Abstract: The Process according to the invention comprises:(1) the preparation of a liquid phase consisting essentially of a solution of the substance in a solvent or in a mixture of solvents to which may be added one or more surfactants,(2) the preparation of a second liquid phase consisting essentially of a non-solvent of a mixture of non-solvents for the substance and to which may be added one or more surfactants, the non-solvent or the mixture of non-solvents for the substance being miscible in all proportions with the solvent or the mixture of solvents for the substance,(3) the addition of one of the liquid phases prepared in (1) or (2) to the other with moderate stirring so as to produce a colloidal suspension of nanoparticles of the substance and,(4) if desired, the removal of all or part of the solvent or the mixture of solvents for the substance and of the non-solvent or the mixture of non-solvents for the substance so as to produce a colloidal suspension of nanoparticles of the desired concentration or to pro

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: 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 slow release pharmaceutical excipient of an inert diluent and a hydrodrophilic material including xanthan gum and a galactomannan gum capable of cross-linking the xanthan gum in the presence of aqueous solutions.

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: The process according to the invention comprises: (1) the preparation of a liquid phase consisting essentially of a solution of the substance in a solvent or in a mixture of solvents to which may be added one or more surfactants, (2) the preparation of a second liquid phase consisting essentially of a non-solvent or a mixture of non-solvents for the substance and to which may be added one or more surfactants, the non-solvent or the mixture of non-solvents for the substance being miscible in all proportions with the solvent or the mixture of solvents for the substance, (3) the addition of one of the liquid phases prepared in (1) or (2) to the other with moderate stirring so as to produce a colloidal suspension of nanoparticles of the substance, and (4) is desired, the removal of all or part of the solvent or the mixture of solvents for the substance and of the non-solvent or the mixture of non-solvents for the substance so as to produce a colloidal suspension of nanoparticles of the desired concentration or to

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: This application describes the preparation and in vivo testing of surface coatings and matrix materials, which when applied to or caused to comprise the carriers for drugs and diagnostic agents, and administered in a fashion that allows efficient vascular access, causes the carriers to recognize determinants present or normal or focally diseased endothelium, and induces the following in vivo effects: 1) rapid, partial or total endothelial envelopment of the drug (diagnostic) carrier; 2) sequestration of the carrier and protecting entrapped agent from blood vascular clearance at an early time (2 minutes) when the endothelial pocket which envelops the carrier still invaginates into the vascular compartment; 3) acceleration of the carrier's transport across or through the vascular endothelium and/or subendothelial structures into the tissue compartment (interstitium); and 4) improvement of the efficiency with which the drug (or diagnostic) carrier migrates across the endothelium, or epi-endothelial or subendothe

Abstract: A weight control product is preferably in the form of agglomerated particles and is reconstitutable in water. The product contains low lactose milk and a dietary fiber system which is a particular blend of soluble, insoluble, fermentable and non-fermentable fibers. The components of the dietary fiber system are oat hull fiber, gum arabic and sodium carboxymethylcellulose. About 27% of the calories provided by the product are contributed by protein, about 50% of the calories are contributed by carbohydrates, and about 23% are contributed by fats.

Abstract: A liquid nutritional product comprising a fat source and a dietary fiber system. The dietary fiber system as a whole comprises by weight: (a) 5% to 50% dietary fiber which is both soluble and fermentable, 5% to 20% dietary fiber which is both soluble and non-fermentable, and 45% to 80% dietary fiber which is both insoluble and non-fermentable. Less than 10% of the total calories in the product comprise saturated fatty acids, no more than 10% of the total calories in the product comprises polyunsaturated fatty acids, and the ratio of the n-6 to n-3 fatty acids in the product being in the range of 2 to 10. Preferably the dietary fiber which is both soluble and fermentable is gum arabic; the fiber which is both soluble and non-fermentable is sodium carboxymethylcellulose, and the fiber which is both insoluble and non-fermentable is oat hull fiber.

Abstract: Taken as a whole a blend of dietary fiber contains, by weight: 5% to 50% of a dietary fiber which is both soluble and fermentable; 5% to 20% of a dietary fiber which is both soluble and non-fermentable; and 45% to 80% of a dietary fiber which is both insoluble and non-fermentable. Preferably, the dietary fiber which is both soluble and fermentable is gum arabic; the dietary fiber which is both soluble and non-fermentable is sodium carboxymethylcellulose; and the dietary fiber which is both insoluble and non-fermentable is oat hull fiber.

