American Home Products Corporation

Merrion Research III Limited

Barr Laboratories, Inc.

American Home Products Corporation (del.)

Applied Analytical Industries, Inc.

Endeavor Pharmaceuticals

Thomas W Leonard

Robert P Waranis

Karol Kay Mikula

Atul M Mehta

Ronald N Warner

Robin P Enever

Marcia S Schlesinger

David C Coughlan

Lizbeth A Bachand

Robert R Whittle

Frederick D Sancilio

Edward N Hill

Maureen M Harrison

Edel O'Toole

Alan Cullen

Kenneth Iain Cumming

Edward S Wilson

James Swarbrick

Dean G Shirazi

David P Hause

Karol K Mikula

Christian L Ofslager

Katherin M Schlipp

Zebunissa Ramtoola

Kishore Chalasani

Bozena Adamczyk

Amanda Lee

R Forrest Waldon

The present invention provides pharmaceutical compositions for oral administration comprising a therapeutically effective amount of a selective factor Xa inhibitor or a pharmaceutically acceptable salt thereof and an enhancer, wherein the enhancer is a medium chain fatty acid or a salt, ester, ether, or derivative of a medium chain fatty acid and has a carbon chain length of from about 4 to about 20 carbon atoms. The present invention also provides a method for obtaining a reproducible bioavailability of selective factor Xa inhibitor in an object after oral administration comprising orally administering a pharmaceutical composition as described above.

Pharmaceutical compositions of selective factor Xa inhibitors for oral administration

The present invention provides compositions of GnRH related compounds that are suitable for oral administration, injectable administration and other forms of administration wherein the gelling characteristics of the composition are a factor. The compositions of the present invention comprise a therapeutically effective amount of one or more GnRH related compound, and a sufficient amount of at least one anti-gelling agents to reduce the gelation of the GnRH related compound. The present invention also provides processes for preparation of a composition of one or more GnRH related compound, wherein the process comprises mixing the GnRH related compound with one or more anti-gelling agents, wherein the anti-gelling agent comprises a medium chain fatty acid salt, or an ester, an ether, or a derivative of a medium chain fatty acid and has a carbon chain length of from about 4 to about 20 carbon atoms or is a surface active agent.

Compositions of GnRH related compounds and processes of preparation

The present invention generally relates to orally administered pharmaceutical compositions of iron compounds with medium chain fatty acid salts. The invention further relates to methods of using the pharmaceutical compositions to treat iron deficiency and related disorders.

Pharmaceutical compositions of iron for oral administration

The invention relates to a pharmaceutical composition and oral dosage forms comprising a bisphosphonate in combination with an enhancer to promote absorption of the bisphosphonate at the GIT cell lining. The enhancer is a medium chain fatty acid or a medium chain fatty acid derivative having a carbon chain length of from 6 to 20 carbon atoms. Preferably, the solid oral dosage form is a controlled release dosage form such as a delayed release dosage form.

Solid oral dosage form containing an enhancer

The present invention includes methods for preventing endometrial hyperplasia associated with estrogen therapy through the administration of a progestin agent. The methods presented may include starting the administration of a progestin agent at a high dose, and then lowering the dose.

Treatment of conditions relating to hormone deficiencies by administration of progestins

The present invention relates to novel estrogenic compounds. The present invention also relates to methods of treating estrogen deprivation in a subject comprising administering novel estrogenic compounds. Additionally, the present invention relates to methods of synthesizing novel estrogenic compounds.

C(14) estrogenic compounds

A composition of matter is provided having a mixture of active estrogenic compounds. The mixture is present in chemically pure form. The mixture includes salts of conjugated estrone, conjugated equilin, conjugated &#x394;-dehydroestrone, conjugated 17&#x3b1;-estradiol, conjugated 17&#x3b1;-dihydroequilin, conjugated 17&#x3b2;-dihydroequilin, conjugated 17&#x3b2;-estradiol, conjugated equilenin, conjugated 17&#x3b1;-dihydroequilenin, and conjugated 17&#x3b2;-dihydroequilenin. The mixture also contains the same essential estrogenic compounds present in naturally derived equine conjugated estrogens. Drug products including the composition of matter are also provided, as are methods of using these drug products to treat mammals in need of treatment. Methods of analyzing mixtures containing conjugated estrogens are also provided.

