Abstract: The present invention provides a process for preparing hardshell gelatin capsule reducing the static electricity and enhancing the lubrication of film having good film distribution in capsule comprising the steps of: i) preparing an emulsion containing 0.4˜0.8 part by weight of diacetylated monoglycerides, 0.05˜0.1 part by weight of sodium lauryl sulfate, and 0.005˜0.01 part by weight of colloidal silicon dioxide; ii) adding the emulsion to gelatin solution containing 100 part by weight of gelatin; iii) mixing and homogenizing the resulting solution; iv) adjusting viscosity of mixture; v) allowing the obtained product to stand; and vi) forming a hardshell gelatin capsule therefrom.

Abstract: The present invention is directed to film coating systems for use on oral dosage forms such as compressed tablets and orally-ingestible substrates which have improved pearlescent qualities. The film coating systems can be applied either directly to a substrate or after the substrate has been coated with a subcoat. In preferred aspects, the pearlescent film coating is prepared as a dry powder mixture containing a cellulosic polymer, a detackifier, a gloss enhancer, and a pearlescent pigment. Film coating compositions containing an aqueous suspension of the powder mixtures, methods of applying the coatings to substrates and the coated substrates are also disclosed.

Abstract: The present invention relates to a pharmaceutical composition in a solid unit dosage form for oral administration in a human or lower animal comprising: a. a safe and effective amount of a therapeutically active agent; b. an inner coating layer selected from the group consisting of poly(methacrylic acid, methyl methacrylate) 1:2, poly(methacrylic acid, methyl methacrylate) 1:1, and mixtures thereof; and c. an outer coating layer comprising an enteric polymer or film coating material; wherein the inner coating layer is not the same as the outer coating layer; wherein if the inner coating layer is poly(methacrylic acid, methyl methacrylate) 1:1 then the outer coating layer is not poly(methacrylic acid, methyl methacrylate) 1:2 or is not a mixture of poly(methacrylic acid, methyl methacrylate) 1:1 and poly(methacrylic acid, methyl methacrylate) 1:2; and wherein the inner coating layer and the outer coating layer do not contain any therapeutically active agent.

Abstract: The present invention describes isolated Fagopyritol A1, isolated Fagopyritol A3, and isolated Fagopyritol B3. Compositions which include two or more of Fagopyritol A1, Fagopyritol A2, Fagopyritol A3, Fagopyritol B1, Fagopyritol B2, Fagopyritol B3, and D-chiro-inositol, at least one of which is an isolated Fagopyritol A1, isolated Fagopyritol A3, or isolated Fagopyritol B3, are also disclosed. Methods for preparing substantially pure Fagopyritol A1, Fagopyritol A3, Fagopyritol B3, or mixtures thereof from buckwheat are also described. The fagopyritols can be used to prepare pharmaceutical compositions, the administration of which can be used to treat diabetes.

Abstract: Disclosed is an osmotic pharmaceutical delivery system comprising (a) a semi-permeable wall that maintains its integrity during pharmaceutical delivery and which has at least one passage therethrough; (b) a single, homogeneous composition within said wall, which composition consists essentially of (i) a pharmaceutically active agent, (ii) at least one non-swelling solubilizing agent which enhances the solubility of the pharmaceutically active agent; (iii) at least one non-swelling osmotic agent and (iv) a non-swelling wicking agent dispersed throughout the composition which enhances the surface area contact of the pharmaceutical agent with the incoming aqueous fluid.

Abstract: There are provided an aqueous shellac coating agent comprising shellac, a basic amino acid and/or a basic phosphate, as well as a production process therefor; a coated food and a coated drug that have been coated with such a coating agent; a glazing composition for oil-based confectionary which is in a liquid form and comprises an aqueous shellac solution (A) containing shellac, a basic amino acid and/or a basic phosphate dissolved in water, a thickener (B), and/or a sugar (C); a process for glazing oil-based confectionary in which this glazing composition is applied to oil-based confectionary to be glazed, thereby generating a glaze; and glazed oil-based confectionary produced using this process for glazing oil-based confectionary.

