 mg/kg, rat ca.13 mg/kg) and I. p. (LD 50 mouse ca.450 mg/kg, rat ca.98 mg/kg) it is highly active and therefore produces also toxic effects. |