Abstract: An oral pharmaceutical dosage form comprising an acid susceptible proton pump inhibitor and one or more antibacterial compounds in a fixed formulation. The fixed formulation is intended for oral use and in the form of an enteric coating layered tablet, an capsule or a multiple unit tableted dosage form. The multiple unit dosage form is most preferred. The new fixed formulation is especially useful in the treatment of disorders associated with Helicobacter infections.

Abstract: An oral pharmaceutical dosage form comprising a proton pump inhibitor and one or more prokinetic agents in a fixed formulation, wherein the proton pump inhibitor is protected by an enteric coating layer. The fixed formulation is in the form of multilayered tablets, capsules or multiple unit tableted dosage forms. The multiple unit dosage forms are most preferred. The new fixed formulation is especially useful in the treatment of disorders associated with gastro oesophageal reflux diseases.

Abstract: The present invention is directed to an active agent dosage form which is adapted for retention in the stomach and useful for the prolonged delivery of an active agent formulation to a fluid environment of use. The active agent dosage form is a polymer matrix that swells upon contact with the fluids of the stomach. A portion of the polymer matrix is surrounded by a band of insoluble material that prevents the covered portion of the polymer matrix from swelling and provides a segment of the dosage form that is of sufficient rigidity to withstand the contractions of the stomach and delay expulsion of the dosage form from the stomach until substantially all of the active agent has been dispensed.

Abstract: The method of making a solid drug with controlled effective ingredient delivery for oral administration includes selecting a predetermined number of at least three of four compressed compositions containing an effective ingredient or effective ingredient combination defined by their release profile of effective ingredient and/or effective ingredient combination. The solid drug or medicinal preparation is formed according to known methods requiring only comparatively small apparatus expense and minimal time. Perorally administered solid drugs are made by this process which can provide widely varying pharmaceutically-required release profiles of effective ingredients or effective ingredient combinations, for example delayed release, uniformly maintained release or pulsatile release adjusted to fit a special rhythm.

Abstract: A solid composition is disclosed comprising an active ingredient that is not in amorphous form in association with polyethylene oxide and conventional additives, excluding basic compounds. Such compositions are suitable for use as pharmaceutical compositions. A method for their preparation is also disclosed.

Abstract: The thermoforming of compositions containing active agents is carried out by processing compositions containing certain fatty esters in combination.

Abstract: A tablet for the controlled release of an active pharmaceutical ingredient. The tablet comprises a core having a donut-like configuration with a cylindrical hole extending through the center of the core. The core of the body comprises at least one active pharmaceutical agent and at least one hydrophilic, water-soluble, polymeric carrier. The core is coated with a hydrophobic, water-insoluble material covering all of the core except that which is defined by the cylindrical hole. Also included is a method of preparing a tablet for the controlled release of an active ingredient. The method comprises the steps of blending an active pharmaceutical ingredient, a water-soluble hydrophilic, polymeric carrier, and optionally an excipient, to form a mix; compressing the mix; punching a tablet from the mix; coating the tablet in a water insoluble, hydrophobic coating, then drilling a hole through the coated tablet.

Abstract: A process for preparing a controlled release composition with a controlled release matrix and containing a pharmaceutically active ingredient, which comprises granulating the active ingredient with a molten matrix material or with a matrix material while it is being melted and with optional additional inactive materials at a first elevated temperature, then cooling and screening the granulate, forming a fluidized bed of the resulting material at a second elevated temperature, and recovering the resulting product; and the product formed by the process.

Abstract: The invention provides a delayed-pulse controlled release pharmaceutical tablet having:(a) from 20 to 60 wt. % of a low molecular weight hydroxypropyl cellulose having a number average molecular weight of 70,000 to 90,000;(b) from 4 to 10 wt. % of a high molecular weight hydroxypropyl cellulose having a number average molecular weight of 1,100,000 to 1,200,000;(c) a pharmacologically acceptable amount of a medicament; and(d) an inert solid diluent.

