Abstract: Rapid-release S(+)-ibuprofen pellets are proposed whose bioavailability is comparable to that of commercially available racemate formulations. The rapid release of the active substance is promoted by using small amounts of basic inorganic salts, preferably sodium carbonate, or dilute alkali metal hydroxide solutions. Pellets with an active substance content of 90-99% by weight are obtainable in this way. The pellets are suitable for the application of coatings. Pellets with a protective coating can be compressed directly to tablets in this form and with small amounts of suitable tableting adjuncts. The use of the pharmacologically active S(+)-ibuprofen and of the small amounts of adjuncts required makes it possible to prepare compact pharmaceutical forms.

Abstract: Humate, a composition of primarily humic acids, carbon, and organic matter, is used as a human dietary supplement. The humate may be mixed with food, liquid drinks, or flavoring and ingested. The powder, granule, or water-soluble powder form of humate may also be mixed with other known dietary supplements such as multi-vitamins and be formed into capsules and tablets. The preferred humate is mined from the Menefee Geological Formation in Northwestern New Mexico.

Abstract: The present invention is related to new oral hygiene compositions that have improved foam, viscosity, clarity and good taste due to the inclusion of a new type of alkyl aldonamide compound, specifically heteroatom containing alkyl aldonamide compounds.

Abstract: A sustained-release multi-granule tablet is obtained by compressing sustained-release granules, which contains a basis, and a formulation adjuvant. Each of the granules has been coated in advance with a layer of the formulation adjuvant and/or a layer of a mixture of the formulation adjuvant and the basis. The tablet releases an active substance at a suitable velocity into the digestion tract, resulting in that the inbalance in the absorption of the drug in each patient and among individual patients is minimized to achieve maximum bioavailability.

Abstract: Articles for the controlled delivery of an active substance into an aqueous phase by erosion of surfaces of the articles at a substantially constant and pH-independent rate, the articles comprising a matrix of crystalline polyethylene glycol polymer and a non-ionic emulsifier having an HLB value in the range of from about 4 to about 16 dispersed in the matrix in an amount of between about 2% and 50% by weight of the crystalline polyethylene glycol polymer and the emulsifier, the emulsifier having at least one domain which enables the emulsifier to become emulsified in the melted crystalline polyethylene glycol polymer and being selected from the group consisting of a fatty acid ester and a fatty alcohol ether, the active substance being dispersed in the matrix or located in geometrically well-defined zones within the crystalline PEG phase or dispersed in the emulsifier and, optionally, a filler.

Abstract: An oral dosage form of azithromycin which does not exhibit an adverse food effect; Specific azithromycin oral dosage forms including tablets, powders for oral suspensions and unit dose packets; Methods of treating microbial infections with the dosage forms; And therapeutic packages containing the dosage forms.

Abstract: A method of making solid oral dosage form for the treatment of gastrointestinal disorders comprising a therapeutically effective amount of a pharmaceutical suitable for the treatment of gastric disorders selected from the group consisting of cimetidine, ranitidine, famotidine, diphenoxylate, loperamide, loperamide-N-oxide, pharmaceutically acceptable salts thereof and combinations thereof; and a therapeutically effective amount of simethicone wherein the pharmaceutical and simethicone are separated by a barrier. The barrier is formed by coating with a polymer impermeable to simethicone.

Abstract: The effervescent mixture contains at least one acidic, insoluble or slightly soluble pharmaceutical active ingredient in the form of its soluble alkali metal salt or lysinate, which is present as an intimate mixture with the alkaline component and preferably coats the particles of the alkaline component of the effervescent system, for example sodium bicarbonate and/or sodium carbonate. Both components in very finely powdered form may also be present as granules, with the aid of a binder. In particular, the effervescent mixture contains, per 100 parts of active ingredient, at least 0.5 part, preferably 1 to 3 parts, of a surfactant, in particular dioctyl sulfosuccinate, and/or at least 1 part, preferably 3 to 5 parts, of a binder or suspending agent, in particular polyvinylpyrrolidone. The acidic component of the effervescent system is passivated on the surface.

Abstract: There is disclosed a stable pharmaceutical solid composition comprising enalapril as the sodium salt, which is made by the steps of:i) mixing enalapril maleate with a carrier, an alkaline sodium compound, and waterii) drying the wet mass, and;iii) further processing the resultant dried mass into tablets.When the water is added in the aforesaid process, an acid-base reaction occurs which converts the enalapril maleate into the more stable enalapril sodium salt.

