Abstract: The present invention is directed compositions of the formula: ##STR1## wherein: D is a residue of a biologically active moiety;X is an electron withdrawing group;Y and Y' are independently O or S;(n) is zero (0) or a positive integer, preferably from 1 to about 12;R.sub.1 and R.sub.2 are independently selected from the group consisting of H, C.sub.1-6 alkyls, aryls, substituted aryls, aralkyls, heteroalkyls, substituted heteroalkyls and substituted C.sub.1-6 alkyls;R.sub.3 is a substantially non-antigenic polymer, C.sub.1-12 straight or branched alkyl or substituted alkyl, C.sub.5-8 cycloalkyl or substituted cycloalkyl, carboxyalkyl, carboalkoxy alkyl, dialkylaminoalkyl, phenylalkyl, phenylaryl or ##STR2## R.sub.4 and R.sub.5 are independently selected from the group consisting of H, C.sub.1-6 alkyls, aryls, substituted aryls, aralkyls, heteroalkyls, substituted heteroalkyls, and substituted C.sub.1-6 alkyls or jointly form a cyclic C.sub.5 -C.sub.7 ring.

Abstract: The present invention relates generally to silver-based antimicrobial compositions and processes for making such compositions. More particularly, the present invention describes stable, purified silver-based antimicrobial compositions, and processes for making such compositions, comprising carrier-free silver thiosulfate ion complexes either suspended in a base or incorporated into a matrix. These silver thiosulfate ion complex antimicrobial compositions are useful in the treatment and prevention of infections and diseases.

Abstract: The subject invention encompasses methods for prevention and treatment of a human or lower animal subject having a gastrointestinal disorder caused or mediated by one or more intestinal helminths comprising administering to the subject bismuth and one or more antimicrobials. The subject invention also encompasses compositions comprising bismuth and one or more antimicrobials for the prevention and treatment of a human or lower animal subject having a gastrointestinal disorder caused or mediated by one or more intestinal helminths.

Abstract: Intra-erythrocytic exogenous bacterial structures or parasites seen by giemsa and phase contrast microscopy in several patients with systemic lupus erythematosus (SLE) and not in controls were identified as bacteria. Treatment of an SLE patient is contemplated with an antibacterial amount of a rifamycin in conjunction with an antibacterial amount of either a macrolide such as clarithromycin or a third generation cephalosporin such as cefpodoxime that is itself more preferably used in conjunction with an adjuvant amount of probenecid.

Abstract: A granulate, containing at least 50 wt. % of a water soluble .beta.-lactam antibiotic, is provided. A process to prepare a granulate containing such .beta.-lactam antibiotic comprises moistening components making up the granulate with an aqueous solution containing no substantial amount of a wet granulation binding agent. Oral dosage-forms, which contain the said antibiotic in a granular form, a cellulose product and a disintegrant and which quickly disperse when placed in an aqueous environment, are disclosed, as well as a method for the preparation of the dosage-forms.

Abstract: Water soluble, powder form compositions suitable for completely and rapidly dissolving active ingredients which usually only dissolve in water in the presence of base salts, such as antibiotics of the betalactamide family, for example penicillins and their derivatives, cephalosporins and their derivatives, or other active ingredients such as sulphamides and quinolones, for oral absorption thereof and their applications. The water soluble powder form compositions contain, in combination and in powder form, at least one water soluble active ingredient, not in salt form, and with an exclusively alkaline pH, an excess of one or more strong base salts, and one or more buffers comprising one or more substances and capable of maintaining the pH of the medium at a level below the normal solubilization pH of said active ingredient. Aqueous solution compositions obtained from said powder form compositions are also described.

Abstract: Methods for screening for compounds which potentiate the activity of antibacterial agents against bacteria resistant to the antibacterial agent alone, pharmaceutical compositions including such potentiators, and methods of treating bacterial infections using a combination of a potentiator and a potentiated antibacterial agent, which are useful for overcoming the resistance of a bacterial strain for an antibacterial agent.

