Oral 1.alpha.-hydroxyprevitamin D
AssigneeBone Care International, Inc.
InventorsJoyce C. Knutson, Charles W. Bishop, Charles R. Valliere
Life of this patent
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Abstract
Method of increasing activated vitamin D blood level by administering orally a 1.alpha.-hydroxyprevitamin D or a delayed and sustained release formulation of activated vitamin D or a combination thereof. Both the previtamin D form and the delayed and sustained release activated vitamin D formulation increase vitamin D blood level without significant risk of hypercalcemia associated with other oral dosing of vitamin D forms.
Claims6
A method for treating or preventing psoriasis in a human being displaying or predisposed to psoriasis, said method comprising:
- the step of administering orally to said human being an oral medicament comprising a matrix containing a vitamin D compound which is activated vitamin D or 1.alpha.-hydroxyprevitamin D,
- said matrix having means for releasably binding and for controlled release of said vitamin D compound over a sustained period of time,
- said activated vitamin D is selected from the group consisting of 1.alpha.,24,25-trihydroxyvitamin D.sub.3 ;
- 1.alpha.-hydroxy-vitamin D.sub.3 ;
- 1.alpha.-hydroxy-25-fluoro-vitamin D.sub.3 ;
- 1.alpha.,24-dihydroxy-vitamin D.sub.3 ;
- 1.alpha.,24-dihydroxy-25-fluoro-vitamin D.sub.3 ;
- 1.alpha.,25-dihydroxy-vitamin D.sub.2 ;
- 1.alpha.,24,25-trihydroxy-vitamin D.sub.2 ;
- 1.alpha.-hydroxy-vitamin D.sub.2 ;
- 1.alpha.-hydroxy-25-fluoro-vitamin D.sub.2 ;
- 1.alpha.,24-dihydroxy vitamin D.sub.2 ;
- 1.alpha.,24-dihydroxy-25-fluoro-vitamin D.sub.2 ;
- 1.alpha.,25-dihydroxy-vitamin D.sub.4 ;
- 1.alpha.,24,25-trihydroxy-vitamin D.sub.4 ;
- 1.alpha.-hydroxy-vitamin D.sub.4 ;
- 1.alpha.-hydroxy-25-fluorovitamin D.sub.4 ;
- 1.alpha.,24-dihydroxy-vitamin D.sub.4 ;
- 1.alpha.,24-dihydroxy-25-fluoro-vitamin D.sub.4 ;
- said 1.alpha.-hydroxyprevitamin D selected from the group consisting of 1.alpha.,25-dihydroxy-previtamin D.sub.3 ;
- 1.alpha.,24,25-trihydroxy-previtamin D.sub.3 ;
- 1.alpha.-hydroxy-previtamin D.sub.3 ;
- 1.alpha.,24-dihydroxy-previtamin D.sub.3 ;
- 1.alpha.,24-dihydroxy-25-fluoro-previtamin D.sub.3 ;
- 1.alpha.,25-dihydroxy-previtamin D.sub.2 ;
- 1.alpha.,24,25-trihydroxy-previtamin D.sub.2 ;
- 1.alpha.-hydroxy-previtamin D.sub.2 ;
- 1.alpha.,24-dihydroxy-previtamin D.sub.2 ;
- 1.alpha.,24-dihydroxy-25-fluoro-previtamin D.sub.2 ;
- 1.alpha.,25-dihydroxy-previtamin D.sub.4 ;
- 1.alpha.,24,25-trihydroxy-previtamin D.sub.4 ;
- 1.alpha.-hydroxy-previtamin D.sub.4 ;
- 1.alpha.,24-dihydroxy-previtamin D.sub.4 ;
- and 1.alpha.,24-dihydroxy-25-fluoro-previtamin D.sub.4.
A composition comprising an oral active vitamin D medicament suitable for use in a human, and having enhanced bioavailability to provide higher sustained blood levels of activated vitamin D, said medicament comprising:
- a vitamin D compound which is 1.alpha.-hydroxyvitamin D or 1.alpha.-hydroxyprevitamin D;
- and
- a matrix charged with said vitamin D compound, said matrix releasably binding and controllably releasing said vitamin D compound over a sustained period of time;
- said 1.alpha.-hydroxyvitamin vitamin D is selected from the group consisting of 1.alpha.,24,25-trihydroxyvitamin D.sub.3 ;
- 1.alpha.-hydroxy-vitamin D.sub.3;
- 1.alpha.-hydroxy-25-fluoro-vitamin D.sub.3 ;
- 1.alpha.,24-dihydroxy-vitamin D.sub.3 ;
- 1.alpha.,24-dihydroxy-25-fluoro-vitamin D.sub.3 ;
- 1.alpha.,25-dihydroxy-vitamin D.sub.2 ;
- 1.alpha.,24,25-trihydroxy-vitamin D.sub.2 ;
- 1.alpha.-hydroxy-vitamin D.sub.2 ;
- 1.alpha.-hydroxy-25-fluoro-vitamin D.sub.2 ;
- 1.alpha.,24-dihydroxy vitamin D.sub.2 ;
- 1.alpha.,24-dihydroxy-25-fluoro-vitamin D.sub.2 ;
- 1.alpha.,25-dihydroxy-vitamin D.sub.4 ;
- 1.alpha.,24,25-trihydroxy-vitamin D.sub.4 ;
- 1.alpha.-hydroxy-vitamin D.sub.4 ;
- 1.alpha.-hydroxy-25-fluorovitamin D.sub.4 ;
- 1.alpha.,24-dihydroxy-vitamin D.sub.4 ;
- 1.alpha.,24-dihydroxy-25-fluoro-vitamin D.sub.4 ;
- said 1.alpha.-hydroxyprevitamin D is selected from the group consisting of 1.alpha.,25-dihydroxy-previtamin D.sub.3 ;
- 1.alpha.,24,25-trihydroxy-previtamin D.sub.3 ;
- 1.alpha.-hydroxy-previtamin D.sub.3 ;
- 1.alpha.,24-dihydroxy-previtamin D.sub.3 ;
- 1.alpha.,24-dihydroxy-25-fluoro-previtamin D.sub.3 ;
- 1.alpha.,25-dihydroxy-previtamin D.sub.2 ;
- 1.alpha.,24,25-trihydroxy-previtamin D.sub.2 ;
- 1.alpha.-hydroxy-previtamin D.sub.2 ;
- 1.alpha.,24-dihydroxy-previtamin D.sub.2 ;
- 1.alpha.,24-dihydroxy-25-fluoro-previtamin D.sub.2 ;
- 1.alpha.,25-dihydroxy-previtamin D.sub.4 ;
- 1.alpha.,24,25-trihydroxy-previtamin D.sub.4 ;
- 1.alpha.-hydroxy-previtamin D.sub.4 ;
- 1.alpha.,24-dihydroxy-previtamin D.sub.4 ;
- and 1.alpha.,24-dihydroxy-25-fluoro-previtamin D.sub.4.
Dependencies are inferred from the claim text.