Abstract: A controlled release preparation for oral administration contains tramadol, or a pharmaceutically acceptable salt thereof, as active ingredient.

Abstract: A composition for inducing or potentiating an immune response, preferably a CTL, T helper cell, or neutralizing antibody response in a subject, comprising an antigen and/or a non-antigen bioactive agent capable of inducing or potentiating such an immune response encapsulated in a polymeric composition, wherein the polymeric composition comprises a blend of (a) a polymer present in an amount sufficient to provide structural integrity to the polymeric composition, and (b) a rapidly biodegradable component, a rapidly dissolving component, a rapidly swelling component, or a component that causes osmotic rupture of the encapsulated polymeric composition is disclosed. Single polymer compositions for achieving such an immune response are also disclosed. Methods for inducing or potentiating a CTL, T helper cell or neutralizing antibody response using the above-identified compositions are disclosed.

Abstract: A powdered, dispersible composition having stable dispersibility over time is provided. The composition exhibits a characteristic glass transition temperature (Tg) and a recommended storage temperature (Ts), wherein the difference between Tg and Ts is at least about 10° C. (i.e. Tg−Ts is greater than 10° C.). The composition comprises a mixture of a pharmaceutically-acceptable glassy matrix and at least one pharmacologically active material within the glassy matrix. It may be further mixed with a powdered, pharmaceutically-acceptable carrier. It is particularly valuable in unit dosage form having a moisture barrier, in combination with appropriate labelling instructions.

Abstract: The present invention relates to pharmaceutical compositions, pharmaceutical systems, and methods for enhanced absorption of hydrophilic therapeutic agents. Compositions and systems of the present invention include an absorption enhancing carrier, where the carrier is formed from a combination of at least two surfactants, at least one of which is hydrophilic. A hydrophilic therapeutic agent can be incorporated into the composition, or can be co-administered with the composition as part of a pharmaceutical system. The invention also provides methods of treatment with hydrophilic therapeutic agents using these compositions and systems.

Abstract: The invention is directed to an improved infant formula containing a lipid blend that softens the firmer stools associated with typical infant formula. A specific formula in accordance with the invention comprises carbohydrates, proteins, vitamins and minerals and a lipid mixture of high oleic safflower oil, soy oil and coconut oil at specific levels and ratios. The invention also discloses novel mixtures of fatty acids that provides infant stool patterns more closely resembling the breast-fed infant.

Abstract: This invention is directed to a multi-vitamin and mineral supplement tailored to men and post-menopausal women, pre-menopausal women, and athletes which supplies the right amount of the right micronutrients at the right time to assure adequate intake of micronutrients needed for disease prevention and protection against nutritional losses and deficiencies due to lifestyle factors and common inadequate dietary patterns. The multi-vitamin and mineral supplement is comprised of vitamin A, vitamin C, vitamin D, vitamin E, vitamin K, vitamin B1, vitamin B2, niacinamide, vitamin B6, vitamin B12, biotin, pantothenic acid, iron, iodine, magnesium, zinc, selenium, copper, chromium, potassium, choline, lycopene, and co-enzyme Q-10.

Abstract: A zero-order sustained-release delivery system for delivery of carbamazepine or a derivative thereof. A polymeric matrix formulation of carbamazepine comprises hydrophilic polymer or hydrophilic/hydropholic polymer mixture which permits carbamazepine or carbamezepine derivative to be released from the polymer matrix in zero-order release kinetics.

Abstract: The present invention encompasses a solid dose delivery vehicle for ballistic administration of a bioactive material to subcutaneous and intradermal tissue, the delivery vehicle being sized and shaped for penetrating the epidermis. The delivery vehicle further comprises a stabilizing polyol glass loaded with the bioactive material and capable of releasing the bioactive material in situ. The present invention further includes methods of making and using the solid dose delivery vehicle of the invention.

Abstract: An ibuprofen composition yielding an aqueous preparation having a pH of less than 7 on the addition of water to said composition which comprises one or more medicaments including an ibuprofen medicament which forms an ibuprofen active ingredient having a melting point less than 100° C., when combined with water to give an aqueous preparation having a pH of less than 7 and a phospholipid material intimately mixed with the ibuprofen medicament. The phospholipid material is capable of forming an aqueous preparation comprising an emulsion or dispersion comprising an aqueous phase substantially free of said ibuprofen active ingredient and a discrete phase consisting essentially of said phospholipid material and insoluble pharmacologically active ingredient including said ibuprofen active ingredient on the addition of water to said composition. The invention also provides aqueous drink preparations (especially heated emulsions) produced thereform and a process to prepare said aqueous drink preparations.

