Abstract: A new method of coupling proteins and other targeting molecules to lipid vesicles has been developed. A bifunctional agent forms a covalent bond without damaging the lipid structure and permits retention of protein activity.

Abstract: Microparticle of cellulose acetate and derivatives thereof characterized by being water soluble, having a large interior void space and having a plurality of open exterior surface pores. These water soluble microparticles can be loaded with a chemical selected from the group consisting of pharmaceuticals, dyes, flavorings, agriculturals, solid catalysts and fragrances.

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: 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 tooth and gum paste in the form of a staple composition for controlling peridontal disease, reduction of plaque and oral oders in which one or more of the ingredients is microencapsulated within the composition.

Abstract: The size of microcapsules having cosmetic emollient oils is increased by the inclusion of viscosity increasing agents with the oils.

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: Microcapsules with controlled-release are prepared by subjecting microcapsules encasing an aqueous solution of a substance to be released from the microcapsules under control to a heat treatment in an aqueous solution containing the substance same with the substance to be released from the microcapsules, while selecting a heating temperature.

Abstract: The present invention provides for a composition of matter useful as an oral dosage form of insulin based upon a two phase liquid aqueous system in which insulin component or components are incorporated. The invention also provides for a method of preparing the oral dosage form of insulin, as well as a further process whereby sustained release dosage forms of oral insulin are produced. The oral form of insulin eliminates or reduces the need to use injection as a mode of administering insulin.

Abstract: A delivery system is disclosed for delivering a beneficial agent to an environment of use. The delivery system comprises a plurality of tiny dosage forms comprising a beneficial agent. The delivery system also comprises means for maintaining (a) the physical and chemical integrity of the dosage form and for (b) inhibiting delivery of the beneficial agent during non-performance of the delivery system.

Abstract: A process is disclosed for the microencapsulation of a substantially water-insoluble liquid material within a porous shell to effect a slow rate of release of said material through said shell which comprises (a) providing an organic solution comprising said material and an etherified urea-formaldehyde 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: Microcapsules are advantageously produced with high take-up of a water-soluble drug by preparing a W/O emulsion composed of a water-soluble drug-containing solution as the inner aqueous phase and a polymer-containing solution as the oil phase, dispersing said emulsion in an aqueous phase and subjecting the resulting W/O/W emulsion to an in-water drying, wherein the viscosity of the W/O emulsion used in preparing the W/O/W emulsion is adjusted to about 150 to about 10,000 centipoises.

Abstract: A membrane of defined pore structure and controlled pore diameter and a method of preparing the membrane which comprises dispersing in a water soluble polymer solution (A) an organic polymer solution (B), the water-soluble polymer solution (A) being a non-solvent for the polymer solution (B), to form micro-spherical droplets of the polymer solution (A) which are enveloped by a solid phase consisting of a coagulated or cross-linked polymer solution (B); evenly casting the dispersion on a flat surface; and evaporating the solvent for the polymer solution (B) to form a microporous membrane comprised of the polymer (B), the porosity, pore size, and void volume of the microporous membrane being a function of the polymer (A) concentration, the microsphere dimensions and the temperature and evaporation rate.

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: A chewable aspirin and buffering material tablet and method for producing same is disclosed herein. In a single dosage form the aspirin and buffering materials are integrally dispersed and bound in a fatty material of chocolate, synthetic chocolate or hydrogenated tallow. The tablet is for gastrointestinal applications and is especially adopted for use with animals, particularly dogs, and can be molded into a variety of shapes including that of a miniature dog bone.

Abstract: A controlled release system for delivery of a biologically-active substance. In one embodiment, there is a delayed release of a biologically-active substance. In a second embodiment, the delayed release is preceded by an initial release of biologically active substance. In other variations of the system, there are mulitple discrete releases over time or a continuous slow release combined with discrete releases. The delayed exposure is achieved through the design and construction of the system, specifically, formation of ionically-coated microcapsules around the biologically-active substance in conjunction with a microcapsule core-degrading enzyme. Release of active substance takes place in a burst at such a time as the core degrading enzyme has reduced the core to a molecular weight too low to support enough interaction with the cationic skin to maintain its integrity as a skin.

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: The invention relates to a completely novel type of micro-capsules, viz. such capsules where an encapsulated hydrophobic or lipophilic substance is surrounded by polar solid crystals of polar lipids which expose their hydrophilic face outwards and their hydrophobic face turned inwards towards the hydrophobic or lipophilic substance. These micro-capsules can be utilized to encapsulate for instance tacky substances or substances to be protected against oxidation or influence from light. Moreover, an especially interesting use according to the invention is the use of said micro-capsules in an ointment base, where the active ingredient is well protected within said capsules up to the use but which at the application on the skin directly comes into contact with the skin surface as a consequence of the crystalline structure of the shell.

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 method for sustained release of molecules from gels or microcapsules has been developed. The method is based on controlling the gel state using chelating agents or ion transfer. The method is particularly useful for controlling the rate of release of insolubilized proteins into physiological solutions.

