Size and optimization of the formulations Active substances Excipients

1.3 Size and optimization of the formulations

All the formulations were developed exclusively on a laboratory scale of the order of 1 kg maximum. For this reason, scale-up for production must therefore be checked and revised, as necessary. It is only in very exceptional cases that the formulations have been opti- mized by a systematic study involving a comparison between different exci- pients or by varying the amounts of excipients. Thus, the formulations are merely suggestions that require fur- ther optimization.

1.4 Active substances

The active substances are almost ex- clusively generic. They were mostly supplied free of charge as samples by pharmaceutical companies. Since the manufacturer’s name was mostly not mentioned, it unfortunately cannot be listed here. Significant differences in the proper- ties of the preparations may occur if the same active substance is used, but has a different grain size or origi- nates from another manufacturer. The reason for this is that the difference in physical properties may exert a strong effect particularly on solid drugs cf. Chapter 2.5.

1.5 Excipients

As far as possible, the manufacturer’s name and the registered trademark are given for excipients. The excipients mostly used in the for- mulations and their suppliers are list- ed in Table 1. The serial numbers in the left-hand column of this table are quoted in the formulations. BASF Fine Chemicals Generic Drug Formulations 1998 Table 1 Supplier and address Excipients [1] BASF AG Cremophor ® products Department MER Kollicoat ® products 67056 Ludwigshafen, Kollidon ® products Germany Ludipress ® Lutrol ® products Propylene glycol Pharma or Sicovit ® BASF subsidiary in the Soluphor ® P country concerned Solutol ® HS 15 [2] Bärlocher GmbH Calcium arachinate 80992 Munich, Germany Magnesium stearate [3] Cerestar GmbH Düsseldorferstrasse 191 Potato starch 47809 Krefeld, Germany Corn starch [4] Degussa AG GB Industry + Fine Chemicals Postfach 1345 63457 Hanau, Germany Aerosil ® 200 [5] FMC Corp. Food + Pharmaceutical Products 735 Market Street Avicel ® products Philadelphia, PA 19103, USA Ac-Di-Sol ® [6] Hüls AG Postfach 45674 Marl, Germany Polyethylene glycol 6000, powder [7] Mallincrodt Inc. P.O. Box 5439 675 McDonnel Boulevard St. Louis, MO 63134, USA Stearic acid [8] Meggle Milchindustrie GmbH Postfach 40 Lactose Monohydrate D 20 83512 Wasserburg, Germany Tablettose ® BASF Fine Chemicals Generic Drug Formulations 1998 [9] Rhône-Poulenc 15, Rue Pierre Pays B.P. 52 69660 Collonges-au Mont d’ Or, Dicalcium phosphate, CaHPO 4 France DITAB ® [10] Riedel-de-Haen AG Wunstdorferstrasse 40 Sorbitol, crystalline 30926 Seelze, Germany Talc BASF Fine Chemicals Generic Drug Formulations 1998 BASF Fine Chemicals Generic Drug Formulations 1998

1.6 Stability data