Abstract: The present invention relates to pharmaceutical compositions that contain a solid pharmaceutically active compound having a melting point ≧37° C. and a fatty acid or a fatty acid salt or a mixture of a fatty acid and a fatty acid salt. Such composition results in a depression in melting point to ≦37° C. upon contact with an aqueous solution thereby providing an improved outlook for absorption.

Abstract: An edible, hardenable coating composition containing microcrystalline cellulose and carrageenan and at least one of a strengthening polymer, a plasticizer, a surface active agent or a combination thereof. The coating composition of the present invention may be applied to pharmaceutical and veterinary solid dosage forms, confectionery, seeds, animal feed, fertilizers, pesticide tablets, and foods and provides an elegant prompt release coating which does not retard the release of active ingredients from the coated substrate.

Abstract: An oral composition which is adapted to be dispersed in an aqueous carrier substantially immediately prior to administration comprises a multiplicity of particles comprising an active substance, the particles being combined with one or more gelling or swelling agents capable of forming a viscous medium around the particles in an aqueous carrier as well as being provided with a masking surface layer when dispersed in the aqueous carrier. This serves to mask uneven surfaces on the particles and prevent them from adhering to oral mucosa when the composition is ingested and thus makes it easier to administer large dosages of an active substance. The masking surface layer is preferably provided by an increased viscosity of the viscous medium in the immediate vicinity of the particles relative to the viscosity of the surrounding aqueous carrier. A ready-to-use composition is prepared by mixing the composition with an aqueous carrier substantially immediately prior to administration of the composition.

Abstract: There is provided a coating composition that masks the undesirable taste of a pharmaceutically active ingredient, i.e. drug or medicine, that is taken orally. The coating composition is comprised of dimethylaminoethyl methacrylate and neutral methacrylic acid ester, a cellulose ester polymer, and an alkaline modifier.

Abstract: Film-forming compositions are disclosed that can comprise, on a dry solids basis, 25 to 75 percent by weight of certain starch derivatives and 25 to 75% primary external plasticizer. The starch derivatives can be chemically modified starches that range in molecular weight from 100,000 to 2,000,000. The high levels of plasticizer in the films give excellent film flexibility and integrity. The films are also resistant to penetration by water, oil and/or grease.

Abstract: Disclosed is an oral controlled release macrolide pharmaceutical formulation. In a preferred embodiment, the formulation comprises a citrate salt of a preferred macrolide, clarithromycin. Also disclosed are methods for preparing, isolating and characterizing soluble and stable citrate salt of macrolides and use thereof in all solid dosage forms of macrolides.

Abstract: A preparation capable of releasing a medicinal substance at a targeted site in the intestine, wherein the preparation dose not releases medicinal substance in endogastri at all, but can quickly release a medicinal substance when it reaches the desired site in the intestine after a certain period of time from discharge of the preparation from the stomach, and wherein a core material containing a medicinal substance is coated with a mixed film of a hydrophobic organic compound—an enteric polymer.

Abstract: A new soft gelatine formulation and process methodology is disclosed herein that increases single Coenzyme Q10 molecules presented to the absorption channels of the small intestines by providing medium chain triglycerides, Vitamin E, and natural beta carotene to Coenzyme Q10 in a soft gel capsule to increase the absorption thereof.

Abstract: Film coatings for enteric and colonic release at selected pH are provided by selecting and/or formulating a shellac of a predetermined acid number. The method includes the selection of the acid number to provide the release at the specified pH and a method of providing a shellac of a predetermined acid number by blending of shellacs of different acid numbers. In general, films that release or dissolve at or above pH 7.4 are based on the selection of shellac with an acid number below 74. Films that release or dissolve above pH 7.0 are comprised of shellac selected with an acid number below 80. Films that release or dissolve at below pH 7.0 are comprised of shellac selected to have an acid number above 80. The film coating may be modified with a water soluble resin and/or a plasticizer. Preferably the shellac will comprise 50% or more of the resin system, and is formed out of water, not alcohol.

