Abstract: A non-invasive and non-systemic method for intradermal prevention OR amelioration of pain from a surgically closed wound is disclosed. The method comprises topical delivery of a local anesthetic to an exterior surface of a surgically closed wound.

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. The compounds precipitate in aqueous environments. 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 period of up to 15 days or even longer.

Abstract: Disclosed are popping pharmaceutical oral administration forms, which comprise an active ingredient, and pressurized gas trapped within cavities in a pharmaceutically acceptable material in a manner that allows the gas to escape from the administration form upon dissolution or shattering of said form.

Abstract: Application of topical synergistic microbicide composition(s) of high practical utility both as a treatment and/or prevention against HSV Type 1 and/or Type 2 and related diseases and secondary opportunist disease causing agents, while reducing the inflammation, prolonged healing times and reduce scaring.

Abstract: The present invention is directed to an improved flowable anesthetic composition that does not need to be applied by an applicator. The anesthetic composition of the present invention may be applied by dripping or spraying the composition onto a wound or other injured area. The composition of the anesthetic includes one or more anesthetics, and a base comprising a surgical lubricant. If desired, the composition may also include one or more vasoconstrictors. The vasoconstrictor is preferably an adrenaline based compound and more preferably epinephrine. The surgical lubricant is preferably water soluble. The anesthetics may include any of the well-known anesthetics such as lidocaine, pontocaine, tetracaine, bupivicaine, procaine and others.

Abstract: A non-invasive and non-systemic method for administering a local anesthetic. The method comprises topical application of a local anesthetic in combination with an intradermal-penetration agent selected from the group consisting an aloe composition, a triglyceride, and a mixture thereof.

Abstract: In certain embodiments, the present invention is directed to a pharmaceutical formulation for topical administration on a mammal, comprising a unit dose of a therapeutically effective amount of a therapeutic agent and a pharmaceutically acceptable carrier medium therefor, said formulation being solid at ambient temperature and having a softening point of not higher than 35° C., such that when the formulation is placed in continuous contact with the skin of a mammalian patient, it is softened to a consistency to effect substantial application of the unit dose of said therapeutic agent onto a desired skin area of the mammalian patient within a time period of less than 10 minutes.

Abstract: Compositions and methods for reducing the decomposition rate of poly(carboxylic acids), such as hyaluronic acid. The compositions include at least one strong, stable chelating agent, preferably an organophosphorous compound such as diethylene triamine penta(methylene phosphonic acid). These biocompatible compositions are especially useful in the ophthalmic field. Also disclosed is a method of performing surgery on an eye including employing a hyaluronic acid material utilizing the inventive composition of the present invention.

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: A method including topically administering an effective amount of local anesthetic to a patient is disclosed. The method is effective for inducing analgesia for treating non-neuropathic pain. Non-neuropathic pain suitable for treatment according to the invention includes pain associated with sports injuries; sprains; strains; soft-tissue injury; repetitive motion injury; carpal tunnel syndrome; injury to tendons, ligament, and muscles; conditions such as fibromyalgia, bursitis, castrochondritis, myofascial pain, and pain associated with arthritis, inflammation, contusions, post-surgical pain, and nociceptive pain. Preferably, the lidocaine is applied via a transdermal patch applied near the locus of pain.

Abstract: The present invention is directed to improved methods for producing solid dispersions, especially pharmaceutical dispersions. These methods involve the dissolution of one or more insoluble or relatively insoluble substances, preferably pharmaceutically active substances, and/or one or more water-soluble substances, preferably carriers, in supercritical fluids and the subsequent removal of solvent by rapid expansion. These methods offer a number of advantages over traditional preparation methods and form formulations with highly desirable dissolution properties, especially for pharmaceuticals.

Abstract: The present invention relates to a liquid formulation for a feminine wipe. The preferred formulation has an anti-irritant agent, a pH adjuster namely citric acid, and at least one preservative.

Abstract: Methods and compositions are disclosed for prevention and/or treatment of diseases in which 5- and 12-lipoxygenase activity contributes to the pathological condition, by administration of 12-methyletradecanoic acids alone and in conjunction with other therapeutic compounds. Methods to inhibit lipoxygenase-mediated inflammations are disclosed.

