Abstract: This invention relates to a process for the production of optimally stable orally administrable solution forms of medicaments containing high-molecular polysaccharides, with controlled release of drugs having beta-blocking action, this process consisting of the reacting of 1 to 20 parts (w/w) of beta-blocking agent (oxprenolol, pindolol, sotalol, metoprolol, alprenolol, acebutolol, atenolol, bopindolol, practolol, nadolol or propranolol) in 100 parts of an aqueous solution with 0.001 to 10.0 parts of a polysaccharide polymer, advantageously with Xanthan Gum having beta-1,4-glucan chain, or dextran, or amylodextrin, or carboxymethylamylum. The reaction is allowed to take place in the course of 20 minutes at a pH adjusted no 2.0-4.5, with vigorous stirring at 80.degree. C. temperature. Following the usual method of the pharmaceutical practice, the system is then formulated by the addition of water to obtain a solution suitable for oral administration.

Abstract: Gepirone compositions having extended release properties contain a gepirone salt, a cellulosic polymer matrix and suitable quantities of pharmaceutical excipients. Dosage forms based thereon require 18 to 24 hours for release of 90 to 95% of gepirone.

Abstract: A microcapsule produced by preparing a water-in-oil emulsion comprising an inner aqueous layer containing said water-soluble drug and a drug retaining substance therefor and an oil layer containing a polymer substance, then thickening or solidifying said inner aqueous layer to a viscosity of not lower than about 5000 centiposes and finally subjecting the resulting emulsion to in water drying gives prolonged release of water-soluble drug.

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 preparation for reducing intraocular pressure consisting essentially of a therapeutically effective amount of the fixed combination of dipivalylepinephrine and carbachol (preparation 1) or dipivalylepinephrine and beta-blocker (preparation 2). The preparations may be prepared both as a solution and as a suspension. Either preparation is administered twice daily.

Abstract: A method for inducing periodontal regeneration including soft tissue, cementum, and bone regeneration, resulting in a type of healing characteristic of the anatomy and architecture of the undiseased tissue, comprising treating the surface of the damaged root with a demineralizing agent, and then applying a growth factor directly to the treated bone surface.

Abstract: A sustained release pharmaceutical formulation includes a sustained release excipient including a gelling agent, an inert pharmaceutical diluent, an optional cationic cross-linking agent, and a medicament having moderate to poor solubility is disclosed. In certain embodiments, the sustained release excipient is granulated with a solution or suspension of a hydrophobic polymer in an amount effective to slow the hydration of the gelling agent when the formulation is exposed to an environmental fluid. In another embodiment, the tablet is coated with a hydrophobic polymer.

Abstract: The present invention is directed to a novel sustained release matrix and oral dosage form comprising a homogeneous matrix formed from a wet granulation containing an effective amount of a medicament and a polymer blend of hydroxypropyl cellulose and hydroxyethyl cellulose. The present invention also discloses a novel process for making a sustained release oral dosage form comprising wet granulating a medicament with a polymer blend of hydroxypropyl cellulose and hydroxyethyl cellulose to form a homogeneous matrix, wherein the polymer blend is provided in an amount effective to control the release of said medicament, then forming the homogenous matrix into a solid oral dosage form.

Abstract: The present invention relates to a cellular cellulosic material containing a biocide agent and to a process for preparing same. Characteristically, matrix type microparticles, containing at least one biocide agent, are distributed in the network of cellulose of said material, ensuring therein, in the presence of moisture or water, a controlled release of the biocide agent or agents.

Abstract: What is provided herein is a stable, emulsifiable gel matrix for an agriculturally active chemical, which matrix will form an emulsifiable gel concentrate upon addition of the agriculturally active chemical, and upon water dilution, a highly stable aqueous macroemulsion which avoids precipitation of the active ingredient on extended storage. In addition, the inventive emulsifiable gel concentrates may contain relatively high concentrations of the agriculturally active chemical, the concentration sometimes referred herein to as "loading", making it advantageous from both the economic and handling viewpoints.

