Method of increasing oral absorption of polar bioactive agents
AssigneeINTERx Research Corporation
InventorsTakeru Higuchi, Toshiaki Nishihata
Life of this patent
Estimating the term…
Abstract
A method and drug form are provided for increasing the oral absorption of polar bioactive agents such as polypeptides by the oral administration of said polar bioactive agents in a suitable pharmaceutically accepted excipient to which has been added a hydroxyaromatic acid or salt as an adjuvant thereof. The adjuvant is present in the drug form in quantities sufficient to be effective in enhancing the rate of oral absorption of the polar bioactive agents.
Claims10
A method for enhancing the rate of absorption of an orally administeredpolypeptide drug having 3 or more residues of amino acid and having a molecular weight of 4000 or less into the bloodstream, said method comprising the steps of preparing a drug form capable of being orally absorbed, said drug form comprising a therapeutically effective dosage amount of said polypeptide drug and an adjuvant of the formula:
- ##STR4## wherein R.sub.1 is CO.sub.2 H,--(CH.sub.2)--COOH, ##STR5## SO.sub.3 H, or a pharmaceutically acceptable salt thereof wherein R.sub.2 is OH, H, a lower alkoxy radical, a lower alkyl radical, a halo radical, or a tri-halo lower alkyl radical, and
- wherein y is an integer of 1 or 2;
- said adjuvant being present in said drug form in a sufficient amount to be effective in enhancing said oral absorption rate and administering said drug form orally to a warm blooded animal.
An orally administered drug form comprising a therapeutically effective amount of a polypeptide drug having 3 or more residues of amino acids and having a molecular weight of 4000 or less and an adjuvant of the Formula ##STR6## wherein R.sub.1 is CO.sub.2 H,--(CH.sub.2)--COOH, ##STR7## or SO.sub.3 H, or a pharmaceutically acceptable sodium or calcium salt thereof wherein R.sub.2 is OH, H, lower alkoxy radical, a lower alkyl radical, a halo radical, or a tri-halo lower alkyl radical, and
- wherein y is an integer of 1 or 2;
- said adjuvant being present in said drug form in sufficient amount to be effective in enhancing the oral absorption rate of said polar bioactive agent.
Dependencies are inferred from the claim text.