Abstract: Novel lysine esters used as absorption enhancing agents for gastrointestinally and rectally administered drugs. Also provided are processes for preparation of said lysine ester compounds as well as pharmaceutical formulations and methods for their use as absorption enhancing agents.
Abstract: Drug delivery device retained in the stomach comprising at least one drug and a continuous solid-stick figure made from polymer(s) that releases said drug slowly over a controlled, predictable and extended period of time.
Type:
Grant
Filed:
May 7, 1987
Date of Patent:
April 5, 1988
Assignee:
Merck & Co., Inc.
Inventors:
Larry J. Caldwell, Colin R. Gardner, Robyn C. Cargill
Abstract: Labile quaternary ammonium salts of the following formula (I) and (II) are provided: ##STR1## wherein N represents a tertiary aliphatic amine; wherein N represents an unsaturated amine; wherein R represents a member selected from the group consisting of a hydrogen atom, a C.sub.1 -C.sub.8 open chain or cyclo alkyl group, a C.sub.1 -C.sub.8 alkoxyalkyl group, a C.sub.1 -C.sub.8 acyloxyalkyl group, a C.sub.1 -C.sub.8 haloalkyl group, a C.sub.1 -C.sub.8 carboxyalkyl group, a C.sub.2 -C.sub.8 alkenylphenyl group, an aryl group, and a substituted aryl group, whose substituents are selected from the group consisting of a halogen atom, an O-lower alkyl (C.sub.1 -C.sub.4) group, an O-acyl group, a nitro group, a carboxyl group, and a carboethoxy group; wherein R.sub.1 which may be the same or different, represents any member defined by R above with the proviso that R.sub.
Abstract: Certain novel cyclic ureas are disclosed herein as dermal penetration enhancers of drug absorption. Also disclosed herein are compositions, methods of treatment and processes for preparing said cyclic urea compounds.
Abstract: The invention relates to novel 1,2-disubstituted-4-nitroimidazole compounds that are useful as potent antiprotozoal agents and simultaneously possess non-mutagenicity as compared to known 4- or 5-nitroimidazole compounds. Also, compositions and methods for antiprotozoal uses of said novel 1,2-disubstituted-4-nitroimidazole compounds are disclosed herein.
Type:
Grant
Filed:
February 28, 1986
Date of Patent:
June 23, 1987
Assignee:
Merck & Co., Inc.
Inventors:
Gerald T. Miwa, Wen-Jen R. Wang, John S. Walsh
Abstract: The invention relates to compositions and methods of enhancing rectal absorption of L-dopa via the formation of an ester prodrug and optionally with a decarboxylase inhibitor.
Abstract: The instant invention is directed to a polymer with at least one labile backbone bond per repeat unit and at least one pendant acid functionality per thousand repeat units.The instant invention is also directed to a controlled release device which comprises:(A) a polymer with at least one labile backbone bond per repeat unit and at least one pendant acid functionality per thousand repeat units; and(B) a beneficial substance incorporated within or surrounded by the matrix of said polymer.
Abstract: This invention relates to a novel and improved process for preparing .alpha.-(trichloromethyl) benzyl alcohols, particularly, trichloromethyl-3-nitrobenzyl alcohol a key intermediate useful in the preparation of clorsulon (4-amino-6-(trichloroethenyl)-1,3-benzene-disulfonamide) via a base-catalyzed condensation reaction of benzaldehydes and chloroform.
Abstract: Novel substituted and unsubstituted 13-(alkoxy)methoxy derivatives of the avermectin aglycones are useful as anthelmintic and antiparasitic agents. The compounds are also useful as pesticides and insecticides against agricultural pests. Included herein are novel intermediates useful in the process for preparing said avermectin aglycone derivatives. Compositions of said derivatives and methods of administering said compositions are also disclosed.
Abstract: This invention relates to an eyeglass frame mounted unit dose ophthalmic drug delivery device. A unit dose of ophthalmic medicament is provided by either a preloaded disposable microsyringe, preloaded disposable tip or manually loaded calibrated microsyringe rigidly mounted on a block which itself is slidably mounted to the eyeglass frame. The device allows for the insertion of ophthalmic medication into the inferior cul de sac of the eye.
Abstract: This invention involves complexes of quinoline carboxylic acid derivatives with guanidine and guanidine carbonate. The complexes have a greater solubility and dissolution rate when compared to the parent quinoline carboxylic acid derivatives and thus are more effective anti bacterials than the parent acids.
Abstract: This invention relates to a unique drug delivery system for delivering drugs to a body cavity. The drug delivery system comprises a medicament and a polymer such that the drug delivery system is a liquid at room temperature but forms a semi-solid or gel at the body temperature in the body cavity.
Type:
Grant
Filed:
May 16, 1983
Date of Patent:
October 23, 1984
Assignee:
Merck & Co., Inc.
Inventors:
John L. Haslam, Takeru Higuchi, Arthur R. Mlodozeniec
Abstract: This invention describes the application of selected polymers as novel drug delivery systems which use the body temperature and pH to induce a liquid to gel transition of the polymer which contains a drug or therapeutic agent therein. The goal of such a delivery system is to achieve a greater degree of bioavailability or sustained concentration of a drug.
Type:
Grant
Filed:
May 16, 1983
Date of Patent:
October 2, 1984
Assignee:
Merck & Co., Inc.
Inventors:
John L. Haslam, Takeru Higuchi, Arthur R. Mlodozeniec
Abstract: Present invention provides a unique drug delivery device for delivering drug by injection into a body. The drug delivery system comprises the drug and polymer which is a liquid at room temperature and a semi-solid or gel at the body temperature.
Type:
Grant
Filed:
May 16, 1983
Date of Patent:
October 2, 1984
Assignee:
Merck & Co., Inc.
Inventors:
John L. Haslam, Takeru Higuchi, Arthur R. Mlodozeniec
Abstract: This invention relates to a unique drug delivery system for application to the skin which drug delivery system is a liquid at room temperature, but when administered topically to the skin becomes a semi-solid or gel when warmed by the body.
Type:
Grant
Filed:
May 16, 1983
Date of Patent:
October 2, 1984
Assignee:
Merck & Co., Inc.
Inventors:
John L. Haslam, Takeru Higuchi, Arthur R. Mlodozeniec