Abstract: A pulsating release composition comprising natural microspheres, such as pollen grains or spores, into which are loaded a biologically active is subsequently releasable therefrom in a predetermined location in or on a plant or animal in a series (generally 3 or more) of pulses. In one preferred embodiment, the composition comprises a group of substantially similar loaded micropheres coated with multiple barrier layers alternating with multiple active substance layers in a concentric onion-like structure, the barrier layers being slowly soluble to delay release of active substance from the underlying layer thereof until after the pulse of active substance provided by the overlying layer has subsided.

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: A controlled release formulation which comprises a compound selected from the group consisting of organic acidic compounds and acid anhydrides or esters capable of generating one of the organic acidic compounds through hydrolysis together with an active ingredient and collagen as a carrier, said formulation being capable of exhibiting a predetermined release profile of the active ingredient. A process for producing said formulation is also provided.

Abstract: The invention provides a method for improving the oral bioavailability of carbamazepine by administering per os, to a warm-blooded animal in need of carbamazepine therapy, a therapeutically effective amount of carbamazepine complexed with cyclodextrin selected from the group consisting of hydroxypropyl and hydroxyethyl derivatives of .beta.- and .gamma.-cyclodextrin.

Abstract: Use in cosmetics, especially as UV screens, of diorganopolysiloxanes containing a 2-hydroxybenzophenone functional group of formula: ##STR1## where R is C.sub.1 -C.sub.10 alkyl, phenyl or 3,3,3-trifluoropropyl, B is R or A, r=0-200, s=0-50, or of formula: ##STR2## where u=1-20 and t=0-20 and t+u.gtoreq.3, A and/or B denoting a 4-alkyleneoxy-2-hydroxybenzophenone radical.

Abstract: Sugar or sugar/starch beads coated with a first coating of a drug, for example 1,2-dihydro-6-(lower alkyl)-2-oxo-5-(4-pyridinyl)-nicotinonitrile (milrinone), hydroxypropyl methylcellulose or hydroxypropyl cellulose and a plasticizer selected from triacetin, diacetylated monoglycerides, glycerin, propylene glycol, polyethylene glycol, diethyl phthalate and triethyl citrate or a mixture of two or more thereof and a second coating of high-viscosity ethylcellulose, low-viscosity ethylcellulose, hydroxypropyl cellulose, polyvinyl acetate phthalate and a plasticizer selected from diacetylated monoglycerides and triacetin or a mixture thereof and optionally coated with additional first coating and capsules filled therewith and method of preparation thereof are disclosed.

Abstract: Preparation for preventing or combating complications in diabetes, characterized in that it comprises:(a) insulin or a salt or complex thereof, and(b) a peptide of the general formula I:H-L-Met(X)-L-Glu-L-His-L-Phe-D-Lys-L-Phe-Yor a salt or a N-acyl derivative thereof, whereinMet(X) represents the amino acid radical Met, Met(O) or Met(O.sub.2),Y represents the group Gly-Z or Z, andZ represents the hydroxyl group, an esterified hydroxyl group or a substituted or unsubstituted amino group.

Abstract: A coated product comprising a water soluble core material having a water insoluble polymeric coating encapsulating said core and a process for the production thereof. The encapsulating coating comprising a water-borne, polyvinylidene chloride-based latex composition which provides for the release of the water soluble core material over an extended period of time.

Abstract: A buoyant controlled release pharmaceutical powder formulation is provided which may be filled into capsules and releases a pharmaceutical of a basic character at a controlled rate regardless of the pH of the environment, which formulation includes a basic pharmaceutical, up to about 45% by weight of a pH dependent polymer which is a salt of alginic acid, such as sodium alginate, up to about 35% by weight of a pH-independent hydrocarbon gelling agent having a viscosity of up to about 100,000 centipoises in 2% solution at 20.degree. C. and excipients.

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 controlled-release pharmaceutical preparation of 3-isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine. The controlled-release preparation is in the form of powder or granule containing 3-isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine, coated with medically non-active substance or in the form of rectal suppository containing 3-isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine. Further the controlled-release is prepared by implanting 3-isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine in fatty materials, or granulating it and coating the resultant particles with medically non-active substance.