Abstract: A method of treating solid tumor cancer in a living being by prolonging the time a therapeutically effective agent remains in the tumor. The method comprises the steps of selecting particles of an aggregated protein and injecting them interstitially into the tumor. The therapeutically effective agent colloidal radioactive phosphorous is injected into the tumor either after the injection of the proteinaceous particles, or simultaneously.

Abstract: This invention provides a powder composition which is composed of particles consisting of a hydrophilic polymer coating having an encapsulated core matrix content of at least two microcrystallites of water-soluble inorganic compound such as sodium bicarbonate. In one embodiment a present invention powder composition has a content of hydrophilic polymer-coated bicarbonate microcrystallites, and a cosmetically safe anti-caking agent such as talc, and has utility as a baby powder product.

Abstract: A controlled release formulation for use with a variety of drugs or hormones are formed in microspherical form. The drug or hormone, e.g. bovine somatropine, is suspended in a polymer matrix. The polymer matrix is formed from at least two highly water soluble biodegradable polymers, selected for example from starch, crosslinked starch, ficoll, polysucrose, polyvinyl alcohol, gelatine, hydroxymethyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxypropyl-ethyl cellulose, hydroxypropyl-methyl cellulose, sodium carboxymethyl cellulose, cellulose acetate, sodium alginate, polymaleic anhydride esters, polyortho esters, polyethyleneimine, polyethylene glycol, methoxypolyethylene glycol, ethoxypolyethylene glycol, polyethylene oxide,poly(1,3 bis(p-carboxyphenoxy) propane-co-sebacic anhydride, N,N-diethylaminoacetate, block copolymers of polyoxyethylene and polyoxypropylene. The microspheres are coated with a (d,1 lactide-glycolide) copolymer.

Abstract: Present invention is a non-toxic, flavor stable, pleasant tasting composition releasing Zn.sup.2+ from compositions containing a highly ionizable zinc compound other than zinc gluconate that reduces the duration of common colds in humans. The composition is used in the oral cavity of a human suffering from a common cold. The composition comprises highly ionizable zinc compounds and a pharmaceutically acceptable carrier such as fructose, dextrose or sucrose with various additions. Compositions are unique in that they are non-toxic, pleasant tasting and do not have an offensive aftertaste, yet deliver zinc ions into oral tissues which may be used to treat common colds, reduce the duration of common colds or cure common colds in humans in need of such treatment. Compositions are non-toxic, thermally, chemically and flavor stable. The compositions may be prepared in the form of compressed tablets, lozenges, powders, liquids or chewing gums.

Abstract: A drug delivery system useful in aiding individuals in the cessation of smoking or chewing nicotine containing products is described. The delivery system includes a physical constraint modulation system (PCMS.TM.) containing lobeline. The drug delivery system is capable of delivering lobeline to an individual in a controlled, sustained release manner and providing long-term therapeutic levels of lobeline to the individual. The delivery of lobeline in such a manner reduces or eliminates the individual's smoking or chewing habit. The PCMS may be a biodegradable polymer containing the lobeline capable of subcutaneous or intramuscular injection or implantation into the individual or may be part of a transdermal patch containing lobeline. Also described are methods of using the drug delivery systems and kits containing the drug delivery systems.

Abstract: There is provided a matrix preparation produced by dispersing a pharmaceutically active ingredient into a matrix which is solid at ambient temperature and comprised of a fatty acid ester of a polyglycerol. The preparation has stable release controlling ability, can be processed to fine granules, granules, capsules, tablets etc., and contributes to reduction of the administration times of the active ingredient and side effects of the ingredient.

