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: The present invention is concerned with a fast-dissolving tablet for oral administration comprising as an active ingredient a therapeutically effective amount of galanthamine hydrobromide (1:1) and a pharmaceutically acceptable carrier, characterized in that said carrier comprises a spray-dried mixture of lactose monohydrate and microcrystalline cellulose (75:25) as a diluent, and a disintegrant; and with a direct compression process of preparing such fast-dissolving tablets.

Abstract: The present invention provides water-soluble, extended-release chemical formulations, in tablet form, for urine pretreatment, that require minimal, if any, use of a binder component, yet are non-dusting, pliable, structurally strong, and not weakened by exposure to aqueous streams. The present invention also provides a simple and reliable method for controlled dispensing of such tableted formulations into a liquid stream that is particularly advantageous for use in micro-gravity environments, such as spacecraft urinal systems.

Abstract: A swellable hydrophillic matrix tablet that delivers drugs in a controlled manner over a long period of time and is easy to manufacture. More specifically, the drug is disposed in a matrix composed of HPMC or polyethylene oxide, in the presence of a salt, which may be a combination of salts. Suitable salts include sodium bicarbonate, sodium chloride, potassium bicarbonate, calcium chloride, sodium bisulfate, sodium sulfite, and magnesium sulfate. Outward diffusion of the drug is controlled by an inwardly progressing hardening reaction between the salt and the dissolution medium, possibly also involving the drug itself.

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

Abstract: A method of producing mechanically stable effervescent tablets with a high dissolving velocity and an according effervescent tablet are described. The effervescent tablets consist of at least one active substance or of a combination of active substances, of at least one binder, of possibly carriers as sweeteners, flavors, colorings, scents, softeners, bleaches, and of sherbets. In producing, propylglycol or glycerin is used as a binder for the effervescent tablets, and the active substances or the combination of active substances and possibly carriers are mixed with the binder. Afterwards, the sherbets are added to this mixture in an air-conditioned room. Then, the mixture including the sherbets is formed into tablets.

Abstract: Water-soluble compositions comprising a lipophilic compound and a solubilizing agent of the general formula:{X--OOC--[(CH.sub.2).sub.n --COO].sub.m }.sub.p --Y (I)wherein:X is a residue of a hydrophobic moiety,Y is a residue of a hydrophilic moiety,p is 1 or 2,m is 0 or 1, andn is an integer greater than or equal to 0are disclosed. The lipophilic compound is preferably selected from the group consisting of water-insoluble ubiquinones, ubiquinols, vitamins, provitamins, polyene macrolide antibiotics, and mixtures thereof. The hydrophobic moiety is preferably a sterol or a tocopherol and the hydrophilic moiety is preferably a polyalkylene glycol. In preferred embodiments, the sterol is cholesterol or sitosterol, the tocopherol is a-(+)-tocopherol, the polyalkylene glycol is a polyethylene glycol or its methyl monoether having an average molecular weight between 600 and 1000, p is equal to 1 or 2, m is equal to 0 or 1 and n is an integer between 2 and 18.

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

Abstract: An oral-delivery pharmaceutical composition for reducing the gastric irritation effect of an NSAID in the upper GI tract of a mammal. The composition includes (a) a mucosal protective amount of a pharmaceutically-acceptable hydrocolloid gum obtainable from higher plants, (b) a dispersion-enhancing amount of another excipient and (c) a therapeutically-effective amount of an NSAID. Also disclosed is a process for preparing the composition and a method for reducing the gastric irritation effect of the NSAID by administering the composition. Also, disclosed is a composition particularly useful for preparing an aqueous suspension.

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: Solid and liquid pharmaceutical preparations containing cilansetron or its acid addition salts as active substance which include an amount sufficient to stabilize cilansetron against racemization, of a physiologically compatible water-soluble acid additive selected from monobasic or multibasic organic acids having 2 to 12 carbon atoms with a first p.sub.s value between 1.1 and 4.8, acid salts of the aforementioned multibasic organic acids, and acid salts of multibasic mineral acids having a first available pK.sub.s value between 1.5 and 7.5, as well as the use of such acid additives for stabilizing cilansetron against racemization in pharmaceutical preparations.

Abstract: This invention provides orally administerable pharmaceutical formulations comprising raloxifene, its ethers or esters, or a pharmaceutically-acceptable salt thereof, in combination with a hydrophilic carrier composition.

