Abstract: A protein-polysaccharide complex is used as a non-toxic and sustained release carrier for insecticides, herbicides, foliar nutrients and mixtures thereof. Methods for using a solution, solid or flowable impregnated protein-polysaccharide complex as a delivery agent for the control of plant populations and insect populations and as a preservative for cut flowers are described.

Abstract: Dextran esters with a molecular weight of 10,000-10,000,000 and ester side chains which are derived from acids with 6-18 carbon atoms, where the degree of esterification is adjusted, depending on the number of carbon atoms in the side chains and the molecular weight, to a value of 0.04-1.1 so that the dextran esters are insoluble in water at room temperature and are broken down by colonic bacteria, and their use for coating and/or embedding pharmaceutical active ingredients or drug formulations.

Abstract: Compositions for trans-mucosal delivery, e.g. intranasal, include a lysophosphatidyl-glycerol compound as the adsorption enhancer. The preferred compounds for delivery are insulin and calcitonin.

Abstract: The disclosed invention provides agricultural chemical compositions containing active carbon-treated thifluzamide as an effective ingredient. Such compositions provide increased release of thifluzamide into water.

Abstract: An inclusion complex of diclofenac, preferably as diclofenac sodium, and an unsubstituted beta-cyclodextrin has the formula 1 molecule of diclofenac to 1 molecule of the unsubstituted beta-cyclodextrin and preferably from 5 to 11 water molecules. The inclusion complex may be formulated as a pharmaceutical composition.

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: Disclosed are novel crosslinked polymeric ammonium salts wherein in said salt: about 25% or more of the groups which link ammonium nitrogen atoms are group Y wherein Y is an-alkylene groups or alkyl substituted n-alkylene group, wherein said n-alkylene group has 7 to about 20 carbon atoms; zero to about 75% of groups which links ammonium nitrogen atoms are group Z wherein Z is a hydrocarbylene radical containing 2 or more carbon atoms, said hydrocarbylene radical optionally containing one or more hydroxyl, ether, amino, thioether, keto, or silyl groups or heterocyclic rings; and about 25% or more of the ammonium atoms are secondary ammonium atoms.

Abstract: A sustained release pharmaceutical formulation and methods of making and using the same are provided. The sustained release pharmaceutical formulation includes a sustained release excipient including a gelling agent, an inert pharmaceutical diluent, an optional hydrophobic material and/or hydrophobic coating, and a medicament for sustained oral administration.

Abstract: A method has been discovered for repelling ants by treating objects or areas with effective amounts of compositions that include (a) one or more C.sub.6 to C.sub.8 carboxylic acids; (b) one or more C.sub.6 to C.sub.14 alcohols; (c) one or more esters which are reaction products of (a) and (b) or an ester which is a reaction product of the repellents and other carboxylic acids or alcohols; (d) one or more C.sub.6 to C.sub.11 carboxylic acid esters; (e) one or more C.sub.6 to C.sub.14 ketones; or (f) mixtures thereof.

Abstract: The present invention relates to a composition for rectal administration which comprises a benzimidazole compound having antiulcer activity and a salt of C.sub.6-20 fatty acid, both of which are intermingled with each other in a base for rectal administration.The composition for rectal administration of the present invention is effective for the treatment of gastrointestinal ulcers, is excellent in the stability of the active ingredient therein and the absorption thereof to thereby insure an early attainment of therapeutically effective blood concentration and permits control of the rate of absorption of the drug. Furthermore, the composition for rectal administration of the present invention swells in the intestinal tract, attaches itself to the mucosa, and releases the active ingredient gradually over a long time to supply the drug at a high concentration and with high efficiency. Therefore, the expected therapeutic efficacy can be obtained at a low dosage level with a minimum of side effect.

Abstract: The invention relates to the use of clindamycin palmitate for the production of pharmaceutical administration forms having a protracted release of the antibiotic active compound clindamycin, and corresponding administration forms which are preferably used in the form of shaped implants.

