Abstract: This invention relates to coating formulations for coating sustained-release drug implants. The coating formulations are capable of formulations are capable of forming a porous film coat over a biologically active agent to provide a release of the active agent at a constant rate over a prolonged period of time. The pore forming agent is used in the formulation of the invention in the amount effective to regulate the release of a biologically active compound at a desired rate. Preferably, the effective amount of the pore forming agent provides long term delivery of the active agent. The invention also provides an improved implant for the sustained administration of a biologically active compound suitable for subcutaneous implantation. The invention also relates to methods for making and using the formulation and the implant of the invention.

Abstract: The specification describes a pharmaceutical combination consisting of dipyridamole or mopidamol and acetylsalicylic acid or the physiologically acceptable salts thereof, processes for preparing this pharmaceutical combination and the use thereof for the controlled prevention of clot formation.

Abstract: A biomaterial composition for the resorption/substitution of organic supporting tissues, including 20-75 wt. % of an inorganic phase consisting of particles that include either hydroxyapatite (A) optionally mixed with tricalcium phosphate .beta. (B), or calcium-titaniumphosphate (Ca(Ti).sub.4 (PO.sub.4).sub.6) (C), and 80-25 wt. % of a liquid phase including an aqueous solution of a water-soluble biocompatible polymer that is cross-linkable under the effect of the pH of the medium. The composition is sterilizable, injectable and curable in biological media to form a biomaterial for replacing supporting tissues.

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: A sodium phosphate bowel cleansing composition which has improved taste over conventional sodium phosphate compositions. The composition comprising free flowing monobasic sodium phosphate and dibasic sodium phosphate powders or crystals which have been coated with at least one edible grade film forming polymer such as hydroxypropylmethyl cellulose or polyethylene glycol.

Abstract: This invention provides rapamycin solid dosage unit which comprises a core and a sugar overcoat, said sugar overcoat comprising rapamycin, one or more surface modifying agents, one or more sugars, and optionally one or more binders.

Abstract: Cross-linked cellulose is an excellent binder disintegrant that can be used in the preparation of pharmaceutical tablets. The tablets that are so prepared are made of a compressed mixture of a powder of a pharmaceutically active ingredient with a powder of a pharmaceutical excipient including a pharmaceutically acceptable form of cross-linked cellulose in an amount up to 35% by weight with respect to the total weight of the tablet. The cross-linked cellulose is prepared by cross-linking microcrystalline or fibrous cellulose with a cross-linking agent such as epichlorhydrin in a relative amount of 2 to 50 g of cross-linking agent per 100 g of cellulose. Tests have proved that cross-linked cellulose is very easy to synthetise and has excellent binding/disintegrating properties that are function of the cross-linking degree. At low cross-linking degree, cross-linked cellulose is more a binder than a disintegrant whereas at high cross-linking degree, it is more a disintegrant than a binder.

Abstract: A method for decreasing the frequency of transmission of human immunodeficiency virus or herpesviruses by administering to a human an anti-human immunodeficiency virus amount or an anti-herpesvirus 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: A coated product in the form of solid particles of a food or pharmaceutical wherein the particles are each coated with a water-soluble hemicellulose. The water-soluble hemicellulose has a viscosity in the range of from 50 to 1,000 mPa.multidot.s at 25.degree. C. when dissolved in water in an amount of 10% by weight and has a reducing sugar content of 5% by weight or less and an amino acid content, as measured by assay with 2,4,6-trinitrobenezene sulfonic acid, of 1.0% by weight or less.

Abstract: An oral drug dosage unit, for administration to a patient, having active drug, and an effective diameter and surface composition sufficient for the unit to be transported from the stomach into the duodenum following substantially complete emptying of chyme from the stomach into the intestine and prior to release of active drug from the unit, wherein the active drug has an absorption rate that is substantially affected by the coinciding presence of food in the stomach, the effective diameter of the unit prevents gastric emptying of the unit prior to gastric emptying of chyme, and the surface composition is an enteric coating which prevents release of the active drug in the stomach and allows release of the active drug in the intestine.