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: Controlled delivery of biologically active agents such as pharmaceuticals to body sites is accomplished by combination with a monoglyceride and a vegetable oil. Upon contact with an aqueous liquid, the composition forms a reverse hexagonal liquid crystalline phase matrix which releases the active agent in controlled fashion. The method of delivery is particularly useful for the treatment of periodontal disease by insertion of the liquid crystalline phase precursor composition directly into the periodontal pocket, where water from the gingival fluid induces the spontaneous in situ formation of the reverse hexagonal liquid crystalline phase matrix.

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

Abstract: An extended release pharmaceutical formulation adapted to approach zero order release of drug over a 12 to at least 24 hour period, comprised of a mixture of 0 to aobut 50% of an immediate release particle containing a drug, inert substrate and binder, coated with talc and up to 100% of an extended release particle comprising the immediate release particle coated with a dissolution modifying system containing plasticizers and a film forming agent.

Abstract: An alginate-based depot drug form for which the rate of release of the active substance in vitro can be adjusted very precisely is described.

Abstract: Pressing having sustained release of active compound for the oral or parenteral administration of medicaments, which contains at least one solid pharmaceutical active compound, polylactic acid and a homo- or copolymer of D(-)-3-hydroxybutyric acid and processes for its production.

Abstract: A controlled release formulation comprising an adsorbate of a mixture of a pharmaceutically useful active ingredient and an inactive substance adsorbed on a cross-linked polymer. The inactive substance is selected to modify the dissolution of the active ingredient from the cross-linked polymer in vivo.

Abstract: A sustained or controlled release tablet is disclosed. The tablet comprises a water soluble medicament, a hydroxypropyl methylcellulose having sustaining action, a pharmaceutical binding agent, and a hydrophobic component.

Abstract: Implant preparations capable of sustained action when inserted are comprised of powder of a natural lipoidal substance in thorough admixture with bioactive macromolecule, followed by compression under pressure into a disc or rod that can be broken and used in small pieces as well.

Abstract: Pharmaceutical compositions for use in the treatment of cough/cold symptoms comprising loratadine, ibuprofen and pseudoephedrine are disclosed.

Abstract: Prolonged parenteral release of a bioactive polypeptide at desirably effective levels can be achieved by administering 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: There is described a new inclusion complex of nicardipine or its hydrochloride with beta-cyclohdextrin, which is prepared by admixing nicardipine or its hydrochloride with beta-cyclodextrin in a molar ratio of the compounds 1:0.9-1.1 under stirring at a temperature from about room temperature to the boiling temperature of the reaction mixture in an aqueous or ethanolic medium, cooling the reaction mixture to 0.degree. to 5.degree. C. and isolating the desired complex.The inclusion complex of nicardipine or its hydrochloride posesses cerebrovascular-vasodilatory and coronary-vasodilatory properties, which are equally well expressed as those of nicardipine or its hydrochloride themselves, yet owing to the better solubility of the complex at a higher pH range, such as it exists e.g. in the intestinal tract, the manufacture of sustained release pharmaceutical forms is made possible, whereby a greater extent of dissolution of the active substance is provided also in the intestinal juice.

Abstract: A process is provided for the condensation polymerizing lactic acid to a polymer with a weight average molecular weight of 2,500 to 4,500 containing less than 4% lactide and for a controlled release dosage form comprising a pharmaceutically active ingredient in a matrix of poly(lactic acid) and its copolymers with glycolic acid, valerolactone, .epsilon.-caprolactone, .epsilon.-decalactone, hydroxybutyric acid, .beta.-hydroxyvaleric acid and dioxanone.

Abstract: A method for increasing growth hormone secretion or inducing the biologic effects of growth hormone by continuous administration of growth hormone releasing factor or analog thereof is disclosed.

Abstract: Polymers from ethylenically unsaturated monomers, cross-linked by a substituted divinylazobenzene are useful as pharmaceutical compositions for the delivery of medicaments. The polymers are degraded by the enzymes of the upper gastrointestinal tract or are transferred intact past the upper gastrointestinal tract, to deliver the medicament to the large intestine. In particular, the polymers contain divinylazobenzene compounds of the formulae ##STR1## wherein R.sub.1 and R.sub.2 are independently selected from the group consisting of H, (except that R.sub.1 and R.sub.2 are not both H), Cl, Br, I, NO.sub.2, NH.sub.2, RO, ArO, COOH or salts thereof, COOR, COOAr, CHO, COR, SO.sub.3 H or salts thereof, R or Ar and wherein R is alkyl of up to 18 carbon atoms and Ar is mono- or bicyclic aryl of up to 15 carbon atoms.