Abstract: The present invention provides an osmotic device containing controlled release pseudoephedrine in the core in combination with a rapid release H1 antagonist in an external coat. A wide range of H1 antagonist antihistamines, especially fexofenadine, can be used in this device. Particular embodiments of the invention provide osmotic devices having predetermined release profiles. One embodiment of the osmotic device includes an external coat that has been spray coated rather compression coated onto the device. The device with spray coated external core is smaller and easier to swallow than the similar device having a compression coated external coat. The device is useful for the treatment of respiratory congestion related disorders and allergy related disorders. The present devices provide PS and an H1 antagonist according to specific release profiles in combination with specific formulations.

Abstract: A multiplex drug delivery system suitable for oral administration containing at least two distinct drug dosage packages, which exhibit equivalent dissolution profiles for an active agent when compare to one another and when compared to that of the entire multiplex drug delivery unit, and substantially enveloped by a scored film coating that allows the separation of the multiplex drug delivery system into individual drug dosage packages can provide a convenient and cost effective drug delivery unit, particularly for patients with a regimen of prescribed dosages that varies during their treatment period.

Abstract: A pharmaceutical composition of omeprazole for oral administration is described which includes: (a) a tabletted core component containing a therapeutically effective amount of a acid-labile compound, e.g., substituted benzamidazole such as omeprazole, an optional surface active agent, a filler, a pharmaceutically acceptable alkaline agent, and a binder; and (b) a single layer of coating on said core which comprises a layer of an enteric coating agent.

Abstract: The present invention provides solid pharmaceutical compositions for improved delivery of a wide variety of pharmaceutical active ingredients contained therein or separately administered. In one embodiment, the solid pharmaceutical composition includes a solid carrier, the solid carrier including a substrate and an encapsulation coat on the substrate. The encapsulation coat can include different combinations of pharmaceutical active ingredients, hydrophilic surfactant, lipophilic surfactants and triglycerides. In another embodiment, the solid pharmaceutical composition includes a solid carrier, the solid carrier being formed of different combinations of pharmaceutical active ingredients, hydrophilic surfactants, lipophilic surfactants and triglycerides. The compositions of the present invention can be used for improved delivery of hydrophilic or hydrophobic pharmaceutical active ingredients, such as drugs, nutrionals, cosmeceuticals and diagnostic agents.

Abstract: There are provided an oral skin improving agent that exhibits good skin improving effects when orally ingested, suppresses problems of discoloration and generation of unpleasant odor during storage, and has excellent storage stability; a food composition for improving skin containing this skin improving agent; and a skin improving method. The oral skin improving agent contains as a principal component refined hyaluronic acid having a purity of at least 90%, preferably at least 95%, and an average molecular weight in a range of 750,000 to 1,200,000, preferably 800,000 to 1,000,000. A person's skin can be improved by having the person ingest the oral skin improving agent such that the ingestion amount thereof is at least 5 mg per day.

Abstract: A degradable PEG hydrogel is described that, upon hydrolysis, releases conjugates of substantially non-peptidic polymers and biologically active molecules. For example, PEG and protein conjugates can be released in vivo from the hydrogels for therapeutic application.

Abstract: A controlled release or delayed release formulation contains a selective serotonin reuptake inhibitor (SSRI) such as paroxetine.

Abstract: The present invention provides a compressed tablet of an antibacterial oxazolidinone agent which provides high drug load and excellent bioavailability.

Abstract: Disclosed is an osmotic pharmaceutical delivery system comprising (a) a semi-permeable wall that maintains its integrity during pharmaceutical delivery and which has at least one passage therethrough; b) a single, homogeneous composition within said wall, which composition consists essentially of (i) a pharmaceutically active agent, (ii) at least one non-swelling solubilizing agent which enhances the solubility of the pharmaceutically active agent; (iii) at least one non-swelling osmotic agent and (iv) a non-swelling wicking agent dispersed throughout the composition which enhances the surface area contact of the pharmaceutical agent with the incoming aqueous fluid.

