Nidhi P. Sapkal, Minal N. Bonde, Pradeep Kataria, Anwar S. Daud

Gurunanak College of Pharmacy, Nari, Kaamgaar Nagar, Kamptee Road, Nagpur, India

Zim Laboratories Ltd. MIDC, Kalmeshwar, Nagpur, India

Abstract:

The pharmaceutical tablet manufacturing industry is always looking for the novel energy efficient and cost effective granulation processes that do not affect the quality of tablets. Literature reports Moisture-Activated Dry Granulation (MADG) as the simple granulation process but requires the use of specialized excipients like Avicel PH 200 LM, Aeroperl 300, PVP K-12, etc. and high sheer mixers. Very few studies are reported for this method. In the present study formulation batches of tablets using model drugs from the three categories namely high dose (paracetamol 500 mg), low dose (dexamethasone 0.5 mg) and combination (theophylline 120 mg, salbutamol 2 mg) were designed and developed. Novelty of the present work is the use of conventional excipients such as lactose, spray dried MCC, PVP-K-30, Silicone dioxide, etc. Planetary mixer was used as the equipment for granulation. Effect of formulation variables like nature of binder (Kollidone VA64, PVP K-30, HPC, HPMC 5 cps), concentration of binder (1% - 3.5%), amount of granulating fluid (3% and 5%), spray pattern (droplet size: 1 mm - 3 mm) on the properties of granules were studied. The process was first developed for 5 kg batch size and then scale up study was carried out for 50 kg batch size. The effect of formulation variables upon pre-compression parameters like particle size distribution, moisture content, bulk density, tapped density, angle of repose, Carr's index, IR, SEM was studied. Various post-compression parameters like friability, hardness, content uniformity, disintegration time and dissolution were also carried out. It was found that to produce acceptable quality of granulation blend, concentration of binder and granulating fluid played a significant role, while a constant droplet size was required to obtain granules and tablets with optimum parameters. The present work discusses the effect of selected variables on precompression, post-compression parameters and on scale up. It can be concluded that MADG process can be routinely used for the manufacturing of these tablet formulations without using any specialized excipients and thus, it is technology development at no additional cost instead with few manufacturing steps.