Abstract: The use of a starch obtained from a plant source that is homozygous in a white recessive gene, such as white common corn starch, has superior compression and ejection forces compared to commercial disintegrantants/binders. The starch derived from common corn containing the homozygous white recessive gene was also found to have comparable whiteness to commercial bleached corn starches used in tableting.

Abstract: Sustained and enhanced antipyretic response is elicited in a mammalian organism in need of such treatment, i.e., a mammal suffering from elevated body temperature (fever), by administering thereto a unit dosage sustainedly enhancing, antipyretically effective amount of the free acid S(+) flurbiprofen enantiomer, said enantiomer being substantially free of its R(-) flurbiprofen antipode.

Abstract: Improved oral formulations are prepared by admixing gemfibrozil with from 1 to 4%, by weight, of a pharmaceutically acceptable surfactant having an HLB value of from about 10 to about 50.

Abstract: The subject invention relates to compositions in dosage form comprising a solid dispersion which is a solidified melt mixture consisting essentially of the following components:(a) from about 15% to about 75% of tebufelone;(b) from about 25% to about 65% of a poloxamer surfactant having a melting point of about 40.degree. C. or greater, the poloxamer surfactant consisting essentially of a block copolymer having three polymer blocks, a middle block of poly(oxypropylene) with a molecular weight of from about 1450 daltons to about 6000 daltons, and end blocks of poly(oxyethylene), the end blocks being from about 50% to about 90% of the copolymer; and(c) from 0% to about 60% of other components, wherein the other components are miscible with a melt mixture of components (a) and (b).

Abstract: A defoaming or antifoaming composition comprises a free flowing granular combinate of 50 to 90 weight percent of a water soluble carbohydrate-based agglomerate selected from the group consisting of maltodextrin agglomerates, maltodextrin/dextrose co-agglomerates, dextrose agglomerates, maltodextrin/sucrose co-agglomerates, maltodextrin/fructose co-agglomerates, sucrose agglomerates, fructose agglomerates, mannitol agglomerates, sorbitol agglomerates, agglomerates of hydrolyzed cereal solids, and agglomerates of corn syrup solids and about 10 to 50 weight percent of a liquid, nonaqueous, defoaming or antifoaming composition such as simethicone, hydrocarbon-based oils or silicone oils. The composition may be combined with one or more suitable excipients and prepared as a unit dosage in the form of a compressed tablet, filled capsule, packet, or granule for various defoaming applications.

Abstract: A functional food which comprises a glucosyltransferase and/or a fructosyltransferase each having a water-soluble polysaccharide production ability, and a base therefor.

Abstract: A stable rapidly dissolving lyophilized composition of cyclophosphamide and an amino acid selected from the group consisting of glycine, valine and serine is provided which contains an amount of water which is equimolar to the amount of amino acid and the amount of cyclophosphamide in said composition; the composition is preferably prepared from a solution containing at least 2% (W/V) of the amino acid and having a pH in the range of 5.0 to 7.0.

Abstract: A pharmaceutical tablet is provided herein having an effective dissolution rate. The tablet contains a pharmaceutically-active ingredient and a substantially linear, i.e. non-crosslinked K-30 to K-120 PVP as a binding agent. The PVP used herein is made by an initiated polymerization process in which vinyl pyrrolidone monomer is polymerized in the presence of an initiator which produces a linear PVP polymerization, i.e. is a poor hydrogen abstractor of PVP polymer backbones, which would produce a disadvantageous crosslinked PVP product. Suitable initiators include low energy peroxyester free radical initiators, such as t-amylperoxy pivalate, an azo initiator, or a redox initiator which can perform at low temperatures.Preferably the residual initiator level in the PVP is reduced to less than 500 ppm, thereby further precluding the possibility of crosslinking of the PVP polymer during the shelf-life of the tablet.

Abstract: This invention relates to highly active and solid pharmaceutical preparations rapidly releasing the active substance for the treatment of diabetes, particularly: 1. liquid formulations of glibenclamide consisting of 1 part of glibenclamide and 4 to 1500 parts of liquid sugar alcohols such as 70% sorbitol solution or glycol such as propylene glycol, hexylene glycol, di-, tri- or polyethylene glycol having a molecular weight from 76 to 600, optionally 0.5 to 2 moles of an alkaline reacting substance and other drug additives; 2.

Abstract: The invention provides a dispersible solid drug formulation comprising finely divided diclofenac as the free acid, from 5 to 25% by weight of a disintegrant and a pharmaceutically acceptable diluent.

Abstract: An excipient for a pharmaceutical compound which melts at body temperature but will not spontaneously deform at higher temperatures encountered in shipment and storage comprises:______________________________________ Low MW Polyethylene glycol 75-90% (M.P. about 37.degree. C.) Medium to high MW polyethylene glycol 0-4% Long chain saturated carboxylic acid 0-4% Polyethylene oxide 0-4% (MW 100,000-5,000,000) Colloidal silica 10-20%. ______________________________________The excipient is particularly advantageous for the preparation of dosage forms for buccal administration of pharmaceutical compounds.

