Pak. J. Pharm. Sci., Vol.21, No.2, April 2008, pp.113-120 113 FORMULATION DEVELOPMENT AND OPTIMIZATION OF IBUPROFEN TABLETS BY DIRECT COMPRESSION METHOD RABIA BUSHRA, MUHAMMAD HARRIS SHOAIB, NOUSHEEN ASLAM, DURRIYA HASHMAT AND MASUD-UR-REHMAN* Department of Pharmaceutics, Faculty of Pharmacy, University of Karachi, Karachi-7520, Pakistan *Ministry of Health, Government of Pakistan ABSTRACT Ibuprofen is widely used as a prescription and non-prescription medicine. The aim of study is to prepare Ibuprofen tablets (200mg) using direct compression technique which is now days considered a cost effective and simple method of manufacturing. It is considered as an appropriate method for hygroscopic and thermolabile substances. In order to obtain the best, optimized product, nine different formulations were developed. Diluent (X1), disintegrant (X2) and lubricant (X3) were taken as independent variables. Weight variation (Y1), thickness (Y2), length and width (Y3), hardness (Y4), friability (Y5), disintegration (Y6), dissolution (Y7) and pharmaceutical assay (Y8) were studied as response variables. The results of all nine formulations were found within the acceptable limits conforming to those given in official compendia. However, F-6 was selected as an optimized product on the basis of high dissolution (99.05%) and Assay (100.04%). The variation of weight among the tablets of F-6 was least which showed best ratio of excipients in the formulation. Optimization has proven as an effective tool in product development. This is because no clear relationship exists between the variables. Keywords: Ibuprofen, direct compression, optimization, independent variables, response variables. INTRODUCTION Ibuprofen is a commonly used NSAID (Abraham et al., 2005). Low-dose Ibuprofen is as effective as aspirin and paracetamol for the indications normally treated with over-the-counter (OTC) medications (Moore, 2003). Ibuprofen is used as an analgesic, anti-inflammatory agent and anti-pyretic agent (Wood et al., 2006). Recemic Ibuprofen and the S (+)-enantiomer are mainly used in the treatment of mild to moderate pain related to dysmenorrhoea, headache, migrane, post operative and in the management of spondylitis, Osteo-arthritis, rheumatoid arthritis, and soft tissue disorders (Potthast, 2005 and Tan et al., 1999). Ibuprofen also studied for the closure of the ductus arteriosus. Results indicate that Ibuprofen is as effective as Indomethacin (Kravs and Pharm, 2005). Dental practitioners have relied on Ibuprofen and other nonsteroidal anti-inflammatory drugs to manage acute and chronic orofacial pain (Moore and Hersh, 2001). The common analgesic drug Ibuprofen (C 13 H 18 O 2 ) shows bad dissolution and tableting behavior due to its hydrophobic structure. Additionally its high cohesivity results in low flowability. Another problem in its manufacturing is its high tendency of sticking to the punches (Rasenack and Muller, 2002). There are three methods of tablet manufacturing with the choice depending upon the dose and the drug’s physical properties, such as, compressibility and flow of the blend (Halbert, 1993). Direct compression is a process by which tablets are compressed directly from mixtures of the drug and excipients, without any preliminary treatment (British Pharamaceutical Codex, 1994). A simple formula is considered to be composed of an active ingredient, a diluent and a lubricant (Martino et al., 2004). Active ingredient Diluent Glidant Mixing Lubricant Disintegrating agent Compression Fig. 1: The direct compression process of tablet manufacturing (Armstrong, 2002). Tablet manufacturing by direct compression has increased steadily over the years. It offers advantages over the other manufacturing processes for tablets, such as wet granulation and provides high efficiency (Zhang et al., 2003). As direct compression is more economic, reducing the cycle time and straight forward in terms of good manufacturing practice requirements. On the other hand wet granulation not only increases the cycle time, but also has certain limits imposed by thermolability and moisture sensitivity of the active. So pharmaceutical industry is Corresponding author: e-mail: harrisshoaib2000@yahoo.com