Abstract: An improved form of administration of 1,4-dihydro-2,6-dimethyl-4-(2-nitrophenyl)-3,5-pyridine-dicarboxylic acid-dimethylester (i.e., Nifedipine) is provided in which the Nifedipine is molecularly dispersed wihtin a solidified melt of polyethylene glycols which are liquid, semi-solid and solid at room temperature. The weight ratio of liquid to non-liquid polyethylene glycols in the solidified melt ranges from about 7:23 to 23:7, the solidification temperature of the mixture ranges from about 25.degree. C. to 62.degree. C. and the mixture has a viscosity of from about 1 to 180,000 poise when measured at 20.degree. C. in admixture with up to about 40 percent by weight of water.

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

Abstract: The invention is a method of stimulating cashmere growth on cashmere-producing goats. The method includes administering melatonin by a sustained release delivery system.

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

Abstract: 5-Amino or substituted amino 1,2,3-triazoles are disclosed as a new class of antiproliferative agents useful in the treating and managing of psoriasis, inflammatory bowel syndrome, cutaneous leishmanilisis and certain types of cancer.

Abstract: Treatment of AIDS or humans carrying or infected with the AIDS virus or having antibodies to the AIDS virus is disclosed using the compound 3'-azido-3'-deoxythymidine or a pharmaceutically acceptable basic salt thereof.Also disclosed is the use of 5'-mono-, di- and triphosphate of 3'-azido-3'-deoxythymidine or a pharmaceutically acceptable basic salt thereof for the same purpose.

Abstract: Soft elastic gelatin capsules containing primarily the crystalline form A of oxytetracycline hydrochloride exhibit increased storage ability.

Abstract: Treatment of AIDS or humans carrying or infected with the AIDS virus or having antibodies to the AIDS virus is disclosed using the compound 3'-azido-3'-deoxythymidine or a pharmaceutically acceptable basic salt thereof.Also disclosed is the use of the 5.dbd.-mono-, di- and triphosphate of 3'-azido-3'-deoxythymidine or a pharmaceutically acceptable basic salt thereof for the same purpose.

Abstract: A sustained release theophylline containing oral dosage formulation comprising theophylline containing micropellets coated with from about 0.5% to about 2% by weight of a pharmaceutically acceptable water-insoluble film former, preferably ethyl cellulose and having first order release. The formulation is an improvement over theophylline containing micropellets coated with two film formers which have zero order release. The oral dosage formulation has superior non-fasting release and absorption characteristics when compared to the zero order release formulation.

Abstract: Biphenylylpropionic acid derivatives of the formula: ##STR1## wherein R is an alkylcarbonyloxyalkyl group or an alkenylcarbonyloxyalkyl group having the formula: ##STR2## wherein R.sup.1 is a lower alkyl group having 1 to 5 carbon atoms and R.sup.2 is an alkyl group having 1 to 15 carbon atoms or an alkenyl group having 2 to 8 carbon atoms, or a lactone having the formula: ##STR3## wherein R.sup.3 and R.sup.4 are hydrogen atom or a lower alkyl group having 1 to 2 carbon atoms, and n is an integer of 1 or 2. The compounds have excellent anti-inflammatory, analgesic and antipyretic activities. Moreover, the compounds have no irritation, rapid and long-acting, and high safety margin.

Abstract: Aromatic heterocyclic derivatives have the formula ##STR1## wherein R.sub.1 represents ##STR2## wherein R.sub.3 represents hydrogen, --OR.sub.4 wherein R.sub.4 represents hydrogen, alkyl having 1-20 carbon atoms or mono- or polyhydroxyalkyl or R.sub.3 represents ##STR3## wherein r' and r" represent hydrogen, lower alkyl or together form a heterocycle, R.sub.2 represents hydrogen or --CH.sub.3 and Ar represents ##STR4## wherein Z is O or S, ##STR5## wherein R.sub.5 is lower alkyl or ##STR6## wherein R.sub.6 is hydrogen or alkyl having 1-10 carbon atoms and R.sub.7 represents alkyl having 4-12 carbon atoms or cycloalkyl, Y is CH or a nitrogen atom and X represents oxygen, sulfur or --N--R.sub.8 when R.sub.8 represents hydrogen, lower alkyl or lower alkoxycarbonyl, with the proviso that (i) when Y is CH and X is oxygen or sulfur Ar is other than C and (ii) when Y is nitrogen and X is oxygen, Ar is other than (C) or (D) in which R.sub.6 is alkyl having 1-4 carbon atoms and R.sub.

