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Method of increasing oral absorption of polar bioactive agents

  • US 4,462,991 A
  • Filed: 06/11/1982
  • Issued: 07/31/1984
  • Est. Priority Date: 03/07/1980
  • Status: Expired due to Fees
First Claim
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1. 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 R1 is CO2 H,--(CH2)--COOH, ##STR5## SO3 H, or a pharmaceutically acceptable salt thereof wherein R2 is OH, H, a lower alkoxy radical, a lower alkyl radical, a halo radical, or a tri-halo lower alkyl radical, andwherein 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.

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