Abstract: A dry moisture barrier film coating composition for forming a moisture barrier film coating for pharmaceutical tablets and the like comprises polyvinyl alcohol, soya lecithin, and optionally a flow aid, a colorant, and/or a suspending agent. A liquid coating solution or dispersion for forming a moisture barrier film coating for pharmaceutical tablets and the like comprises polyvinyl alcohol, soya lecithin, water, and optionally a flow aid, a colorant, and/or a suspending agent. A method of coating pharmaceutical tablets and the like with a moisture barrier film coating comprises forming a liquid coating solution or dispersion for forming a moisture barrier film coating for pharmaceutical tablets and the like comprising polyvinyl alcohol, soya lecithin, water, and optionally a flow aid, a colorant, and/or a suspending agent, applying the coating solution or dispersion onto the tablets to form a film coating on the tablets, and drying the film coating on the tablets.

Abstract: The present invention provides an improved soft chewable multivitamin tablet in which vitamin C is separated from calcium pantothenate and/or minerals such as iron, copper, zinc and mixtures thereof in a core or multilaminate form and a process for preparing the same. The soft chewable multivitamin tablet of the present invention maintains its stability over a long-storage time in terms of the content and potency of vitamins while overcoming the problems of incompatibility, bad mouthfeel and palatability.

Abstract: The present invention provides an improved soft chewable multivitamin tablet in which vitamin C is separated from calcium pantothenate and/or minerals such as iron, copper, zinc and mixtures thereof in a core or multilaminate form and a process for preparing the same. The soft chewable multivitamin tablet of the present invention maintains its stability over a long-storage time in terms of the content and potency of vitamins while overcoming the problems of incompatibility, bad mouthfeel and palatability.

Abstract: The invention provides a tablet and methods for making the tablet comprising a gel-forming material and at least one particle comprising an active agent in contact with a coating material to modify release of the active agent.

Abstract: A solid, oral controlled release pharmaceutical dosage form has a water-soluble active ingredient dispersed in a matrix and releases the active ingredient at such a rate upon administration that the median tmax is 2.5 to 6 hours and the ratio of mean Cmax to mean plasma level of the active ingredient at 24 hours is in the range of 1.5 to 3.5.

Abstract: A controlled release tablet for oral administration is disclosed which has a tablet core including an insoluble therapeutically active agent having an aqueous solubility of less than or equal to about 5 mg/ml in a sufficient amount to render a therapeutic effect. The core provides rapid release of said therapeutically active agent upon exposure to aqueous solutions. The tablet core is coated with a controlled release coating permitting sustained release of said therapeutically active agent when said coated tablet is exposed to aqueous solutions.

Abstract: Disclosed is an osmotic pharmaceutical delivery system comprising (a) a semi-permeable wall that maintains its integrity during pharmaceutical delivery and which has at least one passage therethrough; (b) a single, homogeneous composition within said wall, which composition consists essentially of (i) a pharmaceutically active agent, (ii) at least one non-swelling solubilizing agent which enhances the solubility of the pharmaceutically active agent; (iii) at least one non-swelling osmotic agent and (iv) a non-swelling wicking agent dispersed throughout the composition which enhances the surface area contact of the pharmaceutical agent with the incoming aqueous fluid.

Abstract: A controlled release preparation for oral administration contains tramadol, or a pharmaceutically acceptable salt thereof, as active ingredient.

Abstract: The present invention pertains to a sustained release drug delivery system which comprises a core of active ingredient, an enteric coating, a second coating of active ingredient and lastly a readily gastric-soluble protective coating. In another embodiment, the sustained release drug delivery system comprises a core of active ingredient, an enteric coating; a second coating of active ingredient; a second enteric coating and a third coating of active ingredient The sustained release dosage form of this invention is useful for pharmaceutically active ingredients that have limited aqueous solubility, especially phenytoin sodium, and other pH dependent soluble drugs.

Abstract: A stabilized sustained release oral solid dosage form which includes an effective amount of tramadol or a pharmaceutically acceptable salt thereof dispersed in a matrix of a hydrophobic material comprising a wax-like substance which was melted or softened during the preparation of the matrix, is cured at a temperature from about 35° C. to about 65° C. for a time period from about 4 to about 72 hours, such that the formulation, when subjected to in-vitro dissolution after exposure to accelerated storage conditions of at least one month at 40° C./75% RH, releases an amount of tramadol which does not vary at any given dissolution time point by more than about 20% of the total amount of tramadol released when compared to in-vitro dissolution conducted prior to subjecting the dosage form to the accelerated storage conditions.