Abstract: Foam capsules with telescopically engaged body and cap portions, also known as hard shell capsules, having a special wall structure, obtained by a microdispersion of a gas in a gelatin solution.The capsule body and cap portions are formed by dipmolding the film-forming mixture obtained by a microdispersion of the gas in a gelatin solution; optionally with the inclusion of a plasticizer and/or coloring agent, and/or flavoring agent, and/or foam stabilizer, and/or gelatin extender.By a suitable choice of the gas proportion in the capsule wall and its micronization level, it is possible, within certain limits, to control the capsule wall disintegration speed and its opacity. In addition, inclusion of gas bubbles into the capsule wall lowers the gelatin content for a foam capsule and provides energy saving during the process due to a faster drying of the wall, thereby providing lower cost prices for the production of pharmaceutically acceptable capsules.

Abstract: A pharmaceutical composition comprising a freely flowable powder, the powder comprising a porous, high absorption silica or silicate having absorbed therein at least 10% by volume of a liquid, pharmaceutically active composition, based on the weight of powder plus liquid, provided that when the liquid pharmaceutically active composition is a corticoid solution the silica or silicate has a mean particle size of at least 10 .mu.m in diameter.

Abstract: The invention relates to liquid, transparent, multicomponent systems for use in pharmaceutical products for cutaneous, peroral, vaginal and parenteral administration of pharmaceutical active agents. The multicomponent systems according to the invention contain the active agents in a solution of an oily and optionally an aqueous component in the presence of certain physiologically acceptable surfactants and cosurfactants. Under certain conditions, the cosurfactants can serve as oil components or the latter can optionally take over the cosurfactant function. The biological availability of the active agents applied in the form of the multicomponent systems according to the invention is much better than that of active agents applied in the form of known multicomponent systems.

Abstract: Light-fast capsules for dihydropyridines such as nifedipine and nisoldipine are formed of gelatin colored with a mixture of .beta.-carotene and iron oxide.

Abstract: Soft gelatin capsules containing a solution of from 15 to 30 parts by weight of ibuprofen in from 70 to 85 parts by weight of polyoxyethylene-polyoxypropylene polymer or in a mixture of from 30 to 76 parts by weight of polyalkylene glycol and from 7 to 40 parts by weight of a surfactant have a very rapid and high bio-availability of the active ingredient. The active ingredient is not re-precipitated therefrom by aqueous media such as artificial gastric juice.

Abstract: A soft capsule which is prepared by wrapping an oily substance which is a member selected from the group consisting of tricaprylic acid glyceride and sesame oil, with a gelatin film containing sodium picosulfate.

Abstract: The present invention relates to a coronary therapeutic agent in the form of soft gelatin capsules, which contain the active substance nifedipine in an organic solvent. In the prior art, there where problems regarding the capsule size and with respect to the low nifedipine active substance concentration. These problems are obviated by the invention, in that nifedipine with PVP, optionally as a coprecipitate and without glycerin, is dissolved in THFP and consequently permits a capsule weight of in all only e.g. 162 mg.

Abstract: Disclosed is a method for loading capsules having a semipermeable membrane with a chemically active substance to be released over time. The method first involves gradually deflating and dehydrating the capsules and subsequently soaking the deflated capsules in a solution containing the substance to be encapsulated. After loading, the permeability of the capsule may be adjusted to accommodate the requirements of the end use. The loaded capsules of this invention may be used in a variety of applications, including use as a bioimplantable drug or biochemical delivery system.

Abstract: Particles containing a releasable fill material and method of preparing same. A particle comprises a continuous polyurea surface layer, and an interior portion comprising a polyurea matrix, said matrix having a fill material contained therein, said matrix forming a continuum extending from the surface layer into the interior of the particle.

Abstract: A gelatin capsule dosage form containing triamterene, 2,4,7-triamino-6-phenylpteridine, which results in rapid dissolution of the active ingredient. The dosage form comprises the pharmaceutical binder methylcellulose in combination with low doses of a surfactant or a carbonate salt as disintegrants.

Abstract: The present invention relates to a sequential polymerization process for preparing a water-insoluble dispersion of core/shell particles. In one embodiment the process may be employed to produce a particulate dispersion useful in making water-based coating compositions wherein on drying the particulate dispersion serves as an opacifying agent. In another embodiment the process may be employed to microencapsulate a hydrophobic target material, such as a biocide or herbicide.

Abstract: A dosage form is disclosed for delivering the beneficial drugs pseudoephedrine and brompheniramine to a biological environment of use.

Abstract: Polymers from ethylenically unsaturated monomers, cross-linked by a substituted or unsubstituted divinylazobenzene are useful as carriers or capsules for medicaments, which are degraded by the enzymes of the upper gastrointestinal tract or which must be transferred intact past the upper gastrointestinal tract, to deliver the medicament to the large intestine.Polymers containing monomeric units of the formulaH.sub.2 C.dbd.CH--C.sub.6 H.sub.4 --N.dbd.N--M,wherein M is the residue of an amino-containing medicament, are useful as carriers for therapeutic agents or as therapeutic agents per se.

