Abstract: An improved platelet gel wound healant, and methods of preparation and use thereof for healing wounds are disclosed. The improved wound healant comprises a therapeutically effective amount of activated growth factors and ascorbic acid with optional one or more additional anti-oxidant such as vitamin A and/or E, and optional one or more antibiotics.

Abstract: An improved method of sterilizing the field of surgery prior to an ophthalmic surgical procedure is described. The invention eliminates the need for painful and potentially traumatic injections of antibiotics by utilizing sustained release compositions which allow the antibiotics contained therein to penetrate deeply into the eye, thereby ensuring a sterile field of surgery during intraocular surgical procedures. The compositions may also be utilized to prevent post-surgical infections.

Abstract: The present invention relates to a bio enhancing composition containing extract and/or bioactive fraction/isolate from the plant Zingiber officinale in combinations combination with drugs, nutrients, nutraceuticals, micronutrients and herbal drugs/products and optionally containing piperine as a extract/active fraction obtained from piper nigrum, piper longum or its oleoresin as a bioavailability enhancer and its process for producing the extract or fractions from the plant source.

Abstract: The debridement of wounds, and particularly burn wounds, is more effectively accomplished by starting with a first substance comprising a mixture of collagenase and a non-aqueous excipient and a second substance comprising an aqueous excipient and, preferably, a cream such as an antibiotic cream, both of which substances have a satisfactory shelf life, and treating the wound by combining those two substances and promptly applying the resulting combination to the wound. Shelf life requirements are satisfied, and the effect of applying the resulting combination to the wound promptly after the combination has been formed results in a more effective debridement than would be expected from the application of other collagenase substances.

Abstract: Hydrophilic N-linked pharmaceutical compositions, methods of their preparation and use in neuraxial drug delivery comprising a glycosyl CNS acting anti-infective prodrug compound covalently N-linked with a saccharide through an amide or an amine bond and a formulary consisting of an additive, a stabilizer, a carrier, a binder, a buffer, an excipient, an emollient, a disintegrant, a lubricating agent, with the proviso that the saccharide moiety is not a cyclodextrin or a glucuronide.

Abstract: The present invention provides compositions and methods for extending the release times and lowering the toxicity of pharmacologically active compounds. The compounds comprise a salt of the pharmacologically active compound with a lipophilic counterion and a pharmaceutically acceptable water soluble solvent combined together to form an injectable composition. The lipophilic counterion may be a saturated or unsaturated C8-C22 fatty acid, and preferably may be a saturated or unsaturated C10-C18 fatty acid. When injected into a mammal, at least a portion of the composition precipitates and releases the active compound over time. Thus, the composition forms a slowly releasing drug depot of the active compound in the mammal. Therefore, the present invention enables one to provide a controlled dose administration of the active compound for a periods of up to 15 days or even longer.

Abstract: The present invention relates to a composition for topical use for treating and improving the aesthetic conditions of the skin, which comprises, as an active ingredient, a mixture of ethyllinoleate and triethylcitrate. This composition is active in the treatment of seborrhea and acne.

Abstract: The present invention is directed to analogs of aminoglycoside compounds of the class having a glycosylated 2-deoxystreptamine (2-DOS) ring as well as their preparation and use as prophylactic or therapeutics against microbial infection. Compounds of the invention comprises at least one aryl, heteroaryl, substituted aryl or substituted heteroaryl group in place of a glycosyl group attached to the 2-deoxystreptamine ring.

Abstract: A method of making a derivatized aminoglycoside includes reacting an aminoglycoside with at least 2 equivalents of a divalent metal ion in an aprotic solvent to complex two neighboring amino group and hydroxyl group pairs; reacting the non-complexed amino groups with a protecting reagent to provide protecting groups; removing the divalent metal ion to provide two unprotected amino groups; reacting one of the unprotected amino groups with a reactive substance containing an linker, a carrier, or a label; and removing the protecting groups. This method can be used to produce novel compounds and reagents.