Abstract: A controlled release antihyperglycemic tablet that does not contain an expanding polymer and comprising a core containing the antihyperglycemic drug, a semipermeable membrane coating the core and at least one passageway in the membrane.

Abstract: The invention disclosed pertains to a dosage form comprising an agent formulation comprising drug and pharmaceutical carrier of cooperating particle size and means for dispensing the agent formulation from the dosage form.

Abstract: Sustained release dosage forms of high dose insoluble drugs such as ibuprofen and methods for their manufacture are disclosed.

Abstract: Depot drug formulations include the pharmaceutical itself and a three component release rate controlling matrix composition. The three components of the matrix composition are (1) a pH dependent gelling polymer such as an alginate component, (2) an enteric polymer component, such as Eudragit.RTM. L or S, and (3) a pH independent gelling polymer, such as hydroxy propyl methyl cellulose or polyethylene oxide. The drug release rate can be adjusted by changing the amount of one or more of these components of the composition.

Abstract: A layered tablet for the controlled release of active substances in a liquid medium comprising at least one active substance-containing, layered matrix with contact surfaces to the liquid medium which are at least partially provided with a cover layer delaying or preventing the active substance release, is characterized by the fact that the cover layer is at least one additional layer lying with thickness gradients on contact surfaces of the layered, prefabricated matrix, or that the matrix is at least one additional layer lying with thickness gradients on contact surfaces of the layered, prefabricated cover layer, which additional layer is applied by pressing powdery or granular material on the layered, prefabricated matrix or on the layered, prefabricated cover layer.

Abstract: An orally administered antihyperlipidemia composition according to the present invention includes from about 250 to about 3000 parts by weight of nicotinic acid, and from about 5 to about 50 parts by weight of hydroxypropyl methylcellulose. Also, a method of treating hyperlipidemia in a hyperlipidemic having a substantially periodic physiological loss of consciousness, includes the steps of forming a composition having an effective antihyperlipidemic amount of nicotinic acid and a time release sustaining amount of a swelling agent. The method also includes the step of orally administering the composition to the hyperlipidemic once per day "nocturnally", that is in the evening or at night.

Abstract: This invention comprises a non-vasoactive, supra-vasoactive syndrome ("SVS") minimized dosage form for treatment of migraine in a human comprising (i) rapid availability metoclopramide in at least about an effective local gastrointestinal amount; (ii) at least one long acting NSAID such as naproxen sodium in a therapeutically effective amount; (iii) wherein said dosage form is a coordinated dosage form; and, (iv) wherein the dosage form is absent 5HT agonist vasoactive agents, and preparation thereof. Acid-base stable dosage forms are noted. This invention further comprises methods of migraine treatment, and methods for rapid introduction of oral NSAID into the small bowel.

Abstract: A pharmaceutical composition in the form of a tablet or a capsule for the controlled release of diltiazem, comprises about 30 to about 97% by weight of a hydrophilic polymer, about 0.5 to about 30% by weight of an enteric (pH-dependent) polymer, and about 2.5 to about 60% by weight of diltiazem or a pharmaceutically acceptable salt or ester thereof. The ratio of hydrophilic polymer to enteric polymer is in the range of about 1:1 to about 15:1. Such a pharmaceutical composition releases diltiazem at a rate that allows effective plasma levels of diltiazem to be maintained over a period of twenty-four hours after administration to human adult subjects.

Abstract: The invention provides an immediate-release fenofibrate composition comprising (a) an inert hydrosoluble carrier covered with at least one layer containing fenofibrate in a micronized form having a size less than 20 .mu.m, a hydrophilic polymer and, optionally, a surfactant, the polymer making up at least 20% by weight of (a); and (b) optionally one or several outer phase(s) or layers(s). The invention also provides a method for preparing said composition.

Abstract: A peroral depot medicament with controlled active substance release is composed of a gelatine matrix that continuously dissolves in an aqueous medium above 37.degree. C., and a medicament distributed therein. The release of the medicament, that may be easily or scarcely soluble, lipophilic or hydrophilic, is variable in time and may be adjusted according to the medicament.

