Abstract: The present invention provides sustained release oral solid dosage forms of cisapride by using a multi-particulate system, which are bioavailable and can provide efficient blood level of cisapride over 24 hours. Unit dosage forms of cisapride which comprise a plurality of substrates containing sustained release cisapride, as well as pharmaceutical compositions containing the dosage forms, are also disclosed herein.

Abstract: A rapidly-releasing and taste-masking pharmaceutical dosage form and a process for preparing such oral dosage form are disclosed.

Abstract: The present invention relates to a composition for oral administration to a patient for removal of undesired chemicals or amino acids caused by disease. The composition comprises an entrapped or encapsulated microorganism capable of removing the undesired chemicals or amino acids. The composition may comprise a pharmaceutically acceptable carrier for oral administration to the patient.

Abstract: A microcrystalline cellulose-based excipient having improved compressibility, whether utilized in direct compression, dry granulation or wet granulation formulations, is disclosed. The excipient is an agglomerate of microcrystalline cellulose particles and from about 0.1% to about 20% silicon dioxide particles, by weight of the microcrystalline cellulose, wherein the microcrystalline cellulose and silicon dioxide are in intimate association with each other. The silicon dioxide utilized in the novel excipient has a particle size from about 1 nanometer to about 100 microns. Most preferably, the silicon dioxide is a grade of colloidal silicon dioxide.

Abstract: Disclosed are suspensions suitable for encapsulation in gelatin capsules, comprising a solid phase consisting of solid particles having a mean diameter of at least about 149 &mgr;m, and a liquid phase capable of suspending the solid phase, the suspension having a predetermined rheology at a temperature suitable for encapsulation into gelatin capsules.

Abstract: A controlled absorption diltiazem pellet formulation for oral administration comprises a core having diltiazem or a pharmaceutically acceptable salt thereof as the active ingredient. The core is surrounded by a coating which has only a single layer which is comprised of a relatively major proportion of talc and relatively minor proportion of sodium lauryl sulfate admixed with a minor proportion of a pharmaceutically acceptable film-forming, first polymer permeable to water and diltiazem, and a major proportion of a pharmaceutically acceptable film-forming, second polymer that is less permeable to water and diltiazem than the first polymer. The core and the coating layer both exclude organic acids. The composition of the coating layer as well as the proportion of core to coating layer are effective to permit release of the diltiazem allowing controlled absorption following oral administration.

Abstract: A pharmaceutical composition suitable for preparing an extemporaneous suspension, that promptly releases active agents or ingredients (drugs) is disclosed. These compositions comprise an active agent in microgranule form. The microgranules containing the active agent are coated with a film coating mixture containing at least one lipid material and an optional hydrophilic additive. The coating envelopes the microgranules but does not impart a controlled release property to the composition, and affords prompt release thereof once ingested.

Abstract: A composition, particularly adapted for oral administration, containing omeprazole, and a method for preparing the composition, are disclosed. The composition, being exempt of alkaline-reacting compounds, contains a core constituted of nuclei and said benzimidazole, the nuclei and benzimidazole being compressed together, an intermediate layer, and an enteric layer.

Abstract: An oral dosage form that provides for the controlled release of an analgesic wherein the dosage form comprises a core containing an analgesic that is coated with a mixture of an enteric polymer, a water insoluble polymer and a lubricant.

Abstract: A nasally administrable composition which contains physiologically active compounds such as insulin, calcitonin, prostaglandin (PG) derivatives, monoclonal antibodies or interleukin derivatives (IL), and is enhanced in the in vivo absorbability of the physiologically active compound when administered nasally. The compositions are prepared by mixing fine particulate of the physiologically active compound with fine particulate of carrier having a mean particle size from 15 &mgr;m to 300 &mgr;m, and particle surface area from 0.1 to 0.4 m2/g, a which adhere to the mucous membrane of the nasal cavity, and HPC—H as absorption accelerator.

Abstract: The invention provides a pharmaceutically acceptable solid oral formulation of olanzapine and a process for making such formulation.

Abstract: Fat-like protein compositions for use in foods and cosmetics comprising a protein of gelatin and a water-soluble albumin, a carbohydrate, and a phospholipid wherein said gelatin, albumin, carbohydrate, and phospholipids are in the form of a water-insoluble complex coacervate, and processes for making the same. Preferred are compositions wherein some or all of the ingredients are optionally crosslinked.