Abstract: Allergens are contained in strictly controlled and reproducible amounts on solid supports to provide a progressive release of the allergen perlingually and sublingually. The compositions are prepared by dissolving an allergen in a polar solvent to obtain a mother solution; preparing dilutions of different predetermined concentrations; fractionating each of the dilutions into sub-dilutions; and impregnating a pharmaceutically acceptable solid support with each sub-dilution, each impregnation step being followed by drying in forced, dried air at a temperature not greater than 30.degree. C.; and applying a protective coating onto the composition.

Abstract: The subject invention relates to methods for regulating wrinkles in mammalian skin comprising topical application of a lysophosphatidic acid compound having the structure: ##STR1## or a cyclic derivative thereof having the structure: ##STR2## or a pharmaceutically acceptable salt thereof, wherein --R is unsubstituted or substituted, saturated or unsaturated, straight or branched chain alkyl having from 12 to about 23 carbon atoms; each --X-- is independently --O-- or --S--; and --Y-- is --O-- or --CH.sub.2 --.

Abstract: Dietetic formulations for oral use are described, made up of tablets formed from dense granules of mixtures of keto- or hydroxy-amino acid analogs, possibly coated by protective films, which are dissolved in the gastrointestinal juices. The process for obtaining dense granules includes a coordinated increase in pressure being maintained for a substantial period of time and subsequent tableting and possible coating by immersion or spraying of the granular material.

Abstract: A lyophilized pharmaceutical solid composition containing cyclophosphamide for reconstitution with water to provide a solution for oral or parenteral administration. This lyophilized cyclophosphamide solid composition demonstrates improved stability, solubility characteristics and enhanced appearance compared with currently available dry powder pre-mix compositions of cyclophosphamide. The lyophilized solid composition contains about 20 parts by weight of cyclophosphamide, about 11/4-2 parts by weight of water and from about 10-85 parts by weight of excipient which is comprised mainly of mannitol. Processes for making the composition are disclosed.

Abstract: A tableting aid including magnesium carbonate and an oil adsorbed thereon provides useful lubricating and disintegration properties. A free-flowing particulate flavoring additive including magnesium carbonate and a flavor oil adsorbed thereon, is also described.

Abstract: The stability of compositions of choline salicylate-metal salicylate-carboxymethylcellulose is improved by the incorporation therein of microcrystalline cellulose. The microcrystalline cellulose is linked to the remainder of the composition by liquid bridges and is preferably present in an amount of about 2.5-25% by weight. The microcrystalline cellulose enhances the stability of the composition and thereby enhances solid dosage forms thereof such as tablets, capsules, suppositories and granules.

Abstract: A coated solid medicament form suitable for oral administration having reliable releasability of the active ingredient only in the large intestine is proposed. The medicament form is prepared by coating a core solid medicament form containing the active ingredient first with a chitosan having a specific degree of deacetylation and a specific degree of polymerization and then top-coated with a specific enteric-soluble polymer which is a hydroxypropyl methyl cellulose acetate succinate or a hydroxypropyl methyl cellulose hexahydrophthalate. The releasability of the active ingredient only in the large intestine can be more reliable when the core medicament form is, prior to coating with chitosan, provided with an enteric undercoating layer.

Abstract: The present invention relates to methods of neutralizing or dissipating the electrostatic charge of glutathione so as to render it susceptible to be included in high glutathione content solid dosage forms. Capsules and tablets including high levels of glutathione are also described.

Abstract: This invention relates to an analgesic composition and more particularly, to a directly dry compressible composition comprising at least about 70% by dry weight of the composition of acetaminophen and a metal carboxymethyl starch present in an amount sufficient for it to function both as a binder and as a disintegrating agent.

Abstract: The invention provides a pharmaceutical granule comprising cimetidine and 2-20% (w/w) relative to the cimetidine of a co-polymer of dimethylaminoethylmethacrylate and neutral methacrylic acid esters. Compositions of this invention have good palatability and dissolution characteristics.

Abstract: The subject invention involves compositions, consisting essentially of the drug active 1-3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl-5-hexyn-1-one (tebufelone) at a concentration of at least about 15%, and the balance a pharmaceutically-acceptable vehicle. The vehicle is formulated such that the compositions are homogeneous liquids at 37.degree. C. and provide good solubilization of the drug active.

Abstract: A method for preventing the sickling of sickle cells in a patient having sickle cell disease, the method which comprises administering to the patient a therapeutically effective amount of a compound having the formula: ##STR1## wherein X.sup.- is selected from the group consisting of iodide, chloride, bromide, hydroxyl, nitrite, phosphate and acetate.

