Abstract: Soft gelatin capsules having a capsule shell comprising gelatin, plasticizers and, if desired or required, further auxiliary agents, and a capsule filling containing a solvent including a migrateable solvent such as 1,2-propyleneglycol as a solvent in the capsule filling and in the capsule shell. The manufacture of said capsules is improved, if in the process for making the soft gelatin capsules the gelatin bands are cooled with a liquid, and preferably with water.

Abstract: A process for producing agglomerates with a core/shell structure, in which i) initial agglomerates containing a first particulate solid are prepared; ii) a second particulate solid is agglomerated in the presence of the initial agglomerates with the addition of a binder liquid to give second stage agglomerates and, where appropriate, iii) an nth (n≧3) solid is agglomerated in the presence of the (n−1)th stage agglomerates with the addition of a binder liquid to give nth stage agglomerates.

Abstract: Disclosed herein is sustained-release formulations of tramadol comprising tramadol saccharinate coated with at least one sustained-release coating. The sustained release formulations may also contain tramadol in non-sustained release form, and other pharmaceutically acceptable excipients. Also disclosed are methods of preparation of and methods of treatment using the inventive formulations.

Abstract: The invention relates to adjuvants that contain a lecithin, an oil and an amphiphilic surfactant and that are capable of forming a stable oil-in-water emulsion vaccine so as to minimize local reactions to the vaccine in the injected animal.

Abstract: A process for the manufacturing of microcapsules for sustained release of water soluble peptides, with adjustable release periods of between 1 to 18 weeks. The microcapsule wall are made of a biodegradable polymer. The process is based on the formation of an intermediate complex water/oil/water emulsion. By evaporating the solvent in the emulsion by pressure reduction the microcapsules consolidate, retaining the active peptides in the polymeric matrix. The process produces the complex emulsion in a two mixer, continuous operation. In the first mixer a water/oil emulsion is formed and it is used to form the complex emulsion in the second mixer. By operating in a continuous manner, the process overcome the problems found in existing processes regarding particle size distribution, material losses and process control, among others.

Abstract: A synergistic antimicrobial textile finish comprising a synergistic antimicrobial combination of antibacterial agent selected from the group consisting of 2,4,4′-trichloro-2′-hydroxy diphenol ether and 2-phenylphenol, or a combination of these, and an antifungal agent of diiodomethyl-4-tolylsulfone, which provides for a synergistic antimicrobial textile finish that is nontoxic, stable, and imparts desired broad spectrum antimicrobial efficacy onto the surface of textile substrates.

Abstract: The present invention relates to an orally administrable galenic formulation allowing improved absorption by the transmembrane or paracellular route in the gastrointestinal tract of active ingredients which are hydrophilic or ionizable in physiological media. The galenic formulation comprises at least one active ingredient, an absorption-promoting agent, and one or more pharmaceutically acceptable excipients.

Abstract: There is disclosed an improved copper complex bactericide/fungicide and a method of making and using the same. The improved bactericide/fungicide is prepared by forming an aqueous solution of a partially neutralized, water-soluble polycarboxylic acid having a molecular weight of between approximately 1,000 and 300,000 and a pH of between approximately 3 and 9. To this aqueous solution is added a copper-containing compound which when combined with said aqueous solution releases copper (II) ions which will form a water-soluble complex with said partially neutralized polycarboxylic acid. The water-soluble copper complex is applied to plants to prevent or inhibit bacterial and fungal disease growth thereon.

Abstract: Oral dosage forms are provided for the administration of a bisphosphonic acid compound in the prevention and treatment of conditions involving calcium or phosphate metabolism, i.e., conditions associated with bone resorption such as osteoporosis, Paget's disease, periprosthetic bone loss, osteolysis, malignant hypercalcemia, metastatic bone disease, multiple myeloma, and periodontal disease. The dosage forms are either enterically coated capsules housing the drug in a liquid or semi-solid carrier, or enterically coated osmotically activated drug delivery devices.

Abstract: A cosmetic method of reducing the acidity of sweat excreted from human eccrine glands, said method comprising the topical application of a V-ATPase inhibitor to the skin in the vicinity of the eccrine glands. Said method may result in a range of benefits, including enhanced appreciation of topically-applied perfume and enhanced efficacy of topically-applied antiperspirant salt. Cosmetic products and compositions comprising a V-ATPase inhibitor and selected other components are also claimed.