Abstract: The present invention relates to orally administered suspensions of pharmaceutical active substances of the NSAID type, particularly the antirheumatic agent Meloxicam, which are stabilized by the addition of small amounts of highly dispersed silicon dioxide using high shear forces and adding small amounts of hydrophilic polymers to form a three-dimensional siloid structure, and a process for the preparation thereof.

Abstract: This invention provides a pharmaceutical composition comprising a mycophenolate salt, the composition being adapted to release mycophenolate in the upper part of the intestinal tract.

Abstract: The present invention relates to a fast-release as well as a prolonged release type of nifedipine pellets and the process for the preparation thereof. The fast-release type of nifedipine pellets comprises a particulate core which is covered by a nifedipine coating layer. The particulate core comprises water-soluble or water-insoluble excipient(s) and a pharmacologically acceptable carrier. The nifedipine coating layer comprises an effective amount of nifedipine dissolved in organic solvent(s). This nifedipine coating layer can further be mixed with a suspension which comprises an adhesive, an emulsifier, and a dispersant. The preferred composition of the fast-release type of nifedipine includes 20-70% of the particulate core, 3-15% of nifedipine, 1-20% of emulsifier, 1-20% of adhesive, and 1-30% of dispersant.

Abstract: The invention relates to compositions useful for making taste-masked oral dosage forms which can be easily processed and which disintegrate rapidly when placed in the mouth. The compositions include coated liquiflash particles and shearform floss particles. Tablets are preferred dosage forms.

Abstract: A method for decreasing the frequency of transmission of human immunodeficiency virus or herpesviruses or for preventing the transmission of or treating a sexually transmitted bacterial infection by administering to a human an anti-human immunodeficiency virus amount or an anti-herpesvirus amount or an anti-bacterial amount of cellulose acetate phthalate (CAP) or hydroxypropyl methylcellulose phthalate (HPMCP), such as in micronized form, or a combination thereof, either alone or in combination with a pharmaceutically acceptable carrier or diluent. The CAP and/or HPMCP may be employed as a suspension of micronized particles and may further contain a water miscible, non-solvent for CAP or HPMCP, such as glycerol.

Abstract: An oral pharmaceutical modified release multiple-units composition for the administration of an analgesically effective amount of an opoid. The composition comprises at least two fractions wherein individual units containing an opoid are coated with a sustained release coating. A first fraction is adapted to relatively fast release while a second fraction is adapted to a delayed release. Such compositions make possible to obtain both a relatively fast onset of the analgesic effect and the maintenance of analgesically active plasma concentration for a relatively long period of time. The invention further relates to a process for the preparation of a composition according to the invention.

Abstract: The present invention relates to chitin beads having a uniform and fine particle size and comprising microsporidian spores whose principal cell wall substance is chitin; chitosan beads comprising N-deacetylated chitin and having a uniform fine particle size; methods for preparing these beads; carriers comprising these beads; and a method for preparing microsporidian spores.Microsporidian spores are proliferated in insect's bodies or cultured cells to obtain chitin beads having the uniform and fine particle size and whose cell wall substance is mainly composed of chitin. The chitin as the major cell wall substance is subjected to N-deacetylation to give chitosan beads. When the insect is a larva of domesticated silkworm, microsporidian spores are proliferated by orally or percutaneously inoculating the spores into the 2nd instar domesticated silkworm larvae in a concentration of 5.times.10.sup.2 to 5.times.10.sup.

Abstract: This invention relates to a process for the preparation of an oral solid rapidly disintegrating dosage form of a pharmaceutically active substance which has an unacceptable taste which process comprises: (i) forming a solution or a suspension in a solvent of a water soluble or water dispersible carrier, a filler and the pharmaceutically active substance with the unacceptable taste in association with a lipid, the weight ratio of the pharmaceutically active substance to the lipid being in the range of from 1:1 to 1:10 and the weight ratio of the carrier to the lipid being in the range of from 5:1 to 1:15; (ii) forming discrete units of the suspension or solution; and (iii) removing the solvent from the discrete units under conditions whereby unit dosages are formed comprising a network of carrier/filler carrying a dosage of the pharmaceutically active substance in association with the lipid; oral solid rapidly disintegrating dosage forms prepared by such a process are also provided.

Abstract: The present invention provides a core of predominately microcrystalline cellulose, on which an active drug is layered onto the core via solution coating. The coated particles have a narrower particle size distribution than coated granules provided by other processes. An optional final coating of a pharmaceutically acceptable polymeric coating is provided to provide tastemaking or controlled release, and protection of the drug-layered particles.