Abstract: The invention relates to a method for the antibiotic coating of bodies with interconnecting microcavities as well as bodies coated this way and their usage.

Abstract: The present invention provides a novel pharmaceutical composition based on the use of a particular oil phase which comprises a lipophilic, pharmaceutically active agent, a mixture of diglyceride and monoglyceride in a ratio of from about 9:1 to about 6:4 by weight (diglyceride:monoglyceride) wherein the diglyceride and monoglyceride are mono- or di-unsaturated fatty acid esters of glycerol having sixteen to twenty-two carbon chain length, one or more pharmaceutically acceptable solvents, and one or more pharmaceutically acceptable surfactants. The composition is in a form of self-emulsifying formulation which provides high concentration and high oral bioavailability for lipophilic compounds.

Abstract: Compositions and methods are provided for prophylactic or therapeutic treatment of a mammal for hearing impairments involving neuronal damage, loss, or degeneration, preferably of spinal ganglion neurons, by administration of a therapeutically effective amount of a trkB or trkC agonist, particularly a neurotrophin, more preferably NT-4/5. Also provided are improved compositions and methods for treatments requiring administration of a pharmaceutical having an ototoxic side-effect, wherein the improvement includes administering a therapeutically effective amount of a trkB or trkC agonist to treat the ototoxicity.

Abstract: The invention provides a method of potentiating the activity of antibacterial agents that act on bacterial cell walls, comprising the step of administering to a subject an antibacterial agent and an aminoglycoside to attain a peak concentration of at least 4 mg/l of aminoglycoside and thereafter maintaining the aminoglycoside at a concentration of up to 4 mg/l for at least 1 hour. Compositions comprising an antibacterial agent and an aminoglycoside for efficacious treatment of bacterial infection are also provided.

Abstract: This invention relates to a method of treating an inherited disease due to a point mutation producing a stop codon by administering an effective dose of an aminoglycoside antibiotic or a derivative thereof. Mdx mouse, which is an animal model for Duchenne muscular dystrophy, has been successfully treated with intramuscularly administered 1 and 5 mg gentamicin, which had for effect to suppress the premature stop mutation by inserting an amino acid at the stop codon. Dystrophin positive muscle fibers not different in number from those of normal mouse were detected at the dose of 5 mg gentamicin.

Abstract: Aminoglycoside antibiotics are used to treat genetic ophthalmic diseases caused by premature “stop” mutations.

Abstract: The present invention is directed to analogs of aminoglycoside compounds of the class having a glycosylated 2-deoxystreptamine (2-DOS) ring as well as their preparation and use as prophylactic or therapeutics against microbial infection. Compounds of the invention comprises at least one aryl, heteroaryl, substituted aryl or substituted heteroaryl group in place of a glycosyl group attached to the 2-deoxystreptamine ring.

Abstract: A method of screening for and treating subjects with a therapeutically effective amount of a compound that is effective in reducing cellular damage related to an ischemic condition, such as stroke or glaucoma. Test compounds are selected and therapeutically effective amount determined based on the relative efficacy of test compounds in preventing cell death in primary cultures of excitable cells, such as retinal ganglion cells, in vitro.

Abstract: Methods of preventing or reducing hearing or balance loss, damage to ear cells, weight loss, gastrointestinal toxicity, neurotoxicity, alopecia, and prolonging survival in patients undergoing treatment with therapeutically effective amounts of platinum-containing chemotherapeutic agents such as cisplatin are provided. Methods are also provided for preventing or reducing such symptoms in patients undergoing treatment with loop diuretics, aminoglycoside antibiotics, iron chelating agents, quinine, and quinidine, or those who have been exposed to toxic levels of noise or radiation. These methods comprise administering an effective amount of a methionine protective agent, such as D-methionine, prior to, simultaneously with, or subsequently to administration of the platinum-containing chemotherapeutic agent, loop diuretic agent, etc., or exposure to noise or radiation. Combinations of these time periods can also be employed.