Abstract: The present invention relates to an orally administrable galenic form allowing improved absorption by the transmembrane or paracellular route in the gastrointestinal tract of active ingredients which are hydrophilic or ionizable in physiol. media, comprising at least one such active ingredient, an absorption-promoting agent having an HLB>8, the the absorption-promoting agent consisting of one or more lipid substances chosen from: polysorbates; polyoxyethylene ethers; esters of polyoxyethylene and fatty acids; fatty acids; fatty alcs.; bile acids and their salts with pharmaceutically acceptable cations; esters of C1-C6 alkanol with fatty acids; esters of polyol with fatty acids, the polyol comprising from 2 to 6 hydroxyl functional groups; and polyglycolyzed glycerides; in combination with one or more pharmaceutically acceptable excipients, the pharmaceutical forms comprising captopril being excluded. A controlled-release tablet contained (1) cores contg.

Abstract: Particulate composition comprising one or more physiologically active substances and a fish gelatinous protective colloid containing at least 50% by weight of fish gelatin, wherein the fish gelatin is at least partly composed of fish gelatin having a bloom strength of above 100, and wherein the composition is obtainable by a particle forming spraying or double emulsifying method.

Abstract: The application discloses a method for the treatment of Heliobacter infection in a mammalian host, which comprises administration to said infected host of an immunologically effective amount of one or more Heliobacter antigen(s), optionally in association with a mucosal adjuvant.

Abstract: Methods of coating core materials by providing target materials and core materials; ablating the target materials to form ablated particulate target materials; and coating the core materials with said ablated particulate target materials; wherein the method is performed at a pressure of about 10 Torr or higher. Methods of coating particles with nanometer to multiple nanometer thick coatings in atmospheric pressure, and using pneumatic fluidization, are also provided.

Abstract: The present invention relates to lipid compounds of formula I, wherein said compounds are optionally in a cationic form and are optionally combined with one or more biologically acceptable anions. The present invention also relates to complexes comprising at least one cationic lipid compound of the formula I and an active substance comprising negative charges. The present invention further relates to methods of gene therapy using the complexes of the present invention.

Abstract: Process is provided for preparing an oral solid rapidly disintegrating freeze-dried dosage form of a pharmaceutically active substance having an unacceptable taste, wherein prior to freeze drying, a suspension of uncoated or coated coarse particles of a pharmaceutically active substance in a carrier material is cooled to reduce the viscosity and minimize release of the active substance during processing, as well as beyond the point of disintegration of the form in the mouth, to minimize bad taste from the drug.

Abstract: A multiple pulsed dose drug delivery system for pharmaceutically active amphetamine salts, comprising an immediate-release component and an enteric delayed-release component wherein (1) the enteric release coating has a defined minimum thickness and/or (2) there is a protective layer between the pharmaceutically active amphetamine salt and the enteric release coating and/or (3) there is a protective layer over the enteric release coating. The product can be composed of either one or a number of beads in a dosage form, including either capsule, tablet, or sachet method for administering the beads.

Abstract: A composition comprising gelatin and a polysaccharide which is degradable by a colonic enzyme and, optionally, with an aldehyde and/or a polyvalent metal ion and/or an additional polysaccharide, which is not degraded or disintegrated in the upper gastrointestinal tract, thereby rendering the active substance loaded therein to be selectively delivered to the colon and to be effectively released in the colon.

Abstract: This invention relates to a pharmaceutical composition for oral administration comprising a carrier and, as an active ingredient, a monoamine oxidase B inhibitor, characterised in that the composition is formulated to promote pre-gastric absorption of said monoamine oxidase B inhibitor. A process for preparing such a composition and the use of such a composition for the treatment of Parkinson's disease, the treatment and/or prophylaxis of depression and the treatment and/or prophylaxis of Alzheimer's disease are also provided.

Abstract: Novel proteins are disclosed.

Abstract: Disclosed is a sustained-release preparation characterized in that it is produced by dispersing in an oil phase a rapidly dried product containing a bioactive polypeptide and a surfactant, and subsequent shaping, and a method of its production.

Abstract: Disclosed are compositions including an adenosine analog, wherein the composition comprises a dosage form suitable for oral (co)administration. Also disclosed are compositions including adenosine analogs, wherein the composition is in a dosage form including a pill, capsule, lozenge, or tablet, and compositions including adenosine analogs, wherein the composition is in a dosage form comprising a liquid. Additionally disclosed are methods of administering the inventive composition, and kits including the inventive compositions.

Abstract: An oral pharmaceutical dosage form comprising a proton pump inhibitor and one or more prokinetic agents in a fixed formulation, wherein the proton pump inhibitor is protected by an enteric coating layer. The fixed formulation is in the form of multilayered tablets, capsules or multiple unit tableted dosage forms. The multiple unit dosage forms are most preferred. The new fixed formulation is especially useful in the treatment of disorders associated with gastro oesophageal reflux diseases.

