Abbaraju Prasanna Lakshmi et al. IRJP 2012, 3 (2)
INTERNATIONAL RESEARCH JOURNAL OF PHARMACY www.irjponline.com
ISSN 2230 – 8407
Research Article FORMULATION DEVELOPMENT OF IRBESARTAN (POORLY WATER-SOLUBLE DRUG) IMMEDIATE RELEASE TABLETS Abbaraju Prasanna Lakshmi*, Meka Anand Kumar, M. Vamshi Krishna, K.Annie Vijetha, G. Ashwini Omega College of Pharmacy, Ghatkesar, Edulabad, Andhra Pradesh, India Article Received on: 06/12/11 Revised on: 10/01/12 Approved for publication: 18/02/12
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[email protected] ABSTRACT The aim of the present study is to increase the solubility of poorly water soluble drug Irbesartan by using surfactants and formulating into immediate release tablets by using super disintegrants. Surfactants such as sodium lauryl sulfate, polysorbate, and poloxamer 800 are used for increasing the solubility of drug in water by micellisation technique. Super disintegrant such as croscarmellose sodium was used for fast disintegration. Physical properties for granules such as Bulk density, Tapped density, Hausners ratio, % compressibility, % LOD and physical characteristics for Irbesartan IR tablets such as weight variation, friability, hardness, thickness, disintegration, in-vitro dissolution were studied. % cumulative drug release of formulation T3 (having 2% Tween 80) matched with the innovator product Avapro and the similarity factor between innovator and T3 was 97. KEY WORDS: Irbesartan, Polysorbate, poloxamer, sodium lauryl sulphate.
INTRODUCTION Solubility and dissolution are the key parameters for the therapeutic effect of a drug. Solubility is one of the important parameter to achieve desire concentration of drug in systemic circulation for pharmacological response1. More than 92% of the drugs listed in U.S pharmacopeia are having poor solubility. It is commonly recognized in the pharmaceutical industry that on average more than 40% of newly discovered drug candidates are having poor solubility. Micronization, Nanonization, salt formation, use of surfactants2,3,4, solvent deposition, eutectic mixture, solid dispersion and molecular encapsulation are the several methods for enhancement of solubility of the drugs5. Surfactant acts as an absorption enhancer and hence increases both dissolution and permeability of the drug6. They enhance the dissolution rate by promoting wetting and penetration of dissolution fluid into the drug particles. Both ionic and nonionic surfactants were used for solubility enhancement. Among the ionic surfactants, anionic surfactants have high solubility than cationic. Further enhancement of dissolution can be done by using super disintegrants. Super disintegrants, disintegrate the tablet rapidly which enhances the dissolution rate of the drug7. Irbesartan is an angiotensin II receptor antagonist used in the treatment of hypertension. It may also delay progression of diabetic nephropathy and also indicated for the reduction of renal disease progression in patients with type 2 diabetes8 , hypertension and micro albuminuria or proteinuria. According to BCS classification Irbesartan belongs to class II9. Since it has poor solubility in water, methods has been developed for enhancement of solubility by using different types and concentrations of surfactants by which the solubility of Irbesartan has been increased. The present work is to optimization of Irbesartan immediate release tablets and comparing the best with the innovator product by varying the concentration and type of surfactants.
MATERIAL AND METHODS Materials Irbesartan(Aarey Drugs and Pharmaceuticals Ltd, Andhra Pradesh), Lactose Monohydrate ( Surya Pharmaceuticals Ltd, Himachal pradesh), Croscarmellose sodium(Sun Pharmaceuticals Inds Ltd, Gujarath), Pregelatinized starch (Bliss GVS Pharma Ltd,Mumbai), Sodium Lauryl Sulphate (Neuland Laboratories, Andhra Pradesh), Poloxamer 800 (Neuland Laboratories, Andhra Pradesh), Polysorbate(Neuland Laboratories, Andhra Pradesh), Aerosil 200(Sd fine chemicals, Mumbai), MCC (Avicel 101) (Ozone International, Mumbai), Magnesium state(Rexer pharma private Ltd, cherlapally). Solubility studies of Irbesartan Weigh accurately 300mg (i.e. highest dose of Irbesartan) of Irbesartan (API) and transfer it in to 250ml flask containing media (0.1N HCl, 0.01N HCl, pH 3.0Citrate buffer, pH4.5 Acetate buffer, pH 6.8 Phosphate buffer) and the flask is subjected to sonication at 37°C for 1hr. The solution was filtered and supernatant solution is collected. From this solution 1ml is pipette out and it was diluted to 10ml with water, and the absorbance was checked at 220 nm for 3 times and the average value of the absorbance was taken for calculations to get concentration of drug. Method of preparation Sift Irbesartan, Lactose, Croscarmellose Sodium, Aerosil, Pregelatinized starch, through # 30 mesh and dissolve different surfactant as per table in water. Transfer material into rapid mixing granulator and granulated by mixing with surfactant solution and dried in FBD at 55-60ºC and checking to LOD
