Abstract: The present invention relates to a process for solubilizing at least one difficultly soluble pharmaceutical active in a mixture of polyethylene glycol and polyvinylpyrrolidone. The process does not require water as a solvent or the use of a heating step. In further embodiments, the present invention also relates to a process for encapsulating these solubilized pharmaceutical compositions within soft gelatin shells, which are preferably transparent. Both the resulting compositions and their capsules provide an effective means for oral delivery of a wide variety of difficultly soluble pharmaceutical actives.

Abstract: Zinc acexamate acts by increasing the synthesis of mucus, reinforces the mucous barrier, improves the microcirculation and increases the synthesis of prostaglandins in the gastric mucous membrane, whereby it is effective in the treatment of said gastropathy, contrary to the results obtained with antiacids or antisecretory agents.

Abstract: A percutaneous absorption promoting agent comprising (A) at least one anionic surfactant and one or two or more of surfactants having a nitrogen atom in the molecule other than anionic surfactants, (B) one or two or more of anionic surfactants and one or two or more of nonionic surfactants not having a nitrogen atom in the molecule, (C) one or two or more of surfactants selected from the group consisting of amphoteric surfactant and semi-polar surfactants and at least one nonionic surfactant having a nitrogen atom in the molecule, (D) one or two or more of surfactants selected from the group consisting of nonionic surfactants, amphoteric surfactants, semi-polar surfactants and cationic surfactants having a nitrogen atom in the molecule, and one or two or more of nonionic surfactants not having a nitrogen atom in the molecule, or (E) an amine oxide as the active ingredient, and a dermatological preparation containing these percutaneous absorption promoting agent and drug components.

Abstract: 4-Quinolinecarboxylic acids and derivatives thereof, such as 2-(2'-fluoro-1,1'-biphenyl-4-yl)-6-fluoro-3-methyl-4-quinolinecarboxylic acid, are useful as immunodulatory and anti-inflammatory agents. Pharmaceutical formulations containing such compounds are useful for the treatment of autoimmune diseases, organ transplantation rejection, graft vs. host disease, multiple sclerosis, and chronic inflammatory diseases such as rheumatoid arthritis.

Abstract: Biodegradable absorption enhancers, especially useful in pharmaceutical formulations, are compounds having the formula ##STR1## wherein R is hydrogen, C.sub.1 -C.sub.7 alkyl, benzyl or 4-hydroxybenzyl; n is a whole number from 4 to 18 inclusive; R.sub.1 and R.sub.2 are independently selected from hydrogen and C.sub.1 -C.sub.7 alkyl, or R.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached are combined to form a substituted or unsubstituted heterocycloalkyl radical having a total of 5 to 7 ring atoms, optionally including a hetero ring atom selected from oxygen, sulfur and nitrogen in addition to the indicated nitrogen atom, the substituents when present being one to three C.sub.1 -C.sub.7 alkyl radicals, which may be the same or different; and R.sub.3 and R.sub.4 are independently selected from hydrogen, methyl and ethyl.

Abstract: The invention relates to a therapeutical composition of matter for the treatment by perfusion of shock states comprising as an essential ingredient therein, an effective amount either, of a compound of the formula: ##STR1## wherein R.sub.1 and R.sub.4 stant for H or CH.sub.3 or C.sub.2 H.sub.5,R.sub.2 stands for H or NO.sub.2 andR.sub.3 stands for NHR.sub.4 or CH.sub.3 or C.sub.2 H.sub.5alone or of a mixture of said compound with a cyclooxygenase blocker.

Abstract: A method of treating inflammations of body joints in humans by topical application of anti-inflammatory agents may be used to treat joints afflicted by arthritic conditions such as gouty arthritis. The steps of the method include dissolving a predetermined quantity of a known anti-inflammatory drug, applying the medium with dissolved anti-inflammatory drug directly onto the skin covering a body joint known to be inflamed and allowing the medium with dissolved anti-inflammatory drug to be absorbed into the skin. Possible non-steroidal, anti-inflammatory drugs which may be used with the method include indomethacin, phenylbutazone and colchicine. Steroidal non-inflammatory drugs may also be used.

