Polyestradiol phosphate

Therapeutic Function Estrogen Chemical Name Estradiol phosphate polymer Common Name Polymeric ester of phosphoric acid and estradiol Structural Formula r 

3 g of estradiol was dissolved in 75 ml of anhydrous pyridine. The solution was cooled to -10°C, whereupon a solution of 1.1 ml of phosphorus oxychloride in 10 ml of anhydrous Pyridine was added with agitation. After the addition, which required 7 minutes, the reaction mixture was kept at -10°C for a further period of 3 hours, and then it was left standing at room temperature for 15 hours. A clear solution thus resulted, to which finely crushed ice was then added. The resulting solution was evaporated in vacuum to dryness. After drying in a vacuum desiccator, 3.8 g of a white powder was obtained. This powder was suspended in 2 ml of pyridine, and 25 ml of 0.5 N sodium hydroxide was added, whereupon a solution was obtained which was then diiuted with water to 100 ml. 

The solution was then dialyzed through a cellophane membrane against 4 iiters of water for 10 hours, with stirring. The dialysis was repeated 2 additional times, with fresh amounts of water. To the dialyzed solution there was added 2 mi of 1 N hydrochloric acid, whereupon polyestradiol phosphate was precipitated as a white bulky precipitate. This was centrifuged off and washed repeatedly with 0.1 N hydrochloric acid. Thereafter it was dried in a vacuum desiccator. The yield was 3 g of polyestradiol phosphate. The analysis shows 0.65% of water, 1.35% of pyridine and 9,3% of phosphorus (calculated on a dry sample). 

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Estradiol valerate Estramustine phosphate Estriol succinate Polyestradiol phosphate Estradiol-17/3... 

Fosfestrol is indicated in the treatment of carcinoma of the prostate. It is a synthetic non-steroidal estrogen which is dephosphorylated to stilboestrol. Polyestradiol phosphate is an oestrogen with sustained activity that is exclusively used for prostate cancer. It is stored in tissues and slowly dephosphorylated to estrogen. 

The solution was then dialyzed through a cellophane membrane against 4 liters of water for 10 hours, with stirring. The dialysis was repeated 2 additional times, with fresh amounts of water. To the dialyzed solution there was added 2 ml of 1 N hydrochloric acid, whereupon polyestradiol phosphate... 

Estradurin Injection (Polyestradiol phosphate, Wyeth-Ayerst Labs) uses Niacinamide (12.5 mg/ ml) as a solubilizing agent. Hydeltrasol also contains niacinamide. The concept of hydrotropic agents to increase water solubility has been tried on several compounds, including proteins. " " " ... 

Estradurin polyestradiol phosphate, estramustine [ban, inn. usan] (estramustine sodium phosphate estramustine phosphate sodium Leo 275 ... 

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