Abstract: A non-toxic, edible, enteric film coating, dry powder composition for use in making an aqueous enteric suspension which may be used in coating pharmaceutical tablets comprises a) an acrylic resin, said resin comprising i) from 20 to 85 percent by weight of at least one alkyl acrylate or alkyl methacrylate moiety, ii) from 80 to 15 percent by weight of at least one vinyl or vinylidene moiety having a carboxylic acid group capable of salt formation, and iii) from 0 to 30 percent by weight of at least one other vinyl or vinylidene moiety copolymerizable with i) and ii), b) an alkalizing agent capable of reacting with the acrylic resin such that, after reaction, 0.1 to 10 mole percent of the acidic groups in 1a-ii) are present in the salt form, and c) a detacktifier.

Abstract: An encapsulated material is described of which at least a part of the material is kept encapsulated during heat treatment in an aqueous environment and is released during cooling after a heat treatment. The material is encapsulated in a layer of a hydrophobic film-forming material and a layer of a material having a low critical solution temperature (LCST) below the treatment temperature. The layer containing the hydrophobic material may be situated inside the layer having the LCST and have a melting point below the LCST, but it may also be situated outside the layer having the LCST and have a melting point above the LCST of said layer. Said layers may also be applied together.

Abstract: The present invention relates to a solid dosage form comprising at least one polymeric binder and at least one active ingredient and, where appropriate, conventional additives, wherein the polymeric binder consists of copolymerized units a) 15-83% by weight of at least one N-vinyllactam, b) 15-83% by weight of methyl methacrylate, c) 2-70% by weight of at least one other monomer and d) 0-9.9% by weight of at least one &agr;,&bgr;-ethylenically unsaturated acid.

Abstract: Disclosed is an osmotic pharmaceutical delivery system comprising (a) a semipermeable wall that maintains its integrity during pharmaceutical delivery and which has at least one passage therethrough; (b) a single, homogeneous composition within said wall, which composition consists essentially of (i) a pharmaceutically active agent, (ii) at least one non-swelling solubilizing agent which enhances the solubility of the pharmaceutically active agent; (iii) at least one non-swelling osmotic agent and (iv) a non-swelling wicking agent dispersed throughout the composition which enhances the surface area contact of the pharmaceutical agent with the incoming aqueous fluid.

Abstract: A coated tablet and process for making the same is provided. A molten composition comprising at least 50 weight percent of a thermoplastic material having a melting point of less than about 120° C. is applied to the tablet, and the molten composition is solidified into a protective coating. If desired, one or more outer coatings may be applied over the protective coating.

Abstract: There are provided orally-administrable formulations for the controlled release of granulated garlic, comprising particles of granulated garlic coated with a film comprising a mixture of at least one water soluble polymer and at least one water insoluble polymer, said at least one water soluble polymer and at least one water insoluble polymer being present in a ratio that produces a substantially zero order linear release pattern of at least one active ingredient. Preferably, the formulations are characterized in that the total in vitro dissolution time of said formulations required for release of 75% of the Allicin available from said formulations based upon the total amount of alliin initially present in said formulations is between about 4 and about 12 hours, as determined by U.S.P. XXIII paddle method at a paddle speed of 150 rpm, using simulated intestinal fluid without the digestive enzymes normally found in intestinal fluid, containing 0.1% w/w sodium dodecyl sulfate (SDS), at pH 6.

Abstract: A tablet and process for making the same is provided. The tablet is made from a granular agglomerate comprising a mixture of at least one active ingredient and a binder. The granular agglomerate is heated to melt the binder only at or near its surface, and then cooled, such that the melted binder solidifies into a substantially continuous phase, thereby forming a fused layer on the outside of the tablet.

Abstract: A controlled release preparation for oral administration contains tramadol, or a pharmaceutically acceptable salt thereof, as active ingredient.