Abstract: The composition and method of using a non-steroidal antiinflammatory compound, such as indomethacin and/or a growth factor that causes a change in cell function when bound to specific cell surface receptor, such as epidermal growth factor (EGF), to enhance healing and restore function of the corneal endothelium. The compositions can be administered alone, in combination, or in sequence, before or after injury, for example, in an irrigation solution or in combination with a nutritive solution for storage of cornea prior to transplant.

Abstract: There are disclosed combination products useful for the treatment and/or prevention of a first or recurrent myocardial infarction or a first or recurrent stroke. Said combination products comprise low doses of an oral anticoagulant, preferably warfarin and platelet inhibiting agents, including non-steroidal antiinflammatory agents and preferrably aspirin.

Abstract: A pharmaceutical composition and process for administering non-steroidal drugs which are protected againsts injury to the gastrointestinal tract by a combination of certain H.sub.1 - and H.sub.2 -receptor blockers.

Abstract: This invention relates to a liquid pharmaceutical preparation for topical use on the skin of patients, said preparation containing indomethacin as active ingredient and dimethylisosorbide and isopropanol as excipients.The preparation according to the invention allows an easy and precise local administration by external application on the skin of a solution of indomethacin in the excipients.

Abstract: A pharmaceutically acceptable composition comprising Diflunisal and Naproxen or its salt in combination with a bicarbonate or carbonate.

Abstract: A one phase, liquid composition for oral administration comprises a NSAID such as an indoleacetic acid derivative or a pyrroleacetic acid derivative plus a di- or triglyceride of a medium chain fatty acid edible oil which has the characteristics of a pharmaceutical solvent carrier as known to those skilled in the art. Other pharmaceutical additives may be optionally added. An additional stipulation is that ethanol or other monohydric alcohol solvents should not be present.

Abstract: Injections containing anhydrous sodium indomethacin and methods for producing injections containing an hydrous sodium indomethacin which comprise converting a solution of indomethacin to a solution of sodium indomethacin by adding dropwise an aqueous solution of a carbonate of sodium, followed by freeze-drying and heating.The injections of the present invention are practically useful indomethacin injections in which sodium indomethacin anhydride has high safety and chemically high purity and stability, and the lyophilized pharmaceutical preparations are excellent also in that redissolution thereof is facilitated. By the methods for the production of the present invention, it is possible to produce said anhydrous sodium indomethacin efficiently.

Abstract: Biodegradable absorption enhancers, especially useful in pharmaceutical formulations, are compounds having the formula ##STR1## wherein R is hydrogen, C.sub.1 -C.sub.7 alkyl, benzyl or 4-hydroxybenzyl; n is a whole number from 4 to 18 inclusive; R.sub.1 and R.sub.2 are independently selected from hydrogen and C.sub.1 -C.sub.7 alkyl, or R.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached are combined to form a substituted or unsubstituted heterocycloalkyl radical having a total of 5 to 7 ring atoms, optionally including a hetero ring atom selected from oxygen, sulfur and nitrogen in addition to the indicated nitrogen atom, the substituents when present being one to three C.sub.1 -C.sub.7 alkyl radicals, which may be the same or different; and R.sub.3 and R.sub.4 are independently selected from hydrogen, methyl and ethyl.

Abstract: A pharmaceutical composition for treating an inflammatory condition contains a non-steroidal anti-inflammatory drug (NSAID) and a physiologically acceptable aromatic hydroxysulphonic acid. The two components may be for simultaneous, separate or sequential use. Administration of the two components, for example of aspirin with ethamsylate, reduces the damage which the NSAID does to the gastrointestinal tract while having no deleterious effect on the anti-inflammatory activity.

Abstract: A large group of lipophilic, pharmacologically active compounds can be effectively delivered across intact skin by applying them topically in a binary, penetration-enhancing vehicle containing (1) a C.sub.3 -C.sub.4 diol, diol ester, or diol ether and (2) a cell envelope-disordering compound. This vehicle provides surprising enhancement of skin penetration for the pharmacological active, compared to either component alone.

