Abstract: Injectable compositions having improved injectability. The injectable compositions include microparticles suspended in an aqueous injection vehicle having a viscosity of at least 20 cp at 20° C. The increased viscosity of the injection vehicle that constitutes the fluid phase of the suspension significantly reduces in vivo injectability failures. The injectable compositions can be made by mixing dry microparticles with an aqueous injection vehicle to form a suspension, and then mixing the suspension with a viscosity enhancing agent to increase the viscosity of the fluid phase of the suspension to the desired level for improved injectability.

Abstract: There is disclosed a method for stabilizing active substances that are unstable in acidic medium, unstable when stored for longer periods of time in the presence of water and at the same time sensitive to heating, by means of anhydrous granulation of active substances and dried pharmaceutically acceptable auxiliary substances for the preparation of pellet cores or granules. All pharmaceutically acceptable auxiliary substances employed are dried before use so that their weight loss at drying is less than 1.0% of the total weight of the pharmaceutically acceptable auxiliary substance, preferably less than 0.5%. Organic solvents used in process of anhydrous granulation should contain less than 0.2% of water. A novel pharmaceutical formulation with controlled release of active substances that are unstable in acidic medium, unstable when stored for longer periods of time in the presence of water and at the same time sensitive to heating, is disclosed as well.

Abstract: Particles of water insoluble biologically active compounds, particularly water-insoluble drugs, with an average size of 100 nm to about 300 nm, are prepared by dissolving the compound in a solution then spraying the solution into compressed gaz, liquid or supercritical fluid in the presence of appropriate surface modifiers.

Abstract: A method for controlling the formation of a hydroxyapatite bone filler from dry calcium phosphate precursors in an aqueous solution uses coated sodium phosphate powder. The sodium phosphate powder is coated with a water soluble cellulose. Until the cellulose dissolves in the aqueous solution setting of the calcium phosphate cements proceeds slowly but when the exposed sodium phosphate particles start to solubilize in the aqueous solution the setting rate increases.

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: A gel rehydration electrolyte composition provides a convenient and effective way of replenishing lost fluid and electrolytes. The gel rehydration electrolyte composition masks unpleasant tastes of electrolyte and is readily consumed by young children and elderly who cannot tolerate the liquid or frozen forms of electrolytes.

Abstract: An intravaginal bio-erodible microbicidal barrier device. The device comprises (a) at least one micronized compound selected from the group consisting of cellulose acetate phthalate and hydroxypropylmethylcellulose phthalate, and (b) at least one water soluble or water dispersible cellulose compound selected from the group consisting of hydroxypropylmethylcellulose, methylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, hydroxyethylmethylcellulose, hydroxyethylethylcellulose and hydroxypropylethylcellulose. The device is prepared by a combination of foaming, freezing and freeze-drying processes.

Abstract: The present invention relates to a new layering process, in particular to a process for the manufacture of multiparticulate solid oral dosage forms based on a dry spray layering technique optionally with electrostatic attraction. The invention also relates to an apparatus for use in the process.

Abstract: Conditioning of the surface of silica-based glass or ceramic by differential immersion in a serum protein-containing solution, and the resultant microporous Ca-P surface layer having serum-protein like organic molecules, as defined herein intermingled throughout, is described.

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 method for controlling the formation of a hydroxyapatite bone filler from dry calcium phosphate precursors in an aqueous solution uses coated sodium phosphate powder. The sodium phosphate powder is coated with a water soluble cellulose. Until the cellulose dissolves in the aqueous solution setting of the calcium phosphate cements proceeds slowly but when the exposed sodium phosphate particles start to solubilize in the aqueous solution the setting rate increases.

Abstract: The present invention generally relates to stable pharmaceutical compositions, and methods of making and administering such compositions. In one aspect, the invention features stabilized pharmaceutical compositions that include pharmaceutically active ingredients such as levothyroxine (T4) sodium and liothyronine (T3) sodium (thyroid hormone drugs), preferably in an immediate release solid dosage form. Also provided are methods for making and using such immediate release and stabilized compositions.