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: 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: 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: In a first aspect of the invention there is provided a dosage form for delivery of a fixed amount of a drug to provide a sustained release of said drug to a patient which comprises:(a) a graduated container for accepting a liquid oral sustained release medicament, said graduated container being calibrated in units to permit an accurate total dosage of said drug; and(b) a liquid oral sustained release medicament capable of providing even blood levels of a drug in the bloodstream of a patient over a prolonged period of time, which comprises a suspension comprising microcapsules of said drug suspended in a saturated solution of said drug, the saturated level of said drug being maintained over a prolonged period of time for sustained release to the bloodstream and at a substantially constant level by means of the dissolution of the microcapsules into solution to replace the drug that leaves said solution, thereby maintaining the saturated level of drug in solution.

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. Release of the entrapped substance into the surrounding environment is governed by the permeability of both the liposome and microcapsule walls to the substance.

Abstract: A mixture of at least two aqueous dispersions of non-ionic lipid spherules encapsulating an aqueous phase containing an active substance. The active substance encapsulated in the spherules of one of the dispersions is different from the active substance encapsulated in the spherules of another of the dispersions.

Abstract: Microcapsules containing oil-based biologically active compounds which are stable over extended time periods for release of the encapsulated compound in the intestine. There are a number of biologically active compounds having an oil base which must be orally ingested in order to have a beneficial effect. An example of one such biologically active oil-based compound is a fish oil having a high content of polyunsaturated omega-3 fatty acids which has been demonstrated to reduce plasma levels of triglycerides, very low density lipoprotein, low density lipoproteins and cholesterol in normal and hyperlipidemic subjects. The disclosed microcapsules eliminate the unfortunate problems of the unpleasant taste and smell of the fish oil, as well as the aftertaste, particularly when ingested in large quantities, and provide a palatable and practical means of ingesting efficacious quantities of fish oil. In addition, the normal oxidation of polyunsaturated fatty acids is inhibited.

Abstract: A composition which comprises at least one solid or liquid particle comprising at least one active substance, the or a plurality of such particles being encapsulated by the in situ cationic (co)polymerization there on of at least on cationically polymerizable monomer or prepolymer.

Abstract: Microparticles, such as microspheres and microcapsules, comprising a solid organopolysiloxane are prepared by curing a dispersion of discrete entities by means of a Michael-type addition reaction. The discrete entities are dispersed in a fluid continuous phase and are sphere-like particles of a curable liquid organopolysiloxane composition, or such a liquid organopolysiloxane composition containing a material to be encapsulated. The microparticles may be elastomeric or resinous and are useful as filler particles and time-release capsules.

Abstract: The product consists of tablets which contain at least 600 mg of ibuprofen and a binder, or a mixture of binders, based on cellulose and cellulose derivatives in the form of microspheres which are coated with an acrylic resin of defined nature and are compressed together with a disintegrant; the tablets are preferably also coated with a lacquer layer. As a consequence of the high content of active compound and its delayed release in the body, the therapeutic treatment with ibuprofen can be reduced to a minimum number of intakes and dose units per day.

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: A single step method for preparation of multi-layer polymeric delivery systems. Any two or three different degradable or non-degradable polymers which are not soluble in each other at a particular concentration, as dictated by their phase diagram, can be used. The multi-layer microcapsules produced by the method are distinguished by extremely uniform dimensioned layers of polymer and actual incorporation of the substance to be delivered into the polymer layers.In the preferred embodiment of the method, two polymers are dissolved in a volatile organic solvent, the substance to be encapsulated is dispersed or dissolved in the polymer solution, the mixture is suspended in an aqueous solution and stirred, and the solvent is slowly evaporated, creating microspheres with an inner core formed by one polymer and an outer layer formed by the second polymer. In another embodiment one polymer may be formed within a layer of the other polymer by increasing the rate of evaporation of the volatile solvent.

Abstract: The invention is a method of stimulating cashmere growth on cashmere-producing goats. The method includes administering melatonin by a sustained release delivery system.

Abstract: A delivery system is disclosed for delivering a beneficial agent to an environment of use. The delivery system comprises a plurality of tiny dosage forms comprising a beneficial agent. The delivery system also comprises means for maintaining (a) the physical and chemical integrity of the dosage form and for (b) inhibiting delivery of the beneficial agent during non-performance of the delivery system.

Abstract: Preferred solid core liposomes were prepared through four major steps:(1) Preparation of prevesicles with encapsulated solid cores of agarose-gelatin by emulsification of agarose-gelatin sol in organic solvent containing emulsifiers followed by cooling;(2) Extraction of lipophilic components from prevesicles to obtain microspherules of agarose-gelatin;(3) In an optional step, colloidal gold particles were introduced into the microspherules, which were then coated with a protein or peptide molecule layer;(4) Encapsulation of the microspherules was conducted using a modified organic solvent spherule evaporation method for the formation of the liposomes.Electron micrographs indicate that if liposomes were prepared by using a lipid mixture containing dioleoyl phosphatidyl choline, cholesterol, dioleoylphosphatidylglycerol, and triolein (molar ratio 4.5:4.5:1:1), there was only a single continuous bilayer membrane for each solid core liposome.