Abstract: Controlled release verapamil tablets are disclosed. The tablets include an excipient having a hydrophilic material, preferably containing a mixture of xanthan gum/locust bean gum, and an inert diluent.

Abstract: 8,10-Dideazatetrahydrofolic acid derivatives of the formula: ##STR1## where R.sub.1 and R.sub.2 are selected from hydrogen and alkyl having from one to about eight carbon atoms and the carboxylates and acid addition salts thereof, showing strong inhibition of L1210 murine leukemia cells in culture, modest inhibition of glycinamide ribotide transformylase and aminoimidazole carboxamide ribotide transferase, and insignificant inhibition of dihydrofolate reductase and thymidylate synthase enzymes.

Abstract: A pharmaceutical solid preparation of active form of vitamin D.sub.3 of improved stability which comprises a composition of active form of vitamin D.sub.3 dispersed in an excipient readily soluble in organic solvent and a basic substance.As a basic substance, are cited sodium citrate, magnesium oxide or the like.

Abstract: An excipient for a pharmaceutical compound which melts at body temperature but will not spontaneously deform at higher temperatures encountered in shipment and storage comprises:______________________________________ Low MW Polyethylene glycol 75-90% (M.P. about 37.degree. C.) Medium to high MW polyethylene glycol 0-4% Long chain saturated carboxylic acid 0-4% Polyethylene oxide 0-4% (MW 100,000-5,000,000) Colloidal silica 10-20%. ______________________________________The excipient is particularly advantageous for the preparation of dosage forms for buccal administration of pharmaceutical compounds.

Abstract: In accordance with the present invention an improved tablet composition for drugs or active ingredients prone to poor tabletting properties is disclosed. The improved composition comprises a premixture, consisting essentially of between about 85 and 99.9 percent by weight of the active ingredient and between about 0.1 and 15 percent by weight of citric acid, and one or more other formulation ingredients added to premixture. The present invention also involves the process for making such compositions and products therefrom.

Abstract: A free-flowing directly compressible granulation useful as a slow release pharmaceutical excipient is disclosed. The excipient includes a hydrodrophilic matrix which includes heteropolysaccharide and a polysaccharide material capable of cross-linking the heteropolysaccharide, and an inert diluent.

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 aobut 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.

Abstract: This invention relates to an analgesic composition and more particularly, to a directly dry compressible composition comprising at least about 70% by dry weight of the composition of acetaminophen and a metal carboxymethyl starch present in an amount sufficient for it to function both as a binder and as a disintegrating agent.

Abstract: Pressing having sustained release of active compound for the oral or parenteral administration of medicaments, which contains at least one solid pharmaceutical active compound, polylactic acid and a homo- or copolymer of D(-)-3-hydroxybutyric acid and processes for its production.

Abstract: A slow release pharmaceutical excipient of an inert diluent and a hydrodrophilic material including xanthan gum and a galactomannan gum capable of cross-linking the xanthan gum in the presence of aqueous solutions.

Abstract: A sustained or controlled release tablet is disclosed. The tablet comprises a water soluble medicament, a hydroxypropyl methylcellulose having sustaining action, a pharmaceutical binding agent, and a hydrophobic component.

Abstract: New polysaccharide esters are disclosed, and more precisely esters of acidic polysaccharides chosen from the group formed by carboxymethylcellulose, carboxymethyl starch and carboxymethylchitin. These new esters and some esters of the type already known are useful as medicaments, for the manufacture of pharmaceutical and cosmetic preparations, in the field of biodegradable plastic materials and, therefore, for the manufacture of medical, surgical and sanitary articles, as well as numerous other industrial sectors in the place of acidic polysaccharides now in common use.

Abstract: A free-flowing, spray-dried edible powder is preferably made by partially hydrolyzing a gelatin, followed by making an emulsion of the gelatin and an edible oil, followed by spray-drying the emulsion. The method partially hydrolyzes the gelatin so that the weight average molecular weight of the gelatin is between about 15,000 and 35,000. Preferably the vitamin is vitamin E. Preferably the partial hydrolysis of the gelatin is an enzymatic hydrolysis.

Abstract: A method for preventing the sickling of sickle cells in a patient having sickle cell disease, the method which comprises administering to the patient a therapeutically effective amount of a compound having the formula: ##STR1## wherein X.sup.- is selected from the group consisting of iodide, chloride, bromide, hydroxyl, nitrite, phosphate and acetate.

