Abstract: A controlled release potassium chloride tablet is disclosed which is comprised of potassium chloride crystals having a mesh size of about 30 to about 50 mesh which are coated with a coating material comprised of ethylcellulose and hydroxypropylcellulose. The coated crystals form micro pellets which then can be compressed into tablets. The tablets disintegrate rapidly in an aqueous environment thus assuring a more uniform dissolution of the active component as compared with other types of controlled release potassium chloride dosage formulations. The distribution of the potassium chloride micro pellets over a wide surface area in the gastrointestinal mucosa aids in reducing the risk of gastrointestinal lesions. The formation of the coated micro pellets which disperse quickly upon contact with aqueous environment allow for the repeated chronic oral administration of a relatively large dose of potassium chloride (20 mEq).
Abstract: A high yielding process for converting 3,2',6'-tri-N-acetyl sisomicin to netilmicin comprising the step of silylating the starting material at the 5,2' positions, and optionally at the 4' position, converting the 1-amino substituent to a 1-N-imino substituent, converting the imino to an ethylamino, deprotecting the compound and recovering netilmicin. Also disclosed are novel intermediate compounds.
Type:
Grant
Filed:
November 6, 1986
Date of Patent:
May 16, 1989
Assignee:
Schering Corporation
Inventors:
Chou-Hong Tann, Tiruvettipuram K. Thiruvengadam, John S. Chiu, Cesar Colon
Abstract: This invention relates to a novel process for preparing 3-amino-2-methylbenzotrifluoride from benzotrifluoride. The process comprises nitrating benzotrifluoride to form 3-nitrobenzotrifluoride, reacting this compound with trimethyl sulphoxonium halide to form 3-nitro-2-methylbenzotrifluoride and reducing the nitro group to an amino group.
Type:
Grant
Filed:
June 19, 1987
Date of Patent:
May 16, 1989
Assignee:
Schering Corporation
Inventors:
Joseph F. Lamendola, Dhiru Vashi, Robert G. Tyson
Abstract: An antifungal vaginal suppository is disclosed comprising cis-2-(1H-imidazolylmethyl)-3-(2',6'-difluorobenzyloxy)-2,3-dihydro-5-fluo robenzo[b]thiophene in a suppository base containing biocompatible polymers, a surfactant and an absorbent in a vegetable oil phase.
Abstract: Pharmaceutical preparations comprised of a pharmaceutically active ingredient and a carrier which comprises a percutaneous penetration enhancer comprised of 2-ethyl-1, 3-hexanediol alone or in combination with oleic acid is disclosed. The 2-ethyl-1, 3-hexanediol may be present in an amount in the range of about 50% to 100% based on the weight of the carrier. The oleic acid may be used in combination with 2-ethyl-1, 3-hexanediol in an amount of about 1 to 40% based on the weight of the carrier to provide a synergistic effect with respect to percutaneous penetration enhancement. The compound 2-ethyl-1, 3-hexanediol as used alone and/or in combination with the oleic acid has been found to significantly enhance the delivery of a drug, to a patient, from a transdermal delivery system.
Abstract: A process is disclosed for purifying gamma interferon from various contaminants resulting from disruption of the cell in which the interferon was produced. The process provides for sequential removal of (a) nucleic acids, (b) negatively charged contaminating proteins, (c) positively charged contaminating proteins and (d) low and high molecular weight impurities.
Type:
Grant
Filed:
July 3, 1985
Date of Patent:
June 14, 1988
Inventors:
Tattanahalli L. Nagabhushan, Paul P. Trotta, Hung V. Le, Gail F. Seelig, Robert A. Kosecki
Abstract: This invention relates to organic acid-substituted guanidine compounds. Also disclosed are methods for preparing the compounds, compositions containing them, and methods for their use as anthelmintics.
Type:
Grant
Filed:
September 23, 1983
Date of Patent:
February 2, 1988
Assignee:
Schering Corporation
Inventors:
Dhiru B. Vashi, Jeffrey N. Clark, Neil A. Lindo
Abstract: This invention relates to organic acid-substituted guanidine compounds. Also disclosed are methods for preparing the compounds, compositions containing them, and methods for their use as anthelmintics.
Type:
Grant
Filed:
September 23, 1983
Date of Patent:
October 20, 1987
Assignee:
Schering Corporation
Inventors:
Dhiru B. Vashi, Jeffrey N. Clark, Neil A. Lindo
Abstract: Bronchospastic diseases characterized by airway hyperreactivity are treated by administration of the calcium channel blocker gallopamil. Unlike other calcium channel blockers, the effective dose of gallopamil is small enough that undesirable side effects are not present.