Abstract: What is provided herein is an inert matrix composition (IMC), and a microemulsifiable concentrate (MEC) in the form of a free-flowing, high-melting solid, suitable for making an aqueous microemulsion (AME) of an agriculturally active chemical (AAC) with dilution water. The inert matrix composition comprises about 10-50% of a C.sub.6 -C.sub.18 alkylpyrrolidone, about 10-50% of an anionic surfactant and about 10-70% of a complexing agent characterized by being an organic compound having a melting point >100.degree. C., a molecular weight .ltoreq.500, a water solubility of at least 10% by weight, and being capable of hydrogen-bonding with the alkylpyrrolidone component of the composition. The MEC comprises the IMC and about 1-20% of the agriculturally active ingredient (AAI). Upon dilution with water an AMC is provided having a few ppm to 1% AAI.

Abstract: The present invention relates to a sustained-release injection, which comprises a suspension of a powder comprising an active ingredient and a pharmaceutically acceptable biodegradable carrier (e.g. proteins, polysaccharides and synthetic high molecular compounds, preferably collagen, atelocollagen, gelatin, and a mixture thereof) in a viscous solvent for injection (e.g. vegetable oils, polyethylene glycol, propylene glycol, silicone oil, and medium-chain fatty acid triglycerides). The sustained-release injection can release the active ingredient at an effective level for a long period of time when injected.

Abstract: New solid, porous unitary form comprising micro-particles and/or nano-particles, made by lyophilization are useful for the administration of therapeutically active substances, nutrition agents, diagnostic agents or cosmetic agents.

Abstract: Sulfoalkyl ether cyclodextrin derivatives and their use as solubilizing agents for water insoluble drugs for oral, intranasal, or parenteral administration are disclosed.

Abstract: Methods and compositions are provided for the treatment and repair of defects or lesions in the cartilage of humans and other animals. The defect or lesion in the cartilage may be first treated with an enzyme to remove proteoglycans from the defect area. To induce cartilage formation, the defect is filled or otherwise dressed with a biodegradable matrix having pores sufficiently large to allow repair cells to populate the matrix. The matrix filling the defect contains a proliferation agent at a concentration sufficient to stimulate proliferation of repair cells and a transforming factor in an appropriate delivery system to release the transforming factor at a concentration sufficient to transform repair cells in the matrix and defect area into cartilage-producing chondrocytes. The matrix may also contain a chemotactic agent to attract repair cells. The entire treatment may be carried out in a single arthroscopic or open surgical procedure.

Abstract: This invention relates to pharmaceutical compositions for rectal administration containing semi-synthetic glycerides produced by interesterification, and, as the active ingredient, triazole derivatives of the formula ##STR1## wherein R.sup.1 is phenyl optionally sustituted with from one to three substituents independently selected from the group consisting of F, Cl, Br, I, CF.sub.3,(C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy, and 5-chloropyrid-2-yl; X is OH, F, Cl or Br; R.sub.2 is H.sub.2, CH.sub.3 or F; and R.sub.3 is H or F.

Abstract: Processes for polyphase fluid extraction of concentrated, active therapeutic components from parts of plants identified taxonomically as Symphytum, Taxus and Aloe species are described. The resulting products-by-processes are defined as Concentrated Fluid Plant Extracts (CFPE) of the respective plant types, where P can be S, T or A. The preparation process for CFPE includes multiple/sequential stages of diffusional transfer of the active constituents into liquid and/or vapor extraction phases under contact conditions of forced convection at controlled temperature and pressure. Therapeutic formulations based on CFPE including emulsions, aerosols, liposomes and controlled-release devices are presented. Treatment methods for a variety of skin conditions and complications of specific diseases are indicated.

Abstract: Controlled release pharmaceutical preparations are prepared by homogenizing an organic or inorganic pharmaceutical active substance such as an opium alkaloid or its salts, an opium antagonist or its salts, an aliphatic or aromatic amine derivative or its salts, a phenolate type medicament, or Zn, Fe, Mg, K, Na salts, a fatty acid or its salt necessary to achieve a continuous phase transfer and an ethylene vinyl acetate copolymer and formulating the resulting homogeneous mixture bya) direct compressing orb) admixing with a solvent orc) using a second, auxiliary polymer.The preparations are suitable for oral or rectal administration or for tissue implantation.