Abstract: A method of administering EDTA complexes includes steps of forming a suppository containing an EDTA complex and controlled-release agents which release the EDTA complex over a period of about three to four hours after placement, and then administering the suppository to a patient in lieu of an intravenous drip.

Abstract: Prolonged parenteral release of a bioactive polypeptide at desirably effective levels can be achieved using novel compositions in which the polypeptide is present in a biocompatible oil in an unusually high proportion such as at least about 10% by weight. Also disclosed are certain metal-associated somatotropins that are useful for prolonged parenteral release of such somatotropins.

Abstract: Certain steroidal and non-steroidal compounds have been found to inhibit androgen and estrogen formation. Such inhibition may aid in the reduction of the activity of these hormones and may be useful in the treatment of diseases where, for example, inhibition of androgen or estrogen activity is desired. Preferred inhibitors also possess antiestrogenic activity, thus providing the advantage of a double inhibitory action both on estrogen formation and on estrogen action (blockade of estrogen receptors by antiestrogenic action).

Abstract: Methods for enhancing vascular support of cells housed within an implanted apparatus are disclosed. The methods comprise placing a population of therapeutic substance-producing cells into the cell receiving chamber of an immunoisolation apparatus, implanting the apparatus into a patient, and administering an immunomodulatory agent to the patient. The immunomodulatory agent increases the number of close vascular structures in the vicinity of the implanted device, which increases the long term survival of the cell population housed therein.

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: Methods of treatment and prevention of estrogen-related diseases, and of fertility control, include low dose (e.g. less than 50 nanomolar serum concentration) administration of certain anabolic steroids, progestins and other substantially non-masculinizing androgenic compounds. Sustained release formulations substantially free of organic solvent, and sustained release formulations for maintaining low serum levels of androgen are disclosed.

Abstract: A method of producing a sustained-release preparation which includes permitting a water-soluble polypeptide to permeate into a biodegradable matrix in the aqueous solution. The production method of the present invention makes possible the permeation of a water-soluble polypeptide into a biodegradable matrix without bringing the water-soluble polypeptide into contact with an organic solvent. Hence the water-soluble polypeptide is prepared without affecting the water-soluble polypeptide bioactivity and is thus effective for use as a pharmaceutical.

Abstract: Particles, especially colloidal particles, comprising an interior phase of a non-lamellar reversed cubic, intermediate or hexagonal liquid crystalline phase, or a homogeneous L3 phase, and a surface phase of a lamellar crystalline or liquid crystalline phase, or an L3 phase. A method of preparing such particles by creating a local dispersible phase, within the homogeneous phase, preferably by means of a fragmentation agent, and fragmentating the homogeneous phase so as to form said surface phase. Several medical as well as non-medical uses of the particles referred to, e.g. as an antigen-presenting system, as a delivery system for anticancer, antifungal and antimicrobial drugs, and as carriers of nucleic acids or nucleotides.

Abstract: A powder-form composition of 2-acetyl-1-pyrroline incorporated with a support of maltodextrin and/or cyclodextrin. The composition is prepared by hydrolyzing a 2-(1-alkoxyethenyl)-1-pyrroline with an acid to obtain a reaction medium, adding an equimolar amount of a base to the reaction medium to obtain a neutralized reaction medium containing 2-acetyl-1-pyrroline, combining maltodextrin and/or cyclodextrin with the neutralized reaction medium to obtain a support solution and freeze-drying the support solution to obtain the composition.

Abstract: A sustained release capsule excellent in adhesion characteristics in the gastrointestinal tract, stability and so on is provided. The capsule is characterized in that a polymer excellent in initial adhesion and a polymer excellent in shape-retaining ability are dispersed in a liquid substance in the capsule, that a physiologically active substance is dispersed or dissolved in the liquid substance and that the moisture content in the whole preparation is not more than 2%.

