Abstract: Sustained release microcapsules including a water soluble drug and an organic basic substance as a drug retaining substance of this invention not only have a high rate of incorporation (trapping rate), but also show little initial release so that they can be administered safely and bring about persistent, stable sustained release.

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: A sustained-release pharmaceutical preparation comprising an admixture of uncoated and/or single walled water soluble drug, such as aspirin, and dual walled coated drug. The dual wall structure has an inner wall microencapsular control coating, such as ethyl cellulose, and an outer wall enteric coating such as cellulose acetate phthalate. The dual walled coated drug has a delayed, gradual, long-term release which takes place in the intestines while the uncoated and/or single walled drug has immediate therapeutic properties upon dissolution in the stomach. The outer wall enteric coating may be applied to microencapsulated core drug by a coacervation, spray coating or other process.

Abstract: The present invention relates to a sequential polymerization process for preparing a water-insoluble dispersion of core/shell particles. In one embodiment the process may be employed to produce a particulate dispersion useful in making water-based coating compositions wherein on drying the particulate dispersion serves as an opacifying agent. In another embodiment the process may be employed to microencapsulate a hydrophobic target material, such as a biocide or herbicide.

Abstract: A sustained-release pranoprofen preparation is disclosed. The preparation comprises an effective amount of pranoprofen and one or more sustained-release components selected from the group consisting of oily components, water-soluble components, water-insoluble components, and intestinally soluble components. It controls release of pranoprofen and lowers the maximum pranoprofen concentration in blood, maintaining its concentration in blood at a certain level for a long period of time. It reduces risks of side effects and can effectively treat diseases with dosing once or twice a day.

Abstract: A process for encapsulating a wide variety of target materials, including both hydrophilic and hydrophobic materials, employs condensation of two reactive compounds to form shells around core phase particles including target material dispersed in a continuous phase. One of the reactive compounds has at least two active methylene functional groups per molecule, the other being an active methylene-reactive crosslinking agent. Either type of the reactive compounds can be dispersed in the continuous phase, the other being dispersible in the core phase. Applications include controlled release microencapsulation of agriculture chemicals and biocides.

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: A soft capsule composed of a plurality of cells coalesced to each other and filling substances encapsulated in the individual cells, the wall of at least one of the cells being formed of a material different from a material forming the wall of at least one of the other cells, and said capsule being seamless.

Abstract: Cosmetic or pharmaceutical composition consisting of a dispersion in a physiologically acceptable aqueous phase D of vesicles of ionic and/or nonionic amphiphilic lipid(s), the vesicles being bounded by one or more lipid lamellae, the lipid lamellae containing at least one retinoid compound and the aqueous dispersion phase a pyrimidine derivative. The said composition may be used by topical application on the hair and scalp.

Abstract: Disclosed herein are vesicle compositions for controlled sustained release of an encapsulated therapeutic agent after parenteral administration. By adjusting the osmolarity between the suspending solution and the solution within the vesicles by adjusting the concentration of the suspending solution, the rate of release of the therapeutic agent after parenteral administration can be varied. The compositions can be effectively administered by intramuscular, subcutaneous injection or other means.

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: An insecticidal and/or acaricidal and/or nematicidal composition having a rapid efficacy and residual activity which comprises a mixture of a poorly water-soluble organophosphorus insecticide and/or acaricide and/or nematicide and/or a poorly water-soluble carbamate insecticide and/or acaricide which have been microencapsulated in water-insoluble polymer coatings with a dispersing agent used in forming a microcapsule part, with a poorly water-soluble pyrethroid insecticide and/or acaricide emulsified or suspended in water with the above-mentioned dispersing agent used in forming a flowable part.

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: Biocide treatment of the water system of a papermaking process comprising the steps of encapsulating the biocide as the core of the capsule in a water suspension, in which the shell is degradable at high water dilution, and introducing the microcapsules into the water stream to undergo dilution release.