Abstract: Postsurgical adhesion formation is inhibited by the topical administration to the site of surgical trauma of a non-steroidal anti-inflammatory drug, preferably ibuprofen, suprofen, or tolmetin.

Abstract: A composition for reducing heat and pain and preventing blistering in humans suffering from sunburn comprising indomethacin, benzocaine, and phenol in an aqueous alcoholic base.

Abstract: A method for increasing the water-solubility of highly insoluble organic compounds by forming a novel complex product from the reaction between the organic compound and an oligomer of vinylpyrrolidone. The complex is highly stable and results in solubilities of the organic compounds in excess of 25-fold.

Abstract: Novel external medications comprise, as essential components, the following three components (A) to (C):(A) an .alpha.-monoglyceryl ether represented by the following formula (I): ##STR1## wherein R means an alkyl or alkenyl group having 10 - 24 carbon atoms; (B) a physiologically active material; and(C) an oily material.The external medications have extremely high skin occlusive properties and significantly-improved absorptivity of phosiologically active materials. Therefore, a smaller amount of the medications compared with the conventional ones can give sufficient pharmacological effects and thus side effects can be reduced. The external medications may contain physiologically active materials such as drugs, growth hormones and the like, which are expected to show pharmacological effects upon their percutaneous absorption.

Abstract: A percutaneous absorption preparation which comprises calcium salt of an acidic anti-inflammatory or analgesic drug having carboxyl group as the active ingredient and present in an amount of 0.3-10% by weight; a medium for the active ingredient which is selected form the group consisting of an ethylene glycol mono-lower alkyl ether, propylene glycol, polyethylene glycol and dimethylsulfoxide, the medium being present in an amount at least sufficient to dissolve the active ingredient; an absorption promotor selected from the group consisting of 1-dodecylazacycloheptan-2-one, hexamethylenelauramide, N-methyl-2-pyrrolidone, a sucrose aliphatic acid ester, dimethylsulfoxide and a nonionic surfactant and present in an amount of 0.5-10% by weight; and the remaining being other reagents and/or carriers required for a desired form of the preparation.

Abstract: 1-(fluoro- or perfluoro lower alkyl-substituted benzoyl)-5-methoxy-2-methyl-1H-indole-3-acetic acid carboxymethyl ester is found to have antiinflammatory and analgestic activity with less side effects on gastrointestinal traces than its homologue, acematacin or indometacin.

Abstract: Buffered opthalmic solutions of indomethacin.

Abstract: A method of treating an inflammatory condition in a mammalian subject, particularly arthritis, comprising the steps of administering an effective and nontoxic dose for an inflammation ameliorating period to the subject of at least one metallo-organic complex capable of in vivo superoxide anti-oxidant effects and wherein the metal of the complex is selected from the group which consists of cobalt and iron.

Abstract: A new method of treating a burn is disclosed wherein a cobalt-containing metallo-organic complex is applied to the burn site to promote epithelialization and in some cases hair follicle preservation as well.

Abstract: A percutaneous absorption accelerator and a precutaneous absorbent preparation containing the same and, more particularly, a percutaneous absorption accelerator containing ether derivatives of specific glycerols or polyglycerols and alcohols as effective components and a percutaneous absorbent preparation containing the percutaneous absorption accelerators and pharmaceutically effective components.

Abstract: Pharmaceutical compositions containing thioacetamol and an amount of a non-steroidal anti-inflammatory drug selected from aspirin, indomethacin, dichlofenac, naproxen, sulindac and fenbufen potentiate the activity of these drugs and reduce their undesiderable side-effects.

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: Novel esters of the general formula ##STR1## in which ##STR2## is the acyl residue of a non-steroidal anti-inflammatory compound containing a carboxylic acid function. The novel esters are prepared by reacting an acide R--COOH when R is as above, with 1-haloethyl ethyl carbonate. There are also provided pharmaceutical compositions containing any of the said novel esters.

