Farmarc Nederland Bv

University College Dublin

Pharmatec International S.r.l.

Lawrence John Penkler

Lueta Ann Glintenkamp

Michiel Coenraad Van Oudtshoorn

Mark David Bodley

Douglas George Nicholson

Rainer Helmut M&uuml;ller

Mino Rodolfo Caira

Raphael Darcy

Vittorino Ravelli

Bart Jan Ravoo

Vivienne Jean Griffith

Darryl Vanstone Whittaker

Luigi Renzo Nassimbeni

Stephan Anton Runge

Lu&eacute;ta-Ann De Kock

Soluble amphiphilic macrocycle analogues having lipophilic groups attached to one side of the units making up the macrocycle and hydrophilic groups attached to the other side. These amphiphilic macrocyclic derivatives have the ability to self-assemble in aqueous solvent forming micelles or vesicles and can be used as hosts for the solubilization and/or stabilization of various compounds. Embodiments of the present invention utilize macrocyclic oligosaccharides and preferably cyclodextrin as the macrocyclic derivatives to be modified.

Amphiphilic macrocyclic derivatives and their analogues

A pharmaceutical composition an inclusion complex and methods for treating patients and preparing said complex disclosed for transmucosal delivery comprising an inclusion complex of (a) alprazolam and (b) a water soluble 2-hydroxypropyl-beta-cyclodextrin, and a pharmaceutically acceptable carrier therefor, wherein all the alprazolam is present in ring-closed form.

Alprazolam inclusion complexes and pharmaceutical compositions thereof

The invention relates to solid, particulate lipid-based excipients which are loaded with cyclosporine. Said excipients have improved biopharmaceutical properties for cyclosporines in vivo, are of a better quality (in terms of fineness, homogeneity of the particles, inclusion of the medicament) and are more physically stable in the particulate formulation (no aggregation or gel formation). The invention also relates to a therapeutic treatment with cyclosporine formulations which produce an average blood level concentration in the steady state range of 300 ng/ml to over 1000 ng/ml, preferably over 800 ng/ml, especially up to 900 ng/ml, preferably 400 ng/ml to 800 ng/ml in the absence of high initial blood level concentrations essentially over 1500 ng/ml, especially over 1200 ng/ml. This blood level concentration is preferably maintained for an extended period of at least 5 hours, preferably at least 7 hours.

Pharmaceutical cyclosporin formulation with improved biopharmaceutical properties, improved physical quality and greater stability, and method for producing said formulation

A pharmaceutical composition contains an acid addition salt of a basic drug and a fatty acid or bile acid. The acid addition salts thus formed exhibit enhanced transmucosal and transdermal penetration of the basic drug. The acid addition salts, an inclusion complex containing said salts and a use of said salts are also disclosed.

Pharmaceutical composition containing acid addition salt of basic drug

Pharmaceutical composition

A method of preparing an injectable pharmaceutical or veterinary composition which comprises either diclofenac or a salt thereof and 2-hydroxypropyl beta-cyclodextrin, or an inclusion complex of diclofenac or a salt thereof and 2-hydroxypropyl beta-cyclodextrin, includes the step of dissolving either the diclofenac or salt thereof and the 2-hydroxypropyl beta-cyclodextrin, or the inclusion complex, in water to form a solution, the water having been acidified to a pH such that the pH of the solution is from 6.0 to 8.5 inclusive, in the absence of a phosphate buffer. The composition so produced has good stability on storage.

Pharmaceutical composition comprising diclofenac and cyclodextrin

An inclusion complex of diclofenac, preferably as diclofenac sodium, and an unsubstituted beta-cyclodextrin has the formula 1 molecule of diclofenac to 1 molecule of the unsubstituted beta-cyclodextrin and preferably from 5 to 11 water molecules. The inclusion complex may be formulated as a pharmaceutical composition.

Inclusion complex of beta-cyclodextrin and diclofenac, its preparation

Growing community of inventors

Port Elizabeth, South Africa

Lawrence John Penkler