Abstract: The invention relates to oral pharmaceutical compositions useful as aldosterone receptor blockers comprising the active agent micronized eplerenone in an amount of about 10 mg to about 1000 mg and one or more carrier materials.

Abstract: The present invention relates to water-insoluble solid particles, especially pigments, which characteristically are coated with at least one layer of at least one product resulting from the reaction between at least one molecule capable of becoming hydrated in contact with water and at least one lipophilic molecule. It further relates to cosmetic, pharmaceutical and agricultural compositions comprising such particles and to the manufacture and use of said particles.

Abstract: A liquid composition for oral administration comprising a pharmaceutically active medicament coated with a taste masking effective amount of a polymer blend of (a) dimethylaminoethyl methacrylate and neutral methacrylic acid ester (MM/MAE) and (b) a cellulose ester, in an aqueous vehicle, wherein the polymer weight ratio of the cellulose ester to the MM/MAE is about 40:60 to about 90:10, preferably about 60:40. The liquid composition utilizes a “reverse enteric coating” which is soluble in the acid pH's of the stomach, generally about 1.0 to 4.0, but relatively insoluble at the non-acidic pH's of the mouth. The coatings provide for rapid release and absorption of the drug, which is generally desirable in the case of liquid dosage forms.

Abstract: This invention is directed to a novel solid matrixed controlled release, oral dosage form where the dosage form contains a therapeutically effective amount of a sulfonylurea or a salt or derivative thereof in the matrix. Further, the use of an aqueous alkalizing medium affords substantially complete bioavailability of the drug from the matrix of the tablet. The core tablets may optionally be coated with a coating material in the range of 2% to 10% with an enteric material or with a water insoluble material like ethyl cellulose.

Abstract: The present invention relates to microcapsules with an aqueous core containing at least one water-soluble cosmetic or dermatological active principle, and with a polymeric and/or waxy envelope, in which the said envelope consists of at least one polymer chosen from polycaprolactone, poly(3-hydroxybutyrate), poly(ethylene adipate), poly(butylene adipate), cellulose esters of at least one C1-C4 carboxylic acid, copolymers of styrene and of maleic anhydride, copolymers of styrene and of acrylic acid, styrene-ethylene/butylene-styrene block terpolymers, styrene-ethylene/propylene-styrene block terpolymers and terpolymers of ethylene, of vinyl acetate and of maleic anhydride, and/or of at least one wax chosen from beeswax, polyglycerolated beeswax, hydrogenated plant oils, paraffin with a melting point above 45° C., and silicone waxes.

Abstract: A controlled release diltiazem dosage formulation comprising a plurality of active pellets coated with an extended release coating wherein the active pellets contain diltiazem or a pharmaceutically acceptable salt, a pharmaceutically acceptable inert seed and a binder and the extended release coating contains a water insoluble water permeable polymer, a channeling agent, a lubricant and optionally a surfactant. A single batch intermittent method of manufacturing a heterogeneous population of extended release pellets for use as a dosage formulation is also disclosed.

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: The invention concerns the formulation and method of fabricating rapid dispersion spheroids which can be heavily charged with active substances. These spheroids are formulated using at least one active substance, specifically a solution of vegetable origin, absorbed and/or adsorbed on a dry technological mixture with a slightly substituted hydroxypropylated cellulose ether base at the level of core groups &bgr;-O-glucopyranosil, preferably characterized by having a substitution rate of about 11% and a water soluble fractional percentage of about 4.29%. The spheroids are obtained by an extrusion and spheronization process. This invention is of interest in the fields of health, hygiene, dietetics, cosmetology, nutrition, and agriculture; it may concern humans or animals.

Abstract: A pharmaceutical dosage form comprising a tablet containing a non-steroidal anti inflammatory drug and misoprostol, wherein the non-steroidal anti inflammatory drug is in the form of coated pellets.

Abstract: The invention concerns an oral formulation of cisplatin, in the form of controlled-release microgranules, and its method of formulation by grossing in an aqueous medium. The invention also concerns a pharmaceutical preparation containing controlled-release cisplatin microgranules, optionally combined with an anticancer agent, to be used in anticancer therapy. The invention further provides a use for these microgranules for making orally administered medicaments for polychemotherapy or in combination with radiotherapy.