Abstract: The compounds of the present invention are those of structural formula (I) ##STR1## wherein X is oxygen or sulfur. Pharmaceutical compositions and methods of use of the compounds in the treatment of hyperandrogenic conditions are disclosed. In addition, the combination of the compounds with other active agents such as finasteride, minoxidil and retinoic acid or a derivative thereof is disclosed.

Abstract: This invention provides a compound having the formula: ##STR1## wherein R.sup.1 and R.sup.3 independently are hydrogen, --CHO, --COCH.sub.3, --COR.sup.7, --A--Ar--(Q).sub.z, etc.; wherein D is a C.sub.1-6 linear, C.sub.3-8 branched or cyclic group having from 4 to about 15 atoms, consisting of C, etc.; wherein D is unsubstituted or substituted with one or more groups independently selected from the group consisting of --OH, NH.sub.2, --NHR.sub.7, etc.; wherein each Q is independently --CNH(NHY), --NHCNH(NHY), --SO.sub.2 W, --SOW, etc.; wherein Y is hydrogen, alkyl, alkenyl, --B--NH.sub.2, --B--NHR.sup.8, etc.; wherein W is alkyl, alkenyl, --B--NH.sub.2, etc.; wherein A nd B independently are a bond, or a C.sub.1-6 linear, C.sub.3-8 branched or cyclic linking group having from 1 to about 15 atoms, consisting of C, optionally interrupted by N, S, P and O; wherein A and B independently are unsubstituted or substituted with --OH, NH.sub.2, etc.; wherein R.sup.7 is an alkyl, a branched alkyl, etc.; wherein R.sup.

Abstract: The invention described herein provides for methods of screening for compounds that can be used to prevent or inhibit the growth of microbial eukaryotes, particularly plant or animal pathogens. The screening methods of the invention involve the step of screening compounds for the ability to inhibit Group I intron I splicing. In addition, to directly screening for compounds that inhibit Group I intron splicing, the screening methods of the invention include screening for compounds that bind to prokaryotic 16S ribosomal RNA because of the correlation, described herein, between group I intron inhibition and binding to prokaryotic 16S ribosomal RNA. The range of possible compounds for screening by the screening methods of the invention is preferably limited to 2-deoxystreptamine derivatives.Another aspect of the invention is to provide methods of treating or preventing infections with eukaryotic microbes by administering an effective amount of a compound that inhibits group I intron splicing.

Abstract: A method is disclosed for reducing excitotoxic damage to neurons, which can occur as a result of stroke, cardiac arrest, or other events or conditions. This method involves administering an aminoglycoside that suppresses the flow of calcium ions into neurons through N-type calcium channels. To be effective for such use, an aminoglycoside must suppress N-channel activity at a potency greater than streptomycin. Aminoglycosides which meet this criterion (which includes neomycin and Gentamicin) can suppress the depolarizing activation of neurons, which in turn controls the release of glutamate, a neurotransmitter that becomes an endogenous toxin under excitotoxic conditions. Numerous aminoglycosides were tested in in vitro screening tests using brain cell membrane fragments to evaluate N-channel blocking potency.

Abstract: The invention relates to a liposomal formulation containing a therapeutic agent. The formulation of the invention when administered to animals, allows a substantial increase in antibacterial activity of the agent, through an enhanced penetration of the agent inside the bacterial cell. More specifically, the invention relates to a liposomal formulation containing at least one therapeutic agent such as an antibiotic and to a method of treatment of bacterial infections through the administration of such a formulation.

