Abstract: A pharmaceutical composition for peroral treatment of rheumatoid arthritis and a treatment method therefor are described, wherein said composition comprises 2.5-7 mg of a glucocorticoid as active substance with a regulated sustained release such that at least 90% by weight of the glucocorticoid is released during a period of about 40-80 min, starting about 1-3 h after the entry of said glucocorticoid into the small intestine of a mammal.
Abstract: According to the present invention, there is provided a continuous method for the production of retarded pharmaceutical compositions by an extrusion process. A mixture of an active material, a low and high melting lipid or lipoid components is introduced by means of an extruder screw conveyor into a preheated extruder and brought to a temperature which is at most about 4.degree. C. above the melting temperature of the low melting component at a pressure of about 200 to about 600 kPa(N/m.sup.2). The mass is extruded through a nozzle plate with a nozzle diameter of about 1.2 to about 4 mm and subsequently cooled, and if desired, granulated.
Abstract: One object of the invention, therefore, is to provide encapsulated biologically active solid microparticle agglomerates, each agglomerate comprising eitherIi) at least two closely associated microparticles, each microparticle being coated partially or completely by at least one discrete layer of a polymer, andii) at least one outer discrete coating layer of the same polymer which envelops the coated microparticles to form an agglomerate of closely associated microparticles, orIIi) a cluster of at least two closely associated microparticles, each microparticle being coated partially or completely by at least one layer of a polymer, the microparticles adhering together through the polymer to form said cluster, andii) at least one outer discrete coating layer of the same polymer which envelops said cluster to form a discrete agglomerate, wherein in types I and II an inter-phase boundary is formed between each particle and the first coating layer, between individual coating layers and between the outer agglomerat
Type:
Grant
Filed:
September 29, 1995
Date of Patent:
August 4, 1998
Assignee:
Novartis Corporation
Inventors:
Rudolf Nastke, Ernst Neuenschwander, Andreas Leonhardt
Abstract: In a microcapsule of the multi-core structure comprising a plurality of particles which are made of a core material comprising natural carotenoid and an edible oil, and a wall which is made of a coating material based on gelatin, the particles have a mean particle size of 0.01-5 .mu.m, the gelatin has a jelly strength of at least 100 blooms, and the microcapsule has a water content of up to 10% by weight. The microcapsule has a strength enough to protect natural carotenoid from oxidation and deterioration for a long time and to withstand tableting pressure.
Abstract: Cushioning beads comprising microcrystalline cellulose and a disintegrant (preferably croscarmellose sodium) are disclosed. The cushioning beads are prepared by extrusion-spheronization, followed by freeze-drying. Also disclosed, are water-dispersible tablets having high tensile strength, comprising the cushioning beads and biologically active ingredient-loaded beads, wherein optionally, the tablets can contain a viscosity enhancer in the form of separate beads, or as a component of the biologically active ingredient-loaded beads such that viscosity is rapidly generated when the tablets come in contact with water, and a homogenous suspension is formed, which can be easily swallowed by children and the elderly, with minimal effect of the biologically active ingredient release properties. The tablets are useful for sustained delivery of large doses of biologically active ingredients where swallowing of a large tablet or capsule poses a problem.
Type:
Grant
Filed:
September 6, 1996
Date of Patent:
July 14, 1998
Assignee:
University of Maryland, Baltimore
Inventors:
Yacoub S. Habib, Ralph Shangraw, Larry L. Augsburger
Abstract: A self-propelling aerosol formulation which may be free from CFC's which comprises a medicament, 1,1,1,2-tetrafluoroethane, a surface active agent and at least one compound having a higher polarity than 1,1,1,2-tetrafluoroethane.
Type:
Grant
Filed:
January 16, 1997
Date of Patent:
July 7, 1998
Assignee:
Riker Laboratories, Inc.
Inventors:
Tarlochan S. Purewal, David J. Greenleaf
Abstract: Internally cross-linked albumin microspheres their surface being modified by attachment of polyoxy(C.sub.-)alkylene chains having a terminal ether group, especially such containing pharmacologically active agents, usable for pharmaceutical compositions.