Abstract: Dysglucaemia is treated and/or prevented by the administration of granulated starch, enzymatically degraded and releasing reducing sugars at a rate, adjusted to the metabolism of the patient, suffering from dysglucaemia. For example nocturnal hypoglycaemia in diabetic patients is prevented by administering to said patients a granulate or tablets comprising granulated cornstarch, and preferably also heat treated cornstarch and a low calorie sweetener. The inventive granulation minimises the available surface area and retards the enzymatic degradation of the cornstarch and ensures a controlled, e.g. a substantially linear release of reducing sugars, such as glucose, and a stable blood glucose level during several hours. The granulate or tablets are low in calories and contain no free sugar.

Abstract: A pharmaceutical preparation containing Tolperison or a salt thereof as an active ingredient in the form of a racemic mixture which can be a 50/50/-racemat or a racemat with the perponderant content of the (−) -isomer of Tolperison. The pharmaceutical preparation is formulated as a solid or liquid medicament for oral administration. The active ingredient Tolperison that is present as 50/50-racemat or as racemat with a preponderant content of the (−)-isomer or the (+)-isomer is liberated from the preparation in the human body in a delayed manner and preferably in the intestinal canal.

Abstract: An edible, hardenable coating composition is disclosed containing microcrystalline cellulose, a film forming amount of propylene glycol alginate, and a strengthening polymer, optionally in combination with at least one of a plasticizer, a surfactant, or a filler. The coating composition of the present invention may be applied to pharmaceutical and veterinary solid dosage forms, confectionery, seeds, animal feed, fertilizers, pesticide tablets, and foods and provides an elegant prompt release coating which does not retard the release of active ingredients from the coated substrate.

Abstract: Injectable compositions having improved injectability. The injectable compositions include microparticles suspended in an aqueous injection vehicle having a viscosity of at least 20 cp at 20° C. The increased viscosity of the injection vehicle that constitutes the fluid phase of the suspension significantly reduces in vivo injectability failures. The injectable compositions can be made by mixing dry microparticles with an aqueous injection vehicle to form a suspension, and then mixing the suspension with a viscosity enhancing agent to increase the viscosity of the fluid phase of the suspension to the desired level for improved injectability.

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 process for manufacturing coated particles of &ggr;-aminobutyric acid analogue, whose lactam content by weight relative to the weight of &ggr;-aminobutyric acid analogue is less than 0.5% is disclosed. The process is characterized in that a coating solution of at least one polymer in an organic solvent is sprayed onto the particles of &ggr;-aminobutyric acid analogue.

Abstract: A liquid composition for oral administration comprising a pharmaceutically active medicament coated with a taste masking effective amount of a polymer blend of (a) dimethylaminoethyl methacrylate and neutral methacrylic acid ester (MM/MAE) and (b) a cellulose ester, in an aqueous vehicle, wherein the polymer weight ratio of the cellulose ester to the MM/MAE is about 40:60 to about 90:10, preferably about 60:40. The liquid composition utilizes a “reverse enteric coating” which is soluble in the acid pH's of the stomach, generally about 1.0 to 4.0, but relatively insoluble at the non-acidic pH's of the mouth. The coatings provide for rapid release and absorption of the drug, which is generally desirable in the case of liquid dosage forms.

Abstract: This invention in general relates to novel pharmaceutical compositions for acid labile substances as well as for methods of making such. Specifically, the invention provides a pharmaceutical composition comprising about 1 to 75% by weight acid labile compound, up to about 5% by weight disintegrant, at least one protector coat layer used to separate and protect the acid labile substance from acid reacting groups and gastric juice, and at least one enteric coat layer which surrounds the protector coating layer and ensures delivery of over 80% the acid labile substance to the small intestine.

Abstract: Solid modified release dosage forms, prepared from melt granulated compositions comprising (A) one or more hydrophilic cellulose ether polymers, (B) a hydrophilic melt binder, and (C) a therapeutically active ingredient.