Abstract: The present invention relates to novel amino glycoside salts of sucrose-octa-O-sulfonic acid of formula I:([sucrose-octa-O-sulfonic acid.sup.8- ]-[R-(NH.sub.3.sup.+).sub.x ].sub.y -M.sub.z.sup.n+) (I)(x.multidot.y)+(z.multidot.n)=8x.multidot.y.epsilon.N.vertline.[4.ltoreq.x.multidot.y.ltoreq.8], wherein N is the set of natural numbers,x.epsilon.Z.vertline.[4.ltoreq.x.ltoreq.6], wherein Z is the set of integersz.epsilon.N.vertline.[0.ltoreq.z.ltoreq.4],n.epsilon.Z.vertline.[1.ltoreq.n.ltoreq.3],wherein R is a sugar moiety of an amino glycoside and M is a metal ion or an ammonium ion, said compounds being useful for treating ulcerations of the stomach and duodenum.

Abstract: Polyphosphonate ligands containing three or more phosphonate groups, combined with paramagnetic metal cations and administered in the form of pharmacologically acceptable salts, are useful as MRI contrast enhancement agents, which tend to localize in bone tissue without being conjugated to bone-specific biomolecules. Triazacyclononanes and tetraazacyclododecanes, with dihydroxyphosphorylmethyl or dihydroxyphosphorylethyl groups, optionally substituted at the methyl or ethyl bridges with alkyl, aryl, hydroxyl or amino groups, are particularly preferred.

Abstract: Disclosed is a method for the inhibition of binding of a ligand to an RNA, the inhibition being mediated by a small organic molecule which binds to the RNA, thereby inhibiting ligand binding. A preferred class of small organic molecules are the 2-deoxystreptamine (2-DOS) aminoglycosides. Disclosed herein are members of the 2-DOS class that are useful for the inhibition of binding of Rev to an RNA containing an RRE. In an HIV infected cell, a consequence of the inhibition of the ability of Rev to bind to the RRE in HIV encoded transcripts is inhibition of HIV replication.

Abstract: As new compounds are now synthetized 5-deoxy-5,5-difluoro derivatives of aminoglycosidic antibiotics of neamine, kanamycin A-series, kanamycin B-series, gentamicin-series and seldomycin-series. Further, the 1-N-(.alpha.-hydroxy-.omega.-aminoalkanoyl) derivatives are synthetized from 5-deoxy-5,5-difluorokanamycins A and B, as well as their analogues now obtained. The 5-deoxy-5,5-difluoro derivatives of the aminoglycosidic antibiotics now provided according to this invention have such antibacterial activities enhanced much more than or equal to those of the respectively corresponding parent aminoglycosidic antibiotics, while these 5-deoxy-5,5-difluoro derivatives exhibit values of the 50% lethal dosage (LD.sub.50) which are improved remarkably better when they are intravenously administered to mice, so that they have remarkedly reduced toxicities to mammals.

Abstract: The invention relates to a stabile, aqueous suspoemulsion containing as active ingredient 0.2-5 weight % of primycin, 5-25 weight % of propylene glycol, 0.5-5 weight % of non-ionic surface active agent, if desired 15 weight % of auxiliary agent and distilled water in an amount necessary to 100 weight %, as well as to a process for the preparation thereof.

Abstract: Crosslinked copolymers of monomeric aminosaccharides such as aminoglycosidic antibiotics, e.g. neomycin, or of polymeric aminosaccharides, e.g., chitosan, with dialdehydes are useful antihypercholesterolemic agents due to their ability to bind with bile acids. These copolymers are insoluble in acidic solutions but are swellable to at least about 2.times. their original weight.

Abstract: As new 2'-deamino-2'-hydroxyistamycin B.sub.o derivatives are provided four compounds, namely 2'-deamino-2'-hydroxyistamycin B; 2'-deamino-2'-hydroxy-3-O-demethylistamycin B; 4-N-(.beta.-alanyl)-2'-deamino-2'-hydroxyistamycin B.sub.o ; and 4-N-(.beta.-alanyl)-2'-deamino-2'-hydroxy-3-O-demethylistamycin B.sub.o which all exhibit high antibacterial activity and low acute toxicity in combination. These new compounds are useful as antibacterial agent.