Abstract: The present invention relates to a novel pharmaceutical form, in the form of spheroids, containing tiagabine as active principle. The invention also covers the process for the preparation of such spheroids and multiparticulate pharmaceutical preparations, such as tablets, containing these spheroids. These pharmaceutical preparations are intended for the delivery of the spheroids they contain, and are characterized by the absence of an adverse effect on the release profile of the tiagabine contained in the spheroids following a possible compression step.

Abstract: A taste-masked microcapsule composition for administration of a drug is provided. The composition comprises microcapsules of drug and a substantially water-insoluble polymeric material, typically a cellulosic polymer. The microcapsule composition may be incorporated into any number of pharmaceutical formulations, including chewable tablets, effervescent tablets, powders, liquid dispersions, and the like. A method for masking the taste of drugs is also provided, involving a phase separation coacervation technique in which drug is coated with relatively high levels of a polymeric material. These high coating levels give rise to effective taste masking, while nevertheless allowing targeted release of drug, so that the drug is released shortly after passage through the mouth.

Abstract: The invention relates to flavor-masked pharmaceutical compositions for oral administration, their preparation and their use as medicaments.The new pharmaceutical preparations according to the invention make it possible to administer pharmaceutical active substances having very unpleasant organoleptic properties such as, for example, very bad taste, even in liquid form.

Abstract: A stabilized solid controlled release dosage form having a coating derived from an aqueous dispersion of ethylcellulose is obtained by overcoating a substrate including a therapeutically active with an aqueous dispersion of ethylcellulose and then curing the coated substrate at a temperature and relative humidity elevated to a suitable level above ambient conditions until the coated dosage form attains a stabilized dissolution profile substantially unaffected by exposure to storage conditions of elevated temperature and/or elevated relative humidity.

Abstract: An extended release acetaminophen composition comprises a plurality of discrete particles containing acetaminophen which, when contained within a gelatin capsule and assayed in a USP Apparatus I rotating basket at 50 rpm in 900 mL of phosphate buffer at pH 5.8 and 37.degree. C., exhibits about 40 percent to about 53 percent acetaminophen dissolution at one-half hour, about 50 percent to about 68 percent dissolution at 45 minutes, about 57 percent to about 77 percent acetaminophen dissolution at one hour, and about 82 percent to about 92 percent acetaminophen dissolution at two hours. After six hours, the contemplated extended release acetaminophen composition exhibits substantially complete dissolution. A process for treating a human patient with the extended release acetaminophen composition 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 pharmaceutical form for delivery of active substances to wounds is characterized in that this is designed to be coherent, sheet-like and, in its extent in terms of area, equal to or smaller than the wound area to be managed, and contains active substance in a defined amount in homogeneously dispersed form.

Abstract: A microcapsule having a core, a shell and seeds fully or partially embedded in said shell. The core and seeds are active substances which preferably function as a leavening agent. The shell is composed of either a water soluble or meltable natural polymer, including vegetable waxes. When the shell is ruptured, the active substances will react with each other and the dough mixture thereby producing a leavening effect and/or dough conditioning effect in baked goods.

Abstract: A sustained release cisapride oral dosage formulation suitable for once-daily administration comprises a plurality of mini-tablets containing cisapride or a salt thereof with an organic acid and capable of releasing cisapride at different sites along the gastrointestinal tract. The mini-tablets include a proportion of immediate release tablets and a proportion of tablets which release cisapride in response to the pH environment at a given site in the distal regions of the gastrointestinal tract and which include cisapride or a salt thereof embedded in a matrix of hydrophilic polymer, said matrix being coated with a pH dependent polymer, the formulation having a Cmax/Cmin ratio under steady state conditions of 2:1 or less as evidenced by a substantially flat plasma profile in vivo.

Abstract: The invention relates to a rapidly disintegratable multiparticulate tablet which disintegrates in the mouth in less than 40 seconds and which comprises an excipient and an active ingredient in the form of microcrystals coated with a coating agent.

Abstract: A composition, comprising (a) microcrystalline cellulose; and (b) a compressibility augmenting agent which (i) physically restricts the proximity of the interface between adjacent cellulose surfaces; or (ii) inhibits interactions between adjacent cellulose surfaces; or (iii) accomplishes both (i) and (ii) above, is disclosed. The composition is in the form of agglomerated particles of microcrystalline cellulose and the compressibility augmenting agent in intimate association with each other.

