Abstract: A preparation for intermittently releasing an active agent which comprises a laminated combination of a release-controlling layer and a pharmaceutically active agent-containing layer wherein one or more of pharmaceutically active agent layers are incorporated into said release-controlling layer. The preparation in accordance with the present invention can intermittently control the release of the active agent to decrease a dosage time and is applicable to the mucous membrane or gingivae within the oral cavity.

Abstract: A delayed onset transdermal drug delivery device exhibiting a delay period of at least six hours comprising a laminated composite of (1) a top backing layer; (2) a pressure rupturable layer underlying (1); (3) a reservoir of a solution of drug in a liquid vehicle between (1) and (2); (4) a wick layer underlying (2) for dispersing the drug once (2) is ruptured; (5) a first adhesive layer underlying (4) that is permeable to the drug; (6) a microporous membrane underlying (5) which is itself impermeable to the drug and whose pores are substantially unfilled prior to application of the device to the skin; and (7) a second adhesive layer underlying (6) that is permeable to the drug but is immiscible in the polymer filling the pores of (6).

Abstract: A preparation obtained by coating granules containing both a basic medical agent hydrochloride (e.g. allotinolol hydrochloride) and a polyanion the particles of which are present in the form of a discontinuous layer, with a film containing a slightly water-soluble substance, can release said agent at a controlled rate without influenced by the physiological factors of the gastrointestinal tract of a patient when orally administered.

Abstract: A dosage form is disclosed that comprises means inside the dosage form for providing a substantially drug-free interval before the dosage form delivers a drug from inside the dosage form. The dosage form in an embodiment comprises a drug on the exterior of the dosage form, which drug is available for immediate delivery.

Abstract: A silicone pressure sensitive adhesive composition which is compatible with drugs, excipients, co-solvents and skin penetration enhancers is disclosed which includes a cohesive strengthening agent in combination with a silicone fluid and a silicate resin. The addition of the cohesive strengthening agent helps to maintain the adhesive on the substrate, while reducing cold flow. The adhesive is useful as an improved component in transdermal drug delivery devices and related medical devices.

Abstract: A novel transdermal delivery system for nicotine to satisfy addicted smokers' cravings therefore is comprised of a nicotine base, an acrylate polymer adhesive, a stabilizer and a polyester film backing. The nicotine is absorbed through the skin at sufficiently high levels to reduce or eliminate the desire to smoke, yet its concentration within the acrylate matrix is such that a laminar patch is constructed that is neither bulky nor obvious when worn. A method of manufacture of the transdermal system is also described.

Abstract: Pharmaceutical compositions and transdermal patches comprised of pentamidine and a penetration enhancing amount of a terpene selected from the group consisting of menthol, carvone, carveol, dihydrocarveol, dihydrocarvone, neomenthol, isopulegol, terpene-4-ol, menthone, pulegol, camphor, geraniol, .alpha.-terpineol, citral, linalol, carvacrol, thymol and anethole are disclosed for delivery of a therapeutically effective amount of pentamidine or its pharmaceutically acceptable salts.

Abstract: A non-absorbable and soluble gastrointestinal medicine provided for treating the two levels of the digestive tract, i.e. the stomach and the intestines. The medicine is presented in a gastroresistant oral pharmaceutical form associated with a non-enterically-coated oral pharmaceutical form.

Abstract: Skin permeation enhancer compositions are provided which increase the permeability of skin to transdermally administered pharmacologically active agents. The compositions contain a sorbitan ester in addition to the selected pharmacologically active agent, and may also contain a C.sub.1 -C.sub.4 aliphatic alcohol. Methods and transdermal drug delivery systems for using the compositions are also provided.

Abstract: The present invention relates to a composition of matter for the time-dependent liberation of therapeutic agents. This composition of matter comprises a polymeric slab and a homogeneously dispersed enzyme which degrades the polymeric slab in the presence of moisture. The therapeutic agent is physically entrapped in the polymeric slab by inclusion during polymerization to form the polymeric slab or by mixture of the therapeutic agent with a liquid form of the polymeric slab and conversion of the liquid to a solid form. The therapeutic agent is not chemically bound to the polymer, and thus release of the agent is immediately effected upon the specific moisture-activated enzymatic degradation of the polymer slab. Moisture for enzymatic activation is provided by the biological surface on which the slab is emplaced, such as the dermal surface. The composition comprises a polymer such as poly (DL-lactide) and an enzyme such as proteinase K together with chlorpheniramine maleate as the therapeutic agent.