Abstract: Novel lysine esters used as absorption enhancing agents for gastrointestinally and rectally administered drugs. Also provided are processes for preparation of said lysine ester compounds as well as pharmaceutical formulations and methods for their use as absorption enhancing agents.

Abstract: A method is disclosed for purifying non-homogeneous systems, known as liposomic suspensions, from non-entrapped drugs wherein said suspensions are treated with liquid or solid polymers of synthetic and organic nature having chemical functionality, which are used as ion-exchangers. The liquid or solid polymers are based on styrene, divinylbenzene, acrylic acid, methacrylic acid, and the like, normally known as ion-exchange resins, and may include carboxylic, phosphonic or sulphonic functions of different matrices. The ion-exchange resins may also include salified quaternary ammonium, primary, secondary and tertiary amminic or phosphinic functions or other functions with different matrices, including phenolformaldehyde, styrene-divinylbenzene, acrylates, methacrylates, hydrocarbons and condensation-resins.

Abstract: The invention relates to a synergistic antibiotic composition useful for the treatment of respiratory, gastrointestinal or urinary infections and septicaemia of domestic animals. The composition comprises tiamulin hydrogen fumarate and an aminoglycoside antibiotic or a pharmaceutically acceptable salt thereof in a weight ratio of 5:1 to 1:5. The active components are admixed or diluted with a carrier, used in veterinary therapy, in a weight ratio of 1:1 to 1:50 and formulated for oral or parenteral application.

Abstract: Aminoglycosides and aminoglycoside-aminocyclitols which have been oxygen-radical activated show a broad spectrum of antibacterial activity. The activated compounds are able to penetrate the cell membranes of bacteria and show substantially enhanced activity as compared to the parent unactivated compound.

Abstract: As new semi-synthetic antibiotic derivatives are provided N-methanesulfonic acid derivatives of 3-demethoxyistamycin B which are less toxic than the parent 3-demethoxyistamycin B but retain usefully high antibacterial activity of the parent antibiotic. The new derivatives are produced by a method of N-sulfomethylation where 3-demethoxyistamycin B is reacted with an aldehyde such as paraformaldehyde and sulfurous acid or sulfite reagent.

Abstract: The thioester of N-acetylcysteine with salicylic acid and the pharmacologically acceptable and non-toxic organic and inorganic salts thereof, exhibit anti-pyretic, anti-inflammatory and analgesic activity as well as mucolytic activity. The compounds are prepared by the reaction of N-acetylcysteine with either the acid chloride of acetylsalicylic acid or with the mixed anhydride formed from acetylsalicylic acid and ethyl chloroformate, the reaction taking place in an aqueous medium and at low temperature.

Abstract: This invention relates to novel, 1,4-diaminocyclitol derivatives of antimicrobial and immunostimulating activity of the formula: ##STR1## wherein X.sup.1, X.sup.2 and X.sup.3 are each amino or protected amino, X.sup.4 is hydrogen or hydroxy,R.sup.1 is hydrogen or lower alkyl, andR.sup.2 is higher alkanoyl permissably substituted with hydroxy, amino, azido, epoxy, protected hydroxy or protected amino, or higher alkenoyl, or higher alkylcarbanoyl,and pharmaceutically acceptable salts thereof.

Abstract: New derivatives of the istamycin B series of compounds are provided, which are 3-O-demethylistamycin B.sub.O, 3-O-demethylistamycin B and 3-O-demethyl-2"-N-formimidoylistamycin B represented generally by Formula I or specifically by Formulae Ia, Ib and Ic, respectively. Compound Ia is useful as an intermediate for the preparation of Compounds Ib and Ic and the latter two compounds exhibit a high antibacterial activity against a wide variety of Gram-positive and Gram-negative bacteria and are useful antibiotics. Also provided are processes for the preparation of the new derivatives starting from istamycin B.sub.O.