Abstract: The present invention provides compositions and methods for noninvasive delivery of therapeutic agents across an intact tympanic membrane. For example, the compositions include a penetration enhancer which increases the flux of a therapeutic agent (e.g., antibiotic) across the tympanic membrane. Such compositions are particularly useful in the treatment of otitis media. Additionally, the composition may include a sustained release agents that, in some embodiments form sustained release reservoirs, in situ, once administered to a patient.

Abstract: This invention concerns a synergistic combination of a topical anesthetic and wound barrier forming agent capable of providing extended analgesia of ‘significant open wounds’ (that being, for example, a laceration, surgical incision, abrasion, ulcer or burn, but not being a minor cut, scratch, sting, burn or abrasion) in which conventional management alternatives (such as suturing and/or administration of injected or systemic analgesia) are impractical, unaffordable or otherwise unavailable.

Abstract: Described are ethanol-free foamable microemulsions for topical application, and method of making them. The propellants used in the compositions may be environmentally-friendly hydrofluoroalkanes. The foam compositions may also comprise one or more of a variety of active ingredients, including anti-inflammatory agents, anesthetics, and keratolytic agents.

Abstract: This invention provides methods of controlling pain in a canine comprising transdermally administering a composition comprising fentanyl, a penetration enhancer, and a volatile liquid, wherein the composition is a solution. The invention also provides a single unit dose of the composition.

Abstract: This invention relates to a patch for the expulsion of insect poison from the skin after stings from membranous insects (Hymenoptera). The patch is characterized in comprising a poison-aspirating matrix comprising an expulsion agent as well as a swell layer, which swells after the addition of a liquid through a hole on the top of the patch and thus adds a light pressure to the poison-aspirating matrix towards the skin, whereby a local and relieving effect is achieved. In one embodiment, the matrix further comprises a local anesthetic. The expulsion agent is e.g. a carbohydrate. The swell layer consists e.g. of a silica gel.

Abstract: A topical or transdermal composition including a polar derivative of ketoprofen and a pharmaceutically acceptable topical or transdermal carrier, wherein the polar derivative of ketoprofen comprises a polarity that is greater than that of ketoprofen.

Abstract: A method and composition for treating healed wounds including hypertrophic scars so as to prevent scarring or reduce the size and improve the appearance of scars comprises applying to the healed wound or scar a composition comprising a fluid, film-forming carrier which may contain one or more active topical ingredients, the carrier hardening to a solid, tangible, membrane juxtaposed to the skin. Novel compositions using the film-forming carrier are also useful to treat a variety of adverse skin disorders, and internal physiological conditions.

Abstract: Many chemical and pharmaceutical compositions are known to produce antinociceptive effects that are helpful in relieving pain and inflammation. Both opioids and local anesthetics serve an important function in providing peripheral pain relief. Topical administration of pain-relieving drugs to the periphery offers important advantages over systemic or local, non-topical administration. The present invention provides topical pharmaceutical compositions, formulated with at least one local anesthetic and at least one opioid analgesic in a topical excipient. The present invention also provides methods for relieving pain in a subject through topical administration of the pharmaceutical composition in an amount and a duration sufficient to synergistically potentiate an antinociceptive response. Synergistic potentiation of analgesia through topical administration of a local anesthetic/opioid pharmaceutical composition provides a new and improved approach to peripheral pain management.

Abstract: A method and composition for treating healed wounds including hypertrophic scars so as to prevent scarring or reduce the size and improve the appearance of scars comprises applying to the healed wound or scar a composition comprising a fluid, film-forming carrier which may contain one or more active topical ingredients, the carrier hardening to a solid, tangible, membrane juxtaposed to the skin. Novel compositions using the film-forming carrier are also useful to treat a variety of adverse skin disorders, and internal physiological conditions.

