Prednisolone acetonide

Codelsol > Prednisolone phosphate sodium Coderma - Fluocinolone acetonide Codesin-F Butamirate citrate Codilax - Bisacodyl... 

Examples of group I, i.e. weak or low efficacy topical steroids, are hydrocortisone acetate in various concentrations, methylprednisolone 1.0% and prednisolone 0.5%. Group II, the moderately potent steroids, includes alclometasone dipropionate 0.05%, hydrocortisone butyrate 0.1%, triamcinolone acetonide 0.025% and fluocinolone ace-tonide 0.01%. Group III, the potent steroids, contains among others betamethasone valerate 0.1%, betamethasone dipropionate 0.05%, budesonide 0.025%, desoximetasone 0.05%, fluticasone propionate 0.05%, amcinonide 0.1%, fluocinonide 0.05% and mometasone furoate 0.1%. Group IV comprises the very potent agents such as clobetasol propionate 0.05% and halobetasol propionate 0.05%. 

When A -3-ketosteroids or A -3-ketosteroids are treated with zinc dust in 40% sulfuric acid, a fluorescent product is produced. This product can be extracted by butyl ether and measured quantitatively [115]. The relative order of fluorescence intensities was prednisolone (100), triamcinolone (95), triamcinolone acetonide (60), cortisone (3.7), hydrocortisone (3.5), and progesterone (5.2). 

Triamcinolone, hydrocortisone, prednisolone, cortisone, methylprednisolone, betamethasone, dexamethasone, adrenosterone, fluocortolone, triamcinolone acetonide Hypersil Cl8, 3 pm Acetonitrile-5 mM ammonium acetate, gradient from 17 83 to 38 62 420 mm x 50 pm i.d. 300 mm packed length... 

The introduction of a 16a-hydroxy group into 6a,9-difluoro-prednisolone led to a compound (fluocinolone) with the anticipated favorable biological spectrum, namely high anti-inflammatory activity (35-fold that of hydrocortisone, seven-fold that of triamcinolone) and - in contrast to the C-16 unsubstituted compound - no retention of sodium. The corresponding 16,17-acetonide (fluocinolone acetonide) exhibited 100-fold the anti-inflammatory activity of hydrocortisone, with no sodium retention. In clinical trials, 6a,9-difluoro-16a-hydroxyprednisolone was found to be a potent suppressor of inflammatory conditions such as rheumatoid arthritis, as well as allergic conditions such as asthma, whilst its acetonide proved to be highly effective as topical corticoid. 

The introduction of a 16a-hydroxy-group into 9a-fluoro-prednisolone leads to a compound which is devoid of sodium retention but has anti-inflammatory activity considerably lower than that of the parent compound. The 16a- and 16/7-rnelhyl-9a-fluoro-prednisolones, on the other hand, are more potent than the parent compound yet free of sodium retention. Peculiarly, the conversion of 16a-hydroxy-9a-fluoro-prednisolone to the 16a, 17-acetonide markedly increases topical activity, without significantly affecting oral anti-inflammatory activity. 

Synonyms. Desfluorotriamcinolone Acetonide 16-Hydroxy-prednisolone 16,17-Acetonide. 

Prednisolone Pivalate 463.9 Meclozine Hydrochloride 487.4 Fluclorolone Acetonide... 

Reisch J, Zappel J, Raghu A, Rao R. Photochemical studies part 68. Solid state photochemical investigations of methylprednisolone, prednisolone and triamcinolone acetonide. Acta Pharmaceutica Turcica 1995 XXXV1I 13-17. 

The therapeutic effectiveness of topically applied corticosteroids is attributed primarily to their antiinflammatory activity. The relative efficacy of topical corticosteroids appears to be in the following order hydrocortisone, prednisolone, betamethasone < hydrocortisone valerate or butyrate, betamethasone valerate, triamcinolone acetonide, flucinolone acetonide < betamethasone dipropionate, fluocino-nide. In addition to the nature of the corticosteroid, its solubility, and, to a lesser extent, the concentration used, clinical efficacy is influenced by the formulation of the preparation. Glucocorticoids appear to have greater efficacy when formulated in ointment bases than in cream or lotion vehicles. This could be attributed to the occlusive effect provided by ointments. The application of an occlusive dressing further enhances penetration and persistence of the steroid (reservoir effect) in the stratum corneum. " ... 

So sind das Triamcinolon-acetonid, das 9 a-Fluor-16 a-hydroxy-prednisolon-16 a. 17 a-acetonid,... 

Dehydrogenation with isolated bacterial cell powders have also been reported, 20,21. Triamcinolone has also been obtained from 9a-fluoro-prednisolone (VII)1 by 16-hydroxylation and from triamcinolone acetonide (VI) by hydrolysis with organic acids22 2 . Methods of purification have been patented2. ... 

Reisch, J., Zappel, J., and Rao, A.R.R. (1995) Solid state photochemical investigations of meth-ylprednisolone, prednisolone and triamcmolone acetonide, Acta Phonn. Turc., 37,13-17. 

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