The present invention provides peptidic TGF-β antagonists capable of inhibiting TGF-β signaling and disrupting the biochemical events that promote fibrosis and the epithelial-mesenchymal transition. The peptidic TGF-β antagonist may contain from 11 to 28 amino acid residues (for instance, may consist of from 12 to 16 amino acid residues) and may have the following structure (II):

NH.sub.2′ETWIWLDTNMG-Xaa.sub.1-Y′COON  (II)

wherein Xaa.sub.1 is any amino acid and Y is a peptide having from 0 to 9 amino acids.

The peptidic TGF-β antagonists can advantageously be used for the prevention, treatment, and/or alleviation of the symptoms of a condition associated with an increase in TGF-β activity, including fibrosis (such as fibrosis of the skin, liver, lungs, and heart, among others) and cancer (including various carcinomas, such as squamous cell carcinoma, sarcomas, and metastatic cancers).

A medicament characterized in that (A) a compound represented by the formula (I): ##STR00001##
its pharmaceutically acceptable salt, or a solvate thereof,
wherein P is hydrogen or a group to form a prodrug; A.sup.1 is CR.sup.1AR.sup.1B, S or O; A.sup.2 is CR.sup.2AR.sup.2B, S or O; A.sup.3 is CR.sup.3AR.sup.3B, S or O; A.sup.4 is each independently CR.sup.4AR.sup.4B, S or O; the number of hetero atoms among atoms constituting the ring which consists of A.sup.1, A.sup.2, A.sup.3, A.sup.4, nitrogen atom adjacent to A.sup.1 and carbon atom adjacent to A.sup.4 is 1 or 2; R.sup.1A and R.sup.1B are each independently hydrogen, halogen, alkyl or the like; R.sup.2A and R.sup.2B are each independently hydrogen, halogen, alkyl, or the like; R.sup.3A and R.sup.3B are each independently hydrogen, halogen, alkyl, or the like; R.sup.4A are each independently hydrogen, halogen, alkyl, or the like; R.sup.4B are each independently hydrogen, halogen, alkyl, or the like; R.sup.3A and R.sup.3B may be taken together with an adjacent carbon atom to form non-aromatic carbocycle or non-aromatic heterocycle; n is any integer of 1 to 2; and R.sup.1 is ##STR00002##
or the like,
is combined with (B) compound(s) having an anti-influenza activity, its pharmaceutically acceptable salt or a solvate thereof and/or an antibody having anti-influenza activity, is useful for treating or preventing influenza.

A method and a non-rate controlled, monolithic, subsaturated patch for transdermally administering fentanyl and analogs thereof, for analgetic purposes, to a subject through skin over an extended period of time are disclosed.

A method for producing a gel patch comprising an adhesive mass layer on a backing fabric, comprising a step of applying a composition comprising a physiologically active substance, a water-soluble polymer, glycerin, and water to the backing fabric to form the adhesive mass layer, wherein a loss tangent of the composition in dynamic viscoelasticity measurement at 1 Hz at a time of application to the backing fabric is 0.75 to 1.

A bioelectrode sheet (100) is configured to be affixed to the skin of a subject, a drug (104b) being mixed in an adhesive layer (104) provided at a peripheral position of a conductive gel layer (103) so as to avoid the conductive gel layer (103). The drug (104b) admixed with the adhesive layer (104) can thereby be caused to penetrate the body while biological information is acquired by an electrode (102) via the conductive gel layer (103).

This invention relates to crystalline salts of naloxone and of naltrexone and their use as opioid antagonists. The crystalline salts of the invention include naloxone saccharinate, naltrexone succinate and a methanol solvate of naltrexone succinate. A drug-in-adhesive transdermal patch containing the opioid analgesic fentanyl or an analog thereof and a crystalline salts of naloxone or naltrexone is disclosed. Also disclosed is a method of treating pain, such as acute, chronic or intermittent pain, by applying a drug-in-adhesive transdermal patch of the invention to the skin of a patient in need thereof.

[Problem]

If lidocaine is composed of non-aqueous patch, the adhesive power of the preparation tends to get lower, as the composition amount of lidocaine is higher. It is popular to solve lidocaine in dissolving agent in order to compose lidocaine in patch and release effective amount into skin. However, if the amount of dissolving agent gets higher, the adhesive power gets extremely lower, so that an long-time attachment is difficult.

[Solution]

A non-aqueous patch comprising lidocaine and/or its reactant, and a dissolving agent which are contained in a base of plaster, the plaster being hold by a support, of which strength of 50% stretched to longitudinal direction is less than 2,000 g/50 mm and of biaxially-oriented stretch cloth.

Carefully coordinated patches having camouflaging and/or benefit properties can be formed for application to a desired region of human skin. The patches include a flexible film having a first, adhesive, outwardly facing major surface and a second outwardly facing surface which is textured to correspond to skin covered by the patch during use; wherein the flexible film further comprises at least one pigmented region and at least one region adapted to modify one or more optical properties selected from the group consisting of light transmission, light reflection, and light absorption. Methods of custom use of such patches may include 3D printing processes.

A method for producing a gel patch comprising an adhesive mass layer on a backing fabric, comprising a step of applying a composition comprising a physiologically active substance, a water-soluble polymer, glycerin, and water to the backing fabric to form the adhesive mass layer, wherein a loss tangent of the composition in dynamic viscoelasticity measurement at 1 Hz at a time of application to the backing fabric is 0.75 to 1.

Transdermal delivery systems for the systemic delivery of memantine are described, wherein the system comprises a drug reservoir layer and an adhesive layer, optionally together with one or more intermediate and/or supporting layers, wherein the drug reservoir layer comprises an acrylate polymer or copolymer, a permeation enhancer, a carrier, and memantine base generated in situ by reaction of a memantine salt and an alkaline salt. Compositions and kits comprising the various components, e.g., drug reservoir and/or adhesive compositions are described. Methods relating to treatment of CNS disorders, e.g., Alzheimer's disease and/or dementia, using the aforementioned transdermal delivery devices and/or compositions are also described.