Abstract: An aqueous dentifrice composition comprising an aqueous vehicle containing at least two active ingredients reactive with each other, at least one of the active ingredients being encapsulated in a substantially water immiscible, pressure rupturable shell which is rupturable during use of the dentifrice, causing the same to be released for interaction with the other active ingredient, the shell being formed from a plasticized alkyl cellulose polymer. The dentifrice exhibits increased efficacy for fluoridation of teeth when the active ingredients are soluble fluoride salt and a calcium salt encapsulated in the plasticized alkyl cellulose polymer.

Abstract: Liquisolid systems are acceptably flowing and compressible powdered forms of liquid medications. According to the concept of liquisolid systems, liquid 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. Based on the theory that the carrier and coating materials can retain only certain amounts of liquid and at the same time maintain acceptable flow and compression properties, a new formulation-mathematical model is provided to calculate the optimum quantities of carrier and coating materials required to yield acceptably flowing and compressible liquid/powder admixtures.

Abstract: The present invention pertains to a sustained release drug delivery system hich comprises a core of active ingredient, an enteric coating, a second coating of active ingredient and lastly a readily gastric-soluble protective coating. The sustained release dosage form of this invention is useful for pharmaceutically active ingredients that have limited aqueous solubility, especially phenytoin sodium, and other pH dependent soluble drugs.

Abstract: Sustained release oral solid dosage forms of opioid analgesics are provided as multiparticulate systems which are bioavailable and which provide effective blood levels of the opioid analgesic for at least about 24 hours. A unit dose of the opioid analgesic contains a plurality of substrates including the opioid analgesic in sustained release form. The substrates have a diameter from about 0.1 mm to about 3 mm.

Abstract: Amine functionality-containing materials such as cationic cellulose-based compositions are coated to suppress their tendency to generate "amine odors" in an alkaline pH environment. Further provided are effervescent compositions, liquid or solid soap formulations, fabric softeners, shampoos and the like comprising such materials coated with a suitable coating composition.

Abstract: The invention relates to a novel dosage unit for the sustained-release delivery of active agents as well as compositions and methods for making same.

Abstract: The invention relates to a peroral composition providing controlled release of a drug, the composition comprising a) a core comprising the drug and a drug release controlling agent and b) an enteric coating comprising the drug release controlling agent, wherein the drug release controlling agent consists substantially of a pH-sensitive enteric polymer. Preferably the pH-sensitive enteric polymer has a pH dissolving point of at least 6.5. The composition is preferably in the form of granules. Preferably, the composition is in the form of enteric matrix granules coated with an enteric coating. The composition releases the drug gradually in the lower gastrointestinal tract. The composition is especially suitable for the administration of 3-(3-cyanophenyl)methylene-2,4-pentanedione into the colon.

Abstract: A multiple unit oral pharmaceutical dosage form having a plurality of pellets in a water soluble capsule or in a tablet compressed from the pellets, wherein each pellet contains (a) a substantially inert core, (b) an active ingredient layer over the inert core, and containing (i) a pharmacologically active particulate active ingredient, (ii) a nonembedding amount of a binder for adhering the active ingredient over the inert core, and optionally (iii) a pharmaceutically acceptable, inert adjuvant, such as colloidal silica, and (c) a coating over the active ingredient layer for retarding the release of the active ingredient from the active ingredient layer into an aqueous body fluid solvent in situ, the nonembedding amount of the binder is suitably from about 1% wt. to about 10% wt.

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: A controlled release preparation comprises an ionic polymer matrix loaded with an active compound, particularly a pharmaceutically active compound such as doxorubicin or other cytotoxic or cytostatic drug, the active compound being complexed with a complexing agent such as a metal ion to modify the release of the active compound from the polymer matrix. The ionic polymer matrix may be provided in the form of microspheres, such as microspheres of crosslinked albumin/dextran sulphate.