Abstract: A process for the manufacture of particles comprises mechanically working a mixture of a drug and a hydrophobic and/or hydrophilic fusible carrier in a high speed mixture so as to form agglomerates, breaking the agglomerates to give controlled release particles and optionally continuing the mechanical working with the optional addition of a low percentage of the carrier or diluent.

Abstract: An oral morphine multiparticulate formulation for once-daily administration to a patient, comprising sustained release particles each having a core containing water soluble morphine and an osmotic agent, the core being coated with a rate-controlling polymer coat comprised of ammonio methacrylate copolymers in an amount sufficient to achieve therapeutically effective plasma levels of morphine over at least 24 hours in the patient.

Abstract: The present invention relates to a process for the preparation of spherical or substantially spherical, practically dust-free aromatic and odoriferous granulated material which is free-flowing, mechanically stable and has a narrow grain-size distribution.

Abstract: Disclosed is a process for the preparation of pharmaceutical dosage units containing as an active substance of from 0.005 to 1.0% by weight of micronised Org 30659, comprising (a) a mixing step comprising bringing into association the active substance and a suitable carrier to form a mixture, and (b) a granulating step in which the mixture is granulated to form agglomerates or granules by wetting the mixture with a binder liquid, the wetting being conducted under agitation, characterised in that the granulation step (b) is conducted so as to exert on the granules a shear force which does not exceed the tensile strength of the agglomerates or granules. The process leads to granules and tablets having an excellent content/uniformity.

Abstract: The present invention provides a tablet for the controlled release of an active agent comprising (a) a matrix layer comprising an active agent embedded in a non-swelling, non-gelling hydrophobic matrix; (b) a first barrier layer laminated to a single face of the matrix layer; and (c) an optional second barrier layer laminated to the opposite face of the matrix layer and oppositely disposed to the first barrier layer; wherein the matrix comprises up to about 80% active agent and from about 5% to about 80% by weight of nonswellable waxes or polymeric material insoluble in aqueous medium, and the first and second barrier layers independently comprise (1) polymeric material exhibiting a high degree of swelling and gelling in aqueous medium or (2) nonswellable wax or polymeric material insoluble in aqueous medium.

Abstract: The invention is directed to a hard tablet that can be stored, packaged and processed in bulk. Yet the tablet dissolves rapidly in the mouth of the patient with a minimum of grit. The tablet is created from an active ingredient mixed into a matrix of a non-direct compression filler and a relatively high lubricant content.

Abstract: A new oral pharmaceutical dosage form comprising a core material that contains a proton pump inhibitor, one or more alkaline reacting compounds and optionally pharmaceutical excipients having a water soluble separating layer and an enteric coating layer. The core material as such is alkaline reacting and the separating layer between the alkaline reacting core material and the enteric coating layer is formed in situ as a water soluble salt between the alkaline reacting compound(s) and the enteric coating polymer. The invention also describes a new efficient process for the manufacture of such a dosage form comprising two functionally different layers in one manufacturing step, and its use in medicine.

Abstract: A sustained-release matrix for dental application includes either an anti-microbial agent or a colorant that is released from the matrix when the matrix contacts water. The preferred matrices include a water-soluble polymer and a water-insoluble support resin.

Abstract: A zero-order sustained-release delivery system for delivery of carbamazepine. A matrix tablet formulations of carbamazepine comprising hydrophilic polymer gel which inhibits transformation of carbamazepine into carbamazepine dihydrate by causing morphologic changes of carbamazepine crystals and results in amorphous form of carbamazepine present in the polymer matrix.

Abstract: A process for making pharmaceutical dosage units containing a therapeutic quantity of one or more low dosage medicinal agent comprising granulating said medicinal agent in an aqueous medium which contains a pharmaceutically acceptable surfactant agent and, optionally, further processing the product of said granulating into a tablet or capsule dosage unit.