Abstract: Pharmaceutical compositions for continuous release of a physiologically active substance in which the physiologically active substance comprises a polypeptide covalently conjugated to a water soluble polymer show particularly desirable release characteristics. Polypeptides for use in the pharmaceutical compositions include G-CSF and solution stable derivatives thereof, human calcitonin and interleukin-2. The material of the composition may be a polylactide or biodegradable hydrogel derived from an amphipathic block copolymer.The compositions enable a therapeutically effective polypeptide to be continuously released over a prolonged period of time following a single administration of the pharmaceutical composition to a patient.

Abstract: A film-coated extended release oral dosage composition containing the nasal decongestant pseudoephedrine sulfate in a unique polymer matrix core and a film-coating on such core containing the non-sedating antihistamine, loratadine, and use of the said composition for treating patients showing the signs and symptoms associated with upper respiratory diseases and nasal congestion are disclosed.

Abstract: A preparation for the once-daily, percutaneous administration of nicotine comprises nicotine uniformly distributed in a solid, semi-solid or mucilaginous medium which can be placed in intimate contact with the skin, the solid, semi-solid or mucilaginous medium is formed by adding a given amount of nicotine to a solution of a solidifying or gel-forming agent or mixture thereof in a suitable solvent or mixture of solvents and mixing or heating the mixture thereby obtained so as to form the solid, semi-solid or mucilaginous medium. The preparation can be used in a method of treating withdrawal symptoms associated with smoking cessation and for combating the psychological dependence that occurs through frequent smoking.

Abstract: Compositions and a general method are described to shorten the duration of common colds by administration of medicaments to and into the oral tissues, rather than to the nose, or by injection or by oral administration. Compositions for oral absorption by a human contain medicinal agents including antiviral agents, antirhinoviral agents, interferon, interferon inducers, T-cell lymphocyte mitogens and other agents desirable or theoretically useful in shortening the duration of common colds. All compositions include medicaments contained in a consumable, sweet pharmaceutical carrier, prepared in the form of a pleasant tasting lozenge, powder, liquid or chewable composition. All compositions are for delivery of medicinal agent to the oral and oral pharyngeal mucosa of a human with said composition being absent the normal offensive aftertaste of medicinal agent, and being intended for use in shortening the duration of common colds.

Abstract: Methods and compositions are provided for the treatment and repair of defects in the cartilage or bone of humans and other animals as in full-thickness defects in joints. The defect in bone is filled with a matrix having pores large enough to allow cells to populate the matrix and to form blood vessels. The matrix filling the bone defect contains an angiogenic factor and also contains an osteogenic factor in an appropriate delivery system. To induce cartilage formation, a defect in cartilage is filled with a matrix having pores sufficiently large to allow cartilage repair cells to populate the matrix. The matrix filling the defect in cartilage contains a proliferation agent and also contains a transforming factor in an appropriate delivery system. The matrix may also contain a chemotactic agent to attract cartilage repair cells.

Abstract: Systems and their methods of preparation and use that release an active agent in a controlled manner for an extended period in a vaginal cavity environment. When an antifungal agent such as an imidazole, is incorporated into the system it has been found that the conventional treatment time is reduced by at least 25%.

Abstract: This invention provides compositions comprising a physiologically-active agent and a compound having the structural formula ##STR1## wherein X may represent sulfur or two hydrogen atoms; R' is H or a lower alkyl group having 1-4 carbon atoms; m is 2-6; n is 0-18 and R is --CH.sub.3, ##STR2## wherein R" is H or halogen, in an amount effective to enhance the penetration of the physiologically-active agent through the skin or other membrane of the body of an animal.

