Abstract: An oral pharmaceutical composition comprises a core containing a drug, a first inner layer coating on the core which contains a drug, and a second inner layer coating on the first inner layer coating which also contains drug. This oral pharmaceutical composition is used especially for treating intestinal diseases.

Abstract: A confectionery compressed tablet designed to dissolve in the oral cavity and containing a flavor ingredient intimately bound with a bioadhesive is disclosed. The flavor and bioadhesive composition provide a unique mouthfeel so that as the confection dissolves in the oral cavity, a coating of flavor adheres to the moist areas of the oral cavity. There is also provided a confectionery compressed tablet characterized by a single product body with discrete phases contained therein which act to provide timed release of at least one flavor ingredient sequentially. A flavor and bioadhesive mixture can be prepared with a hydrophilic delivery system providing rapid initial delivery of the flavor and unique mouthfeel or as a part of a hydrophobic delivery system providing extended periods of flavor delivery and unique mouthfeel. There is also provided a process for preparing confectionery compressed tablets containing the unique flavor delivery system and mouthfeel.

Abstract: A pulsating release composition comprising natural microspheres, such as pollen grains or spores, into which are loaded a biologically active is subsequently releasable therefrom in a predetermined location in or on a plant or animal in a series (generally 3 or more) of pulses. In one preferred embodiment, the composition comprises a group of substantially similar loaded micropheres coated with multiple barrier layers alternating with multiple active substance layers in a concentric onion-like structure, the barrier layers being slowly soluble to delay release of active substance from the underlying layer thereof until after the pulse of active substance provided by the overlying layer has subsided.

Abstract: A dosage form is disclosed comprising means for delaying the delivery of drug from the dosage form following the administration of the dosage form to a patient in need of drug therapy.

Abstract: An osmotic device (10) for delivering a beneficial drug, such as an anti-fungal, into the mouth of a human patient is disclosed. The device (10) has a size and shape adapting it to be comfortably retained in the mouth for extended periods of time. The device (10) comprises a wall (12) surrounding a compartment (13) housing a layer of an agent (14) that is insoluble to very soluble in aqueous biological fluids, e.g., saliva, and a layer (16) of a fluid swellable, hydrophilic polymer. A passageway (17) in the wall (12) connects the agent (14) with the exterior of the device (10). The wall (12) is permeable to the passage of aqueous biological fluid but substantially impermeable to the passage of the hydrophilic polymer (16). In one embodiment the beneficial agent (14) has a different color than the hydrophilic polymer (16). The wall (12) is sufficiently translucent to permit the patient to see the amount of drug/beneficial agent (14) remaining to be delivered.

Abstract: A sustained release diltiazem formulation for oral administration comprising a pellet having a central sugar sphere a plurality of alternating first and second layers surrounding the sphere to form a core, the first layer comprising a water soluble pharmaceutically acceptable polymeric material and the second layer comprising diltiazem or a pharmaceutically acceptable salt thereof and an outer membrane surrounding the plurality of layers. The outer membrane comprises first inner membrane layers of ethylcellulose. The outer membrane also comprises an outer membrane coating of a water insoluble pharmaceutically acceptable polymeric material, a plasticizer and a lubricant, in from one to five or more layers.

Abstract: A dosage form is disclosed comprising means for delaying the delivery of drug from the dosage form following the administration of the dosage form to a patient in need of drug therapy.

Abstract: A slow-release pharmaceutical agent which comprises fumaric acid and/or DL-tryptophan in addition to one or more pharmaceutically active substances, and a process for preparation of the same are disclosed. Among many organic acids and amino acids, fumaric acid and DL-tryptophan are remarkably useful for extending the duration of release of a pharmacologically active substance when fumaric acid, DL-tryptophan or both is used for formulation of a pharmaceutical agent. The pharmaceutical agent may be in any solid form of formulations such as powder, granule, tablet, troche, capsule, suppository, etc., and may be used with practically all types of drugs.

Abstract: A dosage form is provided for administering a drug of the formula ##STR1## to a patient to produce an anxiolytic benefit in the patient.

Abstract: A drug delivery device is disclosed for delivering a drug to the intestine and the colon. The device comprises external means for delaying the delivery of drug in the stomach, and hydrophobic means for preventing the passage of fluid through the delay means.

Abstract: Orally administrable pharmaceutical preparation containing an active ingredient to be released in the lower part of the gastrointestinal tract, i.e. in the large intestine, and especially colon, consisting of a core containing a therapeutically active substance and coated with three protection layers at different solubility. The manufacturing and the use of these preparations are also described.

Abstract: A formulation comprising captopril within an enteric or delayed release coated pH stable core combined with additional captopril that is available for immediate release following administration.