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: Microcapsules containing a substantially water-insoluble liquid material, such as an anilide herbicide, and optionally also a herbicide antidote, within a porous shell to effect a slow rate of release of said herbicide (and optionally said antidote) through said shell, are produced by a process which comprises (a) providing an organic solution comprising said material and an etherified amino resin prepolymer dissolved therein which from about 50% to about 98% of the methylol groups of said prepolymer have been etherified with a C.sub.4 -C.sub.

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: 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: A new method of producing paucilamellar lipid vesicles has been developed. The vesicles are made of non-phospholipid surfactants. The paucilamellar lipid vesicles have 2-8 lipid bilayers surrounding a central cavity which may be filled with either an aqueous-based solution or an oil or wax.

Abstract: There is disclosed a process for preparing compositions comprising microcapsules by phase separation microencapsulation wherein the hardening agent employed is a volatile silicone fluid and with the compositions prepared thereby. The use of the volatile silicone fluid as a hardening agent permits the production of microcapsules substantially free of any alkane hardening agent, eliminating potential combustability problems of the prior art processes and toxicity problems of the prior art compositions.

Abstract: A controlled release pharmaceutical preparation comprising a core containing a medicinal compound and a coating layer containing a water-repellent salt and a water-insoluble and slightly water-permeable acrylic polymer having trimethylammoniumethyl group. Said preparation releases a medicinal compound in a sigmoid type dissolution pattern irrespective of the PH of a dissolution medium.

Abstract: Cosmetic or pharmaceutical composition consisting of a dispersion in an aqueous medium D of lipidic spherules to the lipidic phase of which there is associated at least one lipoprotide free of sulfhydryl function selected amongst the mono- or polyacylated derivatives of amino acids or of polypeptides, wherein the acyle residue R--CO comprises a C.sub.13 -C.sub.19, hydrocarbonated chain R, at least one of the functions which connects the polypeptidic chain or the amino acid residue to the lipophilic chain being an amide function, the carboxylic functions of the polypeptidic chain or of the amino acid residue being partially or completely neutralized by means of one or a plurality of alkaline cations, an ammonium ion or a substituted ammonium derived from an amine, said lipoprotide or lipoprotides being present in a ratio from 1 to 15% by weight based on the total weight of said lipidic phase.

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: A controlled-release organic nitrate formulation for once-per-day oral administration is provided by spheres having a core which includes an organic nitrate, and a membrane surrounding the core composed of a pharmaceutically acceptable, film forming polymer. The film forming polymer is effective to permit release of the organic nitrate from the spheres, over a daily dosing period, at a rate that achieves a therapeutically effective level of the organic nitrate, while effecting a drug holiday towards a latter portion of the daily dosing period so as not to induce tolerance.

Abstract: The microcapsules of the invention are comprised of crystallizable polymers which are preferably side-chain crystallizable polymers or cross-linked, side-chain crystallizable polymers having a specific first order transition point or "melt" temperature. The polymers are caused to form microcapsules and thereby encapsulate one or more compounds generally referred to herein as an active ingredient such as a herbicide, insecticide, fungicide, or fertilizer. The polymer of the microcapsule surrounds the active ingredient separating it from the outside environment. Crystallizable polymers used herein have temperature-dependent permeabilities with respect to a given component such that this component is kept out of contact with the active ingredient at a temperature below a given first order transition point and (due to increased permeability) is allowed to contact the active ingredient at a temperature at or above the transition point.

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: Shipping fever, and other stress-related diseases in livestock, are treated by administration of a microencapsulated composition comprising IL-2 conjugated with a polyoxyethylene polymer, and mixed with a release-modulating amount of humen serum albumin. The microcapsules are administered parenterally, and release an effective amount of conjugated IL-2 continuously over a period of 14-30 days. These microcapsules are also effective in the treatment of cancer in mammals.