Abstract: The invention concerns an oral formulation of cisplatin, in the form of controlled-release microgranules, and its method of formulation by grossing in an aqueous medium. The invention also concerns a pharmaceutical preparation containing controlled-release cisplatin microgranules, optionally combined with an anticancer agent, to be used in anticancer therapy. The invention further provides a use for these microgranules for making orally administered medicaments for polychemotherapy or in combination with radiotherapy.

Abstract: The invention relates to a substantially nonaqueous skin cleansing composition comprising a granulated product obtained by granulating particles of a surfactant selected from the group consisting of nonionic surfactants, amphoteric surfactants and anionic surfactants with a binder. The composition scarcely causes damage to and itch on the skin, can give an effective massaged feeling and has excellent cleanability.

Abstract: The present invention provides taste-masked microcapsules of Linezolid or the like (any member of the orally effective oxazolidinone or macrolide antibiotics), suitable for oral administration as a suspension, a fast-disintegrating, effervescent or chewable tablet, and more specifically relates to such oral dosage forms in which the bitter taste of Linezolid contained therein is masked by a combination of microencapsulation by solvent coacervation and subsequent functional membrane coating on said microcapsules. The taste-masked granules thus obtained release less than 5%, most preferably less than 3%, at a pH of 4.0 to 6.0 (pH of the saliva) but rapidly release (as a burst) at pHs of the upper intestinal tract. The taste-masked granules are optionally blended with other pharmaceutically acceptable excipients and filled into unit dose containers or compressed into fast-disintegrating/effervescent/chewable tablets.

Abstract: A process for producing an oral, controlled release preparation of tramadol or a physiologically compatible tramadol salt having a storage stable active substance release profile by coating the active substance preparation with an aqueous ethylcellulose dispersion which contains at least one physiologically compatible, lipophilic diester of a C6-C40 aliphatic or aromatic dicarboxylic acid and a C1-C8 aliphatic alcohol as plasticizer, and, during coating, drying the coating at conventional temperatures, with the result that a storage stable active substance release profile is obtained even without subsequent heat treatment. Optionally, in order to increase the active substance release profile without impairing the storage stability of the preparation, a heat treatment may be performed at temperatures of >35° C. until a desired, increased active substance release profile is achieved.

Abstract: A method for making the potassium and sodium salts of (−)-hydroxycitric acid and mixtures thereof workable, non-hygroscopic and non-reactive in acidic media by encasement in hydrophobic and acidophobic polymers. The calcium and magnesium salts of (−)-hydroxycitric acid likewise can be rendered nonreactive in acidic media. The resulting products are suitable for tableting, encapsulation and use in other dry media for weight loss, appetite suppression, improvements in fat metabolism and postprandial lipemia and other pharmaceutical purposes. Further, the products of this invention can be made nonreactive as components of acidic liquid drink mixes and snack bars and can be used in the production of controlled release administration formats.

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: The present invention provides a complex of human growth hormone and zinc containing human growth hormone and zinc at a molar ratio of about 1:1.6 to about 1:2.4, and a sustained-release preparation which comprises the complex of human growth hormone and zinc and a biodegradable polymer and which has a high entrapment ratio of human growth hormone and exhibits a stable sustained-release suppressing the initial burst.

Abstract: A powdery nasal composition comprising a drug and colloidal cellulose is provided. The composition is a nasal composition providing a superior absorption activity for the drug.

Abstract: A method of producing a free flowing and compressible liquid/power admixture of an active drug substance, by converting the active substance into a liquisolid system. This is accomplished by introducing by the drug into a non-volatile liquid or a mixture of non-volatile and volatile liquids to from a mixture, selecting at least one solid carrier material and admixing these components to produce a non-adherent, free-flowing and compressible liquid/power mass admixture, the amounts of drug and carrier being selected to optimize flow and compressibility.