Abstract: The invention relates to accurately meterable shaped articles, for example granules or pellets, containing hydrophilic macromolecules, active compounds and optionally further pharmaceutically acceptable structure-forming substances and auxiliaries, the active compound being present in a matrix in dissolved, suspended or emulsified form, and a novel process for the production of these shaped articles, the process being particularly economically and ecologically acceptable, and use of the shaped articles as medicaments, in which the bioavailability, shelf life and tolerability is increased. Using the shaped articles or mixtures according to the invention, intermediates or final products for pharmacy, cosmetics, diagnosis, analysis or dietetics (healthcare) can additionally be advantageously prepared.

Abstract: A microcrystalline cellulose-based excipient having improved compressibility, whether utilized in direct compression, dry granulation or wet granulation formulations, is disclosed. The excipient is an agglomerate of microcrystalline cellulose particles and from about 0.1% to about 20% silicon dioxide particles, by weight of the microcrystalline cellulose, wherein the microcrystalline cellulose and silicon dioxide are in intimate association with each other. The silicon dioxide utilized in the novel excipient has a particle size from about 1 nanometer to about 100 microns. Most preferably, the silicon dioxide is a grade of colloidal silicon dioxide.

Abstract: A process for the administration of a flowable solid, semisolid, or liquid medium exhibiting a controlled release of at least one active substance to plants by means of injection using needle-free, pressure-actuated devices is characterized in that the medium comprises active substance-containing microparticles of a maximum size of 100 .mu.m including the following components:a) 0.5-70%-wt. of at least one active substance,b) 10-70%-wt. of at least one biodegradable polymer,c) up to 20%-wt. of formulation adjuvants.

Abstract: The present invention describes the use of croscarmellose sodium to coat bitter-tasting active agents in a manner that will mask the bitter taste of these materials, taste masked pharmaceutical compositions in which the particles of pharmaceutically active agent are coated with croscarmellose sodium, taste masked pharmaceutical tablets made therefrom, in which the rapid disintegration of tablets that is imparted by croscarmellose sodium is preserved, and to a method for preparing such coated particles by preparing them in a fluidized bed coating process.

Abstract: Liquisolid systems are acceptably flowing and compressible powdered forms of liquid medications. According to the concept of liquisolid systems, liduid lipophilic drugs, or water-insoluble solid drugs dissolved in suitable non-volatile solvents, may be converted into free-flowing and readily compressible powders by a simple admixture with selected powder excipients referred to as the carrier and coating materials. Various grades of microcrystalline or amorphous cellulose may be used as carriers, whereas very fine particle size silica powders may be used as coating materials.

Abstract: A solid pharmaceutical composition for oral administration comprising a histamine H.sub.2 -receptor antagonist, a low neutralizing capacity antacid, and a high neutralizing capacity antacid coated with a pH-independent and water-insoluble polymer base, which composition improves the condition of a patient promptly after administration and sustains the effects for an extended period of time in the treatment of digestive disorders on which suppression of gastric acid secretion is effective.

Abstract: Pharmaceutical compositions of bisphosphonic acids, and salts thereof, are prepared by direct compression/dry mix tablet formulation. These pharmaceutical compositions are useful in the treatment of disturbances involving calcium or phosphate metabolism, in particular, the treatment and prevention of diseases involving bone resorption, especially osteoporosis, Paget's disease, malignant hypercalcemia, and metastatic bone disease.

Abstract: The present invention relates to a novel pharmaceutical form, in the form of spheroids, containing one or more active principles, which the exception of tiagabine.The invention also covers the process for the preparation of such spheroids and multiparticulate pharmaceutical preparations, such as tablets, containing these spheroids.These pharmaceutical preparations are intended for the delivery of the spheroids they contain, and are characterized by the absence of an adverse effect on the release profile of the active principle(s) following a possible compression step.

Abstract: Disclosed is a method for delivering an active protein or peptide to the colon. The steps of the method include providing a multiparticulate dosage core particle comprising 3 components, the total weight of the 3 components in dry form defining a batch size. The multiparticulate core particle is produced by the method comprising: a) providing an aqueous PEG solution, the dry weight of the PEG component representing from about 2.5% to about 15% of the batch size (weight/weight), the water component of the aqueous PEG solution representing approximately 30-60% of the batch size (weight/weight); b) providing a homogenous mixture of the active protein or peptide and microcrystalline cellulose, both in dry form, the active protein or peptide comprising from about 50% to about 95% of the batch size (weight/weight) and the microcrystalline cellulose comprising from about 2.