Abstract: Compositions comprising (i) granules comprising a biologically active material in association with a weak base and partially coated with a delayed release material soluble in intestinal juice, (ii) an acidifying agent having a pH between 1.5 to 6, and (iii) a gel forming agent are described. There is also described a composition comprising an acidic gel having a pH between 1.5 to 6 and containing microgranules comprising a biologically active material in association with a weak base and partially coated with a delayed release material soluble in intestinal juice. The compositions may be used in the treatment of diseases associated with intestinal pathogens in animals. Where the biologically active material is a protease, receptor/adhesion sites in the intestines for pathogens may be proteolysed so as to prevent pathogen binding to intestinal surfaces.

Abstract: The present invention relates to a controlled release formulation which includes a therapeutically active medicament, a heterodisperse gum matrix, a pharmaceutically acceptable diluent, and an effective amount of a pharmaceutically acceptable surfactant and/or wetting agent to provide a multi-phasic controlled release of a therapeutically active medicament. The invention also relates to a method of preparing the same.

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: Methods and compositions for preventing or treating non-inflammatory elevated intraocular pressure associated with administered or endogenous steroids including administering to a mammalian organism a composition including (a) an ophthalmologically effective amount of a non-steroidal cyclooxygenase inhibitor, and (b) a pharmaceutically acceptable carrier, to reduce or prevent an elevation of intraocular pressure and/or protein marker induction induced by chronic exposure to glucocorticoids.

Abstract: This invention provides a rectally administered composition for inhibiting epileptic seizure and to its methods of use. The composition contains, in a suitable solvent, an anti-epileptic agent for inhibiting epileptic seizure, a buffer for maintaining pH, and a thickener for imparting a viscosity to the composition effective for rectal administration by injection to a patient in epileptic seizure.

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: Disclosed is a sustained release liquid aqueous ophthalmic delivery system and a method of providing a slow and sustained release of ophthalmic treating agents to the eye of a mammal which comprises administering to the eye of a said mammal an effective amount of a homogeneous liquid aqueous ophthalmic pharmaceutical composition, of pH between about 3.0 and about 6.2, which is adminstrable in drop form and which comprises an ophthalmically effective concentration of a said ophthalmic treating agent and about 0.05% to about 10% by weight of the polymer chitosan; said polymer consisting essentially of(A) monomeric .beta.(1.fwdarw.4)-D-glucosamine linked units and of(B) monomeric .beta.(1.fwdarw.

Abstract: The present invention relates to single and multiple layer collagen films that are useful for improved sustained release delivery of pharmaceuticals.

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: (1) A composition which comprises erythropoietin and hyaluronic acid shows a sustained-release of the medicine in a living body, and(2) A water-soluble composition which comprises (a) a pharmacologically active polypeptide secreted by an animal body or its derivative or a chemically synthesized pharmacologically active substance, (b) a water-soluble species of hyaluronic acid or its nontoxic salt and (c) a water-soluble protein injectable into body fluids without showing any substantial pharmacological activity brings about a prolonged action in vivo of a pharmacologically active substance. In addition, the composition can be administered using a small-gauge needle and thereby contributes ot relieving pain in patients.

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 readily soluble 2',3'-dideoxyinosine composition is prepared by combining 80 to 1 parts by weight of a basic amino acid and 20 to 99 parts by weight of 2',3'-dideoxyinosine. The greater solution velocity of this composition improves solubility for therapeutic uses.

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

Abstract: Novel fusions of a GPI signal domain and a polypeptide heterologous to the GPI signal domain donor polypeptide are provided for industrial use. Therapeutic administration of the GPI-linked product of the fusions enables the targeting of biological activity to cell membrane surfaces.

Abstract: Certain steroidal and non-steroidal compounds have been found to inhibit androgen and estrogen formation. Such inhibition may aid in the reduction of the activity of these hormones and may be useful in the treatment of diseases where, for example, inhibition of androgen or estrogen acitivity is desired. Preferred inhibitors also possess antiestrogenic activity, thus providing the advantage of a double inhibitory action both on estrogen formation and on estrogen action.

