Farmitalia Carlo Erba

Alessandro Rigamonti

Luigi Moro

Guido Neri

Diego Oldani

Grazia Maffione

Gaetano Battelli

A method is disclosed for purifying non-homogeneous systems, known as liposomic suspensions, from non-entrapped drugs wherein said suspensions are treated with liquid or solid polymers of synthetic and organic nature having chemical functionality, which are used as ion-exchangers. The liquid or solid polymers are based on styrene, divinylbenzene, acrylic acid, methacrylic acid, and the like, normally known as ion-exchange resins, and may include carboxylic, phosphonic or sulphonic functions of different matrices. The ion-exchange resins may also include salified quaternary ammonium, primary, secondary and tertiary amminic or phosphinic functions or other functions with different matrices, including phenolformaldehyde, styrene-divinylbenzene, acrylates, methacrylates, hydrocarbons and condensation-resins. Treatment may also be carried out with polymers, copolymers, or mixtures thereof, not having any specific chemical function and which normally, but not exclusively, react according to Van der Waals' forces, commonly known as adsorbents. The invention also includes freeze-dried pharmaceutical compositions consisting or consisting essentially of lyophilic liposomes of drugs, such as doxorubicin hydrochloride, aminosidine sulphate or 5-fluoro-uracil. The pharmaceutical compositions are characterized by a high degree of stability.

Pharmaceutical compositions consisting or consisting essentially of

The present invention relates to the preparation of sterile and stable freeze-dried forms of Cisplatinum containing from 10 to 50 mg of active ingredient, which can be obtained on an industrial scale and which have particular characteristics of facility and rapidity of dissolution which permit them to be used in a more advantageous and rational manner in antitumor chemotherapy, as compared with the freeze-dried forms of Cisplatinum presently on the market. These particular characteristics are achieved as the result of employing special ingredients in respect of formulation (concentration of the solution to be freeze-dried, introduction of alcohols, adjustment of the pH of the solution to an appropriate value), and as the result of using a manufacturing technique having as its final stage the freeze-drying of Cisplatinum in a water-alcoholic medium. The manufacturing method, and in particular the freeze-drying process, have shown themselves to be economically advantageous, and have made it possible to overcome the very considerable problems connected with the freeze-drying of Cisplatinum in aqueous medium (breakage of containers, very low yields), as well as to obtain preparations perfectly adapted to be used therapeutically by intravenous administration.

Novel pharmacological compositions based on Cisplatinum and method for

New pharmaceutical sustained-release compositions, formulated as tablets, are prepared by mixing the active ingredient with excipient already granulated and coated with polymers and/or copolymers or a polymers- and/or copolymers-mixture substantially insoluble in water. Such pharmaceutical preparations enable one to enhance or to decrease very easily and precisely the sustained-release effect by regulating the granulometry of the excipient, the excipient/active ingredient ratio, the hardness, and the percentage of the polymers and/or copolymers or of the polymers- and/or copolymers-mixture.

Pharmaceutical sustained-release compositions

A method is disclosed for purifying non-homogeneous systems, known as liposomic suspensions, from non-entrapped drugs wherein said suspensions are treated with liquid or solid polymers of synthetic and organic nature having chemical functionality, which are used as ion-exchangers. The liquid or solid polymers are based on styrene, divinylbenzene, acrylic acid, methacrylic acid, and the like, normally known as ion-exchange resins, and may include carboxylic, phosphonic, or sulphonic functions of different matrices. The ion-exchange resins may also include salified quaternary ammonium, primary, secondary and tertiary amminic or phosphinic functions or other functions with different matrices, including phenolformaldehyde, styrene-divinylbenzene, acrylates, methacrylates, hydrocarbons and condensation-resins. Treatment may also be carried out with polymers, copolymers, or mixtures thereof, not having any specific chemical function and which normally, but not exclusively, react according to Van der Waals' forces, commonly known as adsorbents. The invention also includes pharmaceutical compositions consisting or consisting essentially of lyophilic liposomes of doxorubicin hydrochloride, aminosidine sulphate or 5-fluoro-uracil.

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Milan, Italy

Alessandro Rigamonti