Abstract: A novel granular drug delivery system having a gel-forming dietary fiber that can be made into a an orally-ingestible dispersion by admixture with a liquid that can deliver an effective dose of a pharmaceutically-active compound. The granular drug delivery system comprises granules consisting essentially of a pharmaceutically active compound, and a gel-forming dietary fiber, the granules being coated with at least one of the following: a gel-forming dietary fiber, a starch or a protein. The composition may further include a mineral salt that releases a physiologically-acceptable gas upon ingestion. The composition of the granular drug delivery system will deliver microgram quantities of a pharmaceutically-active compound in an orally-ingestible dispersion without forming a thick gel and without forming "hot" and "cold" spots of the pharmaceutically-active compound.

Abstract: This invention relates to a transdermal preparation comprising a therapeutically active compound of the formula: ##STR1## where R.sub.1, R.sub.2, and R.sub.3, which can be the same or different are H, CH.sub.3, C.sub.2 H.sub.5 or Cl; X is CH.dbd.CH or (CH.sub.2).sub.n where n is 1 to 3 or X is --C(OR.sub.5)H-- where R.sub.5 is methyl or ethyl; and R.sub.4 is hydrogen or a straight alkyl of 1 to 4 carbon atoms. The transdermal administration of the compounds can be accomplished by preparations in the form of ointments, emulsions, lotions, solutions, creams or transdermal patches.

Abstract: Rate controlled transdermal delivery devices are disclosed which utilize an in-line adhesive to maintain the device on the skin and deliver an agent which is a solvent or a plasticizer for the in-line adhesive. The initial equilibrated concentration of the agent in the agent reservoir and the adhesive is below saturation, and the reservoir comprises the agent dissolved in a solvent with respect to which the rate controlling element of the device is substantially impermeable. In preferred embodiments the initial loading of the agent in reservoir is sufficient to prevent the activity of the agent in the reservoir from decreasing by more than about 50% and preferably no more than about 25% during the predetermined period of administration: and the thicknesses of the adhesive, rate controlling membrane and reservoir layers are selected so that at least 50% and preferably at least 75% initial equilibrated agent loading is in the reservoir layer.

Abstract: A fluid-activated delivery device is disclosed comprising a housing defining an internal compartment, a beneficial agent formulation in the compartment, exit means in the housing for delivering the beneficial agent formulation from the delivery device, and wherein the formulation comprises an active agent in an amount of 50 wt % or greater blended with a glyceride or a mixture of glycerides of a fatty acid.

Abstract: A substance transfer device for topical or transdermal drug delivery to a living body or collection of fluids from a living body, comprises a layer of skin or wound surface compatible adhesive having a surface for contacting the body, and channels therethrough which provide liquid communication with depots of drug or collection means. These channels form discrete, exposed areas of drug composition or drug delivery means, surrounded by the adhesive. The drug contained in the device does not need to pass through the layer of adhesive before contacting the underlying skin. In one arrangement, particularly suitable for delivery of macromolecular drugs, the channels extend through the entire thickness of the adhesive layer, and communicate with reservoirs of drug.

Abstract: The invention relates to a patch for transdermal administration of volatile pharmaceutically active ingredients of chemically basic nature which comprises a multi-element system comprising(a) a matrix having distributed therein as the drug said volatile active ingredient or a physiologically acceptable salt thereof, the matrix comprising a pressure-sensitive adhesive,(b) an element of a pressure-sensitive adhesive composition which--where (a) contains a salt--contains basic groups to liberate the free base from its salt,(c) a backing layer impermeable to the diffusable ingredients of (a) and (b), and(d) a release liner impermeable to the diffusable ingredients of (a) and (b),matrix (a) or at least a part of (b), whichever is in contact with release liner (d), having a tack sufficient for affixing the patch to the skin, any part of (b) positioned between matrix (a) and release liner (d) being permeable for the deprenyl or the salt thereof or both.

Abstract: The invention relates to an improved transdermal administration of pharmacologically active compounds.

Abstract: An efficient transdermal delivery system for delivering an active ingredient to the blood supply of a living body, comprising a vasodilator and/or topical counter irritant, an active ingredient, a permeation enhancer for the active ingredient, and a water soluble gum for binding the foregoing. A non-breathable layer also can be used for controlling the microenvironment at the transport site. Compression can be used to further enhance the blood supply at the transport site.

Abstract: A method of providing testosterone replacement therapy to a woman in need of such therapy comprising applying a testosterone-delivering patch to the skin of said woman which patch transdermally delivers 50 to 500 .mu.g/day of testosterone to the woman.

Abstract: A tamper-resistant dosage form capsule for the oral administration of therapeutic agents comprises a two-part capsule which is shrunk around a caplet so that the outer wall of the caplet is bound to the inner walls of both parts of the capsule. The caplet is placed into the capsule, and the dosage form is then subjected to relatively high humidity and temperature conditions, followed by drying the dosage form in a lower humidity environment, so that the capsule is shrunk to conform to the contours of the caplet and both parts of the capsule are bonded to the caplet.