Abstract: An alstonine composition is useful as a selective marker of tumor cells and/or of chromosomal aberrations, and for the detection thereof by measurement of fluorescence at about 375 nm. Thus, an alstonine preparation can be used as a diagnostic agent designed for selective detection of tumoral diseases, and in cytogenetics. The diagnostic agent has application in preoperative, peroperative and postoperative diagnoses.

Abstract: The present invention relates to a novel pharmaceutical composition for the preparation of effervescent powders or tablets incorporating ibuprofen or one of its pharmaceutically acceptable salts as the active ingredient. This composition comprises an effective amount of ibuprofen or one of its pharmaceutically acceptable salts; a pharmaceutically acceptable effervescent system comprising at least one alkali metal carbonate and at least one organic acid, preferably in a sufficient amount to give a pH below about 8; and at least one pharmaceutically acceptable antioxidant in a sufficient amount to stabilize the ibuprofen. This composition has a remarkable stability both in powder form and in tablet form.

Abstract: This invention relates to the use of purified spray dried animal plasma as a binder for tablet pharmaceutical compositions. Spray dried plasma demonstrates good tablet formation as a direct compression vehicle or solution binder, for conventional and sustained release compositions.

Abstract: Enalapril maleate is unstable when associated with many excipients commonly used in the manufacture of pharmaceutical compositions. Stable solid compositions are provided by mixing enalapril maleate into a carrier that is comprised primarily of water-soluble carbohydrates and contains a lubricant other than magnesium stearate, a preferred lubricant being zinc stearate.

Abstract: A whitening embellisher includes, as an active ingredient, teprenone (chemical name: geranylgeranyl-acetone). A whitening and beautifying composition includes teprenone and one or more substances selected from kojic acid, L-ascorbic acid and the like.The whitening embellisher, and whitening and beautifying composition prevent the skin from pigmenting and darkening due to sunburn and/or aging, and quicken fading, and hence make spots and freckles inconspicuous when the preparations are used for external application as a cream or milky lotion.

Abstract: A controlled release pharmaceutical tablet is disclosed which is based on:(a) a compressed core which contains:(i) a medicament;(ii) from 5 to 20% by weight of a water soluble osmotic agent based on the total weight of the compressed core;(iii) a water soluble pharmaceutically acceptable polymeric binder;(iv) a conventional pharmaceutical excipient; and(b) a dual layer membrane coating around said core which consists essentially of:(i) a first inner coating layer for sustained release of the medicament, said inner coating layer consisting essentially of a plasticized water insoluble pharmaceutically acceptable polymer and a pharmaceutically acceptable water soluble polymer, and;(ii) a second outer coating layer for immediate release of a medicament, said outer coating layer consisting essentially of an effective amount of a medicament and a water soluble polymer.The controlled release formulation is suitable for the once-a-day administration of medicaments.

Abstract: The present invention concerns a smoking substitute composition wherein nicotine is the form of an inclusion complex between nicotine and a cyclodextrincompound.

Abstract: The invention relates to a novel diffusion-osmotic controlled drug-release pharmaceutical composition containing a one-layer tablet core including a polymeric film-coat, a therapeutically active agent and a hydrophilic polymer; if desired, a two-layer tablet core including active agent and hydrophilic polymer in the first layer thereof and a hydrophilic polymer in the second layer thereof; at least one bore on the part of film-coat in contact with the core or core layer containing the active agent; and, if desired, containing one or more bore(s) in the part thereof in contact with the second layer containing the hydrophilic polymer, which comprises an ammonium methacrylate copolymer as coating material and hydroxypropyl-methylcellulose as hydrophilic polymer. The composition according to the invention is useful for preparing controlled drug-release tablets containing as active agents e.g. .beta.-adrenergic inhibitors (e.g. propranolol) calcium-antagonists (e.g.

Abstract: An ibuprofen-containing medicament which contains ibuprofen only in the (S)-(+)-form is disclosed. (S)-(+)-ibuprofen is more than twice as active as the racemate which has until now been used in the treatment of rheumatism. This permits reduction of the quantity of active ingredient and the size of the tablets or dragees.

Abstract: A granulated composition for direct tableting, comprising non-pressed or difficulty pressed, water-soluble, crystalline pharmaceutical substances, binder, lubricant and water, contains at least 98 wt. % of a pharmaceutically active component. The tablets manufactured from said composition have high hardness and the controllable time of dissolution. A method for preparing said composition consists in that the powder of a pharmaceutical substance is pre-granulated with water or its aqueous solution, the resultant granulate is then subjected to subsequent granulation with a binder solution, dried and powdered with lubricant.