Abstract: A solid pharmaceutical preparation comprising a pharmaceutically active ingredient, erythritol, crystalline cellulose and an disintegrants, which exhibits a fast buccal disintegratability and dissolubility.

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

Abstract: A composition for oral administration which contains a pyridazinone compound of the formula (I) ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are each independently a hydrogen atom or a lower alkyl, X is a halogen atom, a cyano or a hydrogen atom, Y is a halogen atom, a trifluoromethyl or a hydrogen atom, and A is a C.sub.1 -C.sub.8 alkylene optionally substituted by hydroxy, or a pharmacologically acceptable salt thereof, and an organic acid. According to the present invention, a composition for oral administration which is stable to heat, light, moisture and the like and which shows improved dissolution and absorption of a pyridazinone compound can be provided.

Abstract: The invention provides a number of new water soluble lubricants and lubricant formulations which facilitate the production of tablets. In particular calcium and potassium sorbates and micronized combinations of polyethylene glycol with calcium ascorbate or with trisodium citrate or mixtures thereof are useful as lubricants, particularly in tablet compositions containing ingredients where rapid dissolution in an aqueous environment is desired for activity or desired for aesthetic purposes. A method is provided for surface treating calcium sorbate with docusate sodium, Simethicone Emulsion, USP or with lecithin to provide particularly useful tablet lubricants. The above lubricant(s) and lubricant formulations have fewer limitations and improved functionality in comparison to standard lubricants presently known. In addition, the lubricant(s) provided may be used with known hydrophobic lubricants to decrease the amount of the hydrophobic lubricant required for lubrication.

Abstract: The invention relates to a process of making pharmaceutical dosage units comprising at least desogestrel or Org 30659 (17.alpha.-17-hydroxy-11-methylene-19-norpregna-4,15-dien-20-yn-3-one), present in an amount of about 0.005 to 1.0 percent by weight of each pharmaceutical dosage unit, characterized in that the steroidal agent, and when required pharmaceutically acceptable excipients, are mixed with water and granulated.

Abstract: This invention relates to novel pharmaceutical compositions and methods for their preparation containing conjugated estrogens for the treatment of peri-menopausal, menopausal and post-menopausal disorders in women. The novel pharmaceutical compositions comprise a carrier base material and conjugated estrogens formed into a solid unit dosage form possessing a regular incremental release of the medicament upon oral administration. Further, the invention comprises the combination of conjugated estrogens with progestogens in a solid, shaped dosage unit. Specifically, the invention comprises the use of an organic excipient such as high molecular weight hydroxyalkyl alkylcelluloses. The use of an organic excipient such as hydroxypropylmethylcellulose in a stable, solid dosage formulation containing either conjugated estrogens alone or in combination with a progestogen is described.

Abstract: Lipophilic active ingredients are co-melted with tocopherol polyethyleneglycol succinate (TPGS) and a dispersion adjuvant to obtain solid dry coprecipitate compositions suitable as an oral dosage form. The solid TPGS coprecipitates of lipophilic active ingredients show improved drug release in vitro and enhanced oral bioavailability in vivo.

Abstract: An oral administration carbamazepine medicament with a retarded active substance release is disclosed. An aqueous plasticised polymer dispersion is applied on carbamazepine crystals without causing formation of carbamazepine dihydrate. The carbamazepine crystals with their aqueous coating may be mixed with appropriate auxiliarly substances, shaped into divisible tablets or filled into capsules.

Abstract: Disclosed is a pharmaceutical controlled release tablet containing an active ingredient in combination with a carrier made of cross-linked amylose in which hydroxymethylpropylcellulose (HPMC) with a viscosity higher than or equal to 4000 cps is added as an adjuvant. The addition of HPMC to the tablet permits to control the effect of enzymes, and more particular alpha-amylase present in the intestinal medium, on the cross-linked amylose used as a carrier, and thus to reduce the dependence of the kinetics of release upon the concentration of enzymes present in the medium.

Abstract: Novel method for applying agrochemicals to plants, which method consists in attaching to the surface of the plants tablets comprisingat least one agrochemically active compound andat least one adjuvant, which is solid, liquid of pasty at room temperature, andoptionally, one or more excipients optionally in admixture with one or more other additives and/or water.

Abstract: The present invention relates to a pharmaceutical composition for improving penile rigidity and/or preventing erectile dysfunction, including premature ejaculation, of a male mammal patient which comprises at least one of seeds from Aframomum species, its closely related species and remote ancestors thereof, mixture thereof and extracts thereof. The pharmaceutical composition may further comprise a pharmaceutically acceptable carrier for topical or oral administration.