Abstract: Disclosed is a novel aqueous suspension of an antimicrobial compound having high stability of the suspension despite the use of such a very small amount of a suspending agent as not to cause any adverse influences on the inherent activity of the active ingredient. The suspending agent is a biocellulose as a microbial products of certain acetic bacteria which is not used in the prior art as a suspending agent in the prior art due to susceptibility to putrefaction while this defect of the biocellulose can be solved in the antimicrobial aqueous suspension by the use of an antimicrobial compound such as 2-methoxycarbonylamino benzimidazole, 2-pyridinethiol zinc-1-oxide and 2-(4-thiazolyl) benzimidazole.

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

Abstract: A method for preparation of multi-layer polymeric microspheres formed from any degradable or non-degradable polymers which are not soluble in each other at a particular concentration, but which have a positive spreading coefficient in solution. The multi-layer microspheres produced by the method are distinguished by extremely uniform dimensioned layers of polymer and actual incorporation of the substance to be delivered into the polymer layers. In the preferred embodiment of the method, two polymers are dissolved in a volatile organic solvent, the substance to be incorporated is dispersed or dissolved in the polymer solution, the mixture is suspended in an aqueous solution and stirred, and the solvent is slowly evaporated, creating microspheres with an inner core formed by one polymer and an outer layer formed by the second polymer. In another embodiment, solvent is removed by spray drying.

Abstract: The present invention discloses the taste masking of drugs by wet granulating the drug with a microcrystaline cellulose compositions then spheronizing the granulation into spheres having a smooth uniform surface and a particle size in the range of 1 to 1000 microns.

Abstract: The use of .alpha.,.alpha.-diphenylacetic acid-4-(N-methyl-piperidyl) ester for the treatment of painful muscular cramp conditions in the region of the abdominal cavity or for the production of drugs for the treatment of painful muscular cramp conditions in the region of the abdominal cavity.

Abstract: Provided are enteric coating compositions which utilize a low viscosity cellulose acetate phthalate polymer as a film former. The cellulose acetate phthalates have an inherent viscosity of about 0.2 to 0.6 dL/g and phthalyl values of from 30 to 40% and can be applied to solid oral medicaments with less solvent than conventional cellulose acetate phthalate polymers. Also provided is a process for preparing the low viscosity cellulose acetate phthalate polymers.

Abstract: A dry moisture barrier film coating composition for forming a moisture barrier film coating for pharmaceutical tablets and the like comprises polyvinyl alcohol, soya lecithin, and optionally a flow aid, a colorant, and/or a suspending agent. A liquid coating solution or dispersion for forming a moisture barrier film coating for pharmaceutical tablets and the like comprises polyvinyl alcohol, soya lecithin, water, and optionally a flow aid, a colorant, and/or a suspending agent. A method of coating pharmaceutical tablets and the like with a moisture barrier film coating comprises forming a liquid coating solution or dispersion for forming a moisture barrier film coating for pharmaceutical tablets and the like comprising polyvinyl alcohol, soya lecithin, water, and optionally a flow aid, a colorant, and/or a suspending agent, applying the coating solution or dispersion onto the tablets to form a film coating on the tablets, and drying the film coating on the tablets.

Abstract: A method of administering an oral bandage to lesions in the oral mucosa is disclosed wherein there is prepared a storage stable topical gel formulation adapted to form an oral bandage adherent to the oral mucosa when applied thereto, the gel containing at least one anesthetic compound, a keratolytic compound, an astringent compound and an ethyl cellulose gelling agent in an amount of at least about 8% by weight and then applying the gel to the area of the oral mucosa experiencing irritation to form an adherent oral bandage.

Abstract: A single bead drug delivery system suitable for oral administration with multiply layered drug and polymer compartments can provide a two-step release of active agent to facilitate an immediate yet sustained drug delivery over a 24 hour period following oral administration with minimized variance between peak and trough levels of therapeutic drug amounts.