Abstract: Direct compressed solid pharmaceutical dosage forms containing:a) from about 40 to about 95% by weight acetaminophen;b) from about 1 to about 60% by weight of a direct compression vehicle comprising microcrystalline cellulose; andc) from about 0.01 to about 4.0% by weight of a pharmaceutically-acceptable lubricant are disclosed. The acetaminophen and direct compression vehicle are combined under high shear conditions which are sufficient to transform acetaminophen and direct compression vehicle into a homogenous granulate without degradation. In preferred aspects of the invention, the lubricant is also combined with the acetaminophen and direct compression vehicle under high shear conditions. Methods of preparing the directly compressed solid pharmaceutical dosage forms and methods of treatment with the dosage forms are also disclosed. The methods are particularly well suited for preparing directly compressed dosage forms containing high load (i.e.

Abstract: A process for the manufacture of particles comprises mechanically working a mixture of a drug and a hydrophobic and/or hydrophilic fusible carrier in a high speed mixture so as to form agglomerates, breaking the agglomerates to give controlled release particles and optionally continuing the mechanical working with the optional addition of a low percentage of the carrier or diluent.

Abstract: A pharmaceutical multiple unit particulate formulation in the form of coated cores which includes a pharmaceutically acceptable carrier selected from calcium carbonate, calcium silicate, calcium magnesium silicate, calcium phosphate, kaolin, sodium hydrogen carbonate, sodium sulfate, barium carbonate, barium sulfate, magnesium sulfate, magnesium carbonate, and activated carbon, and an active substance in a layer on the outer surface of the cores.

Abstract: Non-steroidal anti-inflammatory drugs, such as indomethacin, and other pharmaceutically active compounds, are formulated with bile acids or their salts and conjugates. Bile acids previously proposed for use in such formulations have placed an unacceptable toxic load on the liver and/or cells of the gastrointestinal tract, causing abnormal liver function or cell erosion. In this invention, the bile acid is a low detergent bile acid, such as ursodeoxycholate. Stabilization of the bile acid pool results in enhanced and predictable enterohepatic recycling of NSAIDs (and other drugs) and a reduced risk of toxicity.

Abstract: A tablet for the local and slow release of herbal medication into the oral cavity of a subject. Also provided is a method of making the tablet and a method of using the tablet. The tablet includes a pharmaceutically effective amount of a herbal medication, a polymeric matrix material such as ethyl cellulose, a release enhancer such as PEG 4000 and a filler such as lactose. The tablet is characterized by long dissolution times of up to 120 minutes.

Abstract: A medicament for nasal administration to be used for disease prevention or treatment comprising a vaccine or a pharmacologically active peptide compounded with an ion exchange resin or adsorbent resin powder whose mean particle size is not larger than 200 .mu.m.

Abstract: The present invention is directed to a stable crystalline form of estradiol suitable for incorporation into pharmaceutical formulations. The invention further provides methods of preparing said crystalline form of estradiol. The invention further provides pharmaceutical formulations comprising said crystalline form of estradiol. The invention further provides a method of treatment of an individual in need of such administration by the transdermal administration of estradiol from a polymeric matrix comprising the crystal structure of estradiol of the present invention.

Abstract: The present invention relates to a sustained release formulation used for treatment or prevention of the diseases, which contains a therapeutically effective substance as an active ingredient, collagen as a drug carrier, and glycosaminoglycan as an additive. The formulation allows controlled release of the therapeutically effective substance.

Abstract: Pharmaceutical formulations for oral administration, comprising a matrix which comprises a .beta.-lactam antibiotic optionally in combination with a .beta.-lactamase inhibitor, granules in a delayed release form dispersed within the matrix, which comprise a .beta.-lactam antibiotic optionally in combination with a .beta.-lactamase inhibitor, the overall tablet formulation including a .beta.-lactam antibiotic and a .beta.-lactamase inhibitor.

Abstract: A nutritional supplement contains plural parts. Each of the plural parts is chronologically appropriate for its scheduled time of consumption. The nutritional supplement is contained in a palatable base, for example, a food bar which masks any unpleasant taste or texture of the nutrient. The nutritional supplement may contain any one or several nutrients including drugs, vitamins, herbs, hormones, enzymes and/or other nutrients in chronologically appropriate dosages in each part or sub-part.