Abstract: Inclusion complexes of hydroxypropyl, hydroxyethyl, glucosyl, maltosyl and maltotriosyl derivatives of .beta.- and .gamma.-cyclodextrin with the reduced, biooxidizable, blood-brain barrier penetrating, lipoidal forms of dihydropyridine.revreaction.pyridinium salt redox systems for brain-targeted drug delivery provide a means for stabilizing the redox systems, particularly against oxidation. The redox inclusion complexes also provide a means for decreasing initial drug concentrations in the lungs after administration of the systems, leading to decreased toxicity. In selected instances, complexation results in substantially improved water solubility of the redox systems as well.

Abstract: A pharmaceutical composition for intranasal administration comprising GHRH, a cholinergic agonist and in case a bile salt, suitable for the treatment of growth disorders and for use in the diagnosis of GH hypophyseal functionality.

Abstract: Stable sustained release wax- and polymer-coated drug-ion exchange resin complexes especially useful in preparing oral suspensions are disclosed.

Abstract: A topical preparation of danazol comprising a matrix base, danazol retained therein, and optionally a release-promoting agent is provided.The topical preparation is more effective than oral administration of danazol in the shrinkage of endometriosis tissue, the induction of pregnancy, and the like. It does not show any side effects that have been encountered in the oral administration of danazol. Thus, the preparation is very useful remedy for endometriosis.

Abstract: Disclosed are oral pharmaceutical preparations which comprise a pharmacologically active drug bound to small particles of an ion-exchange resin to provide a drug-resin complex having a drug content above a specified value. The drug-resin complex is subsequently coated with a water-permeable diffusion barrier coating that is insoluble in gastrointestinal fluids thereby providing a controllable sustained release of drug under conditions encountered in the gastrointestinal tract.

Abstract: The invention is an injection molding method for the preparation of sustained release boluses which are useful for administration of insect growth regulators or other veterinary compositions to animals.

Abstract: A pharmaceutical composition comprising a benzoyl urea compound (A) selected from the group consisting of a benzoyl urea compound (I) having the formula: ##STR1## wherein X is a halogen atom, a nitro group or a trifluoromethyl group, provided that when Y is a nitro group, X is a halogen atom or a nitro group, Y is a hydrogen atom, a halogen atom, a nitro group or a trifluoromethyl group, Z.sub.1 is a halogen atom or a trifluoromethyl group, Z.sub.2 is a hydrogen atom or a halogen atom, and A is a .dbd.CH-- group or a nitrogen atom, and a benzoyl urea compound (II) having the formula: ##STR2## wherein each of X.sub.1 and X.sub.2 is a hydrogen atom, a halogen atom or a nitro group, provided that when Y is a nitro group, X.sub.

Abstract: The present invention relates to a multiple-unit-dose comprising L-dopa as pharmaceutically active compound, whereby the composition provides a release of L-dopa in accordance with a test in accordance with U.S. Pharmacopeia Standards in an artificial gastric juice having a pH of at most 1.2 of at most 20% by weight during 1 hr, and in a phosphate buffer according to the same standard a release of at least 35% by weight during 1 hr, and at least 80% by weight during 3 hrs.

Abstract: A dairy cow injected with a sustained release formulation comprising bovine somatotropin, a wax, and an oil produces more milk for 28 days.

Abstract: Biodegradable alkyloxycarbonylmethyl or aryloxycarbonylmethyl polyaspartate and polyglutamate which can be used as a carrier for drugs which are either in the encapsulated state or are incorporated in the polymer matrix. The polypeptide thus loaded degrades enzymatically in the organ where it has been placed and thus gradually releases the drug which it contains.

Abstract: A controlled release formulation comprising an adsorbate of a mixture of a pharmaceutically useful active ingredient and an inactive substance adsorbed on a cross-linked polymer. The inactive substance is selected to modify the dissolution of the active ingredient from the cross-linked polymer in vivo.

Abstract: An active agent delivery system for the controlled administration of macromolecular polypeptides which comprises a micro-suspension of water-soluble components in a polylactide matrix.