Abstract: A method and apparatus for lighting a container which is to be inspected for particulate contamination comprising a first lighting means consisting of two angularly displaced light beams which create an angular shadow zone, a second lighting means of significantly lower intensity than said first lighting means and positioned intermediate the two light beams and a viewing means positioned in the shadow zone.
Type:
Grant
Filed:
November 18, 1983
Date of Patent:
June 30, 1987
Assignee:
Schering-Plough Corporation
Inventors:
Paul M. Bjorndal, Julius Z. Knapp, John C. Zeiss
Abstract: A pharmaceutical preparation containing 1 to 50% urea and 0.05 to 30% of a lactone is disclosed. A preferred lactone is gamma-butyrolactone which is preferably present in an amount of about 0.05 to 0.1 part by weight per 1 part by weight of urea. The lactone stabilizes the urea with respect to various parameters including changes in pH. The pharmaceutical preparation may be any preparation with stabilized urea such as a skin lotion or cream used to moisturize skin, or a post surgical preparation because urea aids in debridement, dissolves coagulum and promotes epithelialization. Alternatively the preparation may be an injectable solution used in the treatment for mobilization of edema fluid, as urea is used for an osmotic diuretic.
Abstract: A stopper for holding fluid in a container comprising a body of vulcanized elastomer having a convex surface, and, laminated to the convex surface without adhesive, a thin layer of thermoplastic, which forms a surface intended to contact the fluid and a side of an opening in the container.
Abstract: Biotin esters, namely biotin C.sub.2-4 -alkyl esters, are prepared by esterifying biotin with a C.sub.2-4 -alkanol. These esters have the capability of being absorbed by the human skin better than biotin and are converted into biotin during or after absorption. Since biotin itself promotes the fat and cholesterol synthesis of the skin, the novel biotin esters of this invention are useful as active ingredients for cosmetic hair-care and skin-care compositions.
Abstract: Heterocyclic compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and X are as defined hereinafter, process for their preparation, as well as pesticidal compositions containing these compounds as the active ingredient and methods for using the pesticidal compositions for the control of pests are described.
Abstract: Carbamic acid ester compounds of the formula ##STR1## wherein A represents the group (a) or (b) ##STR2## wherein R.sup.1 -R.sup.8, X and Y are as defined hereinafter, processes for their preparation, herbicidal compositions containing these compounds and methods for the use of the compounds and the herbicidal compositions are disclosed.
Abstract: There is described a novel process for producing hydroquinone derivatives of the formula ##STR1## wherein R is an ether protecting group, and their conversion into d-.alpha.-tocopherol, starting from compounds of the formula ##STR2## wherein R is an ether protecting group and R.sup.1 is hydrogen or an ether protecting group.
Abstract: A method for the determination of antigens or antibodies in a fluid by incubation of particles, which have antigens on the surface, and antibodies, whereby either the antigens or the antibodies are of known specificity is described. This method comprises introducing the antigen/antibody complex into a container having a conical-shaped or keel-shaped bottom recess, whereby at least the recess of the container is coated with an immunoglobulin-building component which is directed against the antibodies. After centrifugation the amount of the sediment is determined, which indicates whether the antigen or antibody to be determined is present or not.
Abstract: Novel pyridine and pyrazine derivatives of the formula ##STR1## wherein R.sup.4 is 3-pyridyl, 3-pyridyl-1-oxide, 2-pyrazinyl, 2-pyrazinyl-1-oxide, 2-pyrazinyl-4-oxide or 2-pyrazinyl-1,4-dioxide, and R, R.sup.1, R.sup.2 and R.sup.3 are as hereinafter set forth, processes for their preparation, fungicidal compositions containing said compounds, and methods for the use of such compounds or compositions for combatting fungi in agriculture and in horticulture are disclosed. Novel starting materials and fungicidal active substances of the formula ##STR2## wherein R.sup.4' is 3-pyridyl or 2-pyrazinyl, and R and R.sup.1" as hereinafter set forth, which are used for the preparation of the compounds of formula I, and their N-oxides, as well as fungicidal compositions containing these compounds as the active substance, are also described.
Type:
Grant
Filed:
August 27, 1982
Date of Patent:
December 3, 1985
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Franz Dorn, Francois Montavon, Milos Suchy