Abstract: Methods for enhancing the release and/or absorption of poorly water soluble active agents are described herein. The method involves dissolving, melting, or suspending a poorly water soluble active agent in one or more molten fatty acids, conjugated fatty acids, (semi-) solid surfactants of high HLB value, and/or hydrophilic polymers. The molten active agent mixture is then suspended and homogenized in a hydrophilic or lipophilic carrier to form microparticles suspended in the hydrophilic or lipophilic carrier. The particles suspended in the hydrophilic or lipophilic carrier can be encapsulated in a hard or soft gelatin or non-gelatin capsule. It is believed that the microparticles produced by the method described above will exhibit enhanced dissolution profiles. In vitro release studies of formulations containing cilostazol and fenofibrate showed 100% dissolution of cilostazol in 15 minutes and over 90% dissolution of fenofibrate in 35 minutes.

Abstract: A gel mass is provided that is useful for manufacturing enteric soft capsules without coating.

Abstract: A matrix formulation for a soft chewable capsule is provided which includes a gel-forming composition, a plasticizer, a polymer modifier, and water. The polymer modifier may be a carboxylic acid or other organic compound that alters the physical and/or chemical properties of the capsule formulation. A chewable soft capsule is also provided, having enhanced organo-leptic and processing properties. An active material may be delivered to a user using this dosage form. A method of forming the chewable soft capsule is also provided.

Abstract: A gel mass is provided that is useful in manufacturing enteric soft or hard capsules, or enteric tablets without coating.

Abstract: Gastric resistant film-forming compositions are described herein. The composition comprises a gastric resistant natural polymer, a film-forming natural polymer, and optionally a gelling agent. Suitable gastric resistant natural polymers include polysaccharides such as pectin and pectin-like polymers. The film-forming composition can be used to prepare soft or hard shell gelatin capsules which can encapsulate a liquid or semi-solid fill material or a solid tablet (Softlet®) comprising an active agent and one or more pharmaceutically acceptable excipients. Alternatively, the composition can be administered as a liquid with an active agent dissolved or dispersed in the composition. The compositions are not only gastric resistant but may also prevent gastric reflux associated with odor causing liquids, such as fish oil or garlic oil, encapsulated in a unit dosage form and esophageal irritation due to the reflux of irritant drugs delivered orally.

Abstract: Methods for enhancing the release and/or absorption of poorly water soluble active agents are described herein. The method involves dissolving, melting, or suspending a poorly water soluble active agent in one or more molten fatty acids, conjugated fatty acids, (semi-) solid surfactants of high HLB value, and/or hydrophilic polymers. The molten active agent mixture is then suspended and homogenized in a hydrophilic or lipophilic carrier to form microparticles suspended in the hydrophilic or lipophilic carrier. The particles suspended in the hydrophilic or lipophilic carrier can be encapsulated in a hard or soft gelatin or non-gelatin capsule. It is believed that the microparticles produced by the method described above will exhibit enhanced dissolution profiles. In vitro release studies of formulations containing cilostazol and fenofibrate showed 100% dissolution of cilostazol in 15 minutes and over 90% dissolution of fenofibrate in 35 minutes.

Abstract: Methods for enhancing the release and/or absorption of poorly water soluble active agents are described herein. The method involves dissolving, melting, or suspending a poorly water soluble active agent in one or more molten fatty acids, conjugated fatty acids, (semi-) solid surfactants of high HLB value, and/or hydrophilic polymers. The molten active agent mixture is then suspended and homogenized in a hydrophilic or lipophilic carrier to form microparticles suspended in the hydrophilic or lipophilic carrier. The particles suspended in the hydrophilic or lipophilic carrier can be encapsulated in a hard or soft gelatin or non-gelatin capsule. It is believed that the microparticles produced by the method described above will exhibit enhanced dissolution profiles. In vitro release studies of formulations containing cilostazol and fenofibrate showed 100% dissolution of cilostazol in 15 minutes and over 90% dissolution of fenofibrate in 35 minutes.