Pharmaceutical compositions of conjugated estrogens and methods of analyzing mixtures containing estrogenic compounds

Disclosed herein is an aqueous, injectable rapamycin solution comprising 40 to 75 volume percent of a concentrate solution of rapamycin in propylene glycol, at concentrations of rapamycin ranging from 0.25 mg/ml to 8 mg/ml, in combination with a diluent solution comprising water, wherein the diluent comprises 60 to 25 volume percent of the combined solution and the concentration of rapamycin in the combined solution ranges from 0.1 mg/ml to 4 mg/ml.

Rapamycin formulation for IV injection

The present invention comprises oral rapamycin formulations which contain, per 100 ml of the formulation, from about 0.01 to about 10.0 grams per 100 ml of rapamycin, from about 0.1 to about 10 ml of surfactant, from about 0.1 to about 25 ml of N,N-dimethylacetamide, and from about 65 to about 99.8 ml of a lecithin or phospholipid solution.

Rapamycin formulations for oral administration

The present invention provides pharmaceutical capsule compositions for the oral administration of an H.sub.2 -antagonist. The composition includes a capsule containing an emulsion having a water portion and an oil portion. A pharmaceutically acceptable salt of an H.sub.2 -antagonist is dissolved in the water portion. The composition delivers a therapeutically effective amount of the H.sub.2 -antagonist to a patient in need thereof. The present invention also provides methods of making the capsule composition.

Oral compositions of H.sub.2 -antagonists

The present invention provides novel oral rapamycin formulations which have, per 100 ml of the formulation, from about 0.01 grams to about 5.0 grams of rapamycin, from about 0.05% to about 10% by volume of surfactant, and from about 75% to about 99.95% by volume of a solution of phospholipid or lecithin in which the phospholipid or lecithin therein is 40% to 75% by weight.

Disclosed herein is an aqueous, injectable rapamycin solution comprising 0.1 to 10 percent of a concentrate solution of rapamycin in N,N-dimethylacetamide, at concentrations of rapamycin ranging from 0.25 mg/ml to 100 mg/ml, in combination with a diluent solution consisting of 0.1 to 10 weight percent of one or more polyoxyethylene sorbitan esters, 10 to 60 weight percent of either polyethylene glycol 200 or 300 or both and 30 to 90 volume percent water, wherein the concentration of rapamycin in he combined solution ranges from 0.05 mg/ml to 5.0 mg/ml. Also disclosed is an aqueous, injectable solution of rapamycin, said solution comprising rapamycin in 0.1 to 10 weight percent N,N-dimethylacetamide, 0.09 to 7.5 weight percent of one or more polyoxyethylene sorbitan esters, 9 to 60 weight percent of either polyethylene glycol 200 or 300 or both and 30 to 90 volume percent of water, wherein the concentration of rapamycin in the solution ranges from 0.05 mg/ml to 5.0 mg/ml. Preferred aqueous, injectable rapamycin solutions are those wherein one polyoxyethylene sorbitan ester is present and the polyethylene glycol present is polyethylene glycol 300.

Disclosed herein is an aqueous, injectable rapamycin solution, obtained by a process consisting of mixing 5 to 30 volume percent of a concentrate solution of rapamycin in propylene glycol, at concentrations of rapamycin ranging from 0.5 mg/ml to 10 mg/ml, with a diluent solution consisting of 0.1 to 10 weight percent of one or more polyoxyethylene sorbitan esters, 10 to 60 weight percent of polyethylene glycol 200, 300 or 400 or a combination thereof and 30 to 89.9 volume percent water, wherein the concentration of rapamycin in the injectable solution ranges from 0.025 mg/ml to 3 mg/ml.

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Wilmington, NC, United States of America

Thomas W Leonard