Abstract: The present invention provides solid pharmaceutical compositions for improved delivery of a wide variety of pharmaceutical active ingredients contained therein or separately administered. In one embodiment, the solid pharmaceutical composition includes a solid carrier, the solid carrier including a substrate and an encapsulation coat on the substrate. The encapsulation coat can include different combinations of pharmaceutical active ingredients, hydrophilic surfactant, lipophilic surfactants and triglycerides. In another embodiment, the solid pharmaceutical composition includes a solid carrier, the solid carrier being formed of different combinations of pharmaceutical active ingredients, hydrophilic surfactants, lipophilic surfactants and triglycerides. The compositions of the present invention can be used for improved delivery of hydrophilic or hydrophobic pharmaceutical active ingredients, such as drugs, nutrionals, cosmeceuticals and diagnostic agents.

Abstract: The present invention provides a simple multi-tablet system for the treatment of urinary incontinence with oxybutynin. Particular embodiments of the invention provide a first tablet that releases oxybutynin over a short period of time, e.g. less than six hours, and a second tablet that releases oxybutynin over an extended period of time, e.g., eighteen to twenty-four hours, to maintain therapeutically effective levels oxybutynin in the mammal for a period of about twenty four hours. Unlike other systems, this system is easily adaptable to compensate for patient to patient variability in response to oxybutynin therapy. The invention also provides a method of treating urinary incontinence with the above system and a kit comprising various first and second tablets to rapidly develop a patient's preferred dosing regimen, i.e., the dosing regimen which provides the greatest therapeutic benefit and/or least amount or severity of side effects.

Abstract: The present invention provides improved confectionery compositions which have a substantial reduction in the unpleasant organoleptic sensations associated with the release of functional ingredients from the confection in the oral cavity. The confectionery composition comprises a confectionery base, a functional ingredient which is a botanical or a mineral or a mineral salt having an unpleasant mouthfeel, and from about 0.5% to about 5.0% by weight of the composition of one or more fats, said amount being effective to suppress the unpleasant mouthfeel of the functional ingredient. For botanicals the confectionery composition is a hard boiled candy composition or a hard gum composition and the fat is one or more partially hydrogenated vegetable oils or saturated fats. For minerals or their salts the confection is a hard boiled candy composition and the fat is one or more partially hydrogenated vegetable oils.

Abstract: The present invention provides a pharmaceutical composition which is substantially free of unpleasant tastes and orally administrable which comprises: (a) an active medicament, (b) an inner coating layer comprising an oil substance having a melting point at a range of from about 50° C. to about 100° C., (c) an outer coating layer comprising at least a polymeric substance.

Abstract: The present invention provides a pharmaceutical composition which is substantially free of unpleasant tastes and orally administrable which comprises:

Abstract: A controlled release tablet for oral administration is disclosed which has a tablet core including an insoluble therapeutically active agent having an aqueous solubility of less than or equal to about 5 mg/ml in a sufficient amount to render a therapeutic effect. The core provides rapid release of said therapeutically active agent upon exposure to aqueous solutions. The tablet core is coated with a controlled release coating permitting sustained release of said therapeutically active agent when said coated tablet is exposed to aqueous solutions.

Abstract: A coated capsule is disclosed comprising a gelatin shell with a flavored coating. A sugar or sugar substitute is included in the material of the shell and that of the coating to stabilize both compositions and the junction therebetween.

Abstract: The effervescent formulation elation in the form of granules or of a tablet contains, in addition to the effervescent base, at least one water-soluble or at least suspendable plant extract whose particles are coated with at least one oily, fatty or waxy substance. At least one emulsifier and/or at least one antifoam may be present in the coating and/or as a further component of the mixture, in particular applied as a further component of the mixture to a pharmaceutically permissible filler as carrier. The individual phases are prepared by a procedure in which the plant extract or the filler is heated—preferably in a granulator, in particular in a vacuum granulator—and wet or mixed with a melt or solution of the oily, fatty or waxy substance or at least one emulsifier and/or at least one antifoam and then dried—preferably in a vacuum—and sieved to the desired particle size.