Tillotts Pharma Ag

Cancer Prevention Pharmaceuticals, Inc.

University College London

Roberto Carlos Bravo González

Thomas Buser

Abdul Waseh Basit

Ana Cristina Freire

Felipe José Oliveira Varum

Esther Maria Furrer

Jean Ducassou

Patrick Shannon

Felipe Jose Oliveira Varum

Maxim Puchkov

Daniel Preisig

Joerg Huwyler

Felipe Josè Oliveira Varum

Frederic Jean-Claude Goutte

Felipe Jose Varum

Felipe Varum

Laetitia Von Rochow

Carsten Markus Füller

Yalcin Cetinkaya-Coskun

Vipul Yadav

Frédéric Jean-Claude Goutte

Felipe José Oliveria Varum

A method produces a coatable core for a modified release drug formulation for oral administration. The coatable core has a high drug load of at least 70 wt % based on the total weight of the coatable core. The method involves the steps of granulating a composition containing a drug and at least one binder to form granules; blending the granules with a pharmacologically acceptable disintegrant and optionally, one or more additional pharmacologically acceptable excipients, to form a compression blend, wherein the disintegrant is present in an amount from about 0.5 wt % to about 5 wt %, based on the total weight of the coatable core; and compressing the compression blend using an external lubrication compression method to form a coatable core.

Coatable core for a modified release drug formulation

A method produces a coatable core for a delayed release drug formulation for oral administration, to deliver a drug to the colon. The method involves forming a core containing a drug. An outer layer coating preparation is formed by combining a first aqueous preparation of an enzymatically degradable polymer, which is degradable by colonic bacterial enzymes; a second aqueous preparation of a film-forming enteric polymer having a pH threshold of about pH 6 or above; and an organic anti-tack agent. The core is then coated with the outer layer coating preparation to form an outer layer coated core.

Method of producing a delayed release drug formulation

Provided herein are fixed-dose combination formulations of a pharmaceutically effective amount of eflorithine together with a pharmaceutically effective amount of sulindac. Also provided are methods of use and of methods of manufacture of these formulations.

Eflornithine and sulindac, fixed dose combination formulation

Provided herein are fixed-dose combination formulations of a pharmaceutically effective amount of eflornithine together with a pharmaceutically effective amount of sulindac. Also provided are methods of use and of methods of manufacture of these formulations.

In a delayed release formulation comprising a core containing a drug and a delayed release coating for providing intestinal release, release of the drug in the colon is accelerated by including an isolation layer between the core and the delayed release coating. The delayed release coating comprises an inner layer and an outer layer. The outer layer comprises a pH dependently soluble polymeric material which has a pH threshold at about pH 5 or above. The inner layer comprises a soluble polymeric material which is soluble in intestinal fluid or gastrointestinal fluid, said soluble polymeric material being selected from the group consisting of a polycarboxylic acid polymer that is at least partially neutralised, and a non-ionic polymer, provided that, where said soluble polymeric material is a non-ionic polymer, said inner layer comprises at least one additive selected from a buffer agent and a base.

Delayed release drug formulation

The present invention relates to a delayed release pharmaceutical formulation for delivering an active agent to the intestine, a method of preparing such formulation and the use of such formulation in the treatment of gastrointestinal disorders.

Delayed release pharmaceutical formulation and methods of making and using same

In a delayed release formulation comprising a core containing a drug and a delayed release coating for providing intestinal release, release of the drug in the colon is accelerated by including an isolation layer between the core and the delayed release coating. The delayed release coating comprises an inner layer and an outer layer. The outer layer comprises a pH dependently soluble polymeric material which has a pH threshold at about pH 5 or above. The inner layer comprises a soluble polymeric material which is soluble in intestinal fluid or gastrointestinal fluid, said soluble polymeric material being selected from the group consisting of a polycarboxylic acid polymer that is at least partially neutralized, and a non-ionic polymer, provided that, where said soluble polymeric material is a non-ionic polymer, said inner layer comprises at least one additive selected from a buffer agent and a base.

Delayed release of a drug to the colon is achieved from a delayed release formulation comprising a core and a coating for the core. The core comprises a drug and the coating comprises an inner layer and an outer layer. The outer layer comprises a mixture of a first polymeric material which is susceptible to attack by colonic bacteria, and a second polymeric material which has a pH threshold at about pH 5 or above. The inner layer comprises a third polymeric material which is soluble in intestinal fluid or gastrointestinal fluid, said third polymeric material being selected from an at least partially neutralized polycarboxylic acid and a non-ionic polymer. In embodiments in which the third polymeric material is a non-ionic polymer, the inner layer comprises at least one of a buffer agent and a base. Advantages of formulations according to the present invention include accelerated release of the drug when exposed to colonic conditions and reduction or elimination of a food and/or alcohol effect on drug release after administration.

The present invention relates to a delayed release pharmaceutical formulation for delivering an active agent to the intestine, a method of preparing such formulation and the use of such formulation in the treatment of gastrointestinal disorders, wherein the formulation includes at least one active agent associated with porous, functionalized calcium carbonate carrier particles that are surrounded by a material for colon targeting.

Delayed release pharmaceutical formulation containing porous carrier particles for colon targeting

Delayed release of a drug to the colon is achieved from a delayed release formulation comprising a core and a coating for the core. The core comprises a drug and the coating comprises an outer layer and at least one layer between the core and the outer layer selected from the group consisting of an isolation layer and an inner layer. The outer layer comprises a mixture of a first polymeric material which is susceptible to attack by colonic bacteria, and a second polymeric material which has a pH threshold at about pH 5 or above. The inner layer comprises a third polymeric material which is soluble in intestinal fluid or gastrointestinal fluid, said third polymeric material being selected from an at least partially neutralised polycarboxylic acid and a non-ionic polymer. In embodiments in which the third polymeric material is a non-ionic polymer, the inner layer comprises at least one of a buffer agent and a base. The isolation layer comprises a non-ionic polymer which is soluble in intestinal fluid or gastrointestinal fluid. The outer is applied directly to the inner layer or the isolation layer using a coating preparation formed by combining the first polymeric material in an aqueous medium with a second polymeric material in an organic medium. Advantages of formulations according to the present invention include accelerated release of the drug when exposed to colonic conditions and reduction or elimination of a food and/or alcohol effect on drug release after administration.

Growing community of inventors

Binningen, Switzerland

Roberto Carlos Bravo González