Amphiphilic polysaccharide derivatives
First Claim
1. A composition of matter comprising a polysaccharide covalently bonded to a hydrophobic agent, wherein said hydrophobic agent is a member selected from the group consisting of sterols, deoxycholic acid, chenodeoxycholic acid, lithocholic acid, ursocholic acid, ursodeoxycholic acid, isoursodeoxycholic acid, lagodeoxycholic acid, glycocholic acid, taurocholic acid, glycodeoxycholic acid, glycochenodeoxycholic acid, dehydrocholic acid, hyocholic acid, hyodeoxycholic acid, and mixtures thereof.
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Abstract
Polysaccharides, which are widely used as an anticoagulation drugs, especially heparin, are clinically administered only by intravenous or subcutaneous injection because of their strong hydrophilicity and high negative charge. Amphiphilic heparin derivatives were synthesized by conjugate to bile acids, sterols, and alkanoic acids, respectively. The hydrophobicity of the heparin derivatives depended on the feed mole ratio of heparin to hydrophobic agent. The heparin derivatives were slightly hydrophobic and exhibited good solubility in a water-acetone solvent, as well as water. The heparin derivatives have a high anticoagulant activity. These slightly hydrophobic heparin derivatives can be absorbed in gastric intestinal tract and can be used as oral dosage form. Also, the heparin derivatives can be used for the surface modification to prevent anticoagulation for medical devices such as extracorporeal devices and implanted devices.
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Citations
22 Claims
- 1. A composition of matter comprising a polysaccharide covalently bonded to a hydrophobic agent, wherein said hydrophobic agent is a member selected from the group consisting of sterols, deoxycholic acid, chenodeoxycholic acid, lithocholic acid, ursocholic acid, ursodeoxycholic acid, isoursodeoxycholic acid, lagodeoxycholic acid, glycocholic acid, taurocholic acid, glycodeoxycholic acid, glycochenodeoxycholic acid, dehydrocholic acid, hyocholic acid, hyodeoxycholic acid, and mixtures thereof.
- 7. A pharmaceutical composition comprising (a) a pharmaceutically effective amount of a composition of matter comprising a polysaccharide covalently bonded to a hydrophobic agent, wherein the hydrophobic agent is a member selected from the group consisting of sterols, deoxycholic acid, chenodeoxycholic acid, lithocholic acid, ursocholic acid, ursodeoxycholic acid, isoursodeoxycholic acid, lagodeoxycholic acid, glycocholic acid, taurocholic acid, glycodeoxycholic acid, glycochenodeoxvcholic acid, dehydrocholic acid, hyocholic acid, hyodeoxycholic acid, and mixtures thereof and (b) a pharmaceutically acceptable carrier.
- 14. A method for inhibiting blood coagulation on a medical device that comes in contact with blood comprising coating said medical device with a pharmaceutical composition comprising a polymeric matrix intimately admixed with a composition of matter comprising heparin covalently bonded to a hydrophobic agent, wherein the hydrophobic agent is a member selected from the group consisting of sterols, deoxycholic acid, chenodeoxycholic acid, lithocholic acid, ursocholic acid, ursodeoxycholic acid, isoursodeoxycholic acid, lagodeoxycholic acid, glycocholic acid, taurocholic acid, glycodeoxycholic acid, glycochenodeoxycholic acid, dehydrocholic acid, hyocholic acid, hyodeoxycholic acid, and mixtures thereof.
Specification