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: An antimicrobial agent comprising allyl isothiocyanate (AIT) packaged in a packaging material having a structure wherein part of the pores of a porous packaging substrate is filled with, or said pores are partially or entirely narrowed by a resin impervious to AIT vapor, and a method for controlling the AIT vapor release speed comprising enclosing AIT in the above-mentioned packaging material. According to the present invention, the AIT vapor release speed can be controlled, whereby enabling sustained release of AIT vapor and persistent effect of antimicrobial action. In addition, the antimicrobial agent of the present invention can be widely applied to food industries and various other fields where breeding and reproduction of deleterious microorganisms pose problems, since it is economical, compact and easy to use.

Abstract: The present invention relates to a compressed pharmaceutical dosage form containing pharmaceutical particles coated with a taste-masking composition, a water-disintegratable, compressible carbohydrate and a binder. These components are dry blended and compressed into a dosage form, such as a tablet, having a hardness sufficient to cause the carbohydrate to disintegrate within 30 seconds after oral administration, thereby allowing the coated particles to be swallowed.

Abstract: Spray-dried granules comprising pranlukast (A) and one or more saccharide(s) (B) as essential ingredients and further comprising one or more water-soluble polymer(s) (C) and/or one or more surfactant(s) (D); a process for producing the same; and a method for improving adhesiveness of pranlukast are provided. According to the present invention, the very strong adhesiveness of pranlukast is reduced, and pranlukast-containing granules having little adhesiveness, a narrow particle size distribution, and good flow properties can be produced efficiently. The pranlukast-containing granules of the present invention cause no troubles in continuous production of capsules, tablets, and the like, and the resulting pranlukast-containing granules exhibit excellent disintegrating and dispersing properties.

Abstract: The present invention relates to a solid pharmaceutical composition containing (S)-2-(4-isobutylphenyl) propionic acid as active ingredient and it relates to a solid pharmaceutical composition suitable for the preparation of pharmaceutical forms in tablets, sachets and capsules containing (S)-2-(4-isobutylphenyl)-propionic acid as active ingredient. This formulation in tablets contains (S)-Ibupropen, colloidal silica as disintegrating agent, microcrystalline cellulose as diluent and magnesium stearate as lubricant. Tablets are prepared by direct compression of the pharmaceutical composition object of the present invention and may be coated or filmed according to conventional techniques.

Abstract: A process for the production of S(+)-ibuprofen-particles having improved flow properties comprises the steps that coarse-crystalline S(+)-ibuprofen is molten and then in a molten condition is finely distributed in a non-solving medium, preferably in cold water, and is chilled therein. This chilling results in a fine-crystalline primary structure that agglomerates to a secondary structure. In this agglomerate form the product is obtained which is filtered out and is dried. Such particles are suitable for direct pressing of tablets, optionally, tableting auxiliary substances being added, also for the production of tablets having a retarded release of the active substance.

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: Provided is a drug carrier comprising particles of at least one pure active compound which is insoluble, only sparingly soluble or moderately soluble in water, aqueous media and/or organic solvents, wherein said active ingredient is solid at room temperature and has an average diameter, determined by photon correlation spectroscopy (PCS) of 10 nm to 1,000 nm, the proportion of particles larger than 5 .mu.m in the total population being less than 0.1% (number distribution determined with a Coulter counter), and, when introduced into water, aqueous media and/or organic solvents, the active compound has an increased saturation solubility and an increased rate of dissolution compared with powders of the active compound prepared using an ultrasonic probe, a ball mill or a pearl mill, the solid particles having been comminuted, without prior conversion into a melt, by using cavitation or shearing and impact forces with introduction of a high amount of energy.

Abstract: Sustained release formulations include an augmented microcrystalline cellulose, an active agent, and a sustained release carrier and methods for making same are disclosed.