Abstract: Disclosed herein is a preparation for topically delivering and localizing therapeutic agents, comprising: a vasoconstrictor for retarding vascular dispersion of a therapeutic agent; and a penetration enhancer for facilitating penetration of the vasoconstrictor and the therapeutic agent through a patient's skin. Further disclosed is an associated method of topically delivering and localizing therapeutic agents, comprising the steps of: using a vasoconstrictor for retarding vascular dispersion of a therapeutic agent; in combination with using a penetration enhancer for facilitating penetration of the vasoconstrictor and the therapeutic agent through a patient's skin. Also disclosed are various courses of treatment which comprise applying the various disclosed combinations of agents to the patient's skin.

Abstract: Topical analgesics, generally comprising calendula oil and cornmint oil, and methods of use.

Abstract: This invention relates to a pharmaceutical composition for oral administration comprising a carrier and, as active ingredient, an opioid (? receptor) agonist, such as fentanyl, or a salt thereof, characterized in that the composition is in the form of a fast-dispersing dosage form designed to release the active ingredient rapidly in the oral cavity. A process for preparing such a composition and the use of such a composition as an analgesic, for the treatment of chronic pain and/or breakthrough pain, as an anesthetic premedication, for the induction of anesthesia, as a sedative and/or for the treatment of anxiety are also provided.

Abstract: Irritation upon injection of a formulation containing propofol is reduced or substantially eliminated by administering a stable, sterile, and antimicrobial aqueous dispersion comprising a water-insoluble microdroplet matrix of mean diameter from about 50 nm to about 1000 nm consisting essentially of about 1% to about 15% of propofol, up to about 7% of a propofol-soluble diluent, and about 0.8% to about 4% of a surface stabilizing amphiphilic aent. The aqueous phase includes a pharmaceutically acceptable water-soluble polyhydroxy tonicity modifier. The propofol-containing dispersion is devoid of additional bactericidal or bacteriostatic preservative agents.

Abstract: A transcutaneous pain relief composition for applying to the skin, comprising a mixture of dimethyl sulfoxide, stearic acid, emulsifying wax, glycerine, emu oil, sal butter, glucosamine, coconut oil, white beeswax, active calendula oil, slippery elm oil, Chamomile oil, arnica Oil, valenrian oil, peppermint oil, grapefruit seed extract, lavender oil and distilled water is disclosed.

Abstract: Several lines of evidence have shown a role for the nitric oxide (NO)/cyclic guanosine monophosphate (cGMP) signaling pathway in the development of spinal hyperalgesia. However, the roles of effectors for cGMP are not fully understood in the processing of pain in the spinal cord. cGMP-dependent protein kinase (PKG) I? but not PKGI? was localized in the neuronal bodies and processes, and was distributed primarily in the superficial laminae of the spinal cord. Intrathecal administration of an inhibitor of PKGI?, Rp-8-[(4-Chlorophenyl)thio]-cGMPS triethylamine, produces significant antinociception. Moreover, PKGI? protein expression was dramatically increased in the lumbar spinal cord after noxious stimulation. This upregulation of PKGI? expression was completely blocked not only by a neuronal NO synthase inhibitor, and a soluble guanylate cyclase inhibitor, but also by an N-methyl-D-aspartate (NMDA) receptor antagonist, MK-801.

Abstract: Block copolymers based on poly(ortho esters) containing amine groups. These block copolymers have both hydrophilic and hydrophobic blocks. They form micelles in aqueous solution, making them suitable for encapsulation or solubilization of hydrophobic or water-insoluble materials; and they also form bioerodible matrices for the sustained release of active agents.

Abstract: A formulation and methods for inducing sustained regional local anesthesia in a patient comprising a substrate comprising a local anesthetic and an effective amount of a biocompatible, biodegradable, controlled release material prolonging the release of the local anesthetic from the substrate to obtain a reversible local anesthesia when implanted or injected in a patient, and a pharmaceutically acceptable, i.e., non-toxic, non-glucocorticoid augmenting agent effective to prolong the duration of the local anesthesia for a time period longer than that obtainable from the substrate without the augmenting agent.