Abstract: A controlled release formulation of a calcium channel blocker for oral administration contains non-pareil seeds loaded with a calcium channel blocker, particularly diltiazem, nifedipine, or verapamil, and then microencapsulated in ethylcellulose by phase separation techniques. The resultant microcapsules provide an approximately zero order release rate, preferably over 12 to 16 hours. These microcapsules may be filled into gelatin capsules.

Abstract: Encapsulating particles of solid thiocarbonate salts, esters and complexes with air- and water-impermiable coatings produces compositions having long-term stability.

Abstract: A device for the dispensing of a biologically active material into the surrounding environment is disclosed which consists of at least one wall enclosing a compartment which contains a swollen stimuli sensitive hydrogel in which the biologically active material is entrained in solution. The hydrogel deswells or shrinks in response to contact by external physical or chemical stimuli releasing the biologically active material into the portion of the compartment previously occupied by the swollen hydrogel. The wall enclosing the compartment is rigid and contains means allowing the passage of the biologically active material from the compartment to the surrounding environment and also for transmitting the external stimuli to the swollen hydrogel in said compartment. The wall may contain orifices or be permeable to the active material and external stimuli depending upon the drug and the stimuli to be used.

Abstract: The controlled release of therapeutically active agents is achieved from a controlled release matrix of sodium alginate and a calcium salt. When the composition is to be administered rectally, the matrix is combined with a therapeutically active agent and a suitable suppository base. When the composition is to be administered orally, the matrix further includes a higher aliphatic alcohol.

Abstract: Methods and compositions are provided for the treatment and repair of defects or lesions in the cartilage of humans and other animals. The defect or lesion in the cartilage may be first treated with an enzyme to remove proteoglycans from the defect area. To induce cartilage formation, the defect is filled or otherwise dressed with a biodegradable matrix having pores sufficiently large to allow repair cells to populate the matrix. The matrix filling the defect contains a proliferation agent at a concentration sufficient to stimulate proliferation of repair cells and a transforming factor in an appropriate delivery system to release the transforming factor at a concentration sufficient to transform repair cells in the matrix and defect area into cartilage-producing chondrocytes. The matrix may also contain a chemotactic agent to attract repair cells. The entire treatment may be carried out in a single arthroscopic or open surgical procedure.

Abstract: A preparation method of sodium diclofenac enteric-coated microcapsules by spray drying technique comprising the steps of(a) dissolving sodium diclofenac in an appropriate amount of distilled water;(b) adding an effective amount of excipients to the above solution to form a suspension;(c) adding methacrylic acid-ethyl acrylate copolymers (Eudragit L 30D) and polyethyleneglycol 6000 (PEG 6000) as the enteric-coating material to form a slurry;(d) atomizing the slurry to form spray-dried powder;(e) mixing the spray-dried powder with a mixture of microcrystalline cellulose (neocel) and pregelatinized starch (flo-starch); and(f) compressing the powder mixture into a microdispersed enteric tablet.The spray drying technique could be easily performed to prepare the enteric-coated microcapsules with aqueous latex polymer dispersion such as Eudragit L 30D as an enteric-coating polymer.

Abstract: The pharmaceutical composition is intended in particular for the sustained and controlled release of an effective dose of a medicinal substance. It comprises, as a carrier for the medicinal substance, a biodegradable polymer or copolymer or a mixture of biodegradable polymers and/or copolymers derived from a dicarboxylic acid selected from the acids of the Krebs cycle, and from an aliphatic diol containing 4 carbon atoms or from cyclohexane-1,4-dimethanol.

Abstract: The antitumor and antiviral compound avarone, a process for its production, pharmaceutical compositions containing said compound, and a method of combating susceptible viruses and tumors therewith, are disclosed.

Abstract: Nonaqueous pharmaceutical compositions for use in aqueous physiological systems are disclosed comprising drug delivery vehicles suspended in nonaqueous perfluorocarbon or fluorinated silicone liquid carriers. The suspended drug delivery vehicles may be water labile or water stable and incorporate therapeutic or diagnostic compounds which remain stable and pharmaceutically effective for extended periods. The pharmaceutical compositions possess extended shelf-lives and do not leach the incorporated therapeutic or diagnostic compounds into the liquid carriers making them well suited for multi-dose packaging and administration.