Abstract: A sustained release capsule in which an outer surface of a hard capsule mainly composed of gelatin and containing a physiologically active substance is uniformly covered with a film material comprising a natural polysaccharide/polyhydric alcohol composition which is prepared by uniformly kneading at least one natural polysaccharide selected from the group consisting of carrageenan, alginic acid, salts of alginic acid, derivatives of alginic acid, agar, locust bean gum, guar gum, pectin, amylopectin, xanthane gum, glucomannan, chitin and pullulan in at least one system selected from the group consisting of polyhydric alcohols, sugar alcohols, monosaccharides, disaccharides, trisaccharides and oligosaccharides. A capsule formed merely of the natural polysaccharide/polyhydric alcohol composition swells and is permeated by water. It is poor in shape-retaining properties, failing to retain its shape in the stomach, although it is nondigestive.

Abstract: A lipid represented by the following formula:MO--(CO--CH.sub.2 --NH).sub.p --CO--(CH.sub.2).sub.n --CO--(NH--CH.sub.2 --CO).sub.q --OMwherein M represents a hydrogen atom or an alkali metal, n is an integer of 6-18 and p and q each represent an integer of at least 1 with the proviso that a total of p and q is not greater than 6. When an aqueous solution of an alkali metal salt of the lipid is allowed to stand for 2-3 weeks, a fibrous microtube including a tubular body having a diameter of 1-3 .mu.m and a plurality of spherical vesicles contained within the tubular body and having a diameter of 0.1-3 .mu.m is formed.

Abstract: Described is a process for making a liposomal, ion-exchange whey protein and products thereof, which result in the sustained release of amino acids into the body's circulation to generally promote skeletal muscle protein synthesis, decrease body fat in association with diet modification and improve exercise performance. The whey protein is preferably encapsulated in a liposome using a cold, or non-heated, process. After the liposomal, ion-exchange whey protein has been prepared, it is then preferably lyophilized to deliver macronutrients for use as a sports nutrition supplement and for use in medical or clinical catabolic applications.

Abstract: A pharmaceutical composition containing a microemulsion made up of a hydrophilic component, a lipophilic component, a surfactant and a drug, where the hydrophilic component, the lipophilic component and the surfactant form, when examined on a macroscopic scale, a one-phase solution. The hydrophilic component is dispersed as colloidal droplets in the lipophilic component, or the lipophilic component is dispersed as colloidal droplets in the hydrophilic component. According to still another alternative, the hydrophilic and the lipophilic components form a microemulsion with bicontinuous structure where the components form elongated adjacent channels. The drug is dissolved in the dispersed component or, in the case of a microemulsion with bicontinuous structure, in the hydrophilic or the lipophilic component. The microemulsion is stabilized by means of the surfactant. It is characteristic that a gelatinizer and water are added to the microemulsion thereby bringing the microemulsion into a gel form.

Abstract: Process is provided for preparing an oral solid rapidly disintegrating freeze-dried dosage form of a pharmaceutically active substance having an unacceptable taste, wherein prior to freeze drying, a suspension of uncoated or coated coarse particles of a pharmaceutically active substance in a carrier material is cooled to reduce the viscosity and minimize release of the active substance during processing, as well as beyond the point of disintegration of the form in the mouth, to minimize bad taste from the drug.

Abstract: Sustained release oral solid dosage forms of opioid analgesics are provided as multiparticulate systems which are bioavailable and which provide effective blood levels of the opioid analgesic for at least about 24 hours. A unit dose of the opioid analgesic contains a plurality of substrates including the opioid analgesic in sustained release form. The substrates have a diameter from about 0.1 mm to about 3 mm.

Abstract: A lipoprotein particle and a therapeutic lipoprotein composition are disclosed. The lipoprotein particle consists essentially of lecithin phospholipids with low phase transition temperatures and human apoproteins A and C. A therapeutic composition for therapeutic administration to a subject, comprising the lipoprotein particles of the invention, is also disclosed. The composition is useful is treating disease conditions associated with elevated serum Lp(a) levels, as well as hypertension and acute renal failure.

Abstract: The present invention provides a pharmaceutical composition of hCGRP and the preparation of the same. The composition comprises liposomes from nature soybean phospholipid, in which the weight ratio of hCGRP to soybean phospholipid is 1-2 to 100-8000. The half-life of the composition is longer than 72 hours, and the stability of the composition is also enlongated. The composition can be administrated intravenous infusion, oral, nasal mucosal spray in an amount of 0.1-10 pg hCGRP per kg body weigh to treat hypertension and congestive heart failure of a human. The bioavailability of approximately 80%.