Abstract: A prolonged-release unit dosage formulation or pharmaceutical composition, preferably in tablet form, is described. The composition consists essentially of a gel-forming dietary fiber, a biologically-absorbable drug or other active therapeutic agent, and certain specific disintegrants, namely, a physiologically-acceptable edible acid and a mineral salt which releases a physiologically-acceptable gas upon ingestion, preferably carbon dioxide, e.g., a mineral carbonate or bicarbonate, and advantageously dextrose or like soluble sugar. The dietary fiber-containing composition, when compressed into a tablet together with the drug and the specific disintegrants, provides a unique and efficient prolonged-action drug-delivery system.

Abstract: A dieting agent is disclosed which comprises an aqueous solution or a solid substance of a concentration .alpha.-amylase inhibiting substance which is produced by a process which comprises heat treating a supernatant fraction of an aqueous extract of wheat or wheat flour to modify unnecessary protein contaminants in the supernatant fraction, removing a modified protein from said fraction, subjecting a resulting aqueous solution containing an .alpha.-amylase inhibiting substance to a concentration treatment using an ultrafiltration membrane to form an aqueous solution of a concentrated .alpha.-amylase inhibiting substance or drying the aqueous solution. The dieting agent exhibits a body weight gain-inhibiting effect.

Abstract: Ibuprofen tablets/caplets formed by wet granulation of the ibuprofen characterized by a dissolution profile maintained stable on aging by incorporating croscarmellose sodium separately into the wet granulation and the compression mix and further incorporating sodium lauryl sulfate into the compression mix.

Abstract: The present invention pertains to an edible coated composition which comprises (a) a core material comprising sorbitol, (b) a primary coating layer comprising zein over the core material, and (c) a sugarless secondary coasting layer over the primary coating layer. The present invention also pertains to methods for preparing the edible coated compositions.

Abstract: Chewable medicament tablets are made from coated granules of a medicament wherein the coating on said granules comprises a blend of cellulose actate and/or cellulose acetate butyrate and hydroxypropyl cellulose and a process for making such tablets and a method of providing sustained release of medicaments utilizing such coated granules in a tablet.

Abstract: A consumable antigas or antiflatulent composition is produced by combining a water soluble agglomerated maltodextrin and a fluid, nonaqueous, defoaming or antifoaming composition such as simethicone or silicone, mineral or other oils containing silica to form a granular mixture. The granular mixture may be prepared in a unit dose in granular form or as a compressed tablet or capsule.

Abstract: A stable rapidly dissolving lyophilized composition of cyclophosphamide and alanine is provided.

Abstract: This invention relates to analgesic composition and more particularly, to a directly dry compressible composition comprising at least about 70% by dry weight of the composition of acetaminophen and a metal carboxymethyl starch present in an amount sufficient for it to function both as a binder and as a disintegrating agent.

Abstract: Polymers from ethylenically unsaturated monomers, cross-linked by a substituted divinylazobenzene are useful as pharmaceutical compositions for the delivery of medicaments. The polymers are degraded by the enzymes of the upper gastrointestinal tract or are transferred intact past the upper gastrointestinal tract, to deliver the medicament to the large intestine. In particular, the polymers contain divinylazobenzene compounds of the formulae ##STR1## wherein R.sub.1 and R.sub.2 are independently selected from the group consisting of H, (except that R.sub.1 and R.sub.2 are not both H), Cl, Br, I, NO.sub.2, NH.sub.2, RO, ArO, COOH or salts thereof, COOR, COOAr, CHO, COR, SO.sub.3 H or salts thereof, R or Ar and wherein R is alkyl of up to 18 carbon atoms and Ar is mono- or bicyclic aryl of up to 15 carbon atoms.

Abstract: Provided are a solid pharmaceutical preparation which contains disodium adenosine triphosphate together with a vitamin B.sub.1 salt or the like and a method of treatment of human asthenopia by orally administering the same. Also provided are a solid pharmceutical preparation according to the abovementioned preparation, which further contains a low-melting fat- or oil-like substance and has an improved stability of disodium adenosine triphosphate, and a method of producing the same.

Abstract: A composition for treatment and treatment of certain skin diseases is disclosed. The treatment combines furocoumarins, UV-A radiation, and a benzylidene-camphor derivative. The composition and treatment produces the desirable results of the furocoumarin/UV-A radiation treatment without the undesirable phototoxic side effects.

Abstract: Onset-hastened and enhanced antipyretic response is elicited in a mammalian organism in need of such treatment, i.e., a mammal suffering from elevated body temperature (fever), by administering thereto a unit dosage onset-hastening/enhancing antipyretically effective amount of the S(+) ibuprofen enantiomer, said enantiomer being substantially free of its R(-) ibuprofen antipode.

Abstract: Onset-hastened and enhanced antipyretic response is elicited in a human mammal in need of such treatment, i.e., a human mammal suffering from elevated body temperature (fever), by administering thereto a unit dosage onset-hastening/enhancing antipyretically effective amount of the S(+) ketoprofen enantiomer, said enantiomer being substantially free of its R(-) ketoprofen antipode.