Abstract: Microspheres comprising polylactic acid and a water soluble physiologically active substance and having a mean particle size of from about 0.01 .mu.m to 300 .mu.m, which show not more than 30% of an eluted amount of said physiologically active substance based on the content of said physiologically active substance in the polylactic acid type microspheres after 24 hours in in vitro elution test in phosphate buffer of pH 7.4 at 37.degree. C., and a process for preparing the same. The polylactic acid type microspheres of this invention is advantageous in that the active substance can be uniformly incorporated into the microspheres without loss of the activity, can gradually release the active substance for a long time of period of more than one week.

Abstract: This invention relates to the liposome compositions which are characterized in that the phase transition temperature of the membrane is in the range of 40.degree. to 45.degree. C. and the osmotic pressure of a drug-containing solution to be entrapped in liposomes is 1.2 to 2.5 times higher than that of body fluid of warm-blooded animals. The compositions are useful for treatment of solid tumors in hyperthermia therapy.

Abstract: Improved sustained-release delivery forms comprising Lewis acid-Lewis base salt microparticulate material modified by the addition of at least one additional constituent known as an "adjuvant" selected from the group consisting of carbomers, poloxamers and tetronomers. Adjuvants may assist in the manufacture of the microparticle or may provide additional advantageous characteristics such as assisting in solubilizing a core material or forming of the microparticle wall or both. Adjuvant modified microparticles have improved controlled release characteristics, have greater mechanical and thermal stability and have increased capacity for a wide range of core materials.

Abstract: The present invention relates to a process for producing a microcapsule comprising a permeability-controllable membrane. This process comprises adjusting the ionic strength of a solution of a soluble chitin derivative, and then bringing this solution into contact with a solution of a polyanionic polysaccharide, its salt or a mixture thereof.

Abstract: In accordance with the present invention, these and other objects are achieved by a pharmaceutical composition comprised of 1) a pharmaceutical core which is further comprised of a pharmaceutically active dose of a compound and, 2) a microencapsulating polymer which coats the pharmaceutical core and is capable of taste-masking the active compound. The polymer coating maintains its integrity, i.e., does not fracture and release active when tabletted and/or chewed, and can provide immediate release of the active compound in the stomach, or alternatively, in certain embodiments, can release the active agent in the upper intestinal tract or in sustained release fashion. Additionally, the polymeric coating compositions or the pharmaceutical core may contain diluents, fillers, bulking agents, and plasticizers. The polymeric coatings may also contain pigments and opacifiers to promote compliance and enhance the storage stability of light sensitive active agents.

Abstract: A method of delivering a bioactive agent to an animal entailing the steps of encapsulating effective amounts of the agent in a biocompatible excipient to form microcapsules having a size ranging from between approximately one micrometer to approximately ten micrometers and admnistering effective amounts of the microcapsules to the animal. A pulsatile response is obtained, as well as mucosal and systemic immuity. Related compositions are also provided.

Abstract: An active agent delivery device comprises (a) microporous material comprising a matrix consisting essentially of linear ultrahigh molecular weight polyolefin, a large proportion of finely divided water-insoluble filler of which at least about 50 percent by weight is siliceous, and interconnecting pores; and (b) a releasable active agent or precursor thereof associated with at least a portion of the filler.

Abstract: A process for microencapsulating bioactive substances in biocompatible polymers according to the phase-separation principle, wherein an excess of an ethyl or isopropyl ester of a straight-chain fatty acid having 12-18 carbon atoms is used as the hardening liquid, and the pharmaceutical compositions containing the microcapsules prepared by this process. Isopropyl myristate and isopropyl palmitate are preferred hardening liquids.

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: An active principle microencapsulated in an envelope formed by interfacial polymerization of two non-miscible phases A and B, organic phase A comprising at least one water insoluble active principle which do not react with each other, a polyfunctional monomer a and a solvent for the active principle and aqueous phase B comprising a polyfunctional monomber b and a catalyst which allows a progressive diffusion of the active principle and protects the same from the environment.