Abstract: The present invention provides a method for preparing a spray-dried compressible granular formulation for preparing pharmaceutical tablets in which hydrolyzed cellulose is used as a granulation aid, the resulting granulations, and pharmaceutical tablets compressed from such granules. In these formulations there is employed from 1 to 97% by weight pharmaceutical active, from about 3 to 99% by weight hydrolyzed cellulose, based on the dry weight of the granulation, and optionally conventional granulation and/or tableting additives such as surfactants, disintegrants and antiadherents/flow aids.

Abstract: Granules having a core are produced by spraying core granules with a dispersion of a low substituted hydroxypropylcellulose (L-HPC), and, if necessary, simultaneously applying a dusting powder. The granules having a core thus obtained exhibit increased granule strength and improved disintegrating property as compared with those produced by known methods. An active ingredient such as a drug can be contained in the dispersion, dusting powder or core granules.

Abstract: The present invention sets forth an enteric coating composition comprising a blend ofa) an alkali-soluble acrylic latex polymer andb) an aqueous solution of ammonium or alkaline salts of cellulose polymers.The invention also sets forth a method for preparing an enterically-coated dosage form and a method for preparing the present compositions.

Abstract: Water soluble macromers are modified by addition of free radical polymerizable groups, such as those containing a carbon-carbon double or triple bond, which can be polymerized under mild conditions to encapsulate tissues, cells, or biologically active materials. The polymeric materials are particularly useful as tissue adhesives, coatings for tissue lumens including blood vessels, coatings for cells such as islets of Langerhans, coatings, plugs, supports or substrates for contact with biological materials such as the body, and as drug delivery devices for biologically active molecules.

Abstract: A pulsatile drug delivery system comprising of a plurality of particles is able to deliver drug in any desired patterns. A plurality of particles with multi-layer core capable of short-pulse release interlaced with long-duration release is designed for delivery of multi-agents simultaneously or sequentially, or single agent, according to a pre-programmed profile.

Abstract: An enteric preparation prepared by coating a solid dosage form with a fine powder enteric coating agent while spraying a liquid plasticizer.

Abstract: A granulate, containing a drug having a solubility in water of 1:>10 and .ltoreq.15 weight percent of a water dispersible hydrocolloid incorporated into a fast-disintegrating and fast-dissolving composition.

Abstract: A controlled release nifedipine tablet which comprises:(a) a homogeneous compressed core which comprises:(i) a medicament;(ii) a water soluble osmotic compound(iii) one or more osmotic polymers; and(b) a membrane coating which completely covers said core tablet which comprises a mixture of:(i) a water insoluble pharmaceutically acceptable polymer; and(ii) an enteric polymer.

Abstract: The dissolution at pH 6.5 of prednisolone metasulphobenzoate or a pharmacologically acceptable salt thereof from a non-disintegratable solid enteric composition comprising the prednisolone metasulphobenzoate in an excipient matrix is increased by the presence in the matrix of a rheological modifying agent, especially croscarmellose, in an amount of at least 5 percent by weight of the composition but insufficient to cause disintegration. Preferably the composition is in the form of pellets coated with an enteric coating which is substantially insoluble below pH 7 and contained in a capsule or tablet coated with an enteric coating which is soluble at a pH in the range pH 5.5 to pH 7. The coated capsules and tablets are for use in the treatment of inflammatory bowel disease, especially ulcerative colitis and Crohn's disease.

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: Process for preparing an oral rapidly disintegrating dosage form of a hydrophobic pharmaceutically active substance comprising forming a suspension of the hydrophobic pharmaceutically active substance in a solvent containing a pharmaceutically acceptable surfactant together with a water-soluble or water-dispersible carrier material, forming discrete units of the suspension and removing solvent from the discrete units under conditions whereby a network of the carrier material carrying a dosage of the hydrophobic pharmaceutically active substance is formed.

Abstract: A solid oral dosage form for the treatment of gastrointestinal disorders comprising a therapeutically effective amount of a therapeutically effective amount of guanidinothiazole compound; and a therapeutically effective amount of an antacid wherein the pharmaceutical and an antacid are separated by a barrier which is substantially impermeable to an antacid.