Abstract: Healing of injured avascular tissue is promoted by applying angiogenic factor in proximity to the injured tissue.

Abstract: Healing of injured avascular tissue is promoted by applying angiogenic factor in proximity to the injured tissue.

Abstract: Polymers are provided that are useful for making biodegradable sustained release agent dispensers and which contain at least one of the following mer units (I) and (II) ##STR1## wherein X is a quadrivalent organic grouping, A and B are hydrogen or lower alkyl, and R is hydrocarbyl or oxyhydrocarbyl of 1 to 14 carbon atoms and, if oxyhydrocarbyl, containing 1 to 4 oxy groups, and may be either aliphatic or aryl, unsubstituted or substituted with one or more lower alkyl, amino, nitro or halogen moieties. Methods of synthesizing the novel polymers are also provided, as biodegradable beneficial agent dispensers prepared using the novel polymers.

Abstract: A pharmaceutical preparation for the treatment of tinea pedis, containing as basic components about 0.1% to about 2.5% of croconazole hydrochloride and about 1%-15% of an ethyl acrylate-methyl methacrylate copolymer in an aqueous alcohol, and if necessary, about 0.1% to about 2.5% of a thickening agent and/or a plasticizer.

Abstract: Pullulan forms an association complex with PEG in a hydrous system. The assocation complex, as well as its pullulan and PEG components, exerts a decreased solubility in water. The association reduces or even eliminates the excessively high water-solubility, threading and stickiness of pullulan so that this extends the uses of pullulan and PEG such as those in gradually disintegrable- and sustained release-shaped articles for consumer's products, toiletries, cosmetics, pharmaceuticals and feeds.

Abstract: Compositions for the controlled and prolonged release of macromolecular compounds comprise a porous matrix of chitosan having dispersed therein the macromolecular compound. Examples of macromolecules used in the composition are pharmacologically active ones such as peptide hormones, e.g. growth hormone.

Abstract: Tablets containing nutritional and therapeutic substances in conjunction with dietrary fibre substances. The tablets can be formulated in two layers which separate the nutritional and therapeutic substances from the fibre.

Abstract: A device for the controlled release of an active material into an aqueous medium comprises a water soluble capillary tube (11) the bore (12) of which contains an active material (13). Dissolution of the active material is diffusion limited during a delay period while the capillary is dissolving. When dissolution of the tube is complete rapid dissolution of the remaining active material then takes place.

Abstract: An antigen delivery system utilizing a biodegradable polymer with good mechanical properties in combination with a material stimulating the immune system. The material having adjuvant activity may be polymer degradation products or an adjuvant which is contained within or bound to the polymer. In one embodiment, the polymer is formed from tyrosine dipeptides. Poly(CTTH-iminocarbonate) is a preferred tyrosine dipeptide polymer for constructing implantable delivery systems for antigenic material. The polymer is not an adjuvant in itself but degrades into products which stimulate the immune system. The tyrosine dipeptide can also be used as a conventional adjuvant.

Abstract: The invention relates to sustained release compositions of growth hormones and/or related compounds and multiple water-in oil-in-water emulsions. The invention also relates to methods for increasing and maintaining increased levels of growth hormones and/or related compounds in the blood of treated animals for extended periods of time, increasing weight gains in animals and increasing milk production of lactating animals by the administration of a composition of the invention.

Abstract: A method and compositions, for treating an animal with an injured spinal cord, causing loss to sensory function and motor control, to regain such function and control. The method comprises the administration of a guanidine compound and a serotonergic receptor agonist or a dopaminergic receptor agonist, and preferably a combination with an anti-desensitization agent, such as a xanthine, a b-adrenergic receptor agonist or a vascular skeletal muscle dilator. The composition comprises a guanidine compound and a second compound acting in conjunction therewith or preventing desensitization thereof.

Abstract: A composition for use in an aqueous environment which .[.comprise.]. .Iadd.comprises .Iaddend.a formulation containing a water-soluble pharmaceutically beneficial agent, a water-insoluble, water-permeable film coating surrounding the formulation, and particulate, water-soluble, pore-forming material dispersed within the film coating.The questions raised in reexamination request No. 90/001,344, filed Oct. 5, 1987, have been considered and the results thereof are reflected in this reissue patent which constitutes the reexamination certificate required by 35 U.S.C. 307 as provided in 37 CFR 1.570(e).