Abstract: Stabilized transdermal acid sensitive drug formulations and their associated methods of production and use are described. The formulations containing acid sensitive drugs can also an acrylic adhesive, and a pharmaceutically acceptable base. The formulations can further contain other adhesives, permeation enhancers, and other stabilizing compounds such as free radical inhibitors.

Abstract: Drug delivery systems and methods for administering a glucagon-like insulinotropic peptide to the buccal mucosa for transmucosal drug delivery are described. The drug delivery systems comprise a drug composition containing an effective amount of the glucagon-like insulinotropic peptide and an effective amount of a permeation enhancer for enhancing permeation of glucagon-like insulinotropic peptide through the buccal mucosa and means for maintaining the drug composition in a drug transferring relationship with buccal mucosa. These systems can be in free form, such as creams, gels, and ointments, or can comprise a device of determined physical form, such as tablets, patches, and troches. A preferred glucagon-like insulinotropic peptide is GLP-1(7-36)amide.

Abstract: A composition for transmucosally administering a drug to the oral cavity comprises an adhesive layer comprising a hydrophilic polymer having one surface adapted to contact a first tissue of the oral cavity and adhere thereto when wet and an opposing surface in contact with and adhering to an adjacent drug-containing layer comprising an effective amount of a drug and optionally an effective amount of a permeation enhancer, wherein the drug-containing layer is adapted to contact and be in drug transfer relationship with a mucosal tissue of the oral cavity when the adhesive layer contacts and adheres to the first tissue. Preferred drugs include peptides, such as glucagon-like insulinotropic peptides. A method of transmucosally administering a drug to the oral cavity is also disclosed.

Abstract: Drug delivery systems and methods for administering a glucagon-like insulinotropic peptide to the buccal mucosa for transmucosal drug delivery are described. The drug delivery systems comprise a drug composition containing an effective amount of the glucagon-like insulinotropic peptide and an effective amount of a permeation enhancer for enhancing permeation of glucagon-like insulinotropic peptide through the buccal mucosa and means for maintaining the drug composition in a drug transferring relationship with with buccal mucosa. These systems can be in free form, such as creams, gels, and ointments, or can comprise a device of determined physical form, such as tablets, patches, and troches. A preferred glucagon-like insulinotropic peptide is GLP-1(7-36)amide.

Abstract: A method and system for mucosally administering a macromolecular drug to mucosa of the oral cavity is shown. The system comprises an inner drug/enhancer/polymer layer having one surface adapted to contact and adhere to the mucosal tissue of the oral cavity and an opposing surface in contact with and adhering to an overlying inert layer. The inner layer contains from about two to sixty percent by weight of a bile salt enhancer, five to sixty five percent by weight of a hydrophilic polymer which is water soluble or swellable and an effective amount of a macromolecular drug having a molecular weight of at least 500 daltons. Polysaccharides, polypeptides and proteins are preferred forms of macromolecular drugs. The bile salt enhancer facilitates the delivery of macromolecules such as low molecular weight heparin and calcitonin. The polymer serves as a plasticizer to prevent the crystallization and/or aggregation of such macromolecular drugs. Hydroxypropyl cellulose is a particularly suitable polymer.

Abstract: A method and system for mucosally administering a macromolecular drug to mucosa of the oral cavity is shown. The system comprises an inner drug/enhancer/polymer layer having one surface adapted to contact and adhere to the mucosal tissue of the oral cavity and an opposing surface in contact with and adhering to an overlying inert layer. The inner layer contains from about two to sixty percent by weight of a bile salt enhancer, five to sixty five percent by weight of a hydrophilic polymer which is water soluble or swellable and an effective amount of a macromolecular drug having a molecular weight of at least 500 daltons. Polysaccharides, polypeptides and proteins are preferred forms of macromolecular drugs. The bile salt enhancer facilitates the delivery of macromolecules such as low molecular weight heparin and calcitonin. The polymer serves as a plasticizer to prevent the crystallization and/or aggregation of such macromolecular drugs. Hydroxypropyl cellulose is a particularly suitable polymer.

Abstract: A controlled-release, drug-delivery composition which comprises (A) a crosslinked copolymer, capable of swelling in ethanol to give a swollen copolymer containing at least 40% by weight of ethanol, and capable of swelling in water to give a swollen copolymer containing no more than 20% by weight of water, where the swelling ratio (% ethanol: % water) is 2:1 to 22:1, which comprises the copolymerization product of (a) 50 to 99% by weight of said copolymer of a water-insoluble monoolefinic monomer or (a) with 0 to 45% by weight of total monomers of a water-soluble monoolefinic monomer, with (b) 50 to 1% by weight, but not more than 20 mol % of a divinyl or polyvinyl crosslinking agent; and (B) an effective amount of a pharmaceutical medicament is useful for the controlled and prolonged release of drugs when taken orally.

Abstract: Clear, strong, crosslinked polymers are described, which are obtained by copolymerization of (A) 8-70% of a linear or branched polysiloxane of 400-100,000 molecular weight (MW) containing at least two terminal or pendant, polymerizable, vinyl groups per each 5000 MW unit of polysiloxane and which are attached to the polysiloxane through at least two urethane, thiourethane, urea or amide linkages and (B) 30-92% of a mono- or divinyl compound or a mixture of such monomers consisting of 85 to 100% of water insoluble monomers. These polymers are useful in the preparation of hard or soft contact lenses.

Abstract: Non-uniform water-insoluble interpenetrating polymer blend compositions comprising a first permeable water swellable polymer substrate interpenetrated in a gradient substantially normal to the substrate surface by a second less permeable condensation polymer to form a diffusion rate controlling membrane therein. Such compositions are useful as polymers with reduced permeabilities for water and organic solvents and therefore for the controlled delivery of active ingredients such as fragrances and bio-affecting agents into air or aqueous environments, or in membrane separation processes.

Abstract: The disclosure describes an improved process for the preparation of uniform, spherical beads of up to 5 mm diameter of a crosslinked, water-insoluble hydrogel by suspension polymerization in a concentrated aqueous salt solution of 95-30% by weight of a monoolefinic water-soluble monomer containing at least 5% of a hydroxy substituted hydrophilic vinyl monomer with 5-70% by weight of a terminal diolefinic macromer crosslinking agent in the presence of water-insoluble, gelatinous, strong water-bonding inorganic metal hydroxides as suspending agents in the absence of excess alkali. The hydrogels have a host of pharmaceutical and industrial uses.