Abstract: Submicron particles of a biologically active agent are prepared by atomizing using multifluid atomization a dispersed system comprising at least one biologically active agent and at least one solvent to produce droplets, freezing the droplets to produce frozen droplets, lyophilizing the frozen droplets to obtain microstructures capable of being further fragmented into submicron particles by techniques such as probe sonication. The submicron particles can be incorporated into sustained release compositions having a reduced initial release of biologically active agent. The sustained release compositions can be administered to a human or animal.

Abstract: The present invention are dry-feel emollient compositions comprising jojoba oil based esters that have use in personal care, cosmetic, cosmaceutical and pharmaceutical products. These compositions are essentially solid at room temperature, can be provided in various shapes and sizes (especially as particulates such as spheres), and can be produced from combinations of fatty alcohols, isopropyl esters and wax esters obtained from the oil contained in the seed of the jojoba plant. These new compositions also increase the range of applications for cosmetic compositions through an emollient that is more polar and hydrophilic than is found in jojoba oils. The compositions of the present invention may be obtained by a novel process of a base catalyzed alcoholysis reaction between jojoba oil and an alcohol, such as isopropyl alcohol.

Abstract: Pharmaceutical compositions that enable the release of a physiologically active substance over a prolonged period of time following administration to a patient are described. The pharmaceutical compositions are provided by encapsulation of a physiologically active substance into a matrix comprising biodegradable polymers and lipids. The rate of release of the physiologically active substance from the pharmaceutical composition is controlled by varying the ratio of the polymer to the lipid. The compositions can be stored in an aqueous suspension or as a solid dosage form. The physiologically active substances include small molecules, peptides, proteins, nucleic acids and vaccines. The biodegradable polymers include homopolymers, or random or block copolymers. The lipids include phospholipids, cholesterol and glycerides.

Abstract: This invention relates to a composition and method for treating diseases and disorders of the prostate such as prostatitis, benign prostatic hypertrophy, and prostate carcinoma. The prostate is treated by intraprostatic injection of a biodegradable sustained release formulation. By injecting the treatment substance directly into the prostate, improved treatment results are obtained with a much lower treatment substance dosage. Additionally, by incorporating the treatment substance into a biodegradable sustained release formulation, the need for frequent repetition of injections is eliminated.

Abstract: The present inventors have made studies for the purpose of establishing a process for preparing controlled-release preparations which can rapidly release 99% or more of a slightly soluble medicament (which has by itself shows a slow dissolution rate) in the upper part of the small intestine. As a result, the inventors have succeeded in establishing a process comprising carrying a slightly soluble medicament which has a slow intestinal dissolution rate on aggregates of the spherical microparticles of a multivalent metal alginate, in which each of the secondary particles (i.e., the aggregates) has a specific surface area ranging from 1 to 280 m2/g. This success leads to the accomplishment of the present invention.

Abstract: Nanoparticulate compositions comprising an insoluble organic drug and at least one polyethylene glycol-derivatized lipid adsorbed on the surface of the drug are described. The polyethylene glycol-derivatized lipid can be a PEG-phospholipid, PEG-cholesterol, PEG-cholesterol derivative, PEG-vitamin A, PEG-vitamin E, or a mixture thereof The compositions have an effective average particle size of less than about 1 micron. The invention also describes methods of making and using such compositions.

Abstract: A method of treating or preventing an intracellular infection in an animal comprising administering a first effective amount of a suitable drug contained in first biocompatible microspheres that have a diameter of less than or equal to about 10 microns, wherein the first microspheres release the suitable drug upon administration at a first effective rate. A second set of microspheres greater than 10 microns in diameter may also be administered to provide continuing systemic release of the drug.

Abstract: A calcium-based ophthalmic composition for treating dry eye including a hydrophobic carrier, such as petrolatum, and a calcium salt. Also a method for treating dry eye comprising the step of administering the composition according to the present invention.

Abstract: A controlled release preparation for oral administration contains tramadol, or a pharmaceutically acceptable salt thereof, as active ingredient.

Abstract: Water-soluble folic acid compositions and pharmaceutical dosage forms comprising the compositions and methods for making the same are disclosed.

Abstract: A controlled release formulation of an acetonitrile compound and its use in the treatment and/or prophylaxis of certain disorders.