Abstract: The subject invention encompasses methods for prevention and treatment of a human or lower animal subject having a urogenital disorder caused or mediated by one or more parasitic protozoa comprising administering to the subject bismuth and one or more antimicrobials. The subject invention also encompasses compositions comprising bismuth and one or more antimicrobials for the prevention and treatment of a human or lower animal subject having a urogenital disorder caused or mediated by one or more parasitic protozoa.

Abstract: Intra-erythrocytic exogenous bacterial structures or parasites seen by giemsa and phase contrast microscopy in several patients with systemic lupus erythematosus (SLE) and not in controls were identified as bacteria. Treatment of an SLE patient is contemplated with an antibacterial amount of a rifamycin in conjunction with an antibacterial amount of either a macrolide such as clarithromycin or a third generation cephalosporin such as cefpodoxime that is itself more preferably used in conjunction with an adjuvant amount of probenecid.

Abstract: The invention involves pharmaceutical compositions for topical application comprising:(a) a safe and effective amount of a pharmaceutical active; and(b) from about 0.05% to about 5% of a non-ionic polyacrylamide having a molecular wight of from about 1,000,000 to about 30,000,000.

Abstract: This invention is directed to a homogenous water-in-perfluorochemical stable liquid dispersion for acceptable therapeutic administration of a drug to the lung of an animal. The dispersion includes a perfluorochemical liquid, water, surfactant and drug, wherein the water is homogeneously dispersed in the perfluorochemical to form a stable water-in-perfluorochemical liquid dispersion. The perfluorochemical constitutes greater than 50% by volume of the dispersion, and the drug is contained in the dispersion in an effective therapeutic amount.The invention further includes a method of delivering a drug to the lung of an animal. This aspect of the invention includes administering a stable homogenous water-in-perfluorochemical liquid dispersion to the animal lung or a section thereof. If desired, the method may further include delivering a breathable gas to the lung with a mechanical ventilator during the administration.

Abstract: The subject invention encompasses methods for prevention and treatment of a human or lower animal subject having a gastrointestinal disorder caused or mediated by algae and/or cyanobacteria comprising administering to the subject bismuth and one or more antimicrobials. The subject invention also encompasses compositions comprising bismuth and one or more antimicrobials for the prevention and treatment of a human or lower animal subject having a gastrointestinal disorder caused or mediated by algae and/or cyanobacteria.

Abstract: There are described pharmaceutical compositions comprising(a) compounds of the formula ##STR1## in which R signifies lower alkoxycarbonyl, lower alkoxy-carbonylamino, the acyl residue of an .alpha.- or .beta.-amino acid or a residue of the general formulaQ--X--Y-- (a)wherein Q signifies a 3- to 6-membered ring which optionally contains nitrogen, sulphur and/or oxygen and which is optionally bonded with a fused ring, X signifies a direct bond or a linear "spacer" with up to 6 atoms consisting of carbon, nitrogen, oxygen and/or sulphur, of which up to 2 atoms can be nitrogen atoms and 1 atom can be oxygen or sulphur, and Y represents one of the groups --CO--, --CS--, --CONH-- and (where X contains neither sulphur nor carbonyl as a terminal component) --SO.sub.2 --; and in which R.sup.1 and R.sup.2 together signify a group of the formula ##STR2## wherein A represents hydrogen or a residue which is usable in the 3-position of cephalosporin antibiotics, and in which R.sub.