Abstract: A method for applying a topical anesthetic to an area of skin comprising the steps of a) incorporating an anesthetic in a lipophilic base into a volatile solvent, to form a homogeneous solution; b) applying the homogeneous solution into the area of skin to be treated; and c) evaporating the volatile solvent from the homogeneous solution; wherein the volatile solvent is present in the formulation in amounts between 40-80%; and wherein said topical anesthetic rapidly penetrates the skin surface at said skin, leaving a cooling sensation on the skin. The topical anesthetic formulation contains a penetrating enhancer carrier that markedly enhances the delivery of the anesthetic across human skin without altering the acceptable delivery rate of the anesthetic that needs to be delivered through the skin and leaves a cooling sensation on the skin.

Abstract: The present invention relates to a method for reducing inflammation in the skin and/or treating inflammatory skin disorders, pain, or pruritis by topically applying a composition comprising totarol or a pharmaceutically-acceptable ester thereof.

Abstract: The invention provides compositions and methods suitable for ameliorating female sexual dysfunction, and in particular, female sexual arousal disorder. In one embodiment, the invention provides a semisolid composition suitable for topical application comprising: an effective amount of a vasoactive prostaglandin, a polysaccharide thickener, a lipophilic component, and an acidic buffer system.

Abstract: A composition is disclosed which has been shown to stop or control bleeding and seal open small blood vessels while accelerating the healing process of abraded oral “gum” and other “skin” (epithelial) tissues. The composition is preferably in the form of a paste which promotes ease of application and use of the composition. A variety of instruments can be used in application and cleanup of the composition showing versatile unparalleled friendly usage. The composition preferably comprises aluminum chloride, ferric sulfate (subsulfate), regenerated oxidized cellulose, aluminum ammonium sulfate, absorbable gelatin and a solvent. The composition has many dental and medical procedure applications.

Abstract: Many chemical and pharmaceutical compositions are known to produce antinociceptive effects that are helpful in relieving pain and inflammation. Both opioids and local anesthetics serve an important function in providing peripheral pain relief. Topical administration of pain-relieving drugs to the periphery offers important advantages over systemic or local, non-topical administration. The present invention provides topical pharmaceutical compositions, formulated with at least one local anesthetic and at least one opioid analgesic in a topical excipient. The present invention also provides methods for relieving pain in a subject through topical administration of the pharmaceutical composition in an amount and a duration sufficient to synergistically potentiate an antinociceptive response. Synergistic potentiation of analgesia through topical administration of a local anesthetic/opioid pharmaceutical composition provides a new and improved approach to peripheral pain management.

Abstract: The present invention features methods and apparatus'for improving administration of drugs through the use of specifically controlled heat and other physical means. The present invention relates to the use of heat and other physical means in conjunction with specially designed dermal drug delivery systems, conventional commercial dermal drug delivery systems, or drugs delivered into a sub-skin depot site via injection and other methods to alter, mainly increase, the drug release rate from the dermal drug delivery systems or the depot sites to accommodate certain clinical needs.

Abstract: A pharmaceutical composition for therapeutically treating prostate cancer, the pharmaceutical composition containing N-[6-methoxy-5-(2-methoxyphenoxy)-2-(2-pyrimidinyl)-4-pyri midinyl]-2-phenylethenesulfoneamide or a pharmaceutically acceptable salt thereof as the effective component.

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: A composition for topical analgesic and antiseptic use which consists essentially of a approximately equal proportions of alcohol, turpentine, and eucalyptus oil.

Abstract: The invention relates to surgical bone cement compositions and more particularly to bone cement compositions having aneasthetic properties, and to methods for producing analgesia.

Abstract: A topical delivery composition which employs a multivesicular emulsion in combination with a pharmaceutically/pharmacologically active agent is disclosed. The multivesicular emulsion is formed from a quaternary amine salt emulsifier such as behentrimonium methosulfate. The emulsion is multi-lamellar which is a series of concentric spheres or vesiculars of oil and water phase that can be seen microscopically. As a result, the active is time released over a sustained period rather than spike released as is common with most topicals.