Type:
Grant
Filed:
September 29, 1995
Date of Patent:
June 30, 1998
Assignee:
Novartis Corporation
Inventors:
Rudolf Nastke, Ernst Neuenschwander, Andreas Leonhardt
Abstract: The present invention relates to an oral drug delivery system, and in particular to modified amino acids and modified amino acid derivatives for use as a delivery system of sensitive agents such as bioactive peptides. The modified amino acids and derivatives can form non-covalent mixtures with active biological agents and in an alternate embodiment can releasably carry active agents. Modified amino acids can also form drug containing microspheres. These mixtures are suitable for oral administration of biologically active agents to animals. Methods for the preparation of such amino acids are also disclosed.
Type:
Grant
Filed:
October 23, 1995
Date of Patent:
June 16, 1998
Assignee:
Emisphere Technologies, Inc.
Inventors:
Sam J. Milstein, Evgueni N. Barantsevitch, Donald J. Sarubbi, Andrea Leone-Bay, Duncan R. Paton
Abstract: A self-propelling aerosol formulation which may be free from CFC's which comprises a medicament, 1,1,1,2-tetrafluoroethane, a surface active agent and at least one compound having a higher polarity than 1,1,1,2-tetrafluoroethane.
Type:
Grant
Filed:
January 16, 1997
Date of Patent:
June 16, 1998
Assignee:
Riker Laboratories, Inc.
Inventors:
Tarlochan S. Purewal, David J. Greenleaf
Abstract: The present invention relates to pharmaceutical compositions containing as active ingredient micronized nebivolol of formula (I) and ways of preparing said compositions.
Type:
Grant
Filed:
July 9, 1996
Date of Patent:
June 2, 1998
Assignee:
Janssen Pharmaceutica, N.V.
Inventors:
Eugeen Marie Jozef Jans, Guido Franciscus Smans, Paul Marie Victor Gilis
Abstract: The present invention relates to controlled release dosage forms composed of a naproxen layer which contains a delayed release granulate of naproxen compressed with an immediate release granulate of naproxen and an immediate release naproxen sodium layer compressed with the naproxen layer, designed to promptly exert a therapeutic effect while also maintaining the therapeutic blood concentration for a prolonged duration of 24 hours.
Abstract: The present invention relates to a sustained-release formulation of an animal growth hormone and a process for preparation thereof, comprising a step to produce solid pellets by mixing an animal growth hormone and an excipient in accordance with a direct tabletting method and a step to coat the pellets with a film comprising a biodegradable polymer and a poloxamer. The thus obtained formulation has small initial drug release, and shows a continuous and uniform effect when administered. Further, the formulation of the present invention may be produced economically in a large scale.
Abstract: Sustained release formulations include an augmented microcrystalline cellulose, an active agent, and a sustained release carrier and methods for making same are disclosed.
Type:
Grant
Filed:
July 8, 1996
Date of Patent:
April 21, 1998
Assignee:
Edward Mendell Co., Inc.
Inventors:
John N. Staniforth, Bob E. Sherwood, Edward A. Hunter
Abstract: The present invention generally relates to novel overcoating/encapsulation processes which are carried out in solution without the use of droplet generation devices. The processes may be used in the overcoating or encapsulation of a variety of materials, such as biological material, e.g., cells, proteins, etc., as well as pharmaceuticals. Compositions prepared using the methods of the present invention may find use in pharmaceutical formulation as well as coating biological material for a number of applications, including cell culturing and transplant therapy.
Abstract: Formulations are provided for the treatment of patients suffering from disorders that have in common the appearance of muscular hypotonia as a symptom. These disorders include Alzheimer's type diseases, atrophy of the brain, atrophy of the cerebellum, Fragile X syndrome, mental retardation of unknown causes, multiple anomalies in the chromosomes, deletions in one or more chromosome, and fragility in a chromosome other than the X chromosome. The formulations of the invention contain therapeutically effective amounts of gamma amino butyric acid (GABA), an anti-oxidant (such as ascorbic acid and/or vitamin E), folic acid, nicotinamide, and a lithium salt, all in a pharmaceutically acceptable excipient. Methods for the treatment of these disorders by the administration of such formulations are also provided.