Abstract: An aqueous gel in unit dose form and suitable for topical delivery of clonidine and comprising clonidine, a water-gelling amount of a pharmaceutically acceptable gelling agent and having a pH value in the range of about 6 to about 8.5. Clonidine is present in an amount in the range of about 0.05 to about 3.5 milligrams per unit dose and at a concentration in the range of about 0.01 to about 0.5 weight percent.

Abstract: A method of desensitizing the scalp prior to a generally painful hair treatment or manipulation procedure by application of a composition containing a therapeutically effective amount of solubilized topical anesthetic and scalp/skin conditioning oils. The composition can be used for the conditioning and desensitization of scalp and skin areas which are irritated, agitated, or traumatized by hair treatment procedures like braiding, corn-rowing, electrolysis, hair plugging, hair removal or any other hair treatment procedure that causes pain to the hair shaft or follicle.

Abstract: A pharmaceutical composition is provided for topical administration of a local anesthetic agent. The composition comprises (a) a therapeutically effective amount of a local anesthetic agent and (b) a pharmaceutically acceptable, nonliposomal carrier comprised of a monohydric alcohol, a penetration enhancer, and polymer, which may be a hydrophilic polymer, a hydrophobic polymer or a combination thereof. The composition can be in the form of a gel, or it may form a film following application to a patient's body surface and evaporation of the monohydric alcohol. The composition provides rapid onset of local anesthesia as well as penetration of the active agent into the skin. Methods and drug delivery systems for administration of local anesthetic agents are also provided.

Abstract: One aspect of the invention relates to anti-viral composition containing at least one zinc compound and at least one phenolic antioxidant (and optionally other ingredients such as at least one analgesic) at least one hydrocarbyl containing compound, and water. Another aspect of the invention relates to a method of treating lesionous symptoms of a viral infection involving applying an effective amount of the zinc containing anti-viral composition to the lesions.

Abstract: A molluscicide containing a non-toxic animal repellant and metaldehyde, in which the molluscicidal efficacy of the molluscicide greater than that of the molluscicide if it did not contain repellant. The repellant may be an anthranilate compound or d-pulegone which present at a concentration of up to 1%.

Abstract: If the R-enantiomer of metalaxyl, furalaxyl or benalaxyl is used, this results in a markedly increased biodegradability of these plant fungicides in the soil and a higher activity on the plants, as compared with the data of the racemic active ingredients. Fungicidal compositions exhibiting said improved properties comprise either of these fungicides with a content of R-enantiomer of more than 70 percent by weight based on the total amount of active ingredient.

Abstract: Sialyl-Lewisx and sialyl-Lewisa epitope analogues in which the naturally occurring N-acetyl group of the N-acetylglucosamine monomer is replaced by various aliphatic or aromatic substituents and the L-fucose naturally present is replaced by various naturally occurring or non-naturally occurring sugars.

Abstract: Sympathetically maintained peripheral neuropathic pain syndromes are relieved by topically applying, to the affected region of a patient suffering from such pain, a pain relieving amount of an aqueous gel comprising clonidine, a water-gelling amount of a pharmaceutically acceptable gelling agent and having a physiologically tolerable pH value. Pain relief was achieved with applied amounts of clonidine in the range of about 2 milligrams per day to about 6 mg per day.

Abstract: This invention relates to nitrogen-containing oxyalkylene diester compositions for treating disease conditions including cancer and other proliferative diseases. The nitrogen-containing oxyalkylene diesters are represented by the formula ##STR1## where the nitrogen-containing group is R.sub.3 and includes particular alkyl, alkenyl, cycloalkyl, aryl, aralkyl, heterocycloalkyl or heteroaryl groups, which have nitrogen-containing substituents, such as amines, amides, or nitrogen heteroatoms.

Abstract: The present invention is a system which topically delivers pharmaceuticals to the buccal mucosa. Preferred pharmaceuticals include topical local anesthetics, such as tetracaine, which can be applied to the mucosa for rapid pain relief. The system comprises a hard candy matrix in which the pharmaceutical is dispersed. The hard candy matrix may be formed without the addition of dyes, synthetic flavoring agents, alcohols, or preservatives. Also, the candy may be mounted on a handle to form a lollipop, and the handle may be used to position the candy adjacent a particular site where the pharmaceutical is needed.