Abstract: A colonic delivery system for delivering a drug to the colon is provided. The system comprises a drug in combination with a matrix, wherein the matrix comprises a saccharide-containing polymer. According to the invention, the matrix is resistant to chemical and enzymatic degradation in the stomach and small intestine. The matrix is degraded in the colon by bacterial enzymatic action, and the drug is released. The system is useful for targeting drugs to the colon in order to treat colonic disease. The system is also useful for enteric administration of drugs such as proteins and peptides which are otherwise degraded in the stomach and small intestine.

Abstract: An ibuprofen-containing medicament which contains ibuprofen only in the (S)-(+)-form is disclosed. (S)-(+)ibuprofen is more than twice as active as the racemate which has until now been used in the treatment of rheumatism. This permits reduction of the quantity of active ingredient and the size of the tablets or dragees.

Abstract: The present invention provides a novel formulation of matter and a novel process for making it. In particular, the present invention provides unique and novel 1000 mg tablets of Colestipol hydrochloride having the advantageous properties of hardness and low friability and a novel process for making such tablets.

Abstract: Chewable tablets are made from a coated medicament wherein the coating comprises a mixture of dimethylaminoethyl methacrylate and neutral methacrylic acid ester and a cellulose ester, e.g. cellulose acetate, cellulose acetate butyrate, cellulose triacetate or a combination thereof and optionally polyvinyl pyrrolidone, and a process for making such tablets and a method of providing taste masking and sustained releasing of medicaments utilizing such coatings.

Abstract: A solid dosage form, such as a pharmaceutical tablet, containing a rapidly hydratable konjac glucomannan sustained release excipient such as clarified konjac, cryogenically ground konjac and plasticized konjac. The method of making the tablets by compressing excipient and pharmaceutically active ingredient as dry powders.

Abstract: The present invention relates to a novel pharmaceutical composition for the preparation of effervescent powders or tablets incorporating ibuprofen or one of its pharmaceutically acceptable salts as the active ingredient.This composition comprises:an effective amount of ibuprofen or one of its pharmaceutically acceptable salts;a pharmaceutically acceptable effervescent system comprising at least one alkaline carbonate and at least one organic acid, preferably in a sufficient amount to give a pH below about 8; andat least one pharmaceutically acceptable antioxidant in a sufficient amount to stabilize the ibuprofen.This composition has a remarkable stability both in powder form and in tablet form.

Abstract: Hemorrhoidal compositions containing disaccharide polysulfate-aluminum compounds such as sucralfate, above or in combination with other hemorrhoidal products, as an agent effective for alleviating the symptoms of anorectal disease when topically applied to the human skin. Method for alleviating the symptoms of hemorrhoids in humans. Compositions containing disaccharide polysulfate-aluminum compounds such as sucralfate, alone or in combination with antibiotics, antifungal agents, anti-acne agents, or local anesthetics as an active agent effective in promoting the healing of wounds which are not anorectal when topically applied to the surface of a wound. Method for promoting healing at the surface of a wound in humans.

Abstract: The present invention relates to directly-compressible naproxen or naproxen sodium compositions comprising spray-dried naproxen or naproxen sodium. The present invention further relates the processes for preparing the directly-compressible naproxen or naproxen sodium compositions, to aqueous mixtures containing naproxen or sodium naproxen suitable for spray-drying and useful in the processes for preparing the directly-compressible compositions, to naproxen or naproxen sodium tablets prepared from the directly-compressible compositions, and to the processes for preparing the naproxen or naproxen sodium tablets.

Abstract: The invention relates to effervescent pharmaceutical compositions for oral use comprising an effervescent couple consisting essentially of a base component and an acid component, which components react in the presence of water to generate a gas, and a compound which acts as a 5HT.sub.1 -like receptor agonist or a physiologically acceptable salt or solvate thereof as active ingredient.Methods for the manufacture of such compositions and for their use in the treatment of cephalic pain are also described.

Abstract: New polysaccharide esters are disclosed, and more precisely esters of acidic polysaccharides chosen from the group formed by carboxymethylcellulose, carboxymethyl starch and carboxymethylchitin. These new esters and some esters of the type already known are useful as medicaments, for the manufacture of pharmaceutical and cosmetic preparations, in the field of biodegradable plastic materials and, therefore, for the manufacture of medical, surgical and sanitary articles, as well as numerous other industrial sectors in the place of acidic polysaccharides now in common use.