Abstract: A hydrophilic vehicle-based dual controlled-release matrix system, suitable for encapsulation in hard or soft capsules, has been developed. The matrix is in the form of a solution or a suspension, which allows for easier formulation of low dose compounds. The matrix includes two rate controlling barriers for the controlled release of one or more pharmaceutically active agents. The primary rate controlling barrier includes a hydrophilic vehicle. The primary rate controlling barrier can further comprise one or more solvents which are miscible with the hydrophilic vehicle. The secondary rate controlling barrier includes a hydrogel-forming polymeric material dissolved or dispersed in the hydrophilic vehicle. The presence of the hydrogel-forming polymeric material makes extraction of the drug from the dosage form more difficult. This feature could be beneficial in preventing or minimizing the misuse of dosage forms which contain drugs which are prone to abuse.

Abstract: Liquid orlistat-containing fill materials suitable for encapsulating in hard or soft capsules are described herein. The fill material contains orlistat dissolved in one or more medium chain triglycerides or medium chain partial triglycerides, one or more citrate esters, and combinations thereof. The fill material can also contain one or more pharmaceutically acceptable excipients. In one embodiment, the fill material is substantially free of surfactants. The fill material can be encapsulated in hard or soft, gelatin or non-gelatin capsules. The capsules may be coated to modify release of orlistat from the capsule. Alternatively, the fill material can be encapsulated in an enteric capsule, wherein the enteric polymer is a component of the capsule shell, rather than a coating over the capsule shell. The fill materials are stable at elevated temperatures over an extended period of time and allow for high loadings of orlistat (e.g., 20% w/w or higher).

Abstract: A lipophilic vehicle-based dual controlled-release matrix, suitable for encapsulation in hard or soft capsules, has been developed. The matrix is in the form of a suspension, which allows for easier formulation of low dose compounds and/or compounds which are moisture sensitive. The matrix includes two rate controlling barriers for the controlled release of one or more pharmaceutically active agents. The primary rate controlling barrier includes a relatively lipophilic oily vehicle. The primary rate controlling barrier may further comprise or more excipients, dissolved in the lipophilic vehicle, which themselves have rate controlling properties. The secondary rate controlling barrier is a hydrogel-forming polymeric material which is dispersed in the primary rate controlling barrier. As the primary rate controlling barrier breaks down, the pharmaceutically active agent is slowly released and the surrounding aqueous media begins to percolate into the polymer matrix.

Abstract: A matrix formulation for a soft chewable capsule is provided which includes a gel-forming composition, a plasticizer, a polymer modifier, and water. The polymer modifier may be a carboxylic acid or other organic compound that alters the physical and/or chemical properties of the capsule formulation. A chewable soft capsule is also provided, having enhanced organo-leptic and processing properties. An active material may be delivered to a user using this dosage form. A method of forming the chewable soft capsule is also provided.

Abstract: A matrix formulation for a soft chewable capsule is provided which includes a gel-forming composition, a plasticizer, a polymer modifier and water. The polymer modifier may be a carboxylic acid or other organic compound that alters the physical and/or chemical properties of the capsule formulation. A chewable soft capsule is also provided, having enhanced organo-leptic and processing properties. An active material may be delivered to a user using this dosage form. A method of forming the chewable soft capsule is also provided.

Abstract: A film-forming composition comprising a hydrocolloid, a plasticizer, and water is described. A process and apparatus for producing a non-gelatin film comprising a hydrocolloid, a plasticizer, and water is also disclosed. The process includes combining at least one non-gelatin hydrocolloid, water, and at least one plasticizer into a substantially homogeneous film-forming composition comprising at least about 40 percent water by weight. A substantial portion of the water is then extracted from the film-forming composition to form a dried portion having a water content of less than or equal to about 25 percent by weight. The dried portion of the film-forming composition is formed into a film. A film produced according to the process preferably has a tensile strength at rupture of at least about 0.4 N/mn2, and a percent elongation of at least about 50 percent at rupture at room temperature.