Abstract: Pharmaceutical compositions and methods of using same comprising a non-steroidal anti-inflammatory drug in combination with at least one other active component selected from an antihistamine, decongestant, cough suppressant (antitussive) or expectorant are provided for the relief of cough, cold and cold-like symptoms.

Abstract: Pharmaceutical compositions and methods of using same comprising a non-steroidal anti-inflammatory drug in combination with at least one other active component selected from an anti-histamine, decongestant, cough suppressant (antitussive) or expectorant are provided for the relief of cough, cold and cold-like symptoms.

Abstract: This invention relates to a novel process for solubilizing the hydrophobic organic compounds--and namely the pharmaceutical active ingredients--in an aqueous phase.This process is defined in that the hydrophobic compound is prior dissolved in one or several polymers of high molecular weight, then adding to this solution an aqueous medium the pH of which is fixed.The aqueous solutions thus resulting are useful for preparing medicines for parenteral, digestive, mucous or transcutaneous administration.

Abstract: A pharmaceutical composition for external use with the enhanced penetration of a pharmacologically active agent through the skin or mucosa of a warm-blooded animal, said composition comprising(A) a pharmaceutically effective amount of the pharmacologically active agent, and(B) an optically active or inactive pyroglutamate of the following formula ##STR1## wherein R represents a linear, branched or cyclic alkyl or alkenyl group having 10 to 14 carbon atoms,as a penentration enhancer.

Abstract: The invention relates to pyroglutamic acid esters used as dermal penetration enhancers for therapeutic agents having poor skin permeation.

Abstract: In accordance with the present invention, the controlled release formulation contains coated pellets of indomethacin of only one type. The pellet releases indomethacin in both immediate and sustained release form. The immediate release indomethacin is rapidly absorbed from the stomach to provide a bolus dose of active agent. The sustained release indomethacin is gradually released over time to maintain the blood levels at effective concentrations for long periods of time.

Abstract: A method of percutaneously administering a physiologically active agent which comprises applying to the skin of a mammal a physiologically active agent in a carrier system which comprises at least one adjuvant and at least one solvent. The adjuvant can be selected from higher monoalcohols or mixtures thereof. The solvent can be selected from thioglycerols, lactic acid and esters thereof, cyclic ureas, compounds represented by the general formula R.sub.1 R.sub.2 NCONR.sub.3 R.sub.4, pyrrolidone-type compounds, amides, lactones or mixtures thereof.

Abstract: A readily absorbable pharmaceutical composition of pharmacologically active agents, which per se are poorly absorbable, is disclosed which comprises a pharmacologically effective amount of at least one such pharmacologically active agent distributed in a vehicle comprising an absorption-enhancing amount of at least one fatty acid of medium chain length. The preparation is suited for formulating pharmacologically active bases, cardiac glycosides, steroids, antibiotics, sympathicomimetica, tranquilizing agents, or local anaesthetics.

Abstract: An ointment containing Indole or an Indole derivative such as Indomethacin and a base; and a process for treating inflammations and lesions on the human skin including the step of applying an ointment containing such an ingredient to the sore.

Abstract: This invention relates to compounds of the structures: ##STR1## which structure includes its isomers, conventionally designated (E,Z)-4,5,9-trithiadodeca-1,6,11-triene 9-oxide and commonly termed (E,Z)-ajoene. This invention also relates to a process for preparing the compounds which comprises extracting and isolating allyl disulfide oxide (allyl 2-propenethiosulfinate) from the bulbs of garlic plants and thereafter treating it with a lower alkyl alcohol to produce such compound and the compounds as antibiotic and particularly as antithrombotic agents.

Abstract: Novel 6H-dibenz[b,e][1,4]oxathiepin derivatives of the Formulae I and IA are employed in the treatment and control of allergic conditions such as allergic asthma.

Abstract: Novel analgesic and anti-inflammatory compositions of matter for use in eliciting an analgesic or anit-inflammatory response, said compositions comprising caffeine together with a selected non-narcotic analgesic/nonsteroidal anti-inflammatory drug or a selected narcotic analgesic, or both, are disclosed. When used in combination with the selected drugs, caffeine enhances the analgesic or anti-inflammatory response and also hastens its onset.

