Cortisone acetate

Acetoxy-17a-hydroxy-5a-pregnane-3,l 1,20-trione (40) is brominated in acetic acid under equilibrating conditions to give a solution of the 2a,4a-di-bromo compound (41). This is reduced by chromous chloride without further treatment, to the 4a-bromo compound (42). The recrystallized bromo compound (42) is then dehydrobrominated via the semicarbazone (43) which is converted without isolation into cortisone acetate (44) by treatment with pyruvic acid ... 

Further development of the column with 25% ethyl acetate in benzene produces 2.5 g of material, which on repeated crystallization yields 0.22 g of 17a,21-dihydroxypregn-4-ene-3,ll,20-trione 21-acetate mp 248-251°. Identity with cortisone acetate is established by a comparison of infrared spectra. Elution of the column with 30 % ethyl acetate in benzene gives after crystallization, 0.21 g of ll/9,17a,21-trihydroxypregn-4-ene-3,20-dione 21-acetate mp 219-222°. 

The Mattox Rearrangement Cortisone acetate (10 g) is suspended in dry methanolic hydrogen chloride (400 ml, 0.52 N). After 10 min of agitation the material dissolves completely to give a yellow solution which is then kept at 25° for 48 hr. Sodium acetate (22 g) in water (60 ml) is added and the solvent removed in vacuo to a volume of 75 ml. Water (100 ml) is added, and... 

The separated aqueous layer is extracted with chloroform and the eombined chloroform solution washed with water and evaporated to a volume of 10 ml in vacuo. 5 % Aqueous potassium carbonate (10 ml) is added and the mixture stirred 1 hr at room temperature. The chloroform is distilled under reduced pressure and the resulting crystalline product filtered, washed with water and methanol, and dried to give 82 mg (79 %) of the 3-ethylenedioxy derivative of cortisone acetate mp 248-260° (dec). 

A solution of 1.0 g of A -3,11-diketo-20-cyano-21-acetoxy-pregnene in 10 cc of benzene is treated with 1.0 g of osmium tetroxide and 0.43 g of pyridine. After standing at room temperature for 18 hours, the resulting solution is treated successively with 50 cc of alcohol, and with 50 cc of water containing 2.5 g of sodium sulfite. The mixture is stirred for 30 hours, filtered, and the filtrate acidified with 0.5 cc of acetic acid and concentrated to small volume in vacuo. The aqueous suspension is then extracted four times with chloroform, the chloroform extracts are combined, washed with water and concentrated to dryness in vacuo. Recrystallization of the residue from acetone gives 3,11,20-triketo-17(a)-21-dihydroxy-pregnane MP 227° to 229°C. This compound is then treated with acetic anhydride and pyridine for 15 minutes at room temperature to produce 3,11,20-triketo-17(a)-hydroxy-21-acetoxy-pregnane or cortisone acetate. 

Cortisone acetate Demegestone Fluocortolone Medrogestone Norethindrone Chromic anhydride Fludiazepam HCI Nimetazepam Sulpro stone Cinchonidine Melphalan Cinnamoyl chloride Cinnarizine... 

The Rast method uses camphor (Ci0Hi O) as a solvent for determining the molar mass of a compound. When 2.50 g of cortisone acetate is dissolved in 50.00 g of camphor (kf = 40.0°C/m), the freezing point of the mixture is determined to be 173.44°C that of pure camphor is 178.40°C. What is the molar mass of cortisone acetate ... 

Cortone (Banyu) Scheroson (Schering) USA Cortisone Acetate (Merck) Cortone Acetat (Merck)... 

Cortisone acetate has been incorporated into several polyanhydrides (15). The rates of release of cortisone acetate from microcapsules of poly(terephthaUc acid), poly(terephthaUc acid-sebacic acid) 50 50, and poly(carboxyphenoxypropane-sebacic acid) 50 50 are shown in Fig. 8. These microcapsules were produced by an interfacial condensation of a diacyl chloride in methylene chloride with the appropriate dicarboxylic acid in water, with or without the crosslinking agent trimesoyl chloride. This process produces irregular microcapsules with a rough surface. The release rates of cortisone acetate from these microcapsules varied correspondingly with the rate of degradation of the respective polyanhydrides. It can be expected that the duration of release of cortisone acetate from solid microspheres, such as those produced by the hot-melt process, would be considerably longer. 

FIGURE 8 Release of cortisone acetate from 10% loaded microspheres of various polyanhydrides. The microspheres were prepared by an interfacial condensation. Details of the experimental procedure are described in the text. 

JE Carless. Dissolution and crystal growth in aqueous suspension of cortisone acetate. J Pharm Pharmacol... 

Recommended starting total daily doses are hydrocortisone 15 mg, cortisone acetate 20 mg, or prednisone 2.5 mg (Table 18-2). Two-thirds of the dose is given in the morning, and one-third is given in the evening. 

A physician prescribes an ophthalmic suspension to contain 100 mg of cortisone acetate in 8 mL of normal saline solution (NSS). The pharmacist has a 2.5% suspension of cortisone acetate in NSS. How many milliliters of this and how many milliliters of NSS should be used in preparing the medication order ... 

Thus, a suspension of cortisone acetate of desired strength can be obtained by mixing equal parts (i.e., 1.25 parts or 4 mL each) of 2.5% suspension and normal saline. 

Hydrocortisone is available orally. Other corticosteroids also available orally include prednisolone, betamethasone, cortisone acetate, methylprednisolone, dexamethasone and fluocortolone. 

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