Abstract: Vaccine preparations in stable particulate form are disclosed. An immediate-release preparation comprises an immunogen adsorbed to an aluminum adjuvant. A controlled- or delayed-release preparation comprises microspherical particles comprising a continuous matrix of biodegradable polymer containing discrete, immunogen-containing regions.

Abstract: A method of preparing an oral preparation, especially in the form of hard gelatin capsules, tablets or pellets, for use by the administration of drugs or supplementary nutrients for human beings or animals, said preparation on its outer side being provided with an enteric coating which contains or comprises a calcium salt of a polysaccharide. A moisture-resistant layer containing a protein, especially zein, can be provided between the material to be coated and the enteric coating. The enteric coating is formed in situ by spraying the liquid coating substances in a fluidized bed. The present invention also pertains to oral preparations which is prepared by the method.

Abstract: A lipid represented by the following formula:MO--(CO--CH.sub.2 --NH).sub.p --CO--(CH.sub.2).sub.n --CO--(NH--CH.sub.2 --CO).sub.q --OMwherein M represents a hydrogen atom or an alkali metal, n is an integer of 6-18 and p and q each represent an integer of at least 1 with the proviso that a total of p and q is not greater than 6. When an aqueous solution of an alkali metal salt of the lipid is allowed to stand for 2-3 weeks, a fibrous microtube including a tubular body having a diameter of 1-3 .mu.m and a plurality of spherical vesicles contained within the tubular body and having a diameter of 0.1-3 .mu.m is formed.

Abstract: The present invention relates to a new form of biocompatible materials (e.g., lipids, polycations, polysaccharides) which are capable of undergoing free radical polymerization, e.g., by using certain sources of light; methods of modifying certain synthetic and naturally occurring biocompatible materials to make polymerizable microcapsules containing biological material coated with said polymerizable materials, composites of said polymerizable materials, methods of making microcapsules and encapsulating biological materials therein, and apparatus for making microcapsules containing biological cells (particularly islets of Langerhans) coated with polymerizable alginate or with a composite thereof (e.g., alginate and PEG). The present invention also relates to drug delivery systems relating to the foregoing, as well as bioadhesives and wound dressings made utilizing the foregoing technology.

Abstract: A medicament includes a caplet having a peripheral land which is inserted into mating capsule shell halves each with internally formed recesses defining external peripheral lands which align when the shell halves are fitted over the caplet. In one embodiment of the invention, the internal diameter of the capsule shells is selected such that the caplet will fit within the capsule cell regardless of its orientation, while in another embodiment the caplet land mates with the internal recesses of the capsule shells. In a preferred embodiment of the invention, the capsule shells have different lengths and diameters such that one overlaps the other and can be sealed.

Abstract: A composition, and methods of forming and using said composition, for the sustained release of non-aggregated, biologically active, erythropoietin (EPO). The sustained release composition of this invention comprises a polymeric matrix of a biocompatible polymer and particles of biologically active, aggregation-stabilized EPO, wherein said particles are dispersed within the biocompatible polymer.The method of the invention for producing a composition for the sustained release of biologically active EPO, includes dissolving a biocompatible polymer in a polymer solvent to form a polymer solution, dispersing particles of biologically active, aggregation-stabilized EPO in the polymer solution, and then solidifying the polymer to form a polymeric matrix containing a dispersion of said EPO particles.The method for using a composition of the invention is a method for providing a therapeutically effective blood level of biologically active, non-aggregated erythropoietin in a subject for a sustained period.

Abstract: This invention relates to coated medicaments and a process for providing spray coated gelatinous coverings for such medicaments. This invention is also directed to novel gelatinous compositions for spray coating tablets, caplets, pellets, granules and the like.

Abstract: Stable formulations of positively charged, hydrolytically unstable drug compounds are obtained by adding a sulfated polyvinyl alcohol copolymer to the formulations.

Abstract: Process for the manufacturing of gelatin products with improved stability against storage under hot and humid conditions and/or aldehydes characterized in that at least one additive, preferred glutamic acid, tryptophan, or nitrilotrismethylene phosphonic acid or a mixture thereof is incorporated into the gelatin before forming the final product as usual as well as the gelatin compositions used and the products obtained by the process.