Abstract: A dosage form for oral administration of a pharmaceutically active substance characterized in that it includes a encapsulated or embedded pharmaceutically active substance in a pharmaceutically acceptable non-aqueous liquid.

Abstract: A pharmaceutical composition comprising a crystalline sugar alcohol derived from at least one mono- or polysaccharide having uniformly dispersed within its crystal matrix particles of at least one pharmaceutically active compound is disclosed. Also disclosed is a method of producing such a uniformly dispersed pharmaceutical composition by the controlled crystallization of the molten sugar alcohol having the pharmaceutically active material dispersed therein.

Abstract: Processes for producing biocompatible and biodegradable protein microspheres with controlled porosity and microsphere sizes are disclosed. Generally, the processes are accomplished as follows: (a) dissolving a source of protein in a mildly acidic or basic aqueous medium, in the presence or absence of a biomodifying agent, (b) adding a cross-linking reagent to the dissolved protein molecules in an amount effective subsequently to cross-link the protein molecules without gelation; (c) adding a water soluble surfactant to modify the surface of the partially cross-linked protein molecules, (d) adding a water soluble organic desolubilizer to desolubilize the protein molecules to allow cross-linkage of nearby protein molecules into water-insoluble microspheres. Alternatively, the cross-linking step of (b) is employed after desolvation of the microspheres.

Abstract: Systemic antiviral treatment using a narrow class of aliphatic straight-chain saturated monohydric alcohols which have from 27 to 32 carbons in the chain in physiologically compatible compositions for injection or trans-mucus membrance introduction into humans and other mammals is disclosed.

Abstract: Sprayable, starch-based formulations for autoencapsulating biological control agents, such as pathogenic bacteria and viruses, incorporate a sugary material to promote adherence of the encapsulated agent to treated foliage. The autoencapsulated pathogens are characterized by high survivability and are useful in controlling insects and other pest species.

Abstract: Disclosed is a process for preparing polymeric compositions which are suitable for coating medicaments or for use in cosmetic formulations and the novel compositions prepared therefrom. The process makes stable, colloidal, latex-like dispersions of coating polymers which can be readily dried to form polymeric powder materials. The process makes use of a novel combination of a water-in-oil emulsifier and an oil-in-water emulsifier.

Abstract: A solid sustained-release preparation in the form of a needle-like or bar-like shape, which consists essentially of an active ingredient and a pharmaceutically acceptable biodegradable carrier (e.g. proteins, preferably collagen, gelatin, and a mixture thereof). The sustained release preparation can be administered to the body or implanted into the body by injection or an injection-like method and can release the active ingredient at an effective level for a long period of time when administered.

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 sustained release capsule or tablet formulation suitable for once-daily administration comprises an adsorbate of a mixture of a pharmaceutically useful dihydropyridine and a polyvinylpyrrolidone having an average-molecular weight greater than 55,000 adsorbed on a cross-linked polyvinylpyrrolidone and blended with a polymer or mixture of polymers which gel in the presence of water, the amount of said polymer or polymers being effective to produce the desired sustained release effect.

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: The present invention relates to a process of stabilizing micellular particles such as vesicles and increasing the shelf life by suspending the particles in a polymeric gel matrix. The invention also relates to such particles suspended in the gel matrix with a protective gel surface thereabout which is capable of becoming fluid and converting the protective surface of an aqueous suspension.

Abstract: Inclusion complexes of hydroxypropyl-.beta.-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 reodox 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: The invention involves a method for making uniformly sized particles from solid compounds. First, a suitable solid compound is dissolved in a suitable solvent. Then, a precipitating liquid is infused, precipitating non-aggregated particles with substantially uniform mean diameter. The particles are then separated from the solvent. Depending on the solid compound and the desired particle size, the parameters of temperature, ratio of non-solvent to solvent, infusion rate, stir rate, and volume can be varied according to the invention. The precipitating liquid may be aqueous or non-aqueous, depending upon the relative solubility of the compound and the desired suspending vehicle.

Abstract: The instant invention relates to a method for converting phosphorus containing polymers from a two dimensional layered structure into a three dimensional structure by crosslinking such layers. The method and the resulting crosslinked polymers may be used to encapsulate active materials such as catalysts, pesticides, etc. by intercalating such active materials between the layers prior to crosslinking. Thus, the egress of said active materials into the environment during use may be hindered or prevented.