Abstract: The present invention provides improved confectionery compositions which have a substantial reduction in the unpleasant organoleptic sensations associated with the release of functional ingredients from the confection in the oral cavity. The confectionery composition comprises a confectionery base, a functional ingredient which is a botanical or a mineral or a mineral salt having an unpleasant mouthfeel, and from about 0.5% to about 5.0% by weight of the composition of one or more fats, said amount being effective to suppress the unpleasant mouthfeel of the functional ingredient. For botanicals the confectionery composition is a hard boiled candy composition or a hard gum composition and the fat is one or more partially hydrogenated vegetable oils or saturated fats. For minerals or their salts the confection is a hard boiled candy composition and the fat is one or more partially hydrogenated vegetable oils.

Abstract: A composition for the sequestration and sustained delivery of an active ingredient in the form of porous particles, the composition comprising the product of the controlled dehydration of particles formed by the reaction of a polymeric anionic material with a polyvalent cation. The composition may be loaded with an active ingredient by soaking the particles in a solution of the active ingredient; and may then be dehydrated. They may then be soaked in a solution of a polymeric cationic material, to form particles providing the controlled release of the active ingredient.

Abstract: The invention relates to compositions in the form of microcapsules or implants comprising a biodegradable polymeric or copolymeric excipient or a mixture of such excipients with an inherent viscosity of between 0.5 dl/g and 1.6 dl/g in CHCl3, and one active substance or a mixture of active substances, it being possible for said microcapsules or implants to release the active substance or mixture of active substances over a prolonged period of up to three months or more. These compositions may also comprise an active principle having a high specific surface area.

Abstract: A biodegradable, mixed polymeric micelle used to deliver a selected nucleic acid into a targeted host cell contains an amphiphilic polyester-polycation copolymer and an amphiphilic polyester-sugar copolymer. The polyester-polycation copolymer forms an electrostatic interaction with polyanionic nucleic acids, and the polyester-sugar copolymer directs the micelle-nucleic acid complex to cells in vivo. Additional copolymers with similar properties may also be included. The composition improves delivery efficiency by providing a particulate gene carrier for which particle size and charge density are easily controlled by multivariate means. Various kinds of ligands and other functional compounds may be also be introduced using the composition. The composition may be used in a method for transforming a targeted host cell with a selected nucleic acid.

Abstract: A method of producing sustained-release microcapsules which comprises dispersing a physiologically active polypeptide into a solution of a biodegradable polymer and zinc oxide in an organic solvent, followed by removing the organic solvent; which provides a sustained-release preparation showing a high entrapment ratio of the physiologically active polypeptide and its constant high blood concentration levels over a long period of time.

Abstract: Particles comprising (a) a supercooled melt of a poorly water-soluble substance and (b) a stabilizing agent, which have a mean particle size of between 30 and 500 nm, and disperse compositions containing them, as administration forms and delivery systems for drugs, vaccines and other biologically active agents such as herbicides, pesticides, insecticides, fungicides, fertilizers, vitamins, nutrition additives and cosmetics.

Abstract: The present invention provides a complex of human growth hormone and zinc containing human growth hormone and zinc at a molar ratio of about 1:1.6 to about 1:2.4, and a sustained-release preparation which comprises the complex of human growth hormone and zinc and a biodegradable polymer and which has a high entrapment ratio of human growth hormone and exhibits a stable sustained-release suppressing the initial burst.

Abstract: A composition for delivering a stable, bioactive compound to a subject comprising a first component and a second component, the first component comprises microparticles of sugar glass or a phosphate glass containing the bioactive agent. The sugar glass or phosphate glass optionally includes a glass formation facilitator compound, and the second component comprises at least one biocompatible liquid perfluorocarbon in which the first component is insoluble and dispersed. The liquid perfluorocarbon optionally includes a surfactant.

Abstract: The invention relates to a cosmetic composition comprising (A) a polyhydric alcohol and (B) a finely particulate metal oxide, wherein water is substantially not contained. The cosmetic composition has an optimum viscosity, undergoes no precipitation of particles, spreads well upon use and has good easiness of washing off and is hence particularly useful as a massaging cosmetic.

Abstract: The invention relates to compositions useful for making taste-masked oral dosage forms which can be easily processed and which disintegrate rapidly when placed in the mouth. The compositions include coated liquiflash particles and shearform floss particles. Tablets are preferred dosage forms.

Abstract: A pharmaceutical implant for the delivery of an effective amount of a bioactive peptide or peptide analog over a period of 1 to 12 months. This implant has a diameter of about 1 to 2 mm, a length of between about 10 and 25 mm and is obtainable from a process which includes the steps of grinding a copolymer of lactic acid and glycolic acid having a ratio of glycolide to lactide units of from about 0 to 5:1 to a particle size of between about 50 and 150 .mu.m; sterilizing the ground copolymer with a dose of between about 1 and 2.5 Mrads of ionizing .gamma.-radiation; wetting the ground and sterilized copolymer with a sterile aqueous slurry of a bioactive peptide or peptide analog; aseptically blending the copolymer and the slurry to obtain a homogeneous mixture of the copolymer and between about 10 and 50% of the bioactive peptide or peptide analog; drying the mixture at reduced pressure and at temperature not exceeding 25.degree. C.

