Cornell Research Foundation Inc.

Corn Products Development, Inc.

Yeli Zhang

Chih-Chang Chu

Chee-Youb Won

Chaodong Xiao

Wolfgang Bindzus

Vincent R Green

This invention relates to a composition comprising physically modified, partially pregelatinized starch, which is useful as a multi-functional excipient for solid dosage forms, a method of making such composition, and solid dosage forms prepared using the composition. Such composition is characterized by a predominance of particles having both birefringent and non-birefringent portions, a sedimentation volume of between 1.5 and 9 ml/g, and a cold water solubility of between 1 and 8%. This free-flowing starch may have an average particle size greater than 30 &#x3bc;m, and a moisture content of between 5 and 12% by weight. The 500 mg placebo tablet prepared from such composition at 13 kN using a manual tablet press equipped with a 1.11 cm ( 7/16&#x2033;) standard concave punches has a crushing strength of at least 160 Newtons, and a disintegration time of no more than 10 minutes.

Tablet excipient

A hydrogel forming system which comprises a hydrophobic macromer with unsaturated group terminated ends and a hydrophilic polymer which is a polysaccharide containing hydroxy groups which are reacted with unsaturated group introducing compound, is convertible by free radical polymerization to form a hydrogel containing a three dimensional crosslinked polymer network containing hydrophobic and hydrophilic components. Agent can be entrapped in the polymer network, e.g., drugs, macromolecules or synthetic or natural polymers, for controlled release therefrom. In one embodiment, a vascular stent is coated with hydrogel with therapeutic agent entrapped therein.

Hydrogel entrapping therapeutic agent and stent with coating comprising this

A hydrogel forming system which comprises a hydrophobic macromer with unsaturated group terminated ends and a hydrophilic polymer which is a polysaccharide (e.g. dextran) containing hydroxy groups which are reacted with unsaturated group introducing compound, is convertible by free radical polymerization to form a hydrogel containing a three dimensional crosslinked polymer network containing hydrophobic and hydrophilic components. Agent can be entrapped in the polymer network, e.g., drugs, macromolecules or synthetic or natural polymers, for controlled release therefrom.

Hydrogel-forming system with hydrophobic and hydrophilic components

A hydrogel forming system which comprises a hydrophobic macromer with unsaturated group terminated ends and a hydrophilic polymer which is a polysaccharide (e.g., dextran) containing hydroxy groups which are reacted with unsaturated group introducing compound, is convertible by free radical polymerization to form a hydrogel containing a three dimensional crosslinked polymer network containing hydrophobic and hydrophilic components. Agent can be entrapped in the polymer network, e.g., drugs, macromolecules or synthetic or natural polymers, for controlled release therefrom.

A hydrogel forming system which comprises a hydrophobic macromer with unsaturated group terminated ends and a hydrophilic polymer which is a polysaccharide containing hydroxy groups which are reacted with unsaturated group introducing compound, is convertible by free radical polymerization to form a hydrogel containing a three dimensional crosslinked polymer network containing hydrophobic and hydrophilic components. Preferably, the hydrophobic polymer is prepared by reacting the hydroxyls of a diol obtained by converting hydroxy of terminal carboxylic acid group of poly(lactic acid) to aminoethanol group, with an unsaturated group introducing compound which is acryloyl chloride or isocyanate having an unsaturated group at one end of the molecule. Preferably, the hydrophilic polymer is dextran wherein one or more hydroxyls in a glucose unit of the dextran is (are) reacted with an unsaturated group introducing compound which is acryloyl chloride or isocyanate having an unsaturated group at one end of a molecule. Agent can be entrapped in the polymer network, e.g., drugs, water-soluble macromolecules or synthetic or natural polymers, for controlled release therefrom.

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Somerville, NJ, United States of America

Yeli Zhang