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: Anti-smoking oral preparations are provided containing a silver compound as the anti-smoking agent and a sweetener in which the silver compound is present in amounts of from 0.1 mg. to 2.5 mg. and the ratio of sweetness intensity based on sucrose to silver compound content is from 100:1 to 2500:1.

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

Abstract: Active ingredients useful in chewable articles of commerce are physically encased in non-porous, chewable, particles of elastomer and such particles are then incorporated in the articles of commerce. During mastication of the chewable article of commerce the active ingredient is released from the elastomer particles over a prolonged period of time. The active ingredients would include flavorants, intense sweeteners, colorants, medicaments, effervescent agents and tobacco.

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: Compositions comprising phospholipid-encapsulated vesicles of active ingredient and triglyceride are described. In a preferred embodiment the vesicles are composed of a hexamethylmelamine active ingredient, with trilaurin or trimyristin as the triglyceride and a mixture of distearoylphosphatidylcholine, distearoylphosphatidylglycerol and cholesterol in the phospholipid outer layer. Preferably the molar ratios of active ingredient: triglyceride: DSPC: CHOL:DSPG will be from about 1:4:2:1:0 to about 1:4:1:1:1. Glycerol may be added to the carrier phase to reduce agglomeration. The composition may be used to deliver otherwise aqueous-insoluble agents to humans or animals to treat, for example, tumors.

Abstract: A new inclusion complex of ibuproxam with beta-cyclodextrin is described, which is prepared by adding ibuproxam to a boiling aqueous solution of beta-cyclodextrin, stirring the reaction mixture at the boiling temperature, cooling to a temperature of 0.degree. C. to 5.degree. C. and isolating the title complex.The analgesic, antipyretic and antiinflammatory properties of the inclusion complex of ibuproxam with beta-cyclodextrin are equivalent to those of ibuproxam alone, but owing to its better water-solubility the complex can be more easily formulated into pharmaceutical forms.

Abstract: Microspheres, prepared by solvent removal from an oil-in-water emulsion using carboxylic acid salt surfactant, e.g., sodium oleate as the emulsifier.

Abstract: An organic phase which comprises a water-insoluble material to be encapsulated, a capsule-forming or matrix-forming monomer or prepolymer and, should this be desirable, a solvent, is dispersed in droplet form in an aqueous phase. The capsule-forming or matrix-forming monomer or prepolymer forms a sheath around the material to be encapsulated. As a capsule-forming or matrix-forming monomer, an organosilicon compound of the general formula ##STR1## is used, wherein R.sup.1 is a linear or branched, saturated or unsaturated, n-functional hydrocarbon moiety, which may be interrupted by groups containing oxygen, nitrogen or sulfur; R.sup.2 and R.sup.3 are the same or different and represent a hydrocarbon moiety with 1 to 6 carbon atoms or X; X is a hydroxyl group or a hydrolyzable group and n is a whole number greater than or equal to 1, with the proviso that, when n=1, R.sup.1 has at least 12 carbon atoms and R.sup.2 and R.sup.3 represent X or a prepolymer hereof.

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: This application describes the preparation and in vivo testing of surface coatings and matrix materials, which when applied to or caused to comprise the carriers for drugs and diagnostic agents, and administered in a fashion that allows efficient vascular access, causes the carriers to recognize determinants present or normal or focally diseased endothelium, and induces the following in vivo effects: (1) rapid, partial or total endothelial envelopment of the drug (diagnostic) carrier; (2) sequestration of the carrier and protecting entrapped agent from blood vascular clearance at an early time (2 minutes) when the endothelial pocket which envelops the carrier still invaginates into the vascular compartment; (3) acceleration of the carrier's transport across or through the vascular endothelium and/or subendothelial structures into the tissue compartment (interstitium); and (4) improvement of the efficiency with which the drug (or diagnostic) carrier migrates across the endothelium, or epi-endothelial or subend

Abstract: A system for controlled release both in vivo and in vitro of entrapped substances, either at a constant rate over a period of time or in discrete pulses, is disclosed. Biologically active substances, such as drugs, hormones, enzymes, genetic material, antigens including viruses, vaccines, or inorganic material such as dyes and nutrients, are entrapped in liposomes which are protected from the biological environment by encapsulation within semi-permeable microcapsules or a permeable polymeric matrix. Release of the entrapped substance into the surrounding environment is governed by the permeability of both the liposome and surrounding matrix to the substance.