Abstract: A film-forming hydrocolloid composition comprising kappa carrageenan, iota carrageenan, a bulking agent, plasticizer and water is described. The ratio of bulking agent to total carrageenan is from about 1:1 to 20:1. Kappa carrageenan is present in an amount of less than or equal to 50% by weight of total carrageenan present. To form the composition, all dry materials are mixed and added to a heated mixture of all liquid materials. The final mixture is heated until a composition free of particulate materials is formed. The formed composition can be cast or extruded into ribbons, films, sheets, tubes or the like, for encapsulating wet or dry materials including medicinal dosage forms, nutritional supplements, cosmetics, bath oils and gels, and paint balls.

Abstract: The present invention is a process for coloring gelatin-based formulations involving adding a saturated fatty acid to the gelatin-based formulation along with lake pigment, whereby the saturated fatty acid is added in an amount so as to prevent cross-linking between the gelatin-based formulations and the aluminum cations released by the lake pigments. Preferably, this amount is about 10% to about 300% by weight of the added lake pigment content. With this process, the resulting colored gelatin exhibits acceptable machineability characteristics and disintegration. As an example, the colored gelatin produced by this process has a viscosity of less than approximately 10,000 cP at about 60° C. Additionally, the present invention is a gelatin-based formulation made from the above-described process. The gelatin-based formulation includes gelatin, lake pigment(s), and a sufficient amount of fatty acid to prevent cross-linking between the gelatin and the cations released from the lake pigment(s).

Abstract: A medicine tablet is described as a new article of manufacture. The tablet is enrobed in a gelatin coating formed by application of respective layers of elastic gelatin film to opposite sides of the tablet. The applied gelatin layers conform tightly to the tablet surface, bond securely to the tablet, and are sealed together in essentially edge-to-edge manner at a seal line which extends around the tablet at a desired place on the tablet. The gelatin layers can be colored differently from the tablet and differently from each other. A range of formulations are described for film which can be peelable from a tablet or other product core, and for films which bond to the core. A presently preferred formulation for producing tablets having a bonded tamper-evident coating comprises a water-based gelatin preparation having about 45% gelatin and about 9% plasticizer (glycerin and/or sorbitol) by weight, Method and apparatus for producing such new products are also described.

Abstract: The present invention comprises chewable, soft gelatin capsules having a sheath formed of a mixture of a low bloom and a medium bloom gelatins, a plasticizer, water, and preferably a moisture retention agent to enhance the machinability and integrity of the sheath composition; and a fill of an active material in a carrier liquid.

Abstract: Liquid softgel fill formulations containing ibuprofen in free acid form, and softgel capsules comprised of a gelatin sheath enclosing such fill formulations, are prepared by dissolving more than 30% of ibuprofen in free acid form in polyethylene glycol and at least 10% by weight of a polyvinylpyrrolidone having an average molecular weight of from about 2,000 to about 54,000. The formulations may also include a surfactant to increase the bioavailability of the ibuprofen.

Abstract: Gelatin-free capsule for use in oral administration of medicines, cosmetic or bath applications, or dietary supplements can be prepared from compositions comprising a) 8-50% by weight of water-dispersible or water-soluble plasticizer, b) 0.5 to 12% by weight &kgr;-carrageenan, c) 0 to 60% dextrins, and d) 1% to 95% by weight water, with the &kgr;-carrageenan comprising at least 50% by weight of all gums forming or contributing to formation of thermoreversible gels in the composition. A capsule for oral administration or cosmetic application may comprise a fill material to be administered to a patient or subject and a capsule, the capsule comprising an aqueous based film comprising a) water-dispersible or water-soluble plasticizer, and b) carrageenan, with the carrageenan comprising at least 50% or 75% by weight of &kgr;-carrageenan, and the carrageenan comprising at least 50% or 75% by weight of all gums which form or contribute to the formation of thermoreversible gels.

Abstract: A device, and a method for forming a softgel having multiple gelatin layers and softgels having multiple gelatin layers are disclosed. In particular there is provided a device for forming a gelatin sheet having at least two gelatin layers. Each gelatin layer has a thickness. The device comprises a gelatin spreader box which includes at least one opening for extruding a gelatin sheet. The device also includes a first and a second height adjustable gate disposed at least partially across the opening; and a first and a second height adjustment control. Adjustment of the first height adjustment control varies the height of the first gate and adjustment of the second height adjustment control varies the height of the second gate, thereby controlling the thickness of the at least two gelatin layers.