Abstract: A once-a-day controlled release drug delivery system of diltiazem hydrochloride is provided, which is bioequivalent in plasma profile of Cardizem CD. The fast, medium, and slow release fractions are prepared using various compositions and weight gains. The individual fill weights are computed and then are filled into the same capsule using specialized encapsulation equipment using a triple-filling process. A preferred membrane dispersion that is used for preparing the fast release fraction contains 0.2% of sodium lauryl sulfate along with 20% of water soluble plasticizer (triethyl citrate), and 2% silicone dioxide, based on quaternary polymethacrylate on the weight basis. This combination provides an initial pulsatile burst after a lag time of 2 hours, leading to in-vivo bioequivalence. The preferred membrane dispersion that is used for preparing the medium release and the slow release fractions contain 16% of water soluble plasticizer along with 5% silicone dioxide, based on quaternary polymethacrylate.

Abstract: The present invention relates to a process of microfluidization or wet-micronization of hydrophobic drugs in combination with dextrins such as &bgr;-cyclodextrin. The microfluidized particles are useful in controlled swellability, erosion rate-controlled drug delivery systems. The process of microfluidization facilitates reduction of mean particle size of slightly soluble but highly permeable drugs and creates a smooth, latex-like micro-suspension. A blend of swellable polymer and insoluble, hydrophilic excipients granulated with the micro-suspension create a swellable matrix that after compaction erodes uniformly over a 24-hour period. Optimization of drug release is achieved by modification of the geometry of the drug delivery system.

Abstract: A once-a-day controlled release drug delivery system of diltiazem hydrochloride is provided, which is bioequivalent in plasma profile of Cardizem CD. The fast, medium, and slow release fractions are prepared using various compositions and weight gains. The individual fill weights are computed and then are filled into the same capsule using specialized encapsulation equipment using a triple-filling process. A preferred membrane dispersion that is used for preparing the fast release fraction contains 0.2% of sodium lauryl sulfate along with 20% of water soluble plasticizer (triethyl citrate), and 2% silicone dioxide, based on quaternary polymethacrylate on the weight basis. This combination provides an initial pulsatile burst after a lag time of 2 hours, leading to in-vivo bioequivalence. The preferred membrane dispersion that is used for preparing the medium release and the slow release fractions contain 16% of water soluble plasticizer along with 5% silicone dioxide, based on quaternary polymethacrylate.

Abstract: The present invention provides the components for a stable felodipine composition and a process for preparing the composition. The composition includes felodipine, non-covalently bound to &bgr;-cylodextrin, and an optional binder as a moisture carrier component for the migration of hydroxide ions to the non-covalently bound felodipine and &bgr;-cylodextrin. The felodipine composition is combined with a carrier comprising cyclodextrin particles, a water-insoluble alkaline component and a swellable polymer.

Abstract: The present invention relates to a process of microfluidization or wet-micronization of hydrophobic drugs in combination with dextrins such as &bgr;-cyclodextrin. The microfluidized particles are useful in controlled swellability, erosion rate-controlled drug delivery systems. The process of microfluidization facilitates reduction of mean particle size of slightly soluble but highly permeable drugs and creates a smooth, latex-like micro-suspension. A blend of swellable polymer and insoluble, hydrophilic excipients granulated with the micro-suspension create a swellable matrix that after compaction erodes uniformly over a 24-hour period. Optimization of drug release is achieved by modification of the geometry of the drug delivery system.

Abstract: A drug delivery system for diltiazem-HCl comprises:a blend of fast, medium and slow release fractions of a multi-layered diltiazem bead substrate, the fast release fraction comprised of a diltiazem bead substrate layered with a polymeric membrane coating having a membrane coating weight gain of from 14 to 18 percent, the medium release fraction comprised of a diltiazem bead substrate layered with a polymeric membrane coating having a membrane coating weight gain of from 39 to 43 percent, and the slow release fraction comprised of diltiazem bead substrate layered with polymeric membrane coating having a membrane coating weight gain of from 63 to 67 percent, wherein at least one of the polymeric membrane coatings comprises a water-insoluble, slightly permeable polymer and a plasticizer triethyl citrate.

Abstract: There is disclosed a collagen preparation of improved adhesive properties and formed of microparticulate collagen of a particle size of from 0.5 to 2 .mu.m, preferably 0.5 to 1.0 .mu.m preferably submicrosized in a delivery system, such as an aerosol, and thus in sprayable form as a wound dressing alone, or with releasing drugs or other active agents. The microparticulate collagen is formed by ball milling collagen for a time sufficient to form the microparticulate collagen having a particle size of from 0.5 to 2 .mu.m, preferably 0.5 to 1 .mu.m.

Abstract: There is disclosed a collagen preparation of improved adhesive properties and formed of microparticulate collagen of a particle size of from 0.5 to 2 .mu.m, preferably 0.5 to 1.0 .mu.m preferably submicrosized in a delivery system, such as an aerosol, and thus in sprayable form as a wound dressing alone, or with releasing drugs or other active agents. The microparticulate collagen is formed by ball milling collagen for a time sufficient to form the microparticulate collagen having a particle size of from 0.5 to 2 .mu.m, preferably 0.5 to 1 .mu.m.