Abstract: A carbon dioxide-containing viscous composition wherein carbon dioxide bubbles are retained in an aqueous viscous composition. Use of the composition makes it possible to treat or ameliorate itching accompanying mucocutaneous diseases or mucocutaneous disorders, mucocutaneous injury, dental diseases, skin ulcer, cryesthesia and numbness caused by peripheral circulatory disorders, musculoskeletal diseases, nervous system diseases, keratosis, constipation, unwanted hair re-growing after depilation, cosmetic troubles in the skin or hair, partial obesity, etc. while exerting little side effects.

Abstract: This invention relates to a pharmaceutical composition for oral administration comprising a carrier and, as active ingredient, an opioid (&mgr;receptor) agonist, such as fentanyl, or a salt thereof, characterized in that the composition is in the form of a fast-dispersing dosage form designed to release the active ingredient rapidly in the oral cavity. A process for preparing such a composition and the use of such a composition as an analgesic, for the treatment of chronic pain and/or breakthrough pain, as an anesthetic premedication, for the induction of anesthesia, as a sedative and/or for the treatment of anxiety are also provided.

Abstract: A composition is disclosed which has been shown to stop or control bleeding and seal open small blood vessels while accelerating the healing process of abraded oral “gum” and other “skin” (epithelial) tissues. The composition is preferably in the form of a paste which promotes ease of application and use of the composition. A variety of instruments can be used in application and cleanup of the composition showing versatile unparalleled friendly usage. The composition preferably comprises aluminum chloride, ferric sulfate (subsulfate), regenerated oxidized cellulose, aluminum ammonium sulfate, absorbable gelatin and a solvent. The composition has many dental and medical procedure applications.

Abstract: Topical compositions and methods for treating pain. The invention provides oil-in-water emulsions comprising an antidepressant; an NMDA-receptor antagonists; a lipophilic component; water; and a surfactant. The compositions induce a local-anesthetic effect when topically administered to intact skin thereby treating or preventing pain, for example, neuropathic pain.

Abstract: Melatonin (N-acetyl-5-methoxytryptamine), or its biologically active analogues, are used to induce anesthesia.

Abstract: Methods and apparatus for improving administration of drugs through the use of heat and other physical means. The present invention relates to the use of heat and other physical means in conjunction with specially designed dermal drug delivery systems, conventional commercial dermal drug delivery systems, or drugs delivered into a sub-skin depot site via injection and other methods to alter, mainly increase, the drug release rate from the dermal drug delivery systems or the depot sites to accommodate certain clinical needs.

Abstract: The present invention provides novel emulsion formulations which comprise oil bodies. The invention also provides a method for preparing the emulsions and the use of the emulsions in products for topical application to the skin. The products are very mild to the skin and may be easily formulated into a wide variety of personal care and dermatological products.

Abstract: A topical capsaicin preparation for the treatment of painful cutaneous disorders and neural dysfunction is disclosed. The preparation contains a nonionic, amphoteric or cationic surfactant in an amount effective to eliminate or substantially ameliorate burning pain caused by capsaicin.

Abstract: The present invention provides novel emulsion formulations which comprise oil bodies. The invention also provides a method for preparing the emulsions and the use of the emulsions in products for topical application to the skin. The products are very mild to the skin and may be easily formulated into a wide variety of personal care and dermatological products.

Abstract: A composition for topical application to an animal's skin for relief from a variety of symptoms caused by medical conditions or physical injuries. The composition includes at least one compound having analgesic activity, at least one compound having anti-inflammatory activity, at least one compound having antioxidant activity, at least one compound having anti-neuralgic activity, at least one compound having blood circulation promotion activity, and at least one compound having antidepressant activity. A method for relieving pain by topical application of the composition is also provided.

Abstract: A pharmaceutical composition is described. The composition comprises a formulation. The formulation comprises an NMDA antagonist and an alpha-2 adrenergic agonist. In a preferred aspect, there is provided an improved anaesthetic comprising an NMDA antagonist and an alpha-2 adrenergic agonist.