Abstract: Fibrinogen receptor antagonist prodrugs having the structure, for example, of ##STR1## more particularly, ##STR2##

Abstract: A topical anesthetic includes about 1-10% by weight lidocaine hydrochloride, about 0.01-0.10% by weight adrenaline, and about 0.25-4% by weight tetracaine hydrochloride, preferably in an aqueous base with about 2% benzyl alcohol or in a gel including about 3% hydroxyethyl cellulose. The topical anesthetic has been found to be at least as effective as TAC (tetracaine hydrochloride, adrenaline, cocaine), but with fewer harmful side effects and at a greatly reduced cost (about 1/10 of the cost of TAC).

Abstract: Novel 2-cyanoacrylic esters I ##STR1## where the radicals have the following meanings: R.sup.1 and R.sup.2 are each hydrogen or a radical having an iso- or heterocyclic ring system with at least one iso- or heteroaromatic nucleus, and at least one of the radicals R.sup.1 or R.sup.2 must be different from hydrogen,n is from 2 to 10, andX is, when n=2, a radical of the formula II ##STR2## where m is from 2 to 8, and X is, when n>2, the radical of an n-hydric aliphatic or cycloaliphatic polyol having 3-20 carbon atoms, it also being possible for a cycloaliphatic radical to contain 1 or 2 hetero atoms, and for an aliphatic radical to be interrupted by up to 8 non-adjacent oxygen atoms, sulfur atoms, imino or C.sub.1 -C.sub.4 -alkylimino groups, are used as light stabilizers.

Abstract: A pharmaceutical composition for percutaneous anaesthesia comprising amethocaine free base, an aqueous gelling agent, and from 1 to 30% of a pharmaceutically acceptable salt is disclosed.

Abstract: A hazard-free method for controlling insects using a non-toxic composition. The invention includes a process for making the composition in the form of a fragrance and crystalline particles which puncture directly through the exoskeleton of an insect. In operation, the particles work themselves between the insect's protective body plates and then puncture the exoskeleton permitting entry of the fragrance into the body of the insect. Once inside, the particles absorb up to four times their weight of the vital body fluids of the insect and the fragrance has a neural effect on the insect.

Abstract: A topical anesthetic includes about 1-10% by weight lidocaine hydrochloride, about 0.01-0.10% by weight adrenaline, and about 0.25-4% by weight tetracaine hydrochloride, preferably in an aqueous base with about 2% benzyl alcohol or in a gel including about 3% hydroxyethyl cellulose. The topical anesthetic has been found to be at least as effective as TAC (tetracaine hydrochloride, adrenaline, cocaine), but with fewer harmful side effects and at a greatly reduced cost (about 1/10 of the cost of TAC).

Abstract: A storage stable composition for topical anesthesia comprising amethocaine free base, an aqueous gelling agent, and from 1 to 30% by weight of a pharmaceutically acceptable salt is disclosed.

Abstract: Novel topical anesthetic compositions containing high concentrations of benzocaine in a micronized powder form suspended in an emollient vehicle.

Abstract: The present invention provides methods of using compositions containing local anesthetic compounds for facilitating the removal of sucking arthropods from the skin of a mammal; for reducing inflammation associated with a bite of a sucking arthropod; for limiting infection from a sucking arthropod; and for enhancing the facilitated removal of sucking arthropods from the skin of a mammal.

Abstract: Bioadhesive pharmaceutical carrier consisting essentially of a polymer blend of sodium carboxymethyl cellulose and xanthan gum or sodium alginate. The invention also provides for a method of control releasing a pharmaceutical active comprising incorporating an active into the bioadhesive pharmaceutical carrier. The invention is particularly adaptable for oral use and teething gels.

Abstract: The mixture consists of at least one organic peroxide, at least one hydroquinone derivative of the general formulae I and/or II and/or III ##STR1## wherein R and R.sup.1, which may be identical or different, stand for H or t-alkyl, and X stands, for example, for C.sub.1-18 -alkylene, and a crosslinkage promoter, and permits the crosslinkage of polymers and at the same time extends the scorch time, which must be understood as the processing time.

