Abstract: A method and composition are disclosed utilizing the pure (S,R) isomer of formoterol, which is a bronchodilator with reduced adverse effects. (S,R)-Formoterol may be conveniently and safely formulated for aerosol administration.

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: 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.

Abstract: A simulated capsule-like medicament comprising a subcoating of a mixture of a water-soluble, film-forming polymer, e.g. hydroxypropylmethyl cellulose and a hydrophobic plasticizer, e.g. castor oil, which promotes a smooth uniform and substantially bubble free outer coating, e.g. gelatin, for the capsule-like medicament; capsule-like medicaments which are slightly bowed in shape; and a process of making such medicaments.

Abstract: The medicament of the present invention and its process of manufacturing employs a caplet or tablet core with a clear or single color uniform covering which can be applied either through an enrobing process, by spraying or by a single dip-coating step. The core itself can have a first color or be colorless, and its clear or single color covering has the outer surface of one end or one side colored by a suitable dye to provide a two-color appearance. The dye can be applied by dipping or spray painting with a suitable jet-spraying apparatus. In a preferred embodiment, the covering is of a clear gelatinous material.

Abstract: This invention provides a coating composition in which the principal film former is gelatin for use in coating tablets. The gelatin coating may be used with tablets, with or without any subcoating, and may be applied using conventional equipment. For a subcoated tablet, the coating formulation contains gelatin, a surfactant and a drying agent.

Abstract: The present invention relates to microcapsules for the oral administration of medicinal and/or nutritional active principles (AP), which are smaller than or equal to 1000 .mu.m in size. These microcapsules consist of particles which are coated with a coating material consisting of a mixture of a film-forming polymer derivative, a hydrophobic plasticizer, a functional agent and a nitrogen-containing polymer. These microcapsules are also characterized by their ability to remain in the small intestine for a long time (at least 5 hours) and to allow, during the residence, release and absorption of the AP. The invention also relates to a process for the production of the said microcapsules.

Abstract: The present invention relates to a pharmaceutical composition in a unit dosage form for peroral administration in a human or lower animal, having a gastrointestinal tract comprising a small intestine and a colon with a lumen therethrough having an inlet to the colon from the small intestine, comprising:a. a safe and effective amount of a therapeutically active agent incorporated into a compressed, bi-convex tablet, with a maximum diameter of about 4 mm to about 10 mm;b. a non-pH dependent smoothing coat applied to the tablet to provide a smooth tablet surface free from edges or sharp curves; andc. an enteric polymer coating material comprising at least one inner coating layer and only one outer coating layer;wherein the therapeutically active agent is released at a point near the inlet to, or within the colon; each of the inner coating layer(s) is an enteric polymer that begins to dissolve in an aqueous media at a pH between about 5 to about 6.

Abstract: Methods of treatment and prevention of estrogen-related diseases, and of fertility control, include low dose (e.g. less than 50 nanomolar serum concentration) administration of certain anabolic steroids, progestins and other substantially non-masculinizing androgenic compounds. Sustained release formulations substantially free of organic solvent, and sustained release formulations for maintaining low serum levels of androgen are disclosed.

Abstract: A method of making a pharmaceutical composition is disclosed. The method includes the steps of contacting at least one pharmaceutical ingredient with a mixture consisting essentially of gelatin and lecithin to increase the dissolution rate of water-insoluble pharmaceutical ingredients. A pharmaceutical excipient coating for increasing the dissolution rate of water-insoluble pharmaceutical ingredients is also disclosed. The coating consists essentially of gelatin and lecithin.

Abstract: This disclosure is directed to preparation of individual taste-masked, high bioavailability, high payload, microcapsules by microencapsulation of water-insoluble NSAID drug materials in the substantial absence of microcapsule agglomerates. These taste-masked microcapsules contain a high payload, e.g., about 83+ wt. % of said NSAID drug material having high bioavailability and can then be formulated into chewable tablets and liquid aqueous suspensions for medicinal use. Both cellulose acetate phthalate and gelatin are the microencapsulating polymer wall material.

Abstract: Protective enclosures for seeds provide a self-contained environment for protecting the seeds in their early growth stages in arid or hostile environments. A protective enclosure (10) for one or more seeds (15) comprising an outer shell (11), said shell (11) being permanently or temporarily liquid-impermeable in at least one direction, and a hygroscopic material (14) contained within the the shell (11) surrounding at least one seed (15), said material (14) being capable of absorbing and storing liquid.

