715 results about "Potentiator" patented technology

Sustained release local anesthetic formulations are administered intra articularly and/or into body spaces/cavities. The formulation is preferably a plurality of injectable microparticles including a local anesthetic and an effective amount of a biocompatible, biodegradable, sustained release material prolonging the release of the local anesthetic and optionally and a pharmaceutically acceptable, i.e., non-toxic, augmenting agent effective to prolong the duration of the local anesthesia for a time period longer than that obtainable without the augmenting agent.

Anti-infective foamable composition and kits include a foamable carrier; a therapeutically safe and effective concentration of an anti-infective agent; an augmenting agent selected from the group consisting of a keratolytic agent and a skin penetration enhancer; and a propellant. The composition is housed in a container and upon release is expandable to form a breakable foam. The foamable carrier is selected to generate a foam of good or excellent quality in the presence of the augmenting agent and anti-infective agent. Methods for treating, alleviating or preventing a disorder of the skin, a body cavity or mucosal surface, wherein the disorder involves a fungal, bacterial or viral infection as one of its etiological factors, is described.

The subject invention relates to the surprising discovery that toxin complex (TC) proteins, obtainable from Xenorhabdus, Photorhabdus, and Paenibacillus, can be used interchangeably with each other. In particularly preferred embodiments of the subject invention, the toxicity of a “stand-alone” TC protein (from Photorhabdus, Xenorhabdus, or Paenibacillus, for example) is enhanced by one or more TC protein “potentiators” derived from a source organism of a different genus from which the toxin was derived. As one skilled in the art will recognize with the benefit of this disclosure, this has broad implications and expands the range of utility that individual types of TC proteins will now be recognized to have. Among the most important advantages is that one skilled in the art will now be able to use a single set of potentiators to enhance the activity of a stand-alone Xenorhabdus protein toxin as well as a stand-alone Photorhabdus protein toxin. (As one skilled in the art knows, Xenorhabdus toxin proteins tend to be more desirable for controlling lepidopterans while Photorhabdus toxin proteins tend to be more desirable for controlling coleopterans.) This reduces the number of genes, and transformation events, needed to be expressed by a transgenic plant to achieve effective control of a wider spectrum of target pests. Certain preferred combinations of heterologous TC proteins are also disclosed herein. Other objects, advantages, and features of the subject invention will be apparent to one skilled in the art having the benefit of the subject disclosure.

A high throughput screening and isolation system identifies rare enhancer mixtures from a candidate pool of penetration enhancer combinations. The combinations are screened for high penetration but low irritation potential using a unique data mining method to find new potent and safe chemical penetration enhancer combinations. The members of a library of chemical penetration enhancer combinations are screened with a high throughput device to identify “hot spots”, particular combinations that show higher chemical penetration enhancement compared to neighboring compositions. The irritation potentials of the hot spot combinations are measured to identify combinations that also show low irritation potential. A active component, such as a drug, is then combined with the combination in a formulation which is tested for the ability of the drug to penetrate into or through skin. It is then assessed whether the formulation can deliver the quantity of drug required, and animal tests are conducted to confirm in vivo the ability of the chemical penetration enhancer combinations to facilitate transport of sufficient active molecules across the skin to achieve therapeutic levels of the active molecule in the animal's blood. The invention provides specific unique and rare mixtures of chemical penetration enhancers that enhance skin permeability to hydrophilic macromolecules by more than 50-fold without inducing skin irritation, such as combinations of sodium laurel ether sulfate and 1-phenyl piperazine, and combinations of N-lauryl sarcosine and Span 20/sorbitan monolaurate.

This invention provides a method of inactivating human noroviruses and other acid stable viruses. The method includes the step of contacting the virus with a virucidally-enhanced alcoholic composition that includes an alcohol, and an enhancer selected from cationic oligomers and polymers, chaotropic agents, and mixtures thereof.

An object of the present invention is to provide an enhancing agent for effect of anticancer agent for achieving an excellent therapeutic effect on cancer. The enhancing agent for effect of anticancer agent according to the present invention which is a solving means therefor is characterized in that a nitric oxide donor is an effective ingredient. In accordance with the present invention, an excellent therapeutic effect is able to be achieved on non-small cell lung cancer which is still in such a state that no effective therapeutic method has been established yet for a progressive cancer which is not operable and is one of cancers where chemotherapy is most difficult to apply.

Methods are provided for purifying peptides and proteins by incorporating the peptide or protein into a diketopiperazine or competitive complexing agent to facilitate removal of one or more impurities from the peptide or protein. Formulations and methods also are provided for the improved transport of active agents across biological membranes, resulting for example in a rapid increase in blood agent concentration. The formulations include microparticles formed of (i) the active agent, which may be charged or neutral, and (ii) a transport enhancer that masks the charge of the agent and/or that forms hydrogen bonds with the target biological membrane in order to facilitate transport. In one embodiment insulin is administered via the pulmonary delivery of microparticles comprising fumaryl diketopiperazine and insulin in its biologically active form. This method of delivering insulin results in a rapid increase in blood insulin concentration that is comparable to the increase resulting from intravenous delivery.

