Pentech Pharmaceuticals, Inc.

Greenwich Pharmaceuticals Incorporated

501 Greenwich Pharmaceuticals Incorporated

Bruce Ronsen

Ragab El-Rashidy

Albert V Thomas

Sudershan K Arora

Yogesh Sadhale

Emad Eldin Hassan

Venkata R Kota

Method for preparing a wet granule formulation of paroxetine hydrochloride are disclosed. The formulations are suitable for tabletting and capsulation.

Paroxetine tablets and capsules

A free-flowing, amorphous paroxetine hydrochloride composition suitable as a therapeutic agent for premature ejaculation can be prepared by dissolving paroxetine free base in a hydrochloric acid-ethanol solution followed by drying. The present compositions comprise amorphous paroxetine hydrochloride and at least one hydroxyl-bearing compound. In one preferred embodiment, the hydroxyl-bearing compound is ethanol and the amount of ethanol present in the amorphous product is in the range of 1 to 4 weight percent based on paroxetine hydrochloride. The amorphous product is stable and substantially non-hygroscopic.

Amorphous paroxetine composition

Impotence can be ameliorated without substantial undesirable side effects by nasal administration of apomorphine, optionally with an antiemetic agent present in an amount sufficient to substantially reduce nausea symptoms that may be associated with the use of apomorphine.

Apomorphine-containing dosage form for ameliorating male erectile dysfunction

A stable amorphous paroxetine hydrochloride composition suitable as a therapeutic agent is prepared employing an aqueous solvent medium containing an acidulant and polyvinylpyrrolidone and drying the resulting solid dispersion. The preferred compositions include amorphous paroxetine hydrochloride, polyvinylpyrrolidone and citric acid.

Psychogenic impotence can be ameliorated without substantial undesirable side effects by administration of apomorphine and an antiemetic agent in an amount sufficient to substantially reduce nausea symptoms associated with the use of apomorphine.

Apomorphine-containing dosage forms for ameliorating male erectile dysfunction

Sexual dysfunction in human females can be ameliorated, without substantial undesirable side effects, by apomorphine. Administration of apomorphine increases nerve stimulated clitoral intracavernosal blood flow and vaginal wall blood flow for enhanced clitoral erection and vaginal engorgement in a female. A plasma concentration of apomorphine of no more than about 5.5 nanograms per milliliter is preferably maintained.

Female sexual dysfunction treatment

Apomorphine-containing dosage forms for ameliorating male erectile

Symptoms of Parkinson's disease and psychogenic male erectile dysfunction (MED) can be ameliorated through the use of apomorphine. The adverse side effects of apomorphine administration, such as nausea, vomiting, yawning, and cardiovascular effects, can be significantly reduced by a dose escalating method of acclimatization. An initial dose of apomorphine is administered to the patient, and subsequently increased over a period of time until a final apomorphine dose in excess of a desired therapeutic dose has been received by the patient. Thereafter a therapeutic dose of apomorphine, less than the final apomorphine dose, is administered to the patient with attendant reduced side effects.

Amelioration of apomorphine adverse effects

Sexual dysfunction in human females can be ameliorated, without substantial undesirable side effects, by sublingual administration of apomorphine dosage forms. Administration of apomorphine increases nerve stimulated clitoral intracavernosal blood flow and vaginal wall blood flow for enhanced clitoral erection and vaginal engorgement in a female. A plasma concentration of apomorphine of no more than about 5.5 nanograms per milliliter is preferably maintained.

Treatment of female sexual dysfunction

A composition providing a relatively slow release of water-soluble drugs, such as apomorphine, for delivery via the sublingual or buccal routes.

Controlled release of drugs delivered by sublingual or buccal

A direct compression tablet exhibiting relatively low hardness provides a relatively rapid release of fluoxetine. The tablet has a hardness of no more than about 6 kilopascals and a dicalcium phosphate dihydrate-to-disintegrant weight ratio of about 3 to about 7.

Low dose fluoxetine tablet

A free-flowing, amorphous paroxetine hydrochloride-ethanol composition suitable as a therapeutic agent for premature ejaculation can be prepared by dissolving paroxetine free base in a hydrochloric acid-ethanol solution followed by drying. In a preferred embodiment, the amount of ethanol present in the amorphous product is in the range of 1 to 4 weight percent based on paroxetine hydrochloride. The amorphous product is stable and substantially non-hygroscopic.

Derivatives of 1,2-O-isopropylidene-.alpha.,D-glucofuranose and intermediates for preparing these derivatives are described. These derivatives are useful for treating animals and mammals with inflammatory and/or autoimmune disorders such as autoimmune deficiency syndrome, psoriasis, atopic dermatitus, rheumatoid arthritis, osteoarthritis, scleroderma and systemic lupus erythematosus.

3,5,6-substituted derivatives of

Derivatives of -.alpha.,D-glucofuranose .alpha.,D-allanfuranose and intermediates for preparing these derivatives are described. These derivatives are useful for treating animals and mammals with inflammatory and/or autoimmune disorders such as psoriasis, atopic dermatitus, rheumatoid arthritis, osterarthritis, scleroderma and systemic lupus erythematosus.

Growing community of inventors

River Forest, IL, United States of America

Bruce Ronsen