Abstract: This invention relates to a process for the preparation of an oral solid rapidly disintegrating dosage form of a pharmaceutically active substance which has an unacceptable taste which process comprises: (i) forming a solution or a suspension in a solvent of a water soluble or water dispersible carrier, a filler and the pharmaceutically active substance with the unacceptable taste in association with a lipid, the weight ratio of the pharmaceutically active substance to the lipid being in the range of from 1:1 to 1:10 and the weight ratio of the carrier to the lipid being in the range of from 5:1 to 1:15; (ii) forming discrete units of the suspension or solution; and (iii) removing the solvent from the discrete units under conditions whereby unit dosages are formed comprising a network of carrier/filler carrying a dosage of the pharmaceutically active substance in association with the lipid; oral solid rapidly disintegrating dosage forms prepared by such a process are also provided.

Abstract: Disclosed is a substantially water-free insecticidal granular bait suitable for controlling crawling insects such as cockroaches and ants. The bait includes an insecticide, several feeding stimulants which are typically carbohydrates and proteins, and a lipid. These bait compositions are in granular form, which are useful for application in hard-to-reach areas and are particularly useful in wet conditions, as well as hot, dry areas.

Abstract: A method and apparatus for coating a fiber used in oral hygiene. The method comprises aerosolizing a coating and projecting the aerosolized coating particles onto a target area of the fiber. The method also comprises recycling recaptured coating particles for reuse in fiber coating. An apparatus for coating oral hygiene fibers is also described.

Abstract: A container comprising an aqueous lipid suspension and a gaseous phase substantially separate from the aqueous stabilizing phase, useful in diagnostic imaging such as ultrasound and magnetic resonance imaging and in therapeutic applications, is disclosed.

Abstract: This invention relates to stabilized nanoparticles which may be filtered under sterile conditions, comprising at least one hydrophobic, water-insoluble and non-water-dispersible polymer or copolymer (and optionally an active principle) which is emulsified in an aqueous solution or suspension comprising a phospholipid and a bile salt.

Abstract: Novel methods for delivering bioactive agents to particular regions or tissues of the body of a patient are provided.

Abstract: A solid hair colorant composition in powder or granular form containing from 1 to 10% by weight of at least one oxidation dye precursor, from 10 to 35% by weight of an oxidizing agent, from 3 to 25% by weight of a substantive plant dye or 25 to 70% by weight of henna neutral, and optionally conventional cosmetic additives.

Abstract: A method for universally distributing a therapeutic agent, in an encapsulated form, to the brain of a subject using intrathecal administration, excluding the lumbar region, is described. Methods for treating stroke and/or Traumatic Brain Injury (TBI) are also described. The methods involve intrathecal administration into the cerebrospinal fluid of a subject, of a therapeutic agent in an encapsulated form. Pharmaceutical compositions intended for the amelioration of stroke and/or Traumatic Brain Injury (TBI) are also described. The pharmaceutical compositions comprise a therapeutic agent encapsulated in a pharmaceutically acceptable polymer, suitable for injection into the cerebrospinal fluid of a subject suffering from stroke and/or Traumatic Brain Injury (TBI).

Abstract: An arrangement for the investigation of hydrophilic macromolecules (1) in an aqueous solution having a solid carrier surface (5) onto which a lipid film (24) is disposed, wherein the molecules (1) to be investigated are bound, by means of a molecular coupling system (20), to the lipid film (24) and thus are immobilized, is characterized in that the molecular coupling system (20) comprises at least two, preferably three molecular or nuclear components (21, 22, 23), which can be coupled to each other, of which a first component (21) is bound to the lipid film (24) and a second component (22) is bound to a hydrophilic macromolecule (1) to be investigated. In this way, it is rendered possible to immobilize and investigate any hydrophilic macromolecules, wherein the coating of the solid carrier surface should be able to be carried out in an as easy as possible and reversible manner.

Abstract: Biocompatible microspheres containing one or more active principals, a biodegradable and biocompatible polymer and a surface-active agent which is also biodegradable and biocompatible, contain less than 10 ppm of heavy metals. These microspheres are prepared by providing a solution of the polymer and of the active principal in a water-immiscible solvent which is more volatile than water and mixing with an aqueous solution of the surface-active agent, followed by evaporation of the solvent.