Abstract: A method of treating skin includes applying a topical composition to an affected area of skin, such as a burn, irritation, blister, rash or other similar skin condition. The topical composition has as the active ingredients an anesthetic and a surfactant. The anesthetic is preferably tetracaine in a concentration of from about 1% to 2% by weight and the surfactant is preferably sodium lauryl sulfate in a concentration of from about 0.5% to about 5.0% by weight.

Abstract: Melatonin (N-acetyl-5-methoxytryptamine), or its biologically active analogues, are used to induce anesthesia.

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: This invention relates to an apparatus and method of drug delivery on a human body surface. The formulation comprises a drug, a conversion agent capable of converting the formulation from a less solid phase to a coherent, soft, solid phase, and a vehicle medium or carrier for the drug and conversion agent. The drug formulation is applied to this human body surface in its less than solid phase and is subsequently converted to a soft solid phase while the drug is being delivered through the human body surface. After delivery of the drug is complete, the soft solid formulation can be removed or peeled from the body surface as a coherent solid formulation. The drug formulation provides control over drug delivery rates and allows the formulation to be removed without leaving a messy, residual formulation on the body surface.

Abstract: A formulation and methods for inducing sustained regional local anesthesia in a patient comprising a substrate comprising a local anesthetic and an effective amount of a biocompatible, biodegradable, controlled release material prolonging the release of the local anesthetic from the substrate to obtain a reversible local anesthesia when inplanted or injected in a patient, and a pharmaceutically acceptable, i.e., non-toxic, non-glucocorticoid augmenting agent effective to prolong the duration of the local anesthesia for a time period longer than that obtainable from the substrate without the augmenting agent.

Abstract: Compositions useful for long-lasting pain relief from mucosal damage, such as mucosal inflamation, abrasions, ulcerations, lesions, trauma and incisions, without significant systemic absorption. The compositions of the invention are particularly suitable for application to the mucous membrane of the nasal cavity and buccal cavity. To relieve pain, the compositions or the invention are topically applied directly to the affected area.

Abstract: Novel disulfide derivatives useful for preventing or treating allergic diseases of the eye, nose, skin, ear, gastrointestinal tract, airways or lung and preventing or treating manifestations of systemic mastocytosis are disclosed. The disulfide derivatives act as mast cell stabilizers.

Abstract: A cream carrier is provided which has use as a cream-type carrier for topical delivery of medicaments including analgesics. The carrier comprises a mixture of: squalane NF, an emulsifier such as Tween 80, glycerin, cetyl alcohol NF, glyceryl monostearate, lecithin organogel preserved, BHT, urea USP, EDTA, water, stearic acid, simethicone USP, and ethoxy diglycol reagent. The invention also comprises a combination of the carrier, with either or both of ketamine hydrochloride and amitriptyline hydrochloride, which has use as a topically applied analgesic.

Abstract: A local anesthetic for external use is prepared by blending a) an active ingredient selected from lidocaine, prilocaine, and pharmaceutically acceptable salts thereof; b) a percutaneous absorption accelerator, c) ethanol and/or isopropyl alcohol, and d) water, such that the blending ratio of ethanol and/or isopropyl alcohol to water is 0.5 to 1.2 by weight, and the pH is 6.0 to 8.5.

Abstract: Liposome-encapsulated opioid analgesic agents delivered by the pulmonary route provide local, or systemic analgesia superior to that produced by the solution form of these agents administered by parentral (intravenous, intramuscular, or subcutaneous injection) or oral routes.

Abstract: Sympathetically maintained pain is treated topically by administering to the site where sympathetically maintained pain is present an ?-1-adrenergic antagonist, ?-2-adrenergic agonist, or other drug that depletes or blocks synthesis of sympathetic norepinephrine, known collectively as sympatholytic agents. Chemical formulas for several sympatholytic agents are given.