Stabilized hydroxyvitamin D
0 Assignments
0 Petitions
Accused Products
Abstract
The invention provides a stabilized 1α-hydroxyvitamin D (“SHVD”) which is particularly well suited for pharmaceutical formulations.
-
Citations
95 Claims
-
1-41. -41. (canceled)
-
42. A method of making stabilized 1α
- -hydroxyvitamin D2 comprising;
a) tosylating the hydroxy group in the 3-position of a starting material which is a vitamin D compound to which a hydroxy is to be added in the 1α
-position;
b) converting the tosylated form to a cyclovitamin;
c) hydroxylating the cyclovitamin in the 1α
-position;
d) converting the cyclovitamin to the cis and trans vitamin forms;
e) irradiating the trans vitamin form to yield the cis form;
f) recrystallizing the cis form in an organic solvent, g) milling the recrystallized cis form into a powder and vacuum oven drying the recrystallized form for 72-120 hours and at 55°
C. to yield the stabilized 1α
-hydroxyvitamin D2. - View Dependent Claims (43, 50)
- -hydroxyvitamin D2 comprising;
-
44-50. -50. (canceled)
-
51-78. -78. (canceled)
-
79. A pharmaceutical composition consisting essentially of 1α
- -hydroxyvitamin D2 in a pharmaceutically acceptable carrier, wherein, relative to the amount of 1α
-hydroxyvitamin D2 present in the composition,(i) impurities are present at no more than 2% (w/w) as determined by HPLC;
(ii) no single impurity is present in an amount greater than 0.5% (w/w); and
(iii) residual solvents from the process used to prepare the 1α
-hydroxyvitamin D2 are present in an amount of no more than 0.5% (w/w). - View Dependent Claims (80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92)
- -hydroxyvitamin D2 in a pharmaceutically acceptable carrier, wherein, relative to the amount of 1α
-
94. A process for making a pharmaceutical composition comprising combining a pharmaceutically acceptable carrier with a stabilized 1α
- -hydroxyvitamin D2 characterized by a purity equal to or greater than 98% by a weight-based HPLC assay, residual solvents of 0.5% or less, a total impurity of 1.5% or less, and no single impurity of greater than 0.5%.
- View Dependent Claims (95)
Specification