Abstract: There are described pharmaceutical compositions comprising(a) compounds of the formula ##STR1## in which R signifies lower alkoxycarbonyl, lower alkoxy-carbonylamino, the acyl residue of an .alpha.- or .beta.-amino acid or a residue of the general formulaQ--X--Y-- (a)wherein Q signifies a 3- to 6-membered ring which optionally contains nitrogen, sulphur and/or oxygen and which is optionally bonded with a fused ring, X signifies a direct bond or a linear "spacer" with up to 6 atoms consisting of carbon, nitrogen, oxygen and/or sulphur, of which up to 2 atoms can be nitrogen atoms and 1 atom can be oxygen or sulphur, and Y represents one of the groups --CO--, --CS--, --CONH-- and (where X contains neither sulphur nor carbonyl as a terminal component) --SO.sub.2 --; and in which R.sup.1 signifies hydrogen, halogen, carbamoyloxy, lower alkanoyloxy or a group of the formula --S--Het, wherein Het represents a 5- or 6-membered heteroaromatic group containing nitrogen, sulphur and/or oxygen, and R.sup.

Abstract: A method of administering a drug to an eye including the steps of: (a) admixing a pharmaceutically acceptable hydrocarbonaceous semi-solid or oil which contains the drug with water at a temperature above the melting point of the semi-solid or oil; and (b) nebulizing the admixture to form liquid drops; and (c) applying the liquid drops to the eye.

Abstract: The use is described of both (i) ranitidine bismuth citrate and (ii) one or more Helicobacter pylori-inhibiting antibiotics in treating or preventing gastrointestinal disorders.Pharmaceutical compositions containing both (i) and (ii) and methods for the preparation of pharmaceutical compositions containing (i) and (ii) are also described.

Abstract: A formulation comprising amoxycillin or a veterinarily acceptable derivative thereof, clavulanic acid or a veterinarily acceptable derivative thereof, and a veterinarily acceptable carrier is used in the treatment of farrowing fever and/or bacterial pneumonia in pigs.

Abstract: A class of chemical compounds comprising fatty acid ester derivatives used to inhibit beta-lactamase production by infectious bacteria. These inhibitors have been found to retard the resistance of certain strains of bacteria to beta-lactam antibiotics, such as penicillin, by interfering with the transcription of the beta-lactamase gene and precluding expression of beta-lactamase. In accordance therewith, these inhibitors permit effective treatment of infections of otherwise resistive bacteria with antibiotics.

Abstract: A synergistic pharmaceutical combination or composition is disclosed for the treatment of gastritis and peptic ulcer containing a therapeutic amount of a histamine H.sub.2 receptor blocking agent, which increases intragastric pH, and an acid degradable antibacterial compound. In particular, the combination is directed to the treatment of infections by Helicobacter pylori by raising the bioavailability of acid degradable antibacterial compounds.

Abstract: .beta.-Phenethanolamines are effective in promoting growth and improving feed efficiency and leanness in animals.

Abstract: A synergistic pharmaceutical combination and composition are disclosed for the treatment of gastritis and peptic ulcer containing a therapeutic amount of a proton pump inhibitor such as e.g., omeprazole or lansoprazole, which increases intragastric pH, and a therapeutic amount of an acid degradable antibacterial compound such as a penicillin or a macrolide. In particular, the combination is directed to the treatment of infections caused by Helicobacter pylori by raising the bioavailability of acid degradable antibacterial compounds.

Abstract: The present invention is directed to a method for the treatment of Helicobacter pylori infection wherein a composition containing protease and an antibacterial agent as active ingredients, which can remove Helicobacter pylori from a stomach at high probability without causing side effects or the occurrence of resistant bacteria, and which can treat and prevent peptic ulcer caused by Helicobacter pylori infection and can prevent the recurrence of peptic ulcer is employed.

Abstract: The oral delivery of many classes of drugs is facilitated by converting drugs having suitable functional groups to 1-O-alkyl-, 1-O-acyl-, 1-S-acyl, and 1-S-alkyl-sn-glycero-3-phosphate derivatives. The method confers the ability to be absorbed through the digestive tract to drugs that are not orally bioavailable in the non-derivatized state, and enhances the effectiveness of drugs that are poorly absorbed or rapidly eliminated. The method provides orally bioavailable lipid prodrugs of zaxol and taxol-related compounds. Potency of the lipid prodrugs is comparable to that of the corresponding nonderivatized drugs. In a preferred embodiment, taxol or substituted taxol is covalently bound to a phospholipid.