Abstract: A concentrated suspension of calcium carbonate particles in a liquid carrier that is compatible with a capsule shell material. The suspension is pourable and pumpable and may be used to provide antacid capsules.

Abstract: This invention relates to vehicles for the administration of mopidamol. More specifically, this invention relates to a method of treating cardiovascular disorders, malignancy, or thrombosis in a host in need of such treatment which comprises administering to said host a cardiovascularly, antimetastic, or antithrombotic effective amount of a composition comprised of (i) mopidamol or an acid addition salt thereof and (ii) at least one pharmacologically acceptable acid or acid substance, the total amount of acid from acid addition salt present and acid or acid substance being in a ratio of at least about 1 acid equivalent to 1 mol of mopidamol or its acid addition salt.

Abstract: Pharmaceutical compositions produced with liquid, hydrophilic lubricants possessing markedly improved dissolution rates.

Abstract: The present invention is concerned with the simultaneous formation and encapsulation of small particles from aqueous solutions of compounds whose solubility is greater at a first pH than at a second pH. The process is preferably used to prepare a readily soluble encapsulated pharmaceutically active compound.

Abstract: The present invention is concerned with the simultaneous formation and encapsulation of small particles of organic compounds whose solubility in water is greater at a first pH than at a second pH by concurrently precipitating said organic compounds as small particles and forming a coacervate of an anionic (or cationic) surfactant and an amphoteric surfactant. The process is preferably used to prepare a readily soluble encapsulated pharmaceutically active compound.

Abstract: Process for the formation and the simultaneous encapsulation of small particles of a compound from solution which comprises:(a) dissolving said compound in a first solvent;(b) preparing a solution of encapsulating material and an electrolyte in a second solvent which is miscible with the first solvent and in which the compound to be encapsulated is more or less insoluble, in an amount which is effective, but present in an amount just insufficient to cause coacervation of the encapsulating material without interacting with it;(c) mixing the solutions from step (a) and (b) while stirring to cause the concurrent precipitation of the compound as small particles and formation of a coacervate of the encapsulating material; and(d) gelling the encapsulating material.

Abstract: The invention relates to a process and a preparation for deactivating viruses inside living human and animal organisms by application of a terpene obtainable from aromatic plants by steam distillation. The terpenes cited are: black pepper oil, cinnamon flower oil, cardamon oil, linallyl acetate, cinnamic aldehyde, safrol, carvon and cis/trans citral.

Abstract: A dry sustained release oral dosage formulation of theophylline and a method of orally administering theophylline is disclosed. The oral formulation is comprised of a capsule which includes upper and lower parts which are connectible and easily separable from each other, and a plurality of micropellets present in the capsule. The micropellets provide sustained release of theophylline when taken by a patient and are comprised of inner seeds coated with a mixture of theophylline and polyvinylpyrrolidone which is further coated with a mixture of ethylcellulose and hydroxypropylcellulose. The oral dosage formulation is administered by separating the upper and lower parts of the capsule and placing the micropellets on a food which is preferably soft to the extent of not requiring chewing and then eating the food with the micropellets thereon.

Abstract: A process for the formation of microcapsules having at least two polymeric substances forming the final microcapsule walls comprising forming a stable emulsion droplet comprising an amphiphilic polymeric agent and the material to be encapsulated and coupling to said amphiphilic polymeric agent at least one polymeric substance to form a substantially impermeable wall about said material, said at least one polymeric substance being capable alone of reacting with said amphiphilic polymeric agent or capable of coupling with said amphiphilic polymeric agent in the presence of a coupling agent capable of reacting with said amphiphilic polymeric agent and said at least one polymeric substance. Also the resultant microcapsules and products, preferably, transfer sheet materials utilizing said microcapsules.

Abstract: A chewable, filled, one-piece soft elastic gelatin (SEG) capsule. The capsule includes a shell which is formed from a formulation of gelatin, water, a plasticizer, and a masticatory substance. The masticatory substance is present in the shell in an amount of about 1-75 percent by weight and the gelatin is present in the shell in an amount of about 10-90 percent by weight. A fill material is contained within the shell. The fill may be selected from a variety of materials, including candy, various confectionaries, antacids, cough and cold preparations, sore throat remedies, antiseptics, dental preparations, such as fluorides, breath fresheners, and the like. In manufacturing the SEG capsules, a molten gel mass is prepared with a dispersion of a molten masticatory substance therein. A suitable fill material is also prepared. The gelatin formulation containing the masticatory substance dispersed therein is formed as a shell around the fill material.

Abstract: Novel pyridine compounds and the pharmaceutically acceptable salts thereof having a specific inhibitory activity on thromboxane A.sub.2 biosynthesis in mammals useful for prevention and treatment of various disorders caused by thromboxane A.sub.2, for example, thrombosis, cardiac infarction, diabetic vascular complications, asthma, etc. are disclosed.