Abstract: A biocompatible microcapsule containing living cells encapsulated in a membrane is disclosed. The membrane is a complex formed by the cohesion of two polymer layers. An inner layer comprises a substrate biopolymer and an outer layer comprises a synthetic polyelectrolyte having an electrolytic charge opposite that of the substrate biopolymer. Droplets of a solution of substrate biopolymer containing a suspension of living cells can be added to a solution comprising the synthetic polyelectrolyte to form the encapsulates. The membrane is formed by the cohesion of the oppositely-charge polymer layers to form a complex of substrate biopolymer and synthetic polyelectrolyte. Preferably, the inner layer contains a cationic biopolymer, such as collagen modified to have a pKI of 9, or an anionic biopolymer such as esterified or modified hyaluronic acid.

Abstract: An oral dosage form comprising: (a) granulocyte colony stimulating factor or erythropoietin; (b) surfactant(s); (c) fatty acid(s); and (d) enteric material. The oral drug preparations provided by the present invention avoid inactivation of the principal ingredient during the process of pharmaceutical manufacturing and display enhanced absorption of the ingredient from the intestinal tract, particularly as a result of the addition of fatty acid(s) to the drug composition. As such, oral dosage forms of the present invention can allow for dosage reductions, facilitate accurate dose control, and increase the practical usefulness of the bioactive proteins.

Abstract: A microgranular preparation having a core of biologically active material that is encapsulated by a water soluble film that is covered by an enteric coating of either an alkali soluble, acid insoluble polymer or a high molecular weight polymer whose structure is substituted with or contains windows of fatty acids or other material capable of being solubilized by intestinal juices. Useful for protecting pH sensitive and other biologically active materials from inactivation or contact with the stomach or rumen, and releasing the same in active form in the intestinal tract, particularly the duodenum.

Abstract: Pharmaceutical formulations comprise a mono- or di-aminopyridine active agent for administration on a once- or twice-daily basis for use in the treatment of neurological diseases, in particular multiple sclerosis and Alzheimer's disease. The formulations, which are suitable for oral or percutaneous administration of the active agent, include the active agent in a carrier effective to permit release of the mono- or di-aminopyridine at a rate allowing controlled absorption thereof over, on the average, not less than a 12 hour period and at a rate sufficient to achieve therapeutically effective blood levels over a period of 12-24 hours following administration.

Abstract: Water soluble macromers are modified by addition of free radical polymerizable groups, such as those containing a carbon-carbon double or triple bond, which can be polymerized under mild conditions to encapsulate tissues, cells, or biologically active materials. The polymeric materials are particularly useful as tissue adhesives, coatings for tissue lumens including blood vessels, coatings for cells such as islets of Langerhans, coatings, plugs, supports or substrates for contact with biological materials such as the body, and as drug delivery devices for biologically active molecules.

Abstract: A dosage unit form comprises a biologically active agent, such as a pharmaceutical, nutritional supplement or diagnostic, dissolved or suspended in a carrier liquid encapsulated in a soft elastic gel capsule. The carrier liquid comprises maltitol syrup as a major component. Maltitol syrup may be the only component of the carrier liquid, or may be blended with other liquids and/or excipients.

Abstract: Pharmaceutical formulations comprise a mono- or di-aminopyridine active agent for administration on a once- or twice-daily basis for use in the treatment of neurological diseases, in particular multiple sclerosis and Alzheimer's disease. The formulations, which are suitable for oral or percutaneous administration of the active agent, include the active agent in a carrier effective to permit release of the mono- or di-aminopyridine at a rate allowing controlled absorption thereof over, on the average, not less than a 12 hour period and at a rate sufficient to achieve therapeutically effective blood levels over a period of 12-24 hours following administration.

Abstract: A method of providing a patient needing clonidine with an extended dosage of clonidine over a prolonged period of time. Such method involves administering to the patient an oral dosage unit comprising a homogenous mixture of a therapeutically effective amount of clonidine, about 30 to about 70 percent by weight of one or more cellulose ethers such as hydroxypropyl methylcellulose, and about 30 to about 70 percent by weight of an inert substance such as cornstarch. The oral dosage unit may be contained in a gelatin capsule or in the form of a tablet.

Abstract: Stable, cold water-dispersible, liquid or pulverous compositions of fat-soluble substances which contain fish gelatin as the protective colloid and a method of making same are described.

Abstract: An extended release pharmaceutical formulation adapted to approach zero order release of drug over a 12 to at least 24 hour period, comprised of a mixture of 0 to about 50% of an immediate release particle containing a drug, inert substrate and binder, coated with talc and up to 100% of an extended release particle comprising the immediate release particle coated with a dissolution modifying system containing plasticizers and a film forming agent.