Compaction characteristics of a micro-structured fillerbinder “Microcrystarcellactose B3” for direct compression tableting

Abstract

A research was conducted to develop and evaluate a highly compressible micro-structured filler- binder for direct compression tableting. Tapioca starch (TS) was annealed, hydrolyzed and coprocessed with α -lactose monohydrate (α-LMH) and microcrystalline cellulose (MCC) to yield a novel microcrystarcellactose (MSCL B3). The powder suspensions were prepared at a concentration of 40 %w/w in five separate conical flasks. The TS granules were annealed for 1 h and subsequently hydrolyzed with α-amylase at 58 o and pH 7 for 1, 2, 3, 4, and 5 h respectively. The reaction was terminated and neutralized with 0.1 N HCL and 0.1 N NaOH respectively. The enzyme hydrolyzed starch (EHS) at 3 h, sieved fraction >75-250 μm was coprocessed with α-LMH and MCC and compressed with load ranging from 2.5 to 12.5 KN. MSCL B3 (component ratio of EHS, α-LMH, and MCC ‘35: 35:30’) possessed improved functionality over direct physical mixture of the excipients. The Py (yield values) are: Cellactose (24.2 MNm -2 ) > MCC (25 MNm -2 ) > MSCL B3 (50.0 MNm -2 ) > Starlac (143 MNm -2 ). The degree of plastic deformation occurring “Pk” are in the following order: MSCL B3 (17.0 MNm -2 ) = Cellactose ® (17.0 MNm -2 ) > MCC (18.6 MNm -2 ) > Starlac ® (19.1 MNm -2 ). MSCL B3 is as good as Cellactose ® and more superior in functionality than Starlac ® and MCC. The dilution potential for MSCL B3 in PCM and AA tablets were: 45% and 50 % respectively. MSCL B3 can be used to formulate softer tablet of both poorly compressible API and moisture sensitive API Keywords: Microcrystarcellactose; Coprocessed excipient; Directly compressible excipient; Highly functional fillerbinder; Tapioca starch