The present invention relates to a kit and an intervenously administrable preparation, both, with a signal transmitter precursor, an enhancer of precursor uptake, and an inhibitor of neurotransmitter reuptake or signal transmitter catabolism. The kit also contains an appropriate swab for obtaining oral cells suitable for allelic analysis. The intervenous formulation contains similar materials and, in some cases, ethanol. Either the kit composition or the intervenous formulation may be used as guided by a subjects allelic analysis. Collections of particular alleles, especially those relating to neural system are comprehensible in terms of likelihood of success in the administration of an interveinous formulation or ingestion of components of the subject kit.

Polymerized liposome particles which are linked to a targeting agent and may also be linked to a contrast enhancement agent and/or linked to or encapsulating a treatment agent. The targeting imaging enhancement polymerized liposome particles interact with biological targets holding the image enhancement agent to specific sites providing in vitro and in vivo study by magnetic resonance, radioactive, x-ray or optical imaging of the expression of molecules in cells and tissues during disease and pathology. Targeting polymerized liposomes may be linked to or encapsulate a treatment agent, such as, proteins, drugs or hormones for directed delivery to specific biological sites for treatment.

The invention relates to a low-temperature scouring and bleaching promoter composition and a preparation method thereof. The composition comprises 2.5-5.5% of Tetra acetyl ethylene diamine (TAED), 0-0.5% of hydrogen peroxide decomposition catalyst, 5-15% of bleaching potentiator, 10-15% of chelating agent, 77-54.5% of carrier and 5-10% of surfactant, according to the weight percentage. The preparation method comprises the steps as follows: the carrier, the TAED, the hydrogen peroxide decomposition catalyst, the chelating agent and the bleaching potentiator are sequentially added in a powder mixer and mixed uniformly for 45-60min; subsequently, the surfactant is added and all mixtures are mixed for 15-30min and then discharged, thus obtaining the composition. The low-temperature scouring and bleaching promoter composition belongs to the environment-protective promoter composition, contains no phosphor and other substances harmful to the environmental protection, has no AOX problem, achieves the object that one promoter replaces more than four promoters, and facilitates processing and quality control.

The present invention relates to small molecule potentiators of metabotropic receptors, in particular of the mGlu2 receptor. The present invention also relates to the use of these compounds for the prevention or treatment of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The present invention thus provides compounds of formula I

wherein X¹ is N or C—R¹, X² is N or C—R², X³ is N or C—R³, X⁴ is N or C—R⁴ provided that none or one of X¹, X², X³ or X⁴ is N; Y¹ is N, C or C—R⁵, Y² is N, C or C—R⁶, Y³ is Y¹, Y², N, C or C—R⁷, Y⁴ is N, C or C—R⁸ provided that only the moiety Y¹, Y², Y³ or Y⁴ to which Z is bound is C and further provided at most one of Y¹, Y², Y³ or Y⁴ is N; Z is O, S, S(O), S(O)₂ or NR^Z; Q is CH₂ or CH₂CH₂, where one or two of the hydrogen atoms in CH₂ or CH₂CH₂ may be replaced by halogen, C₁-C₄-alkyl or C₁-C₄-haloalkyl; R¹ is inter alia hydrogen, halogen, C₁-C₆-alkyl, C₁-C₆-haloalkyl, C₁-C₆-alkoxy, C₁-C₄-haloalkoxy, C₃-C₈-cycloalkyl, a radical NR^1aR^1b, C-bound 3- to 7-membered, saturated heterocyclyl having 1 or 2 nitrogen atoms and 0 or 1 heteroatoms, selected from O and S, as ring members, aryl, aryl-CH₂, aryloxy, hetaryl, hetaryloxy or hetaryl-CH₂, wherein the heterocyclyl, aryl and hetaryl rings ring in the last six radicals themselves are unsubstituted or carry 1, 2, 3, 4 or 5 identical or different radicals R^1c; R² has one of the meanings given for R¹; R³ and R⁴ are, inter alia, selected from hydrogen, halogen, C₁-C₄-alkyl, C₁-C₄-haloalkyl, C₃-C₆-cycloalkyl, C₁-C₄-alkoxy, C₁-C₄-alkoxy-C₁-C₄-alkyl, phenyl, C₁-C₄-haloalkoxy, a radical (CH₂)_nNR′R″; R⁵, R⁶, R⁷, R⁸ are, independently of each other, selected from hydrogen, halogen, etc.; R^a is C₃-C₆-cycloalkyl, C₁-C₆-haloalkyl or C₁-C₆-alkyl, which is unsubstituted or carries one radical selected from C₁-C₄-alkoxy, C₁-C₄-haloalkoxy and a radical NR^a1R^a2; and the N-oxides and the pharmaceutically acceptable salts thereof.