Abstract: A simulated capsule-like medicament comprising a subcoating of a mixture of a water-soluble, film-forming polymer, e.g. hydroxypropylmethyl cellulose and a hydrophobic plasticizer, e.g. castor oil, which promotes a smooth uniform and substantially bubble free outer coating, e.g. gelatin, for the capsule-like medicament; capsule-like medicaments which are slightly bowed in shape; and a process of making such medicaments.

Abstract: Gelatin coated pharmaceutical dosage units containing, for example, analgesic compounds, such as aspirin, stabilized with a proteolytic enzyme, such as pepsin, are described.

Abstract: The present invention relates to a saliva-soluble stimulant unit comprising an active ingredient in a gel, wherein the gel is prepared by gelling a water-binding gelling agent, and the active ingredient comprises nicotine or alkaloid having the same direction of activity, said unit having a texture profile, with parameter values of firmness, hardness, brittleness, adhesiveness, elasticity and cohesiveness within given ranges; a disintegration time within the range 5-60 minutes; and a nicotine content from 0.5 to 10 mg.

Abstract: Solid mucoadhesive therapeutic or hygienic composition, for human or veterinary use, intended to be administered by application to the buccal or nasal mucous membrane, containing, in a mixture, 15 to 25% by weight of a cellulosic ether gelifiable in the presence of an aqueous liquid, 10 to 15% by weight of a homopolymer or copolymer of acrylic acid or a physiologically acceptable salt thereof, 30 to 45% by weight of a gelatin, and one or more therapeutic or hygienic active constituents. The cellulosic ether preferably is a C.sub.1 -C.sub.4 alkyl ether of cellulose, a C.sub.1 -C.sub.4 hydroxyalkyl ether of cellulose, or mixtures thereof.

Abstract: To improve the efficacy and tolerability of customary topical applications for transdermal systemically acting pharmaceutical substances, single dosage topical pharmaceutical forms which are therapeutically exactly ready-to-administer are formed from suitable semi-solid pharmaceutical forms. The topical single doses are specified pharmaceutically with respect to their dose, their topical spreading behaviour and their permeation properties. Several of the topically ready-to-administer single doses are in this case accommodated in a common commercial packaging container. Complex treatments can be developed by means of different individual dosages or alternatively active compound combinations. As pharmacological active compounds, steroids, peptides, various analgesics, local anaesthetics and non-steroidal antirheumatics are employed in particular.

Abstract: A simulated capsule-like medicament comprising a subcoating of a mixture of a water-soluble, film-forming polymer, e.g. hydroxypropylmethylcellulose and a hydrophobic plasticizer, e.g. castor oil, which promotes a smooth uniform and substantially bubble free outer coating, e.g. gelatin, for the capsule-like medicament; capsule-like medicaments which are slightly bowed in shape; and a process of making such medicaments.

Abstract: A presentation which, in the form of a film, permits the individual dosage of drugs, confectionary, other food, cosmetics and the like for oral application or intake. The presentation is characterized by the fact that it comprises a mass of 20 to 60%-wt. of at least a film former, 2 to 40%-wt. of at least a gel former, 0.1 to 35%-wt. of at least an active substance, and up to 40%-wt. of an inert filling agent, being applied on a carrier, or by consisting of a mass having the aforementioned composition but is unsupported. In the production thereof, an intimate mixture of said components is prepared, optionally with the addition of up to 30%-wt. of a polar solvent, and processed to form a homogeneous, spreadable or extrudable mass.

Abstract: The invention relates to a process for the production of a tablet containing S-ibuprofen which rapidly releases the active compound, and to S-ibuprofen-containing tablets prepared by this process.

Abstract: A pharmaceutical composition is provided for treating hyperlipidemia or hypercholesterolemia or both in a mammal, which contains an effective amount of each of fenofibrate and an excipient containing one or more polyglycolyzed glycerides.

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: A tamper-resistant, caplet like medicament that masks the taste of poor tasting drugs and possesses an improved lubricity for easier swallowing is produced by shrinking a gelatin-based capsule about a caplet-shaped tablet of the medicament at specific temperatures, pressure and relative humidity.

Abstract: An improved bioactive agent delivery composition and method of application are described. The composition comprises a bioactive agent, a hydrophilic polymer in an incompletely hydrated state and a substantially water-miscible solvent system. The agent and polymer are essentially dissolved in the solvent system to form a sprayable composition having a viscosity of less than 350 cP. Upon dilution with water, the viscosity of the composition increases to in excess of 1000 cP to produce a retentive coating at the site of application which provides enhanced bioavailability of the agent.