Abstract: In a process of producing a sustained release preparation containing indomethacin or niomethacin, the active ingredient in the form of a powder as well as one or more food grade substances having a solubility of at least 1 gram per 10 milliliters in an aqueous liquid at any pH value from 1 to 9 and a temperature of 37.degree. C., and one or more food grade substances having a solubility of at least 1 gram per 100 milliliters in an aqueous liquid at any pH value from 1 to 9 and a temperature of 37.degree. C. are thoroughly mixed and the resulting mixture is mixed with a solution of one or more food grade substances which in an aqueous liquid have(a) a solubility below 1 gram per 1000 milliliters in an aqueous liquid at any pH value from 1 to 9 and a temperature of 37.degree. C., or(b) a solubility below 1 gram per 1000 milliliters at a pH value of 1 and a temperature of 37.degree. C.

Abstract: This invention relates to novel organic trithio oxides of the formula:R.sup.1 --X --R--X.sup.1 --R.sup.1wherein R is selected from --CH.sub.2 CH.dbd.CH--, ##STR1## and (CH.sub.2).sub.3 ; X is selected from ##STR2## X.sup.1 is selected from --S--S, ##STR3## and, each R.sup.1 is independently selected from carboxyalkyl, alkoxy, alkylthio, amino, alkylamino and acyl substituted and unsubstituted lower alkyl, lower alkenyl, lower alkynyl, phenyl and lower alkylphenyl; provided when R is --CH.sub.2 CH.dbd.CH--, X is ##STR4## and X.sup.1 is --S--S--, then R.sup.1 is not in both instances --CH.sub.2 CH.dbd.CH.sub.2.This invention also relates to a method of preparing the above-identified compounds by heating and further oxidizing various oxides of organic disulfides and to antithrombotic uses of the compounds.

Abstract: In a therapeutic system such as a plaster for administration of an active compound through the skin and comprising a covering layer which is essentially impermeable to the active compound, an active coupound reservoir layer and a protective layer which can be pulled off and which is essentially impermeable to the active compound, the improvement wherein the reservoir layer contains about 1-30% of active compound in an elastomer mixture comprising a diene rubber which can optionally be copolymerized with an .alpha.-olefin, mixed with from 0 up to about 70% by weight of a polyisobutylene, polybutadiene oil and/or paraffin oil, and a tackifying resin. Thereby the active compound can be released in regulated relatively large quantity over a prolonged period of time.

Abstract: 13-thiaprostaglandins of Formula I ##STR1## wherein B is --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--,R.sup.1 is phenyl, CH.sub.3, or NH.sub.2,R.sup.2 is H or CH.sub.3, andR.sup.3 is pentyl, hexyl, 1-methylpentyl, or 1,1-dimethylpentylhave valuable pharmacological properties, e.g., as cytoprotective agents.

Abstract: The invention relates to depot formulations containing, as an active antiinflammatory and/or analgesic agent a compound of Formula I, infra together with a suspension medium. Typical suspension agents are glycerides and/or esters of mono- or poly-hydric alcohols as well as selected ethers, alcohols and amides.

Abstract: A composition for topical application to the skin contains, as a fatty product to provide a nongreasy protective and emollient film thereon, a polyether oligomer having the formula ##STR1## wherein R is alkyl having 1-12 carbon atoms; R.sub.1, R.sub.2, R.sub.3 and R.sub.4 represent hydrogen or alkyl having 1-6 carbon atoms, with at least two of R.sub.1, R.sub.2, R.sub.3 and R.sub.4 being hydrogen; m is 1-4; n has an average value equal to or greater than 2; and the number of carbon atoms in each repetitive unit being at least 4.

Abstract: 3-methylflavone derivatives which are useful in the treatment of allergies, asthma and inflammation.

Abstract: Novel pharmaceutical compositions of matter are provided comprising analgesic/non-steroidal anti-inflammatory drugs and diphenhydramine and methods of using said compositions to elicit an enhanced analgesic and/or anti-inflammatory response in mammalian organisms in need of such treatment.