Abstract: A pharmaceutical sustained release tablet for oral administration is made of a compressed blend of at least two dry powders including a powder of a pharmaceutical drug and a powder of a sustained release matrix for the drug. The sustained release matrix is made of substituted amylose prepared by reacting, in a basic medium, amylose with an organic substituent having a reactive function that reacts with the hydroxy groups of the amylose molecule. This substituent is preferably an epoxy or halogen alkane or alcohol with such a matrix controlled and sustained release of a drug are achieved with a remarkable close-to-linear profile and a release time of from 9 to 20 hours.

Abstract: The present invention provides water-soluble, extended-release chemical formulations, in tablet form, for urine pretreatment, that require minimal, if any, use of a binder component, yet are non-dusting, pliable, structurally strong, and not weakened by exposure to aqueous streams. The present invention also provides a simple and reliable method for controlled dispensing of such tableted formulations into a liquid stream that is particularly advantageous for use in micro-gravity environments, such as spacecraft urinal systems.

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

Abstract: 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: The present invention discloses tablet formulations, produced by dry roller compaction comprising compacted granulates of a mixture of a medicament and an intra-granular disintegrant. The granulates are compacted together into a tablet with an extra-granular disintegrant, an optional extragranular lubricant and excipients.

Abstract: Pharmaceutical formulations of cefaclor, suitable for the direct-compression manufacture of dispersible tablets, containing the antibiotic cefaclor in an amount between 35% and 50% by weight of the total weight of the formulation, along with suitable excipients and coadjuvants selected from disintegrators, diluents, lubricants, antiadherents, sweeteners, fragrances and, optionally, flavorings, opacifiers and colorants. Said formulations are suitable for the manufacture of dispersible tablets which disintegrate in less than three minutes in water at 19.degree.-21.degree. C., and are suitable for the treatment of infections caused by bacteria strains sensitive to cefaclor.

Abstract: The invention is directed to a method of treating a T cell-mediated autoimmune disease in animals, including humans, by the oral administration of autoantigens, fragments of autoantigens, or analogs structurally related to those autoantigens, which are specific for the particular autoimmune disease. The method of the invention includes both prophylactic and therapeutic measures.

Abstract: Tablets of increased strength are manufactured by combining and compressing a meltable binder, excipients and a pharmaceutically active agent into a tablet, melting the binder in the tablet, and then solidifying the binder.

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

Abstract: A directly compressible non-cariogenic free-flowing lactitol granulate comprising milled lactitol and a physiologically acceptable, binder taken from the group consisting of sugar alcohols, polymerized reducing sugars, alkali carboxymethylcellulose, hydrogenated starch hydrolysate, hydroxypropylcellulose, physiologically acceptable cellulose derivatives, polyvinylpyrrolidone, gum arabic, and other physiologically acceptable gums. The granulate is directly compressible, and manifests the taste profile, metabolic, and non-cariogenic properties of lactitol. In one embodiment, the milled lactitol is present in the granulate in the range of about 70% to about 98% by dry weight and the physiologically acceptable, non-cariogenic binder is present in the granulate in the range of about 2% to about 30% by dry weight. In a preferred embodiment of the invention, the granulate consists of 70-98% milled lactitol and 2-30% of a lactitol binder.

Abstract: Method for the preparation of an improved oral formulation of active ingredients belonging to the class of quinolones. The method is characterized by an intermediate compacting and grinding stage, before compression of the mixture of the active ingredient and excipients.

Abstract: Pharmaceutical compositions for orally delivering a therapeutically effective amount of a drug to the colon without significant release of the drug in the upper GI tract after oral administration of the composition are described. The composition is a unit dosage in the form of a tablet that comprises about 0.01% by weight to about 10% by weight of the drug that is useful in treating a colonic disorder or that is absorbed from the colon; about 40% by weight to about 98% by weight of a hydrocolloid gum obtainable from higher plants; and about 2% by weight to about 50% by weight of a pharmaceutically acceptable binder. The compositions are useful for treating lower GI disorders in human subjects by administering a suitable amount to a subject in need thereof. A particularly preferred aspect is the process for preparing such composition in the form of a tablet.