Abstract: Stabilized medicinal substances, a process for the preparation thereof, and stable medicinal formulationsStabilized compounds of the formula I ##STR1## in which R, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 have the stated meanings, and a process for the preparation thereof, are described. The stabilized compounds are suitable for the manufacture of medicinal formulations. The formula I compounds are stabilized by a polymeric protective coating before being compressed in tablet form.

Abstract: There are disclosed herein a gelatin coating composition which comprises succinated gelatin as the main component and polyethylene glycol, and a hard gelatin capsule formed from said gelatin coating composition. The hard gelatin capsule has sufficient mechanical strength for filling operation. Moreover, it does not become insoluble due to reaction with a special drug having an aldehyde group filled therein. Therefore, it can be used for various drugs, especially macrolide antibiotics for which conventional hard gelatin capsules are inadequate.

Abstract: Disclosed is a novel simulated capsule medicament consisting of a solid core covered with two shrink-wrapped, hard-shell gelatin capsule halves. The solid cores are covered with the hard-shell gelatin capsule halves by individually shrink-wrapping onto first one end of the core a first hard-shell gelatin capsule half and then individually shrink-wrapping onto a second end of the core a second hard-shell gelatin capsule half.

Abstract: Pharmaceutical formulations for oral administration coated by an enterosoluble gastroresistant film, preferably selected from gastroresistant granulates, gastroresistant tablets, gastroresistant hard gelatine capsules containing powders or granulates or two or more tablets or oily suspensions, gastroresistant soft gelatine capsules containing oily suspensions and hard gelatine capsules containing gastroresistant granulates or two or more gastroresistant tablets, containing therapeutically effective amounts of bile acids mixed with physiologically compatible basic substances which favor bile acids salification and therefore bile acids absorption in the intestinal tract, process for their preparation and therapeutic use thereof in the treatment of biliary calculoses, biliary dyspepsias, biliary cirrhosis and chronic and cholestatic hepatopathies.

Abstract: A simulated capsule-like medicament comprising a dual subcoating comprising an initial subcoating of a water soluble film forming polymer, e.g. povidone and a secondary subcoating of a mixture of two soluble film forming polymers, e.g. povidone and hydroxypropyl methylcellulose and a hydrophobic plasticizer, e.g. castor oil, which provides for a smooth uniform and substantially bubble free outer coating, e.g. gelatin, for the capsule-like medicament; and a process of making such medicaments.

Abstract: A high content of 2-(4-isobutylphenyl)propionic acid is achieved in a pharmaceutical composition by solidifying molten 2-(4-isobutylphenyl)propionic acid to provide a unit dose composition. The composition may be prepared by heating the 2-(4-isobutylphenyl)-propionic acid until molten, optionally mixing with pharmaceutically acceptable excipients, forming into a unit dosage presentation and allowing the composition to solidify. Preferably the composition contains greater than 80% ibuprofen or S(+)-ibuprofen and is filled into a hard gelatin capsule.

Abstract: An osmotic device (10) for the controlled systemic delivery of nicotine through an oral mucosal membrane of a human patient is disclosed. The device (10) has a size and shape adapting it to be comfortably retained in the mouth for extended periods of time. The device (10) comprises a semipermeable wall (12) surrounding a compartment (13) containing a nicotine salt (14) and optionally an alkaline salt which is capable of reacting with the nicotine salt in the presence of water to form nicotine base. The conversion of nicotine salt to nicotine base may take place within the device (10) and/or outside the device and in the patient's mouth. Nicotine base and/or salt is delivered from the compartment (13) through a passageway (17) in the wall (12). The nicotine salt exhibits good stability and shelf life while the nicotine base exhibits excellent absorption through oral mucosal membranes.

Abstract: Pharmaceutical tablets having increased slipperiness and swallowability are provided. The enhanced swallowability is imparted by an overcoat of a low bloom gelatin, which overcoat has a lower coefficient of friction than other known coatings.

Abstract: A method for treating azaribine-responsive diseases in patient's who exhibit severe pyridoxal phosphate depletion following the oral administration of azaribine comprises first encapsulating azaribine in a film-forming substance which is selectively soluble in the digestive juice of the intestines. The encapsulated azaribine is then orally administered to the patient in an amount effective for the treatment of the disease, preferably in an amount to provide from about 1.5 to about 15 grams of azaribine per square meter of patient body surface area per day.