Abstract: This invention relates to microcapsules based on gelatin and anionic polysaccharides of low molecular weight which may contain solid or liquid matters, prepared by coacervation. The aqueous polysaccharide solutions which may be used present a low viscosity, the value of which is a function of the nature of the polysaccharide; for a concentration of 15 g/l, it is, at 75.degree. C., generally between 1 and 20 mPa.s. These polysaccharides are depolymerization products of natural products:alginates, carragheenans, pectins and pectates, carboxymethylcelluloses, carboxymethylguars and carboxymethyl starches. The microcapsules may be isolated and dried.

Abstract: The process according to the invention comprises:(1) the preparation of a liquid phase consisting essentially of a solution of a substance A in a solvent or in a mixture of solvents, and containing the substance B in solution or as a dispersion,(2) the preparation of a second liquid phase consisting essentially of a non-solvent or a mixture of non-solvents for the substances A and B, and supplemented with one or more surfactants, the solvent or mixture of solvents of the first phase being miscible in all proportions with the non-solvent or mixture of non-solvents of the second phase,(3) the addition of the first phase to the second phase with moderate agitation so as to produce a colloidal suspension of nanocapsules, the wall of which is constituted by the substance A and the core by the substance B,(4) if desired, the removal of all or part of the solvent or the mixture of solvents and of the non-solvent or the mixture of non-solvents so as to produce a colloidal suspension of nanocapsules of the desired con

Abstract: Disclosed are slow-release vermin-repellent microcapsules composed of a core substance and a wall film formed around the said core substance to encapsulate the same, in which the core substance is diethyltoluamide of a formula: ##STR1## and the wall film has a function of slow-releasability.

Abstract: Capsules containing a hygroscopic or deliquescent component are stabilized by a) forming a mixture of the hydrogscopic or deliquescent compound with a sufficient quantity of water to achieve an equilibrium, b) adding a thickening agent and c) heating the solution or suspension; and introducing the heated composition so formed into the capsule. Preferably an equilibrium-protecting agent, such as glycerin, is also added.

Abstract: An active agent delivery device comprises (a) microporous material comprising a matrix consisting essentially of linear ultrahigh molecular weight polyolefin, a large proportion of finely divided water-insoluble filler of which at least about 50 percent by weight is siliceous, and interconnecting pores; and (b) a releasable active agent or precursor thereof associated with at least a portion of the filler.

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: Fish feed compositions supplemented with up to 0.5% L-carnitine, preferably between 0.01% to 0.3% L-carnitine, produce greater growth gains, decreased fat levels in tissues, and increased resistance to stress (ammonia toxicity) in fish, as compared to fish fed the same diet without supplemental carnitine.

Abstract: The present invention relates to encapsulated parasiticides, a method for their production, and methods of treatment to prevent or eradicate infestation using the encapsulated parasiticides. The formulations of the present invention are water or oil-based and have many advantages over conventional formulations in safety, cost, and utility.

Abstract: The present invention provides an apparatus and method for manufacture of multilamellar or paucilamellar lipid vesicles. The apparatus and method use shear mixing in a substantially cylindrical mixing chamber having at least one tangential input for rapid production of the lipid vesicles.

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: There are herein disclosed rodent-repellent microcapsules in which a core material is coated with a wall material of the microcapsules, the core material being a solution containing cycloheximide; a rodent-repellent resin composition comprising said microcapsules; a rodent-repellent coating material comprising said microcapsules; and a rodent-repellent adhesive comprising said microcapsules.

Abstract: There is disclosed a process for preparing compositions comprising microcapsules by phase separation microencapsulation wherein the hardening agent employed is a volatile silicone fluid and with the compositions prepared thereby. The use of the volatile silicone fluid as a hardening agent permits the production of microcapsules substantially free of any alkane hardening agent, eliminating potential combustability problems of the prior art processes and toxicity problems of the prior art compositions.

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).