Abstract: A solid preparation soluble in the buccal cavity, which is composed of a sugar comprising lactose and/or mannitol and 0.1-1.2 w/w%, based on the sugar, of agar and an active ingredient and has a density of 400 to 1,000 mg/ml and such a strength as to withstand the handling in the manufacture thereof. It has such a sufficient practical solubility in the buccal cavity that even the aged or children having difficulty in swallowing a solid preparation, such as a tablet, can take it. It has an exceedingly high strength as compared with conventional open matrix structures and hence can withstand satisfactorily carrying and PTP packaging.

Abstract: A method for reducing abrasion during film coating of susceptible solid dosage forms by applying to an uncoated dosage form, a subcoat containing a pharmaceutically acceptable polyalkylene glycol and the resulting solid pharmaceutical dosage form.

Abstract: The present invention relates to a novel oral dosage form of a bisphosphonic active ingredient for use in treatment of diseases involving bone resorption and formulated in an enteric-coated form for administration to subjects exhibiting upper gastrointestinal tract sensitivity to bisphosphonic acid compounds.

Abstract: A whitening embellisher includes, as an active ingredient, teprenone (chemical name: geranylgeranylacetone). A whitening and beautifying composition includes teprenone and one or more substances selected from kojic acid, L-ascorbic acid and the like. The whitening embellisher, and whitening and beautifying composition prevent the skin from pigmenting and darkening due to sunburn and/or aging, and quicken fading, and hence make spots and freckles inconspicuous when the preparations are used for external application as a cream or milky lotion.

Abstract: A controlled sustained release tablet having at least one year shelf life and containing bupropion hydrochloride, hydroxypropyl methylcellulose and cysteine hydrochloride or glycine hydrochloride with the tablet having a surface area to volume ratio to effectively control bupropion hydrochloride release in the body.

Abstract: Solid compositions of certain cholinergic compounds are stabilized in starch. Especially compositions of corn starch combined or mixed with the 0-substituted-1,2,5,6-tetrahydro-3-pyridine oxime ether, CI-979 HCl, a cognition activator, have been found stable in a heated environment of up to 60.degree. C. over 17 days such that no losses were detected by HPLC analysis. A solid peroral pharmaceutical formulation for the treatment of cognitive disorders is based on the bicomponent composition of active ingredient and stabilizer using appropriate amounts of other excipients or components known in the formulation art.

Abstract: A rapid method to prepare low crystallinity cellulose (crystallinity 15-45% of polymerization 35-150), suitable for use as a direct compression excipient (e.g., binder, disintegrant, and diluent) in pharmaceutical solid dosage forms design and as a bodying and/or film forming agent in the development of sustained- and/or film forming agent in the development of sustained- and/or controlled-release pharmaceutical (topical and transdermal products), cosmetics, agricultural, personal care and like products, is provided by reacting cellulose materials with 85% or higher weight percentage phosphoric acid under controlled sequenced temperature conditions that involve treatment first at room temperature for an hour and then at 50.degree.-55.degree. C./ for 3-6 hours, followed by separating by a precipitation method,. and subsequently isolating as a powder or converting into a head or hydrated form.

Abstract: A process for preparing a pharmaceutical preparation consisting essentially of a lyophilized cake of cyclophosphamide monohydrate and a bulking agent which comprises freezing cyclophosphamide, a bulking agent, and water, lyophilizing part of the water, obtaining and melting a supersaturated cyclophosphamide-bulking agent solution, precipitating cyclophosphamide as a hydrated polymorph, refreezing the solution and lyophilizing the water not bound to cyclophosphamide or the bulking agent.

Abstract: A tableting aid including magnesium carbonate and an oil adsorbed thereon provides useful lubricating and disintegration properties. A free-flowing particulate flavoring additive including magnesium carbonate and a flavor oil adsorbed thereon, is also described.

Abstract: The invention pertains to a process for preparing a phenylalanine-free dietetic product comprising L-amino acids, and optionally comprising carbohydrates, minerals, trace elements and/or vitamins, for persons afflicted with phenylketonuria particularly adults, juveniles and pregnant women. The process comprises preparing a wet batch by dispersing in water the L-amino acids, some or all of the optional components, and at least one fatty material as an emulsifier, after which the wet batch is spray-dried. The spray-dried wet batch is then mixed with additional vitamins and/or carbohydrates and at least one fatty material as a separation agent to produce a mass. The mass thus produced is processed into cores for dragees or tablets, and the dragee or tablet cores are provided with coatings or dragee covers. The dietetic product is used as a nutrition supplement.