Abstract: A new visualizing and anesthetic composition and the process for the preparation thereof. The composition, generally as a gel, contains an effective amount of a topical anesthetic, an effective amount of a visualizing agent and a pharmaceutically acceptable gelling reservoir as a heat exchanger and/or a light transmitter. The composition is useful for topical application to a region of mammalian skin to supply visualization to a lesion therein and to anesthetize the region for a subsequent destructive therapy.

Abstract: A composition, for producing pain relief in a body region, comprises a sterile, stable suspension of butyl aminobenzoate in a non-toxic, aqueous carrying medium in which the butyl aminobenzoate is substantially insoluble. The aqueous carrying medium consists essentially of water as the major constituent and a suspending agent composed of (a) polyethylene glycol and (b) a wetting agent for the butyl aminobenzoate, with a ratio of (a) to (b) in the range of about 50/1 to 125/1. The butyl aminobenzoate is milled to a particle size in the range of about 5 to 50 microns in the presence of the suspending agent.

Abstract: Bioadhesive pharmaceutical carrier consisting essentially of a polymer blend of sodium carboxymethyl cellulose and xanthan gum or sodium alginate. The invention also provides for a method of control releasing a pharmaceutical active comprising incorporating an active into the bioadhesive pharmaceutical carrier. The invention is particularly adaptable for oral use and teething gels.

Abstract: The invention presented is a composition for the treatment of individuals addicted to narcotics or individuals having age-related conditions such as tinnitus and Alzheimer's disease, comprising a protected complex of procaine and a complexing agent for procaine in an amount effective to reduce the withdrawal symptoms of individuals addicted to narcotics or the symptoms of tinnitus and Alzheimer's disease.

Abstract: Etofenamate is used for the preparation of compositions useful in the treatment of bacterial, viral or fungicidal inflammations in the region of the oral cavity.

Abstract: A guanidinobenzoic ester derivative having the formula is novel and effective to inhibit enzymes such as trypsin, plasmin and thrombin, being useful for treatment of the pancreatitis and hemorrhagic disease and thrombosis. ##STR1## wherein X represents a group of the formula: ##STR2## in which Y is a group of the formula: --(CH.sub.2).sub.m--, m being an integer of 2 or 3, ##STR3## or a group of the formula:--ORin which R is a hydrogen atom or a lower alkyl group, and n represents an integer of 1 to 5.

Abstract: A composition suitable for use in the aversion therapy treatment of cocaine abuse. The composition has the physical characteristics, taste, and anesthetic effect similar to cocaine. The composition comprises an amount of a local anesthetic sufficient to induce a degree of anesthesia similar to that induced by cocaine. The composition further comprises a carrier compound possessing the physical characteristics of cocaine. The composition may further comprise additional components which aid in imparting the physical characteristics, odor, taste, or anesthetic effect of cocaine to the composition of the present invention.

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: Medicament preparations contain 2-(2-hydroxyethoxy)-ethyl N-(.alpha.,.alpha.,.alpha.-trifluoro-m-tolyl)-anthranilate and dimethyl sulphoxide.

Abstract: Novel liquid anesthetic aerosol composition comprising high concentrations of benzocaine in a water washable base with propellants which are resistant to cold temperatures are disclosed.

Abstract: A method of inducing short-term pupil diameter enlargement and reducing intraocular pressure in animals without significant systemic effects is disclosed. There is provided a site-specific chemical delivery method for topically applying to the eye of an animal, an effective ophthalmologically acceptable amount of an adrenalone diester of the general formula: ##STR1## wherein R prepresents a member selected from the group consisting of hydrogen or a C.sub.1 -C.sub.3 straight alkyl group; and wherein R.sub.1 and R.sub.2 independently represent an acyl group or derivative thereof; or an opthalmologically acceptable acid addition salt thereof. The method allows the pupil diameter to be enlarged for a short period after which the pupil returns to normal and thus restores normal eye sight.

Abstract: Eucalyptol is used to enhance skin permeation of bio-affecting agents.

Abstract: Pesticidal mixtures of carbamate insecticides and synthetic pyrethroids can be improved by the addition of stabilizers to prevent racemization of the pyrethroid to a less pesticidally-active isomeric form.