Abstract: A dosage form comprising (1) an immediately available dose of a beneficial drug followed by a timed delayed dose of drug, or (2) a timed delayed dose of drug.

Abstract: An osmotic device is disclosed comprising an exterior coat comprising an estrogenic and a progestogenic steroid that are delivered immediately as a contraceptive pair for fertility regulation in a female, and a compartment comprising an estrogenic steroid that is delivered at a controlled rate over a prolonged period of time for fertility regulation in a female.

Abstract: A process for spray-coating tablets and the like utilizing only an acrylate enteric polymer and plasticizer in water is disclosed. The process can be practiced on a commercial scale and requires no antiadherent in the coating formulation. The process comprises providing inlet air having a dew point below about 10.degree. C. and a temperature between 35.degree. and 60.degree. C.

Abstract: The present invention provides a dual-action tablet composition comprising:(a) an outer tablet comprising a first dose of active ingredient dispersed in a pH independent hydrophilic polymer matrix; and(b) an inner tablet comprising a second dose of active ingredient in a rapidly disintegrating excipient base.This dual-action tablet is especially efficacious for those active ingredients which have half lives of less than two hours and which experience decreased absorption efficiency in the lower gastrointestinal tract. Among the preferred dual-action tablet compositions is one wherein the active ingredient in both the inner and outer tablets is guaifenesin. Upon administration, the outer tablet provides a controlled release of the active ingredient while the inner tablet gives a second dose of active ingredient after the outer tablet has partially dissolved.

Abstract: A method for disinfecting a contact lens comprises immersing the lens in an aqueous solution of H.sub.2 O.sub.2 having a pH of 4 or below and adding to the solution a neutralizing agent comprising a catalyst for decomposing any residual H.sub.2 O.sub.2 and a retarding agent for delaying the decomposition of the H.sub.2 O.sub.2 for a predetermined time in order to permit sterilization of the lens to be substantially complete. The retarding agent preferably comprises either a polymeric coating which dissolves gradually in the H.sub.2 O.sub.2 solution or a semipermeable membrane enveloping the catalyst. The neutralizing agent preferably also contains an auxiliary material which raises the pH of the acidic H.sub.2 O.sub.2 solution. The enzymatic decomposing agent can be embedded in a particulate carrier substance forming the bottom part of a two part container, the upper part of which contains an aqueous solution of H.sub.2 O.sub.

Abstract: The present invention is directed to a multi-layered tablet containing an ibuprofen layer, a piperidino-alkanol antihistamine layer, and a layer or layers containing conventional pharmaceutical excipients which is interspersed between the ibuprofen and piperidino-alkanol layer and serves to physically separate them. This tablet solves the problems associated with the physical and chemical incompatibilities between ibuprofen and the piperidinoalkanol antihistamines.

Abstract: A dosage form comprising (1) an immediately available dose of a beneficial drug followed by a timed delayed dose of drug, or (2) a timed delayed dose of drug.

Abstract: A solid medicament preparation having long-lasting action containing a sparingly soluble dihydropyridine active compound of the Formula (I) ##STR1## the preparation having a core-coating construction, the core containing at least one of the above mentioned dihydropyridines in slow-release form, the inner-most coating situated around the core contains no active compound and only dissolves slowly and adjacent to the inner-most coating a rapid release initial dose of the active compound mixed with a polymer.

Abstract: A process for preparing a controlled release medicine containing fenofibrate in an intermediate layer in the form of cyrstalline microparticles included within pores of an inert matrix prepared by a process involving the sequential steps of dampening said inert core with a solution based on said biner, then projecting said fenofibrate microparticles in a single layer onto said dampened core, and thereafter drying before said solution based on said binder dissolves said fenofibrate microparticles and repeating said three steps in sequence until said intermediate layer is formed.

Abstract: A dosage form comprising (1) an immediately available dose of a beneficial drug followed by a timed delayed dose of drug, or (2) a timed delayed dose of drug.

Abstract: The present invention relates to a bioactive composition having a controlled, sustained release delivery pattern when contacted with a suitable surrounding media. The composition comprises a pharmaceutically, insecticidally, herbicidally or fertilizing bioactive material core, soluble in a given surrounding media, the core present in an amount at least sufficient for a total dosage during a specified treatment period; a first coating enveloping the bioactive material core comprising a polymer or a blend of polymers, said polymer or blend of polymers being swellable upon penetration by the surrounding media; and a second coating enveloping the first coating, the second coating comprising a polymer or a blend of polymers being water-insoluble and forming a semi-permeable barrier to the inward diffusion of the surrounding media and the outward diffusion of the bioactive material dissolved in the surrounding media.