Abstract: Pharmacologically inactive spherical seed cores comprising at least 50% by weight of microcrystalline cellulose having an average degree of polymerization of 60 to 375, wherein the spherical seed cores have an average particle size of 100 to 1000 .mu.m, a tapped bulk density of at least 0.65 g/ml, an aspect ratio of at least 0.7, a water absorption capacity of 0.5 to 1.5 ml/g, and a friability of no more than 1%; spherical granules comprising the spherical seed cores coated with a powdery layer comprising active ingredients and having an outer layer of coating provided on the powdery layer; and a process for the production of spherical granules, comprising the steps of coating the spherical seed cores with powder comprising active ingredients using an aqueous binding solution, spraying an aqueous solution or suspension of a coating agent thereon, and drying the resulting coated granules.

Abstract: Disclosed are dry pharmaceutical preparations containing potent steroidal medicinal agents in combination with an excipient capable of binding the agent to an extent greater than 80% and a having a demixing potential of less than 10% for said agent. Such excipients include spray-dried polyalcohols, granulated .alpha.-lactose monohydrate, or mixtures thereof. Also disclosed is a process of manufacturing stable tablets containing nearly identical amounts of at least one steroidal medicinal agent present in each tablet in an amount varying from 0.005 to 0.5 percent by weight of the tablet. Also disclosed is a dry mix consisting essentially of 1 to 100 parts, by weight, of at least one medicinal agent uniformly distributed throughout 2000 to 20,000 parts, by weight, of the described excipients. The mixture can be used to make dry dosage forms such as capsules, tablets, powders, and slugged granulates.

Abstract: Pharmaceutical forms of pimobendan for oral administration comprising citric acid, whereby a constant, satisfactory resorption is ensured even when there are major pH fluctuations in the gastrointestinal tract.

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 invention discloses an aqueous granulating solution containing sodium, potassium or mixed sodium potassium salt of an edible organic acid selected from the group consisting of citric, malic, tartaric and fumaric acid and optionally containing sodium or potassium bicarbonate. The granulating solution is especially useful for granulating finely divided solids including acetaminophen, ketoprofen or calcium carbonate. The resulting granulate may be used to prepare a swallow tablet or mixed with an edible organic acid and the mixture tableted to provide an effervescent tablet without resorting to controlled reaction or special handling techniques.

Abstract: A salt-excretion promoting composition, characterized by containing (i) 10 parts by weight of agar and (ii) 1 to 15 parts by weight of at least one polysaccharide selected from the group consisting of sodium alginate, .lambda.- and .kappa.-carrageenan and xanthane gum.

Abstract: A parmaceutical preparation consisting essentially of a lyophilized cake of cyclophosphamide monohydrate and lactose prepared by the process of freezing cyclophosphamide, lactose and water, lyophilizing part of the water, obtaining and melting a supersaturated cyclophosphamide-lactose solution, precipitating cyclophosphamide as a hydrated polymorph, refreezing the solution and lyophilizing the water not bound to cyclophosphamide or lactose.

Abstract: The present invention relates to compositions for the sustained release of drugs and to methods for the production of such compositions. In one embodiment, somatotropin is layered onto non-pareil seeds, which, in turn are sprayed with a glycine solution. Next, a coating of a wax mixture is applied.

Abstract: A composition for solid pharmaceutical preparations containing a vitamin D.sub.3 derivative capable of permitting the derivative to be uniformly distributed in the composition while being stabilized. The composition contains an excipient consisting of mannitol and sugar, a degradative agent consisting of hydroxypropyl cellulose, and a binder consisting of polyvinyl pyrrolidone and hydroxypropylmethyl cellulose.

Abstract: The present invention is directed to gelatin treated polyhydric alcohol compositions, their preparation, and to pharmaceutical lozenges prepared therefrom. The pre-granulation of a polyhydric alcohol with an aqueous gelatin solution prior to compression, produces lozenges having a delayed rate of dissolution.

Abstract: The invention relates to a process for the preparation of a tablet or dragee composition containing a moisture-, heat- and light-sensitive compounds having monoclinic crystalline structure as active ingredients, which comprises homogenizing the active ingredient with 0.2 to 1.5 parts by weight of an anhydrous alkaline earth metal salt and 0.5 to 2.5 parts by weight of microcrystalline cellulose calculated for the active ingredient and optionally with one or more pharmaceutically acceptable carrier(s) and/or additive(s) and compressing the homogeneous mixture obtained to tablets in a manner known per se and, if desired, coating the tablet thus obtained in a manner known per se.