Abstract: The invention is directed to oral modified/controlled release drug formulations which provide a rapid initial onset of effect and a prolonged duration of effect. Preferably, the peak concentration is lower than that provided by the reference standard for immediate release formulations of the drug, and the duration of effect falls rapidly at the end of the dosing interval.

Abstract: An improved termite bait composition comprises a powdered cellulosic attractant having a particle size in the range of approximately 1 to 100 micrometers and a termite killing agent. Also disclosed are a method for controlling termites by applying the termite bait composition to a termite infested area and a termite bait composition package for use in a termite bait station comprising the termite bait composition contained within a termite attractive package.

Abstract: An easy to swallow pharmaceutical composition consists of one or several coated particles with a core which contains an active substance and a coat with one or several layers. The coating layer(s) contain at least one hydratable, pharmaceutically acceptable polymer which in contact with saliva or water forms a coherent, mouldable, viscous mass with a slippery surface which does not adhere to the mucous membranes of the mouth and which prevents the active substance-containing particles from leaving the mass and releasing the active substance in the mouth cavity. The coating layer or the outermost coating layer contains an effective amount of at least one salivation promoting agent. The formation of a mouldable, slippery mass and the taste-masking properties of the coating make the composition suitable in particular for administering highly dosed or bad tasting active substances, and can preferably be swallowed even without any liquid.

Abstract: The present invention provides an improved process for the preparation of a agglomerated solid dosage form, comprising preparing an aqueous slurry of microcrystalline cellulose and a microcrystalline cellulose compressibility augmenting agent and an active agent. The augmenting agent is capable of physically restricting the proximity of the interface between adjacent cellulose surfaces and/or inhibiting interactions between adjacent cellulose surfaces, for example, via the creation of a hydrophobic boundary at cellulose surfaces. The resulting aqueous slurry is dried in a manner which inhibits quasi-hornification, thereby obtaining an agglomerated material which is directly compressible into a solid dosage form.

Abstract: The invention concerns pharmaceutical forms of administration that are in the form of pellets which contain a retarding agent in which the release rate of the active substance is not delayed or is substantially identical compared to corresponding pellets that contain no retarding agent. The release rate of these rapidly disintegrating pellets is at least about 90% within a time period of 30 minutes. In addition the present invention also concerns processes for the production these pellets.

Abstract: The invention provides a sustained release composition free of food effect comprising a core comprising an active agent except for carbamazepine or verapamil, and a coating comprising, based on the weight of the coating, from 30 to 80% of a gastroresistant polymer and from 10 to 40% of a hydrophilic silicon dioxide. The invention also provides a method of alleviating food effect in a pharmaceutical composition. The invention also provides a dispersion useful thereof.

Abstract: The present invention relates to a potassium containing dosage form which is capable of rapidly disintegrating in a patient's mouth to form an easy to swallow slurry.

Abstract: An oral pharmaceutical dosage form comprising an acid susceptible proton pump inhibitor and one or more NSAIDs in a fixed formulation, wherein the proton pump inhibitor is protected by an enteric coating layer. The fixed formulation is in the form of an enteric coating layered tablet, a capsule or a multiple unit tableted dosage form. The multiple unit dosage forms are most preferred. The new fixed formulation is especially useful in the treatment of gastrointestinal side-effects associated with NSAID treatment.

Abstract: A microcapsule capable of thoroughly encapsulating environmentally-sensitive or volatile core materials and capable of releasing said core material on contact with water. A process for manufacture of water soluble microcapsules comprising the admixture of a water soluble cellulosic material, a water soluble glucopyranosidyl material, at least two surfactants and core material, subjecting said mixture to an abrupt pressure change and drying the pressure-treated mixture.

Abstract: Provided herein are compositions and methods of making compositions of ibuprofen in combination with a narcotic analgesic. Specifically provided is a pharmaceutical tablet composition comprising ibuprofen; a narcotic analgesic; colloidal silicon dioxide; a filler selected from the group consisting of microcrystalline cellulose and powdered cellulose; a disintegrant selected from the group consisting of croscarmellose sodium, crospovidone, and sodium starch glycolate; a binder consisting of an akylhydroxy methylcellulose; a starch; and a lubricant.