Abstract: An oral pharmaceutical composition of pantoprazole in pellet or tablet form, wherein the pantoprazole is at least partly in slow-release form, is distinguished, on combined administration with an antimicrobially-active ingredient, by an enhanced action of rapid onset against disorders caused by Helicobacter.

Abstract: The invention provides a method for detecting the presence of Serpulina hyodysenteriae in a biological sample, an oligonucleotide primer and an S. hyodysenteriae-specific oligonucleotide probe useful in that method, and an article of manufacture that contains the primers and/or probe. Also provided are an about 2.3-kb DNA fragment derived from genomic DNA of S. hyodysenteriae and encoding for an about 56 kDa polypeptide, a recombinant expression vector containing the DNA fragment, the 56 kDa polypeptide and a monoclonal antibody reactive with the peptide, and a method of assaying for antibodies reactive with the 56 kDa peptide.

Abstract: The present invention describes formulations of nanoparticulate HIV protease inhibitors comprising a cellulosic surface stabilizer. The nanoparticulate formulations have an increased rate of dissolution in vitro, an increased rate of absorption in vivo, a decreased fed/fasted ratio variability, and a decreased variability in absorption. The present invention is also directed to methods of making the novel formulations. In particular, nanoparticulate formulations of HIV type 1 (HIV-1) and type 2 (HV-2) protease inhibitors are described.

Abstract: The present invention describes formulations of nanoparticulate HIV protease inhibitors comprising a cellulosic surface stabilizer. The nanoparticulate formulations have an increased rate of dissolution in vitro, an increase rate of absorption in vivo, a decreased fed/fasted ratio variability, and a decreased variability in absorption. The present invention is also directed to methods of making the novel formulations. In particular, nanoparticulate formulations of HIV type 1 (HIV-1) and type 2 (HIV-2) protease inhibitors are described.

Abstract: The invention relates to a multiparticulate pharmaceutical form with delayed and pulsed release, enabling to obtain the onset of the availability of the active ingredient within 4 to 8 hours after the ingestion of the pharmaceutical form, and then a progressive release of the totality of the active ingredient within the 8 to 20 following hours, characterized by the fact that it is free of organic acid and that it is in the form of medicinal spheroids consisting of a neutral spherical core comprising a first coating based on a mixture of at least one hydrosoluble polymer and of at least one non hydrosoluble polymer throughout which are uniformly distributed the constitutive particles of an active ingredient, the whole comprising a second coating based on at least two pH independent polymers presenting rates of permeability different from one another with respect to the gastric and intestinal mediums, optionally at least one pH dependent polymer, at least one plasticizer and at least one inert carrier uniformly

Abstract: A controlled absorption diltiazem pellet formulation for oral administration comprises a core having diltiazem or a pharmaceutically acceptable salt thereof as the active ingredient. The core is surrounded by a coating which has only a single layer which is comprised of a relatively major proportion of talc and relatively minor proportion of sodium lauryl sulfate admixed with a minor proportion of a pharmaceutically acceptable film-forming, first polymer permeable to water and diltiazem, and a major proportion of a pharmaceutically acceptable film-forming, second polymer that is less permeable to water and diltiazem than the first polymer. The core and the coating layer both exclude organic acids. The composition of the coating layer as well as the proportion of core to coating layer are effective to permit release of the diltiazem allowing controlled absorption following oral administration.

Abstract: The invention is concerned with a flowable dry particle consisting of at least one oleophilic substance as the active ingredient present in a matrix of at least one carrier material and a coating. The coating consists of calcium silicate or of a mixture of calcium silicate with one or more mixture components, with the mixture components being microcrystalline cellulose, magnesium silicate, magnesium oxide, stearic acid, calcium stearate, magnesium stearate, silicon dioxide, kaolin and/or hydrogenated vegetable oil.

Abstract: Disclosed are pharmaceutical compositions which have been modified to release pharmaceutically acceptable mycophenolate salts in the upper part of the intestinal tract and methods of treatment using the pharmaceutical compositions.

Abstract: Perfume is absorbed within organic polymer particles which have a further polymer at their exterior. The further polymer incorporates free hydroxyl groups and serves to promote deposition of the particles from a wash or rinse liquor. The further polymer may be part of an encapsulating shell, but more conveniently is used as a stabiliser during polymerisation of the particles. Highly hydrolysed polyvinyl alcohol is preferred.