Transcutaneous immunization can deliver antigen to the immune system through the stratum corneum without physical or chemical penetration to the dermis layer of the skin. This delivery system induces an antigen-specific immune response without the use of a heterologous adjuvant. Although perforation of intact skin is not required, superficial penetration or micropenetration of the skin can act as an enhancer; similarly, hydration may enhance the immune response. This system can induce antigen-specific immune effectors after epicutaneous application of a formulation containing one or more antigens. The formulation may initiate processes such as antigen uptake, processing, and presentation; Langerhans cell activation, migration from the skin to other immune organs, and differentiation to mature dendritic cells; contacting antigen with lymphocytes bearing cognate antigen receptors on the cell surface and their stimulation; and combinations thereof. Systemic and/or regional immunity may be induced. Immune responses that provide prophylactic and/or therapeutic treatments are preferred. Antigenic activities in the formulation may be found in the same molecule, two or more different molecules dissociated from each other, or multiple molecules in a complex formed by covalent or non-covalent bonds. For antigens which are proteinaceous, they may be provided in the formulation as a polynucleotide for transcutaneous genetic immunization. Besides simple application of a dry or liquid formulation to the skin, patches and other medical devices may be used to deliver antigen for immunization.

The topical medicament gel formulation of the present invention includes an anesthetic, an anti-microbial, an oxidant, a nutrient, a diuretic, an opioid, an anti-emetic, an anti-seizure drug, and a non-steroidal anti-inflammatory drug (NSAID), USP in a molecular, as opposed to a salt form, as the active ingredient. Additional constituents illustratively include a skin penetration enhancer and a gelling agent. This invention deals with problems commonly associated with topical application of local medicaments such as: slow onset of action; need for occlusion; and rapid loss of effect due to rapid systemic dispersion. The invention permits enhanced penetration of the medicament and thereby allows for a lesser total dosage of pharmaceutically active ingredient. The use of a lesser total dosage also decreases systemic toxicity.

A formulation for drug delivery, providing enhanced modulation of solubility, stability, absorption, metabolism, and/or pharmacokinetic profile of a lipophilic therapeutic agent by formulation with sterols and/or sterol esters, resulting in higher bioavailability of a therapeutic agent administered to a subject in need of such therapeutic agent. The formulation contains a therapeutic agent and a sterol or sterol ester, and can, optionally, further contain a solubilizer and/or an enhancing agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.

The present invention provides an approach for the simultaneous determination of the activation states of a plurality of proteins in single cells. This approach permits the rapid detection of heterogeneity in a complex cell population based on activation states, and the identification of cellular subsets that exhibit correlated changes in activation within the cell population. Moreover, this approach allows the correlation of cellular activities or properties. In addition, the use of potentiators of cellular activation allows for characterization of such pathways and cell populations.

Compositions and methods for transport or release of therapeutic and diagnostic agents or metabolites or other analytes from cells, compartments within cells, or through cell layers or barriers are described. The compositions include a membrane barrier transport enhancing agent and are usually administered in combination with an enhancer and/or exposure to stimuli to effect disruption or altered permeability, transport or release. In a preferred embodiment, the compositions include compounds which disrupt endosomal membranes in response to the low pH in the endosomes but which are relatively inactive toward cell membranes, coupled directly or indirectly to a therapeutic or diagnostic agent. Other disruptive agents can also be used, responsive to stimuli and/or enhancers other than pH, such as light, electrical stimuli, electromagnetic stimuli, ultrasound, temperature, or combinations thereof. The compounds can be coupled by ionic, covalent or H bonds to an agent to be delivered or to a ligand which forms a complex with the agent to be delivered. Agents to be delivered can be therapeutic and/or diagnostic agents. Treatments which enhance delivery such as ultrasound, iontopheresis, and/or electrophereis can also be used with the disrupting agents.

The invention discloses a kit for determining glycocholic acid in human blood. The kit comprises a reagent A, a reagent B and a calibrator for glycocholic acid with known concentration, wherein the mass ratio of the reagent A to the reagent B is (1-5):1; the reagent A comprises a microorganism inhibiting agent, EDTA (Ethylene Diamine Tetraacetic Acid), glycerol, albumin bovine serum, a surface active agent, a reactive reinforcing agent, sodium chloride and a Good's buffer solution with the pH of 6-8; and the reagent B comprises the microorganism inhibiting agent, the EDTA (Ethylene Diamine Tetraacetic Acid), the glycerol, the albumin bovine serum, the surface active agent, the reactive reinforcing agent, sodium chloride, the Good's buffer solution with the pH of 6-8 and nanoparticles crosslinked with a glycocholic acid monoclonal antibody. The kit is simple, convenient and fast in detection and operation, can be used for simultaneously and quickly determining a large amount of samples and has good detection accuracy and sensitivity.