Abstract: A method of and composition for treating a Helicobacter pylori infection in a mammal. The method comprises administering to said mammal orally a therapeutically effective amount of a Helicobacter pylori eradicating antibiotic and a phospholipid. The composition comprises a Helicobacter pylori eradicating antibiotic and a phospholipid.

Abstract: A method is disclosed for preventing the recurrence of duodenal ulcer associated with Campylobacter pylori (Helicobacter pylori) infection in a patient suffering from duodenal ulcer disease associated with Campylobacter pylori infection by administering a pharmaceutically acceptable bismuth compound, a first antibiotic selected from the group consisting of tetracycline and penicillins, and a second antibiotic which is metronidazole.

Abstract: A class of chemical compounds comprising fatty acid ester derivatives used to inhibit beta-lactamase production by infectious bacteria. These inhibitors have been found to retard the resistance of certain strains of bacteria to beta-lactam antibiotics, such as penicillin, by interfering with the transcription of the beta-lactamase gene and precluding expression of beta-lactamase. In accordance therewith, these inhibitors permit effective treatment of infections of otherwise resistive bacteria with antibiotics.

Abstract: The oral delivery of many classes of drugs is facilitated by converting drugs having suitable functional groups to 1-O-alkyl-, 1-O-acyl-, 1-S-acyl, and 1-S-alkyl-sn-glycero-3-phosphate derivatives. The method confers the ability to be absorbed through the digestive tract to drugs that are not orally bioavailable in the non-derivatized state, and enhances the effectiveness of drugs that are poorly absorbed or rapidly eliminated. The method provides orally bioavailable lipid prodrugs of pharmaceutical compounds having diverse physiological activities, including anticancer and antiviral agents, anti-inflammatory agents, antihypertensives and antibiotics. Potency of the lipid prodrugs is comparable to that of the corresponding non-derivatized drugs.

Abstract: A method of killing microorganisms which form a biofilm on a tissue or implant surfaces in a patient, and which are refractory to a biocide at a dose which is effective to kill the microorganism in planktonic form. The effect of the biocide is potentiated, to an effective killing level, by applying an electric field across the surface containing the biofilm.

Abstract: Methods, for the treatment of humans and lower animal subjects having a gastrointestinal disorder, comprising administering bismuth and administering an antimicrobial. From about 50 to about 5000 milligrams of bismuth are administered, per day, for from 3 to 56 days. A safe and effective amount of antimicrobial is administered for from 1 to 21 days. Preferred processes also include a step for performing a diagnostic test on the subject for detection of a campylobacter-like organism infection of the subject. The invention also provides compositions containing a safe and effective amount of bismuth and a safe and effective amount of antimicrobial.

Abstract: A method is disclosed for preventing recurrence of duodenal ulcer associated with Campylobacter pylori infection in a patient suffering from duodenal ulcer disease associated with Campylobacter pylori infection by administering a pharmaceutically acceptable bismuth compound; a first antibiotic selected from the group consisting of tetracycline and penicillins and second antibiotic which is metronidazole.

Abstract: A non-aqueous pharmaceutical liquid suspension having improved bioavailability for oral administration comprises an active ingredient suspended in an edible, non-aqueous carrier vehicle such as an oil, wherein the active ingredient is in the form of controlled release particles containing the active ingredient and optionally an excipient in intimate admixture with at least one non-toxic polymer, the particles being coated with, distributed through or adsorbed onto said polymer, and the particles further having an average size in the range 0.1 to 150 microns and a predetermined release of active ingredient.

Abstract: An unpressurized container containing a palatable pharmaceutical formulation comprising a homogeneous, non-aqueous suspension of an orally active medicament, an edible oily vehicle, an edible emulsifier and a finely particulate sugar having no oily after taste.