Abstract: An antimicrobial wound dressing and method of wound treatment, the wound dressing having a layer of a collagen dressing material impregnated with lyophilized, stabilized chlorine-containing compounds which generate on activation chlorine dioxide, like a mixture of sodium chlorate and sodium chlorite, and an adjacent layer secured thereto containing a dry, activating amount of an acidic compound, such as citric acid, whereby moisture from the wound activates the dry chlorine moiety to treat the wound.

Abstract: A controlled release treatment composition method of use are disclosed. The composition includes a bioadhesive and an effective amount of a treating agent. The bioadhesive is a water-swellable, but water-insoluble, fibrous, cross-linked carboxy-functional polymer containing (a) a plurality of repeating units of which at least about 80 percent contain at least one carboxyl functionality, and (b) about 0.05 to about 1.5 percent cross-linking agent substantially free from polyalkenyl polyether.

Abstract: Method and laminated composite for administering short or intermediate half-life benzodiazepines such as alprazolamine or triazolam transdermally to treat conditions such as anxiety in the case of alprazolam and insomnia in the case of triazolam. The composite comprises an impermeable backing layer and a reservoir layer containing the benzodiazepine and a permeation enhancer combined with a solvent-based acrylic polymer adhesive with the amounts of benzodiazepine and enhancer being sufficient to cause the benzodiazepine to pass through the skin at a rate in excess of about one .mu.g/cm.sup.2 /hr.

Abstract: A poorly soluble medicament is incorporated into particles of a crosslinked polymer which is swellable in water but insoluble in water, and the product obtained is brought into contact with a solvent able to swell the polymer. The product obtained by this treatment, and after being dried under vacuum, has a medicament dissolving rate which is considerably higher than that of the pure medicament.

Abstract: A pressure-sensitive adhesive sheet material for delivering estradiol to skin, the sheet material comprising a backing with a layer of a pressure-sensitive adhesive adjacent thereto, said pressure-sensitive adhesive layer comprising a pressure-sensitive adhesive polymer, two or more skin penetration-enhancing ingredients and estradiol. The sheet material is useful for systemic treatment of conditions associated with estradiol deficiency. Methods of using such adhesive sheet material are also described.

Abstract: A system for transdermally delivering a hydrophobic alkanol soluble active agent to the skin at a constant rate utilizing a lower alkanol penetration enhancer. The system comprises an overlying solvent reservoir containing a lower alkanol solvent and a drug compartment containing an active agent in aqueous alkanol. A one-way membrane is sandwiched between and divides the solvent reservoir from the drum compartment. The one-way membrane is permeable to the alkanol solvent and substantially impermeable to back flux of drug and water into the reservoir. An outer membrane permeable to the alkanol solvent and drug is attached to the outer surface of the drug compartment. Adhesive means is contained on the outer surface of this membrane for attaching the delivery system to the skin of a wearer. Alkanol from the reservoir permeates into the drug compartment and drug and alkanol pass through the outer membrane to the skin of the wearer for transdermal absorption.

Abstract: A dosage form is disclosed comprising an anti-Parkinson's disease drug for administering to a patient in need of anti-Parkinson's disease therapy.

Abstract: A controlled release delivery device for macromolecular proteins which comprises a water-soluble outer capsule completely surrounding an inner compartment containing a plurality of non-uniform beadlets. The beadlets comprise a rupturable wax shell which completely surrounds a core matrix containing the macromolecular proteins and optional "core agents" such as excipients, stabilizers, binders, surfactants, preservatives, or mixtures thereof, and the like.The water-soluble outer capsule dissolves when the device is administered to an animal and simultaneously exposes substantially all of the beadlets to an aqueous environment. Each beadlet absorbs fluid from the environment and separately ruptures over a prolonged period thus delivering the macromolecular protein to the animal.

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: The present invention relates to a therapeutic system for the retarded and controlled transdermal and transmucous administration of active substances via an impermeable backing layer, an active substance containing reservoir, a substantially drug-free but drug-permeable layer, and a removable protective layer, whereby the drug-free layer is brought into contact with the active substance reservoir only immediately prior or after application and then lies between reservoir and application surface, whereby at least a portion of the active substance diffusing from the reservoir is converted in the retardation layer into a non-bioavailable form. In this connection, the conversion into the non-bioavailable form may be carried out either by immobilization of the active substance, by chemical reactions, or by physical interactions.