Abstract: A sustained-release coating composition is described that contains an ethylcellulose and/or a methacrylic methylester together with a plasticizer and a detackifying agent. Sized drug granules are coated with this composition and then mixed with a polymeric composition containing at least one viscosity agent and formed into drug dosage units for the administration and sustained release of the drug in a patient. The sustained-release drug dosage units described produce a continuous, slow release of the drug at a therapeutically effective dosage level when administered to a patient.

Abstract: Controlled release verapamil tablets are disclosed. The tablets include an excipient having a hydrophilic material, preferably containing a mixture of xanthan gum/locust bean gum, and an inert diluent.

Abstract: A process for preparing complexes of piroxicam with cyclodextrins in which the two components in the powder state are premixed and then co-ground in a high energy mill in the presence of steam.The products obtained have technological, physical and biopharmacological characteristics which are advantageous compared with those of liquid-state complexes obtained by traditional methods, and are suitable for preparing pharmaceutical compositions for oral, rectal and topical use.

Abstract: A method for preparing biodegradable microspheres having a three-dimensional network in which biologically active macromolecular agents are physically entrapped therein. The microsphere is able to degrade and release the macromolecular agent at a controlled rate. The method involves emulsifying a vinyl derivative of a biodegradable hydrophilic polymer, a water-soluble monovinyl monomer and a biologically active macromolecule in water, and copolymerizing the biodegradable hydrophilic polymer and the water-soluble monovinyl monomer such that the biologically active macromolecule is entrapped therein.

Abstract: Intersticed materials, including woven and nonwoven fabrics, open-cellular materials and the like, are impregnated with functional substances by incorporating the substances in microscopic porous particles in which the pores form an interconnected network open to the particles in the interstices of the materials. The functional substances thus impart useful properties to the material in a controlled release manner.

Abstract: This invention relates to an anhydrous, liquid phase process for entrapping droplets of a silicon compound in an organic polymer which involves precharging a reactor at between about 50.degree. and about 80.degree. C. with a polymerization initiator and a non-polar solvent in which the silicon compound is soluble; adding to the precharged reactor, silicon compound under vigorous agitation and gradually introducing from about 50 to about 99 wt. %, based on silicon compound, of a polymerizably precipitatable, aliphatically unsaturated monomer at a controlled rate; continuously polymerizing the monomer component, under vigorous agitation with the silicon compound, at between about 50.degree. and about 165.degree. C. while maintaining a desired monomer level of not more than 10% in the reactor and recovering a solid particulate product of silicon droplets entrapped in said polymerized monomer.

Abstract: A method and product for preparing a controlled-release composition are provided. The method comprises formation of a mixture containing at least one amphiphilic substance capable of forming a liquid crystalline phase, in contact with a liquid selected from the group consisting of water, glycerol, ethylene glycol, propylene glycol and mixtures thereof. The method includes a step of providing in such mixture a bioactive material. Preferred controlled-release compositions include an alkylbetaine zwitterionic surfactant therein.

Abstract: Bicontinuous microemulsions wherein both the oil and the surfactant are addition-polymerizable and which on polymerization yield transparent solids wherein both the solid and the aqueous liquid phases are continuous. Such solids may be used in separation processes.

Abstract: A free-flowing directly compressible granulation useful as a slow release pharmaceutical excipient is disclosed. The excipient includes a hydrodrophilic matrix which includes heteropolysaccharide and a polysaccharide material capable of cross-linking the heteropolysaccharide, and an inert diluent.

Abstract: Sulfoalkyl ether cyclodextrin derivatives and their use as solubilizing agents for water insoluble drugs for oral, intranasal, or parenteral administration are disclosed.