Stabilized, dilute aqueous preparation of 1.alpha.,25-dihydroxycholecalciferol for neonatal administration
AssigneeAbbott Laboratories
InventorsNancy M. Conway, Lewis I. Krimen
Life of this patent
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Abstract
1.alpha.,25-Dihydroxycholecalciferol, also known as 1.alpha.,25-dihydroxyvitamin D.sub.3, calcitriol or 1.alpha.,25(OH).sub.2 D.sub.3, occurs naturally in man as the active form of cholecalciferol or vitamin D.sub.3. The natural supply of vitamin D.sub.3 depends on the conversion of 7-dehydrocholesterol to vitamin D.sub.3 in the skin by ultraviolet light. Vitamin D.sub.3 is then converted to calcitriol in a two-step process in the liver and kidney before its acts on its target tissue.
Claims20
A pharmaceutical dosage form of 1.alpha.,25-dihydroxycholecalciferol comprising a therapeutically effective amount of 1.alpha.,25-dihydroxycholecalciferol to prevent hypocalcemia solubilized in water with a nonionic surfactant and stabilized with a combination of a metal ascorbate and a chelating agent in the presence of an inert atmosphere at pH 6.4 to 7.8.
A pharmaceutical composition which is a dilute, stable, aqueous solution of 1.alpha.,25-dihydroxycholecalciferol comprising 1 part by weight of said 1.alpha.,25-dihydroxycholecalciferol, 10,000 parts by weight of sodium ascorbate, 4,000 parts by weight of a polysorbate 20 nonionic surfactant, 1,000 parts by weight of disodium edetate, 1,500 parts by weight of sodium chloride, 7,600 parts by weight of sodium phosphate dibasic, 1,840 parts by weight of sodium phosphate monobasic, water q.s. and nitrogen q.s. and having a pH of between 6.4 and 7.8.
A process for preparing a stable, dilute, aqueous solution of 1.alpha.,25-dihydroxycholecalciferol comprising the steps of:
- preparing a concentrate of said 1.alpha.,25-dihydroxycholecalciferol and a nonionic surfactant under an inert atmosphere;
- preparing an aqueous solution of a metal ascorbate, a chelating agent and a buffering agent under an inert atmosphere, said solution having a pH of from 7.0 to 7.8;
- and, adding said concentrate to said aqueous, buffered solution, with stirring under an inert atmosphere.
Dependencies are inferred from the claim text.