Abstract: The subject compounds, which are adapted for the site-specific/sustained delivery of centrally acting drug species to the brain, are:(a) compounds of the formula[D-DHC] (I)wherein [D] is a centrally acting drug species, and [DHC] is the reduced, biooxidizable, blood-brain barrier penetrating lipoidal form of a dihydropyridine.revreaction.pyridinium salt redox carrier, with the proviso that when [DHC] is ##STR1## wherein R is a lower alkyl or benzyl and [D] is a drug species containing a single NH.sub.2 or OH functional group, the single OH group when present being a primary or secondary OH group, said drug species being linked directly through said NH.sub.

Abstract: A solid pharmaceutical composition comprising one or more .beta.-lactam antibiotics in acid or amphoteric form in association with at least one physiologically acceptable base in the presence of a gaseous atmosphere containing a stabilizing amount of carbon dioxide at a concentration greater than that of atmospheric air. The compositions exhibit enhanced stability. A preferred antibiotic for the compositions is ceftazidime or a hydrate thereof, and a preferred base is sodium cabonate or a mixture thereof with one or more other bases.

Abstract: The rectal absorption of the beta-lactam antibiotic ceftriaxone in a solid dosage form is enhanced with chenodeoxycholic acid or its sodium salt, in the presence of a carrier consisting of a mixture of two or more glycerides of C.sub.12 to C.sub.18 fatty acids.

Abstract: Suppositories containing as the active substance a therapeutically effective amount of ceftriaxone, a pharmaceutically compatible salt thereof or a hydrate of one of these compounds, a stabilizer consisting of a mono-, di- or triglyceride of a C.sub.12 -C.sub.18 -fatty acid or of a mixture of such glycerides, a potentiator consisting of an aliphatic C.sub.2 -C.sub.18 -fatty acid, a mono-, di- or triglyceride of a C.sub.2 -C.sub.12 -fatty acid, a partial ester or complete ester of propylene glycol, polyethylene glycol or a carbohydrate with a C.sub.2 -C.sub.12 -fatty acid, a pharmaceutically compatible ester or ether thereof or of a mixutre of the said potentiators and, if desired, customary therapeutically inert adjuvants for suppositories, and their manufacture are described. These have valuable antimicrobial properties.

Abstract: Acylcarnitine used as a nasal, buccal, sublingual and vaginal drug absorption enhancing vehicle for poorly absorbed drugs.

Abstract: Choline ester salts are used as drug absorption enhancing agents for orally and rectally administered drugs.

Abstract: Choline esters are used as drug absorption enhancing agents for drugs which are poorly absorbed from the nasal, oral, and vaginal cavities.

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: This invention relates to penicillanic acid derviatives of the formula I ##STR1## in which X stands for chlorine, bromine or iodine, to pharmaceutically acceptable, non-toxic salts of the compounds of formula I, to pharmaceutically acceptable, easily hydrolyzable esters thereof, including salts of such esters, to pharmaceutical compositions containing the compounds of the invention and dosage units thereof, to methods for the preparation of the compounds of the invention, and to methods of using the said new compounds in the human and veterinary therapy.The 6.beta.-halopenicillanic acids of formula I are potent inhibitors of .beta.-lactamases from a variety of gram-positive and gram-negative bacteria, making the 6.beta.-halopenicillanic acids as well as their salts and easily hydrolyzable esters valuable in human and veterinary medicine.

Abstract: Methylsulfonylmethane (CH.sub.3 SO.sub.2 CH.sub.3) administered orally is effective in ameliorating the symptoms of gastrointestinal upset, e.g., produced by the ingestion of aspirin and other pharmaceuticals, and of allergic reactions. Oral compositions containing a mixture of such a pharmaceutical and methylsulfonylmethane are useful in avoiding the gastrointestinal upset which otherwise occurs when ingesting the former.

Abstract: The present invention provides a method for inhibiting the synthesis and release of toxins from bacteria which comprises contacting the bacteria with an antitoxic prostaglandin.