Abstract: A tablet for pharmaceutical use able to release active substances at successive times, comprising at least; a first layer containing a portion of the active substance with suitable excipients, a barrier layer of polymer material gellable and/or soluble in water and/or aqueous liquids, which is interposed between said first layer and a third layer containing the remaining portion of active substance with suitable excipients, said barrier layer and said third layer being housed in a casing consisting of polymer material impermeable and insoluble in water or soluble in an alkaline environment.That part of the active substance not inserted in the casing is immediately available for dissolving, whereas the part inserted in the casing is available only after dissolution or rupture of the barrier layer and/or after solubilization of the casing.

Abstract: Isolated chlorogenic acid or the physiologically acceptable derivatives thereof when used before or simultaneously with the administration of gastric acid secretion-stimulating and/or gastric mucosa-irritating or attacking foods, beverages and/or medicaments lead to a reduction of gastric acid secretion and/or to the protection of the gastric mucosa.

Abstract: A controlled absorption verapamil containing pellet formulation for oral adminstration comprises a core of a powder mixture containing verapamil or a pharmaceutically acceptable salt thereof and an organic acid and a polymeric material, said core comprising layers of said powder mixture and said polymeric material superimposed one upon the other and said polymeric material being present in an amount effective to ensure that all of said powder mixture is coated into said core and a multi-layer membrane surrounding said core, the number of layers in said membrane and the ratio of the various polymers comprising the membrane being effective to permit release of the verapamil from the pellet at a rate allowing controlled absorption thereof over a 24 hour period following oral administration, said rate being measured in vivo and having a Tmax between 6 and 16 hours.

Abstract: An osmotic dosage form is disclosed for delivering chlorpheniramine.

Abstract: A dosage form comprising (1) an immediately available dose of a beneficial drug followed by a timed delayed dose of drug, or (2) a timed delayed dose of drug.

Abstract: Sustained-release formulations which can release a water-soluble active ingredient or ingredients at the zero-order over a long period of time, comprising:a. an inert core,b. a powder-coating layer containing a water-soluble active ingredient or ingredients,c. a powder-coating layer of practically water-repellent material, andd. a film-coating layer composed of practically pH-independent and water-insoluble film-coating material.

Abstract: The discovery presented herewith concerns a pharmaceutical product in the form of a pellet with improved continous, delayed medicament substance emission through a coating, which is made of a material that does not dilute in gastric and intestinal juices and which is impermeable for gastric and intestinal juices and which tightly seals the core made of material that is dilutable in gastric and intestinal juices.

Abstract: An enteric coated tablet and process is described in which a core tablet of a pharmaceutically active ingredient is provided with an enteric coating layer of a film forming enteric polymer and an overcoat layer of non-enteric film forming polymer; optionally, the tablet may also be provided with the non-enteric undercoat layer of a film forming polymer.

Abstract: A spherical pellet like composition of nicardipine composed of small granular nuclei such as sugar particles coated with amorphous nicardipine or a salt thereof, a pH-dependent additive and a surface active agent. The spherical pellet like composition of nicardipine may have a further coating of a medicament permeating material as an outermost coating. The spherical pellet like composition may be mixed with the spherical pellet like composition coated with the medicament permeating material.

Abstract: A controlled release pharmaceutical formulation which undergoes substantially or approaches zero order release of active drug is provided, preferably in the form of a coated tablet, containing a core portion from which medicament, such as procainamide hydrochloride, is slowly released over a controlled length of time. The core also includes one or more primary hydrocolloid gelling agents which is a hydropropylmethyl cellulose having a viscosity of within the range of from about 1,000 to about 6,000 centipoises in 2% solution at 20.degree. C., and a methoxyl content of 28-30%, optionally a secondary hydrocarbon gelling agent, such as hydroxypropyl cellulose and/or methyl cellulose, one or more non-swellable binders and/or wax binders (where the medicament and/or hydrocolloid gelling agents are non-compressible), one or more inert fillers or excipients, one or more lubricants, and optionally one or more anti-adherents such as silicon dioxide and water.

Abstract: A multi vitamin and mineral dietary supplement composition for oral administration containing, per unit dose,(a) one or more divalent dietary mineral components selected from the group consisting of bioavailable calcium and magnesium, and in the further presence or absence of one or more additional non-ferrous mineral and vitamin components, adapted to be released in the upper gastrointestinal tract, and(b) a bioavailable iron component, present in controlled release form, so adapted so as to be subsequently released in a controlled manner lower in the gastrointestinal tract, and a method of preventing or treating iron deficiency using such compositions.