Prednisolone-21-acetate

Chemical Name 11/3,17,21-Trihydroxypregna-1,4-diene-3,20-dione 21-acetate Common Name — 

Trade Name Manufacturer Country Year Introduced 

To a solution of 0.85 gram of 1,4-pregnadiene-11, 17a,21-triol-3,20-dione (prednisolone) in 5 ml of pyridine are added 3 ml of acetic anhydride. The reaction mixture is allowed to stand at room temperature overnight and is then diluted with ice water. The resulting precipitate is filtered from the mixture and recrystallized from acetone-hexane. There is recovered 0.45 gram of 1,4-pregnadiene-11 3,17a,21-triol-3,20-dione 21-acetate, IMP 235°-239°C. On recrystallization, the MP rose to 237°-239°C. 

Chemical Name 11 j3,17,21 -Tritiydroxypregna-1,4-dlene-3,20-dione 21 -acetate Common Name — 

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Prednisolone acetate (21-acetoxypregna-l,4-diene-ll3-17a-diol-3,20-dione) [52-21-1] M 402.5, m 237-239 , 240-242°, 240-243 , 244 , [a]], +116° (c 1, dioxane). Recrystd from EtOH, Mc2CO, Me2CO-hexane, and has UV 243nm in EtOH. [Joly et al. Bull Soc Chim Fr 366... 

Dehydration of prednisolone acetate (175b) yields the corresponding 9,11 olefin. As a variation on the chemistry we have seen previously, this olefin is allowed to react with chlorine in the presence of lithium chloride. If this addition is assumed to proceed by the customary mechanism, the first intermediate should be the 9a,11a-chioronium ion. Axial attack by chloride anion from the 110 position will lead to the observed stereochemistry of the product dichlorisone (240). ... 

Oxyphenisatin acetate Pancuronium bromide Prednisolone acetate Quingestanol acetate Sulfacetamide Testosterone 17/3[Pg.1609]

Suspension. If the drug is not sufficiently soluble, it can be formulated as a suspension. A suspension may also be desired to improve stability, bioavailability, or efficacy. The major topical ophthalmic suspensions are the steroid anti-inflammatory agents prednisolone acetate, dexamethasone, fluorometholone, and rimex-olone. Water-soluble salts of prednisolone phosphate and dexamethasone phosphate are available however, they have a lower steroid potency and are poorly absorbed. 

A Kupferman, HM Leibowitz. (1974). Topically applied steroids in comeal disease. IV. The role of drug concentration in stromal absorption of prednisolone acetate. Arch Ophthalmol 91 377-380. 

Econopred (Alcon), Econopred Plus (Alcon), Precf M/cf (Allergan), Pred Forte (Allergan), Prednisolone Acetate Ophthalmic (Falcon)... 

The system just described has been modified to identify corticosteroidal salts, including cortisone acetate. The solvent is a saturated solution of formamide in a 1 1 mixture of benzene and chloroform. Development is descending, until the solvent front has advanced about 22 cm [2,125], and the spot location is the same as described for the preceding method. The reported Rf values were cortisone acetate = 0.80, hydrocortisone acetate = 0.59, prednisone acetate = 0.74, and prednisolone acetate = 0.49. 

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