Abstract: When a transdermal therapeutic composition which contains a pharmaceutically effective ingredient, a water-soluble absorption enhancer, a fat-soluble absorption enhancer and a super water-absorbent resin is applied to the skin of mammals, release of the pharmaceutically effective ingredient and the absorption enhancers is controlled and the pharmacological action lasts for a long period of time.

Abstract: The invention relates to a novel advantageous oral dosage form for methanediphosphonates, especially the active ingredient disodium pamidronate. A preferred dosage form comprises:a) disodium-3-amino-1-hydroxypropane-1,1-diphosphonate (disodium pamidronate),b) a cationic macroporous ion exchange resin based on a styrene/divinylbenzene copolymer having an exchangeable aminophosphonate group and, where appropriate,c) further pharmaceutically acceptable excipients.The ingredients can be processed to form tablets, dragees, capsules etc.

Abstract: Pharmaceutical compositions comprising a cyclosporin, e.g. Ciclosporin or [Nva].sup.2 -Ciclosporin, in "microemulsion pre-concentrate" and microemulsion form. The compositions typically comprise (1.1) a C.sub.1-5 alkyl or tetrahydrofurfuryl di- or partial-ether of a low molecular weight mono- or poly-oxy-alkane diol, e.g. Transcutol or Glycofurol, as hydrophilic component. Compositions are also provided comprising a cyclosporin and (1.1) and, suitably, also a saccharide monoester, e.g. raffinose or saccharose monolaurate. Dosage forms include topical formulations and, in particular, oral dosage forms.

Abstract: A new series of degradable polymeric matrices were prepared by blending polymers that degrade by hydrolysis such as poly(L-lactic acid)(PLA), and nonionic Pluronic.TM. surfactants, block copolymers of polyethyleneoxide (PEO) and polypropyleneoxide (PPO). The water content of the polymer blend films was controlled by mixing different types of block copolymers and by adjusting their amount. In aqueous solution, the blends revealed the typical liquid-crystalline phase transition of Pluronic.TM. polymers, suggesting the formation of a gel-like structure within the polymer skeleton. Poly(lactic acid) degradation rates were not affected by the blending procedure, although the hydration degree in these matrices was higher. When used as drug-releasing matrices, these blends extended protein release and minimized the initial protein burst, as compared to the pure polymer.

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: A process for coating at least one medicinal and/or foodstuff active principle useful for ruminants. At least one monomer is polymerized in an oil-in-water emulsion in the presence of a surfactant to synthesize a pH-sensitive-polymer composition, the composition being obtained in an oil-in-water emulsion. Without isolation of the pH-sensitive polymer, the oil-in-water emulsion is used to coat the active principle, preferably methionine or lysine or a derivative thereof. The pH-sensitive polymer is not dissolved in an organic solvent(s) in either the polymerization or coating steps. The pH-sensitive polymer is stable at pH 6 but at pH 2, the coated active principle is released.

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: A transdermal fluoride medication for providing fluoride ion for the prevention and treatment of bone loss disease, which may have an estrogen-containing substance for not only treating hormonal imbalance but to obtain more advantageous use of the fluoride ion within the body. A transdermal enhancer is present. The preferred form is a transdermal patch containing sodium monofluorophosphate and further optionally including an estrogen-containing substance and a transdermal enhancer, which is adhesively attached on the skin of the patient for slow release of fluoride ion and, optionally, estrogen to the bloodstream of the patient. Up to ten percent of sodium fluoride and/or calcium can be added.

Abstract: The invention relates to compositions and methods of using clay-enclosed paramagnetic ions as image brightening or image contrast agents. In particular, T.sub.1 relaxivity measurements on Hectorite and mortmorillonite clay-enclosed trivalent gadolinium suggest improved imaging over zeolite-enclosed paramagnetic species. Clay-enclosed gadolinium complexes are amenable to convenient administration in oral preparations and are readily formulated in stable aqueous suspensions. Other transition metal ions, including divalent manganese, may be enclosed in the clay structures, either as free metals or in the forms of chelated complexes. Alternatively, improved relaxivities are envisioned for clays incorporating a paramagnetic metal ion as part of the framework structure.