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US 5,376,645 AGranted
Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof
AssigneeUniversity of Kansas
InventorsValentino J. Stella, Roger Rajewski
Life of this patent
Estimating the term…
Abstract
Sulfoalkyl ether cyclodextrin derivatives and their use as solubilizing agents for water insoluble drugs for oral, intranasal, or parenteral administration are disclosed.
Claims47
A cyclodextrin derivative composition which comprises a cyclodextrin derivative of formula ##STR3## wherein:
- n is 4, 5 or 6;
- R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.9 are each, independently, O.sup.- or a O-(C.sub.2-6 alkylene)-SO.sub.3.sup.- group, and at least one of R.sub.1 and R.sub.2 is, independently, said O-(C.sub.2-6 alkylene)-SO.sub.3.sup.- group;
- and
- S.sub.1, S.sub.2, S.sub.3, S.sub..sub.4, S.sub.5, S.sub.6, S.sub.7, S.sub.8 and S.sub.9 are each, independently, a pharmaceutically acceptable cation, and wherein said composition contains less than about 50% of underivatized cyclodextrin.
1 more element
A composition comprising a drug complexed to a cyclodextrin derivative of formula (2):
- ##STR4## wherein:
- n is 4, 5 or 6;
- R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.9 are each independently O.sup.- or a O-(C.sub.2-6 alkylene)-SO.sub.3.sup.- group, and at least one of R.sub.1 and R.sub.2 is, independently, said O-(C.sub.2-6 alkylene)-SO.sub.3.sup.- group;
- and
- S.sub.1 to S.sub.9 are each, independently, a pharmaceutically acceptable cation;
- wherein said composition contains not more than about 50 wt. % of underivatized cyclodextrin.
3 more elements
A pharmaceutical composition for oral administration comprising a pharmaceutically, orally suitable carrier and a clathrate complex comprising a drug complexed to a cyclodextrin derivative of formula (2):
- ##STR5## wherein:
- n is 4, 5 or 6;
- R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.9 are each independently O.sup.- or a O-(C.sub.2-6 alkylene)-SO.sub.3.sup.- group, and at least one of R.sub.1 and R.sub.2 is, independently, said O-(C.sub.2-6 alkylene)-SO.sub.3.sup.- group;
- and
- S.sub.1 to S.sub.9 are each, independently, a pharmaceutically acceptable cation;
- wherein said composition contains not more than 50 wt. % of underivatized cyclodextrin.
3 more elements
Dependencies are inferred from the claim text.