Abstract: The present invention is directed to charged lipids, compositions comprising charged lipids, and the use of these compositions in drug delivery, targeted drug delivery, therapeutic imaging and diagnostic imaging, as well as their use as contrast agents.

Abstract: Formulations for controlled, prolonged release of GM-CSF have been developed. These are based on solid microparticles formed of the combination of biodegradable, synthetic polymers such as poly(lactic acid) (PLA), poly(glycolic acid) (PGA), and copolymers thereof with excipients and drug loadings that yield zero order or first order release, or multiphasic release over a period of approximately three to twenty one days, preferably one week, when administered by injection. In the preferred embodiment, the microparticles are microspheres having diameters in the range of 10 to 60 microns, formed of a blend of PLGA having different molecular weights, most preferably 6,000, 30,000 and 41,000. Other embodiments hare been developed to alter the release kinetics or the manner in which the drug is distributed in vivo.

Abstract: The thermoforming of compositions containing active agents is carried out by processing compositions containing certain fatty esters in combination.

Abstract: A method for preparing biodegradable, biocompatible microparticles. A first phase is prepared that includes a biodegradable, biocompatible polymer, an active agent, and a solvent. An immiscible second phase is prepared. The first and second phases are combined to form an emulsion in which the first phase is discontinuous and the second phase is continuous. The two phases are immersed in a quench liquid that includes a quench medium and a quantity of the solvent. The quantity of the solvent is selected to control a rate of extraction of the solvent from the first phase. The first phase is isolated in the form of microparticles. Also disclosed is a microencapsulated active agent prepared by the method for preparing biodegradable, biocompatible microparticles.

Abstract: A process for the administration of a flowable solid, semisolid, or liquid medium exhibiting a controlled release of at least one active substance to plants by means of injection using needle-free, pressure-actuated devices is characterized in that the medium comprises active substance-containing microparticles of a maximum size of 100 .mu.m including the following components:a) 0.5-70%-wt. of at least one active substance,b) 10-70%-wt. of at least one biodegradable polymer,c) up to 20%-wt. of formulation adjuvants.

Abstract: A pharmaceutical implant for the delivery of an effective amount of a bioactive peptide or peptide analog over a period of 1 to 12 months. This implant has a diameter of about 1 to 2 mm, a length of between about 10 and 25 mm and is obtainable from a process which includes the steps of grinding a copolymer of lactic acid and glycolic acid having a ratio of glycolide to lactide units of from about 0 to 5:1 to a particle size of between about 50 and 150 .mu.m; sterilizing the ground copolymer with a dose of between about 1 and 2.5 Mrads of ionizing .gamma.-radiation; wetting the ground and sterilized copolymer with a sterile aqueous slurry of a bioactive peptide or peptide analog; aseptically blending the copolymer and the slurry to obtain a homogeneous mixture of the copolymer and between about 10 and 50% of the bioactive peptide or peptide analog; drying the mixture at reduced pressure and at temperature not exceeding 25.degree. C.

Abstract: Methods for preparing dry powders having hydrophobic and hydrophilic components comprise combining solutions of the components and spray drying them simultaneously in a spray dryer. The hydrophilic and hydrophobic component are separately dissolved in separate solvents and directed simultaneously through a nozzle, usually a coaxial nozzle, into the spray dryer. The method provides dry powders having relatively uniform characteristics.

Abstract: The present invention is directed to an implantable, slow-release, self-absorbing, biologically compatible drug delivery system such as slow-release pharmaceutical compositions, including for example, slow-release, allergy desensitization compositions containing one or more allergens in combination with a biologically-compatible, self-absorbing matrix. The present system is useful for treating disorders including, for example, infections, deficiencies or allergies. The present invention is also directed to methods of treating a patient suffering from a disorder, as well as methods for desensitizing a patient to one or more allergens. The present invention also relates to a device for implanting the present composition in a patient.

Abstract: The present invention provides, inter alia, formulations useful to ameliorate symptoms associated with mucosal abrasions, specifically those due to dental orthodontic brackets; oral surgery; periodontal surgery or other procedures. For instance, there is a formulation comprising: 65 to 75% microcrystalline wax; 5 to 15% non-ionic polymer; 15 to 25% topical anesthetic; and 1 to 5% surfactant, wherein the ratio of non-ionic polymer to microcrystalline wax is no greater than 0.2. Preferably, for solid topical anesthetics, the particle size is less than the apertures of a 100-mesh screen. However, the topical anesthetic may also be a liquid. Formulations wherein the mixture is a homogeneous matrix is preferred.