Abstract: The invention relates to pharmaceutical preparations having controlled release of active compound and to processes for their preparation, in particular for poorly soluble active compounds having problematic bioavailability.

Abstract: A method is provided to treat inflammatory bowel disease by locally administering to the colon an effective amount of nicotine or a pharmaceutically acceptable salt thereof, preferably via formulations adapted for delayed oral release or rectal administration. Further provided is a novel formulation for the oral administration of nicotine comprising a polyacrylic polymer complexed with nicotine.

Abstract: A controlled-release pharmaceutical composition for oral administration comprising a multitude of granules made by dissolving or dispersing a drug and a water-insoluble polymer in a molten carrier, solidifying the resultant material, and grinding the resultant solid into granules.

Abstract: An osmotic caplet is disclosed comprising an osmotic caplet exit for delivering a preselected dose of drug to a patient in need of therapy.

Abstract: This invention describes novel formulations containing a water soluble disulfide, 2,2'-dithio-bis-ethane sulfonate, with or without cis-diammine dichloro platinum present in the same formulation, wherein the parenteral or oral administration of 2,2'-dithio-bis-ethane sulfonate is used to reduce the risk or prevent or retard the development of cisplatin induced nephrotoxicity, myelosuppression, and neurotoxicity, and wherein the parenteral or oral administration of 2,2'-dithio-bis-ethane sulfonate potentiates the antitumor activity of cisplatin when treating human patients with cancer. This invention also teaches novel formulations containing 2,2'-dithio-bis-ethane sulfonate alone or in combination with cisplatin in lyophilized or dissolved in an aqueous formulations which can be administered to patients with cancer who are being treated with cisplatin.

Abstract: The present invention is a method of preparing rapidly dissolving comestible units such as tablets. The present invention also includes an apparatus for making the comestible units and the units themselves. The product prepared in accordance with the present invention can include active ingredients and is capable of dissolving in the mouth of the consumer within several seconds. The unit dosage forms prepared in accordance with the present invention are particularly useful as antacids and as a delivery vehicle for biologically active ingredients, especially those which are ideally combined with antacid ingredients in order to ameliorate the effects of antacid environment.

Abstract: The present invention provides oral formulations of Ranitidine Hydrochloride in the form of coated tablets and capsules which produce controlled or regulated dissolution and release at a fairly uniform rate over long periods--as long as 12 to 24 hours--to maintain Ranitidine at desired levels above the MEC.

Abstract: The present invention is a method and a dosage unit for delivery of a controlled-release system. The dosage unit is a quick dissolve unit which can be prepared by mixing uncured shearform matrix and a controlled-release system, either molding or compacting a unit dosage form and curing the shearform matrix. The controlled-release systems used in the present invention include instantaneous release components, delayed release components, sustained release components, and combinations thereof.

Abstract: Diseases of the colon are treated by oral ingestion of a unit dosage form containing a plurality of porous microscopic beads, the pores containing an active agent or drug and plugged with a polysaccharide that is chemically degradable by colon-specific bacteria. The dosage form further contains a coating of an enteric material that remains intact until the dosage form reaches the colon.

Abstract: A process is described for preparing pharmaceutical compositions by co-grinding or dry mixing the active substance with cyclodextrins or with hydrophilic polymer materials which swell on contact with water. Homogeneous compositions are obtained from which the active substance is released very rapidly into an aqueous medium.

Abstract: The invention relates to a method for inhibiting angiogenesis and proliferation of endothelial cells by administering an inhibitory amount of a 7-?substituted amino!-9-?(substituted glycyl)amido!-6-demethyl-6-deoxytetracycline of Formula I: ##STR1## wherein R, R.sub.2, R.sub.3, and W are as defined in the specification. The invention also relates to a method for inhibiting proliferation of tumor cells and tumor growth by administering an inhibitory amount of a compound of Formula I in combination with a chemotherapeutic agent or radiation therapy. The invention also relates to compositions containing an effective inhibitory amount of a compound of Formula I in a pharmaceutically acceptable carrier.