Abstract: This invention provides solid orally administerable pharmaceutical formulations comprising raloxifene hydrochloride, a surfactant being sorbitan fatty acid ester or a polyoxyethylene sorbitan fatty acid ester, polyvinylpyrrolidone, and a water soluble diluent which is polyol or sugar.

Abstract: The present invention comprises a tablet, and method for making such, which disintegrates or dissolves in a matter of just a few seconds once placed into the oral cavity. Generally, the method of the present invention comprises up to four steps. First, a porous particulate powder which will serve as the tablet support matrix is produced. In the second step, the pharmaceutical, for example an antihistamine, decongestant, or antibiotic is combined with the powder. Other additives may also be added to the mixture. In the third step the mixture is formed into a tablet. Finally, in the fourth step, a coating may be applied to the outer surface of the tablet to enhance the intactness and durability of the tablet.

Abstract: Methods and compositions for treating type I immunoglobin E (IgE)-dependent hypersensitivity by the administration of monophosphoryl lipid A (MLA) or 3-deacylated monophosphoryl lipid A (3D-MLA) are disclosed. MLA or 3D-MLA administered alone or in combination with an allergen to a patient suffering from type I hypersensitivity reduces levels of total or allergen specific IgE and increases levels of IgG antibody in that patient. MLA and 3D-MLA can be administered as part of a desensitization regimen or as a component of a prophylactic vaccine to prevent a type I hypersensitivity reaction.

Abstract: Hydrolyzed gelatin has been found to provide an improvement in taste and mouthfeel when incorporated in small amounts into chewable tablets containing ingredients requiring taste masking. Medicinals and nutritional supplements may now be prepared as chewables for those who find tablets difficult to swallow, for example children and older adults, or for those who prefer the convenience. There is a particularly large improvement in the taste and mouthfeel of chewables incorporating magaldrate and/or calcium carbonate.

Abstract: Verapamil depot drug formulations include the pharmaceutical itself and a three component release rate controlling matrix composition. The three components of the matrix composition are (1) an alginate component, such as sodium alginate, (2) an enteric polymer component, such as methacrylic acid copolymer, and (3) a pH independent gelling polymer, such as hydroxypropyl methylcellulose or polyethyleneoxide. The drug release rate can be adjusted by changing the amount of one or more of these components of the composition.

Abstract: Pharmaceutical compositions having analgesic activity containing (S)-2-(6-methoxy-2-naphthyl)-propionic acid as active ingredient and arginine, useful for the preparation of pharmaceutical forms for oral route, are described,

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: Bioadhesive pharmaceutical composition for the controlled release of active principles locally across the buccal cavity or systemically across a mucous membrane, wherein it is composed of an active principle, a compound (A), a compound (B) and excipients as defined in the description.

Abstract: Hydrolyzed gelatin has been found to provide an improvement in taste and mouthfeel when incorporated in small amounts into chewable tablets containing ingredients requiring taste masking. Medicinals and nutritional supplements may now be prepared as chewables for those who find tablets difficult to swallow, for example children and older adults, or for those who prefer the convenience. There is a particularly large improvement in the taste and mouthfeel of chewables incorporating magaldrate and/or calcium carbonate.

Abstract: Invented are stabilized tablet formulations of substituted 3,5-diene steroidal compounds. Also invented are methods of preparing stabilized tablet formulations of substituted 3,5-diene steroidal compounds.

Abstract: The present invention provides water-soluble, extended-release chemical formulations, in tablet form, for urine pretreatment, that require minimal, if any, use of a binder component, yet are non-dusting, pliable, structurally strong, and not weakened by exposure to aqueous streams. The present invention also provides a simple and reliable method for controlled dispensing of such tableted formulations into a liquid stream that is particularly advantageous for use in micro-gravity environments, such as spacecraft urinal systems.

Abstract: The invention concerns tablets with improved bioavailability of the active substance dichloromethylenediphosphonic acid or of a physiologically tolerated salt thereof and with a content of microcrystalline cellulose as a pharmaceutical auxiliary substance, pharmaceutical packs containing these tablets, the use of the active substance dichloromethylenediphosphonic acid together with microcrystalline cellulose for the production of a tablet with improved bioavailability and the process for producing the tablet.

Abstract: The invention relates to pharmaceutical compositions in the form of pleasant-tasting chewable tablets or chewable coated tablets which, besides the pharmaceutically active ingredient sucralfate, essentially contain at least one rapidly swellable physiologically acceptable gel former plus sugars or sugar substitutes.

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.