Abstract: A diuretically active combination comprising furosemide and triamterene in a ratio of 1:1 to 1:2, in which furosemide is in the form of controlled release so as to facilitate solubilization of the furosemide in triamterene micelles to stabilize the combination as mixed micelles of low polydispersity yielding dissolution rates in in vitro tests of furosemide of not more than about 1.5% after about one hour at pH 1.5 to 3.5 and a slow release of not more than about 4.5% at pH 5.5 concurrent with a release of triamterene of about 60-70% and 80%, respectively, and with a release of not more than 85% furosemide after eight hours at pH 7.5 in salt solutions of adjusted pH.

Abstract: The permeability of the walls of chitosan alginate capsules is adjusted by substituting with esterified alginic acid a portion of the metal alginate normally used in the fabrication of such capsules.

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-making 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: Sustained-released delivery forms comprising the reaction product of a Lewis acid salt with a Lewis base salt at the phase interface of their respective aqueous and non-aqueous solution to form an anisotropic high molecular weight salt of the acid and base and a neutral salt of the inorganic cation and anion in what is termed a "double decomposition" or "salt exchange" reaction.

Abstract: A controlled release treatment composition and method of use are disclosed. The composition includes a bioadhesive and an effective amount of a treating agent. The bioadhesive is a water-swellable, but water-insoluble, fibrous, cross-linked carboxy-functional polymer containing (a) a plurality of repeating units of which at least about 80 percent contain at least one carboxyl functionality, and (b) about 0.05 to about 1.5 percent cross-linking agent substantially free from polyalkenyl polyether.

Abstract: A controlled-release pharmaceutical unit dosage form is provided comprising a gelatin capsule enclosing a solid matrix formed by the cation-assisted gellation of a liquid fill incorporating vegatable gum and a pharmaceutically-active compound, as well as methods for the preparation thereof.

Abstract: The present invention provides for an oral drug delivery system based on a two phase liquid coacervate system prepared from water and one or more surfactants selected from anionic, cationic, amphoteric, and non-toxic surfactants, polysaccharides, synthetic polymers and polysorbates and their derivatives, and in which a pharmaceutical component is incorporated. The delivery system may be prepared in the form of a microemulsion as well as other forms including encapuslated microparticles. The claimed oral composition is useful to delivery oral dosage forms of drugs, their salts and derivatives thereof; biologicals, enzymes, and other pharmocologically active compositions. A method to prepare the oral drug delivery system is also disclosed.

Abstract: Permeable capsules are loaded with a reservoir of the substance to be dispensed at a concentration sufficient to provide an osmotic pressure above threshold level, and the pore size of the capsule membrane is controlled so that the passage of the substance through the membrane becomes the rate-limiting factor in dispensing. Shape-retaining spheres are formed from a water-soluble polymer containing plural anionic or cationic groups and cross-linking surface layers of the spheres by contact with a polymer having plural groups of charge opposite that of the water-soluble polymer. After loading, the capsules are again treated with the same or a different cross-linking polymer to reduce the dimensions of the pores.

Abstract: A mixture of a cyclodextrin and an alkoxy silane compound, e.g., tetraethoxy silane, is admixed with water and an acidic or alkaline catalyst, e.g., acetic acid, to effect ligand exchange and hydrolysis of the alkoxy silane followed by gelation into a gelled mass which is dried and, preferably, leached with water to remove excess of the cyclodextrin. The thus obtained gelled material is a composite having a structure in which the cyclodextrin molecules are incorporated into the matrix of amorphous silica presumably by forming Si-O-C linkages. The composite has characteristics as a combination of the properties of both of the component materials and can expand the applicability of the materials, for example, as a carrier of catalysts and immobilized enzymes, absorbent and adsorbent and so on.

Abstract: The present invention relates to a process for the microencapsulation of a medicament by means of at least one coating agent, characterized in that is comprises the following steps:(a) Dissolution of the coating agent in water, by salification;(b) Dispersion of the particles of medicament to be microencapsulated, first in water, and then into the solution of the salified coating agent according to (a);(c) Addition to the so-obtained suspension of an acidifying substance, which causes the precipitation of the coating agent onto the particles of medicament while these are being kept in suspension by stirring, thus microcapsules being formed.(d) Recovery of microcapsules.

Abstract: It has been found that certain derivatives of poly(diallylmethylamine) are therapeutically effective serum cholesterol lowering agents.

Abstract: A wide range of materials may be encapsulated in a starch matrix by combining the material with a high temperature-stabilized pressurized dispersion of starch in the presence of salt. The temperature-stabilized starch dispersion acts as a protective colloid; upon subsequent rapid reduction of the pressure, the mixture cools and the starch polymer chains collapse upon themselves, encapsulating the core material in particulate form.