Abstract: A capsule-like medicament, method for producing such medicaments and apparatus. Such medicaments are achieved by individually dipping and drying first one end, and then the other end, of each caplet to provide a coating which is smoother and easier to swallow than an uncoated caplet. The production of these capsule-like medicaments is readily facilitated by simple and inexpensive modifications which can be made to existing empty gelatin capsule making equipment.

Abstract: A benzoylaminophenoxybutanoic acid derivative of general formula: ##STR1## [wherein A represents oxygen atom, sulfur atom or sulfinyl (SO) group,R.sup.1 represents hydrogen atom or methyl group,R.sup.2 represents a group of the general formula: ##STR2## {wherein B represents oxygen atom, sulfur atom or a group of general formula: NR" (wherein R" represents hydrogen atom or alkyl group of from 1 to 4 carbon atoms(s)), R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 represent, independently, hydrogen atom, alkyl group of from 1 to 4 carbon atom(s), halogen atom or trifluoromethyl group,m represents 0 or 1,n represents an integer of from 1 to 4, andR.sup.9 and R.sup.10 represent, independently, hydrogen atom, alkyl group of from 1 to 5 carbon atom(s) or a group of general formula: ##STR3## (wherein R.sup.12, R.sup.13, R.sup.14 and R.sup.15 represent, independently, hydrogen atom, alkyl group of from 1 to 4 carbon atom(s), halogen atom or trifluoromethyl group, and 1 represents an integer of from 1 to 4.

Abstract: A tablet composition for a phthalazineacetic acid compound to be employed in treating clinical effects associated with diabetes is described. The composition permits formation of tablets having a relatively high dose of drug in a relatively small size useful for gaining patient compliance. The preferred phthalazineacetic acid compound is 3-((4-bromo-2-fluorophenyl)methyl)-3,4-dihydro-4-oxo-1-phthalazineacetic acid.

Abstract: A chewable delivery system for actives comprising:(a) an active pre-coated with at least one material selected from the group consisting of lecithin, polyoxyalkylenes having chain lengths of about 4 carbons or less, glycerides having a melting point of 100.degree. C. or less, polyalkyleneglycols having a molecular weight of 3,700 or less, synthetic and natural waxes and mixtures thereof; and(b) a confectionery matrix comprising a binder system comprising gelatin and a humectant material selected from the group consisting of glycerin and its lower alkyl (C.sub.2-7) ester derivatives; a sweetener; and about 1% to about 30% by weight water.

Abstract: A process for producing an administration or dosage form of drugs, reagents or other active ingredients. A watersoluble foil composed of starch, gelatin, glycerin and/or sorbit and if necessary other additives is coated by a roll coating process with a layer containing the active ingredients and composed of the samebasic ingredients. After a corresponding prefragmentation, the administration form thus produced is particularly useful as an oral administration drug.

Abstract: Sustained-release formulations which can release a water-soluble active ingredient or ingredients at the zero-order over a long period of time, comprising:a. an inert core,b. a powder-coating layer containing a water-soluble active ingredient or ingredients,c. a powder-coating layer of practically water-repellent material, andd. a film-coating layer composed of practically pH-independent and water-insoluble film-coating material.

Abstract: A method for the preparation of tablets slowly releasing the active principle, characterized in that (I) during the granulation step a solution in organic solvents of a polymer insoluble in biological juices is sprayed on a mixture containing an active principle, slightly swelling polymers and usual excipients; (II) the granulated obtained in this way is added with a highly hydroswelling colloidal polymer; (III) a solution, in organic solvents, of an entero-soluble polymer, is sprayed on the granulate; (IV) the resulting granulate is submitted to compression; (V) the obtained tablets are hardened by washing with organic solvents; and (VI) they are then optionally coated.

Abstract: A chewable delivery system for actives comprising:(a) an active pre-coated with at least one material selected from the group consisting of lecithin, polyoxyalkylenes having chain lengths of about 4 carbons or less, glycerides having a melting point of 100.degree. C. or less, polyalkyleneglycols having a molecular weight of 3,700 or less, synthetic and natural waxes and mixtures thereof; and(b) a confectionery matrix comprising a binder system comprising gelatin and a humectant material selected from the group consisting of glycerin and its lower alkyl (C.sub.2-7) ester derivatives; a sweetener; and about 1% to about 30% by weight water.