Type:
Grant
Filed:
September 27, 1996
Date of Patent:
April 14, 1998
Assignees:
Herman Bleiweiss, Eduardo Samuel Bleiweiss, Daniel Gustavo Bleiweiss
Inventors:
Herman Bleiweiss, Eduardo Samuel Bleiweiss, Daniel Gustavo Bleiweiss
Abstract: Hard gelatin capsules contain: (a) a fat-soluble nutrient, such as a fat-soluble vitamin (A, D, E or K) or an unsaturated fatty acid glyceride; (b) a nonionic surfactant, such as a polyoxyethylated (optionally hydrogenated) castor oil, and/or a polyethylene glycol; (c) a gelatin softening agent such as glycerol, propylene glycol or, preferably, glyceryl mono-oleate; and optionally (d) water. The problems of embrittlement conventionally encountered with hard gelatin capsules containing fat-soluble nutrients are reduced or avoided.
Abstract: Method for the preparation of a pharmaceutical composition in the form of microspheres controllably releasing at least one water-soluble active ingredient. The method comprises the steps of dissolving the active ingredient in a suitable quantity of water, emulsifying the aqueous solution containing the active ingredient with a solution of at least a dl-lactide-co-glycolide-type matrix copolymer in chlorinated hydrocarbon also containing a low molecular weight polyactide release-modulating agent, which results in a first microfine and homogeneous emulsion; emulsifying the first emulsion thus obtained in an external aqueous phase containing a surface active agent; and removing and evaporating the solvent to produce microspheres which are recovered after filtering, washing, and drying. The microspheres themselves.
Type:
Grant
Filed:
October 11, 1996
Date of Patent:
March 31, 1998
Assignee:
Pierre Fabre Medicament
Inventors:
Rosa Arola, Miguel Angel Asin, Eulalia Ferret, Eric Goutay, Amadeo Perez, Pere Tarin
Abstract: A non-toxic edible enteric film coating dry powder composition for use in making an aqueous enteric coating suspension which may be used in coating pharmaceutical tablets and the like comprises an enteric film forming polymer, a detackifier, a viscosity modifier, and an alkalizing/anti-coagulating agent. Advantageously, the inventive dry powder compositions may include a solid plasticizer, a lubricant, an anti-caking agent, a liquid plasticizer, and a pigment.
Type:
Grant
Filed:
October 7, 1994
Date of Patent:
March 31, 1998
Assignee:
BPSI Holdings, Inc.
Inventors:
Dev K. Mehra, Chittamuru Ramireddy, Li-Juan Tang, Stuart C. Porter
Abstract: Direct compressed solid pharmaceutical dosage forms containing:a) from about 40 to about 95% by weight acetaminophen;b) from about 1 to about 60% by weight of a direct compression vehicle comprising microcrystalline cellulose; andc) from about 0.01 to about 4.0% by weight of a pharmaceutically-acceptable lubricant are disclosed. The acetaminophen and direct compression vehicle are combined under high shear conditions which are sufficient to transform acetaminophen and direct compression vehicle into a homogenous granulate without degradation. In preferred aspects of the invention, the lubricant is also combined with the acetaminophen and direct compression vehicle under high shear conditions. Methods of preparing the directly compressed solid pharmaceutical dosage forms and methods of treatment with the dosage forms are also disclosed. The methods are particularly well suited for preparing directly compressed dosage forms containing high load (i.e.
Type:
Grant
Filed:
November 15, 1995
Date of Patent:
March 31, 1998
Assignee:
Edward Mendell Co., Inc.
Inventors:
Edward A. Hunter, Bob E. Sherwood, Joseph A. Zeleznik
Abstract: A composition, a method, and a kit are provided for at-home chemical skin peeling, which is gentle in that the concentrations of the active skin peeling ingredients is far lower than that used in dermatologists' or aestheticians' offices. The composition of the present invention is designed to be used daily over a period of weeks to produce the same or a superior result compared to superficial or light chemical peels available in a professional setting alone and superior to any product, method, kit or composition for home use in skin peeling.