Abstract: Provided are enhancing transdermal absorption compositions useful in transdermal absorption of progestins including progesterone and optionally an estrogen for contraceptive or hormone replacement and dosage forms using the novel enhancing compositions. The enhancing compositions comprise a combination of a lower alkyl ester of a polycarboxylic acid, an aliphatic monohydroxy alcohol and an aliphatic diol. Also provided are processes of administration of progestins and optionally estrogens using the novel dosage forms.

Abstract: The present invention is directed to the transdermal administration of methyl nicotinate and an irritating or sensitizing drug. The invention includes a transdermal drug delivery device comprising a matrix adapted to be placed in irritating/sensitizing drug- and methyl nicotinate-transmitting relation with the skin site. The matrix contains sufficient amounts of irritating/sensitizing drug and of methyl nicotinate, in combination, to continuously administer to the skin for a predetermined period of time the drug to provide an effective therapeutic result. The invention is also directed to a method for either 1) preventing or reducing the irritation caused by an irritating drug or 2) preventing or reducing sensitization from occurring, as well as reducing or eliminating pain and discomfort occurring during the elicitation phase after sensitization has already been induced.

Abstract: A prolonged-release unit dosage formulation or pharmaceutical composition, preferably in tablet form, is described. The composition consists essentially of a gel-forming fiber, preferably hydrocolloid-coated, a biologically-absorbable drug or other active therapeutic agent which is also preferably hydrocolloid-coated, a mineral salt which releases a physiologically-acceptable gas upon ingestion, preferably carbon dioxide, e.g., a mineral carbonate or bicarbonate, and optionally an organic or phosphoric acid and a dextrose or like soluble sugar. The fiber-containing composition, when in the form of a tablet or other unit dosage form together with the drug or agent and the stated disintegrants, provides a unique, efficient and controllable prolonged-action drug-delivery system.

Abstract: A sustained release suppository comprising in a usual suppository basea) a water-soluble therapeutically active substance, the average particle size of which is smaller than 20 .mu.m,b) a physiologically acceptable organic substance which is swellable in contact with water, andc) hydrophobic silicium dioxide.The suppository base is usually a fat having a melting range of from 29.degree. to 38.degree. C. As ingredient b) cellulose derivatives such as hydroxypropylmethylcellulose may be used, in a quantity of from 5 to 40% by weight, preferably 9 to 15% by weight. Ingredient c) is preferably used in a quantity of from 3 to 6% by weight. Also a process for manufacturing the suppositories is described.

Abstract: The present invention is concerned with improving the delivery of a drug from a ruminal delivery device to give a consistent delivery of drug to the ruminal environment. Thus, the invention is directed to an improved ruminal drug delivery device comprising a semipermeable membrane having an exit orifice and defining a compartment, the compartment containing a swellable osmotic agent expandable member, a drug to be dispensed, a density element and, optionally, a partition layer between the osmotic expandable member and the drug formulation, wherein the improvement comprises an essentially gas-impermeable barrier means that separates the density element from the other components within the delivery device for isolating gases evolved from the density element from the other components within the delivery device. The invention is also directed to methods and articles for providing a consistent delivery of drug from a ruminal drug delivery device.

Abstract: An oral medication delivery system and method for pharmaceutically active agents having local and/or systemic effect is provided. The system provides three embodiments of containers in which medication is stably stored, either in liquid suspension or in dry powder form with a delivery liquid, until dispensed for use by a patient. The medication is mixed as required and frozen in the storage container until hard, when it is administered to the patient in the form of a frozen popsicle. One embodiment of the system includes a flexible plastic container which contains the pharmaceutically active agent mixed with a delivery liquid. In other embodiments the medication in powder form and a delivery liquid are stored in a chambered container separated by a rupturable membrane which is ruptured to mix the container contents prior to freezing.

Abstract: A controlled sustained release tablet having at least one year shelf life and containing bupropion hydrochloride, hydroxypropyl methylcellulose and cysteine hydrochloride or glycine hydrochloride with the tablet having a surface area to volume ratio to effectively control bupropion hydrochloride release in the body.

Abstract: Novel ingestible polymeric phosphonium salts have the formula: ##STR1## wherein P' represents a cross-linked and non-digestible polymer backbone; R is a lower alkyl radical; X.sup.- is a pharmaceutically acceptable anion; n, n.sub.1 and n.sub.2 are, independently, integers varying from 0 to 6 inclusive, with the proviso that when m.sub.1 .gtoreq.1, n.sub.2 .gtoreq.1; and o.sub.1, o.sub.2, p.sub.1 p.sub.2, q.sub.1 and q.sub.2 are, independently, integers varying from 1 to 6 inclusive. The polymeric phosphonium salts of the invention are highly efficient sorbents for bile acids and salts and can thus be used for reducing hypercholesterolemia in affected humans.

Abstract: A delivery system for providing growth promoters to food animals is provided and a method of promoting growth in food animals using such delivery systems is described.

Abstract: The present invention relates to novel, quick drying nail enamel compositions which dry in a period of time no greater than three minutes. The compositions of the present invention preferably dry in a period no greater than about two minutes and most preferably dry in a period no greater than about 90 seconds. Compositions drying in a period less than 60 seconds are especially preferred and are also described. The compositions of the present invention have acceptable static viscosities ranging from about 400 to about 1200 centipoises and may accommodate numerous pigments to produce nail enamel compositions exhibiting favorable characteristics, including acceptable durability and gloss.