Multi-day delivery of biologically active substances

摘要

Compositions and methods for modifying biologically active substances to achieve multi-day delivery of such substances, particularly through oral or parenteral administration, are disclosed. The compositions include the biologically active substance conjugated to a carrier having a suitably long half life, typically more than one day, wherein the conjugate optionally contains a spacer linking the carrier to the biologically active substance. Pharmaceutical formulations of the conjugates are also disclosed, as are methods of extending delivery of a single dose of a biologically active substance for more than one day.

主权项

1. An oral pharmaceutical dosage form comprising a drug linked to a carrier by a spacer, wherein: (1) the drug is hydromorphone, zetia, lipitor, crestor, atacand, ethinyl estradiol, 17 beta-estradiol, levonorgestrel, norgestimate, norethisterone and rotigotine; (2) the carrier is pimozide, tamoxifen, fluoxetine, linoleic acid, zeaxanthin, eicosapentaenoic acid, chloroquine, or hydroxychloroquine; and (3) the spacer is hydrolyzable or enzymatically cleavable in the gastrointestinal tract of a patient ingesting the dosage form.