Abstract: Process for the preparation of submicroscopic particles formed of a polymerized alkyl cyanoacrylate and containing a biologically active substance.At least one alkyl cyanoacrylate, in which the term "alkyl" denotes an alkyl radical having 1 to 12 carbon atoms, is added, with stirring, to pure water or to an aqueous solution or aqueous colloidal solution of an acid and/or of another water-soluble substance, and the stirring is continued until substantially all the alkyl cyanoacrylate has been converted to submicroscopic particles formed of polyalkyl cyanoacrylate; a biologically active substance is introduced into the reaction medium before the introduction of the monomer or after formation of the submicroscopic particles.The submicroscopic particles are useful as carriers for substances such as medical substances or products for diagnosis.

Abstract: Chemical biological agents to be encapsulated are blended into an aqueous dispersion of an unmodified starch comprising about 5% to about 25% by weight amylose. The dispersion, having an initial starch solids content of about 20% by weight, is characterized by completely disrupted starch granules and completely disassociated amylose molecules that are not significantly depolymerized. Subsequent drying is accomplished by reassociation of the amylose molecules which converts the dispersion into a protective matrix and binds the agents within the interstices of the reassociating starch chains. Rate of release of agents to the environment can be altered by varying the proportion of amylose in the starch. Encapsulation of biologically active compositions provides protection against degradative environmental conditions, improves safety in handling, and slows the release of such compounds to the surrounding medium.

Abstract: Forming a solution (preferably a true or complete solution) of mer in any permeant, reacting mer in presence of permeant substantially without rearrangement of the liquid system into separate phases and substantially without encapsulation (defined as any form of entrapment by polymeric solidification, including microencapsulation) and recovering a liquid product useful in formulating slow-release products.

Abstract: A sustained absorption propranolol-containing pellet for oral administration comprises a core of propranolol or a pharmaceutically acceptable salt thereof and an organic acid embedded in a polymeric material in a multi-layer arrangement and an outer membrane which permits release of the propranolol at a controlled rate in an aqueous medium. The pellet has a dissolution rate in vitro in an aqueous medium, which when measured in a basket assembly according to U.S. Pharmacopoeia XX at 37.degree. C. and 75 r.p.m., is not more than 15% of the total propranol after 2 hours of measurement in a buffer solution at pH 7.5. Not more than 30% of the total propranolol is released after a total of 4 hours of measurement and not more than 63% of the total propranolol is released after a total of 6 hours.

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: This invention relates to solid compositions wherein a non-cosmetic functional material is entrapped in the lattice of the cross-linked polymer during in situ polymerization of the monomers forming the polymer lattice. The invention provides for conversion of solid and/or liquid products into solid, free-flowing forms by entrapment of the functional materials in a hydrophobic polymer lattice.

Abstract: A slow release formulation to be administered to humans or animals, comprising primary granules which contain an active ingredient and are in a secondary matrix of a water soluble/dispersible slow release material, the granules themselves comprising particles containing the active ingredients and in a primary matrix of a water soluble/dispersible slow release material.Optionally the formulation comprises a binder phase of a water insoluble slow release material having embedded therein secondary granules comprising the secondary matrix containing the primary matrix granules.The water soluble/dispersible material may be a polysaccharide and acacia and low viscosity methylcellulose are exemplified, as well as alginate and gelatine.

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: Treatment of cellular disorders involving abnormal solid cellular growths involves introduction of cytotoxic reagents dispersed in a physiologically acceptable proteinaceous matrix into the solid cellular growth or area of an existing or removed solid cellular growth. Enhanced effectiveness of the drug is observed, with reduced cytotoxic effects on cells distant from the site of introduction. Other drugs may be included to enhance therapeutic gain and reduce adverse affects to normal tissue.

Abstract: A granular pesticide composition is prepared by reacting polyvinyl alcohol, pesticide, a borate, and optional filler(s) in water until a gel is formed, drying the gel, and then grinding the product to the desired particle size. The product is then applied to the soil for controlling pests.

Abstract: Human Growth Hormone-Releasing Factor (hGRF) analogs having the sequence [X.sup.3, Y.sup.8, Z.sup.25, Nle.sup.27 ]-hGRF(1-A)--B, wherein X, Y and Z are selected from the group consisting of Asn and Asp, A has a value from 29-44, and B is NH.sub.2 or OH are synthesized and administered to animals to stimulate the release of Growth Hormone (GH).