Additives dexamethasone acetate

Dexamethasone acetate (Dalalone DP, Forest, Decadron-LA, Merck) and Dexamethasone sodium phosphate (Merck) are available as a suspension or a solution. These dexamethasone formulations contain creatine or creatinine as additives. 

A large number of solvates have been reported, especially for steroids and antibiotics. It has been observed that cortisone acetate and dexamethasone acetate can be crystallized as 10 different solvates. Dirithromycin, a semisynthetic macrolide antibiotic, crystallizes in two anhydrous polymorphic forms and in at least nine stoichiometric solvate forms. Six of the known solvates are isomorphic, having nearly identical x-ray powder diffraction patterns [76]. In addition to the anhydrate and dihydrate, erythromycin also forms solvates with acetone, chloroform, ethanol, n-butanol, and/-propanol [77]. 

A masked study using male volimteers compared ocular pressure elevations with dexamethasone phosphate 0.1%, fluorometholone alcohol 0.1%, and medrysone 1% applied four times daily for 6 weeks. Figure 12-3 shows the relative ability of these steroids to raise lOP. At the end of 6 weeks of treatment, the mean pressure increases fiar dexamethasone, fluorometholone, and medrysone were 63.1%, 33.8%, and 8.3%, respectively. Additional studies have compared the effects of fluorometholone alcohol suspension 0.25% with dexamethasone sodium phosphate solution 0.1% in steroid-responsive patients. Subjects received the medication in one eye four times daily for up to 6 weeks. Although both drugs elevated lOP, mean pressure increases from baseline in eyes treated with fluorometholone were significantly lower than those in eyes treated with dexamethasone at weeks 2,4, and 6. Further studies are needed to compare the effects of the alcohol and acetate derivatives of fluorometholone on lOP in both nonsteroid and steroid responders. 

Intermediate 20-5 is next subjected to the sequence used to incorporate a 9a-fluoro group (see Scheme 7.14) to afford 21-1 (Scheme 7.21). Hydrolysis of the acetal groups with mild acid restores the carbonyl groups at C3 and C20 (21-2). Dehydrogenation of this last intermediate by means of selenium dioxide introduces an additional double bond in ring A this product, dexamethasone (21-3), is yet another widely used corticoid. 

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