Pc. Schmidt et Cjw. Rubensdorfer, EVALUATION OF LUDIPRESS AS A MULTIPURPOSE-EXCIPIENT FOR DIRECT COMPRESSION .2. INTERACTIVE BLENDING AND TABLETING WITH MICRONIZED GLIBENCLAMIDE, Drug development and industrial pharmacy, 20(18), 1994, pp. 2927-2952
In the second part of this publication the differing interactions of m
icronized glibenclamide during mixing with four filler/binders for dir
ect compression were studied. The excipients used were: Ludipress, Cel
lactose, Avicel PH 200 and Karion Instant. In order to prepare interac
tive mixtures, increasing amounts of micronized glibenclamide were ble
nded with filler/binder fractions of 125 to 500 mu m. The degree of in
teractivity was determined by air jet sifting of the mixes, comparing
drug content in the mixes before and after sieving. Cellactose showed
the highest adhesion tendency for glibenclamide due to the large cavit
ies in the particles, leading to a reagglomeration within these caviti
es. Tablets containing 1.75, 3.50, 5.00 and 10.00 mg of glibenclamide
per tablet were compressed with Cellactose and Ludipress. As previousl
y reported (1) for Cellactose based placebo tablets, Cellactose also s
howed a tremendous increase in disintegration time and a prolonged dis
solution rate at compaction pressures above 100 MPa. The corresponding
values of Ludipress were not influenced. Therefore in terms of a mult
ipurpose-excipient, Ludipress should be given preference in the formul
ation of low dosed drugs.