ALGINATE BASED GASTRO-RETENTIVE RAFT FORMING TABLETS FOR ENHANCED BIOAVAILABILITY OF TINIDAZOLE
Keywords:Tinidazole, Raft, Sodium alginate, HPMC, Solid dispersion
Objective: Tinidazole, a nitroimidazole derivative is having low aqueous solubility which is a major barrier for systemic drug absorption. The aim of the present research was to develop gastro retentive raft forming tablets of tinidazole to achieve prolonged gastric residence time and thus higher bioavailability.
Methods: Solid dispersion of tinidazole was prepared by kneading method by using methanol and polyvinylpyrrolidone (PVP). Different concentration of sodium alginate and hydroxypropyl methylcellulose (HPMC) was used to formulate a suitable raft forming tablets and then evaluated for drug content, floating lag time, raft strength, raft volume, raft weight, drug release and release kinetics.
Results: Fourier transform infra-red (FT-IR) study confirms compatibility between drug and polymer. The floating lag time was found in the range of 40Â±4 to 60Â±5 s for all the formulation. Raft strength for all the formulations was within the range from 3.03Â±0.12 to 5.92Â±0.06 g. The raft volume for all the formulation was found within the range of 7.37Â±1.86 to 9.84Â±2.76 ml. Raft weight was measured after completion of raft formation for each formulation and was found in the range of 5.21Â±1.17 to 7.88Â±1.95 g. In vitro dissolution was carried up to 8 h and percentage of drug release was found to vary between 79.71Â±2.18 to 94.32Â±1.79 %.
Conclusion: It can be concluded that the combination of solid dispersion and raft formation increases the bioavailability of tinidazole in tablet formulation.
Nayak AK, Maji R, Das B. Gastroretentive drug delivery systems: a review. Asian J Pharm Clin Res 2010;3:2-10.
Mathur P, Saroha K, Syan N, Verma S, Nanda S, Valecha V. An overview on recent advancements and developments in gastro retentive buoyant drug delivery system. Der Pharm Sin 2011;2:161-9.
Mudie DM, Amidon GL, Amidon GE. Physiological parameters for oral delivery and in vitro testing. Mol Pharm 2010;7:1388â€“405.
Nayak AK, Malakar J, Sen KK. Gastroretentive drug delivery technologies: current approaches and future potential. J Pharm Edu Res 2010;1:1â€“12.
Govikari KR, Praveen KM, Rajendraprasad M, Veerareddy PR. Development and in vivo evaluation of gastro retentive delivery systems for cefuroxime axetil. Saudi Pharm J 2013;21:53â€“9.
Juan T, Jean-Yves LH, Phillipe M. Narrow therapeutic index drugs: a clinical pharmacological consideration to flecainide. Eur J Clin Pharmacol 2015;71:549â€“67.
Ajay V, Senthilnathan B, Ravichandiran V. A review article on different types of floating drug delivery systems. Int J Pharm Pharm Sci 2012;4:45-50.
Mandel KG, Daggy BP, Brodie DA, Jacoby HI. Alginate-raft formulations in the treatment of heartburn and acid reflux. Aliment Pharmacol Ther 2000;14:669-90.
Mosab A. Approaches to achieve an oral controlled release drug delivery system using polymers: a recent review. Int J Pharm Pharm Sci 2015;7:16-21.
Fabregas J, Claramunt J, Cucala J. In vitro testing of an antacid formulation with a prolonged gastric residence time (Almagate Flot-Coat). Drug Dev Ind Pharm 1994;20:1199-212.
Washington N, Greaves JL, Wilson CG. Effect of time of dosing relative to a meal on the raft formation anti-reflux agent. J Pharm Pharmacol 1990;42:50-3.
Fung HB, Doan TL. Tinidazole: a nitroimidazole antiprotozoal agent. Clin Ther 2005;27:1859-84.
Timothy BG, David RH. Treatment of giardiasis. Clin Microbiol Rev 2001;14:114â€“28.
Ripal G, Hari KA, Ashwin P, Ashim KM. Ocular drug delivery. AAPS J 2010;12:348â€“60.
Swati S, George M, Lincy J. Improvement in solubility of poorly water-soluble drugs by solid dispersion. Int J Pharm Investig 2012;2:12â€“7.
Aejaz A, Azmail K, Sanaullah S, Mohsin AA. Formulation and in vitro evaluation of aceclofenac solid dispersion incorporated gels. Int J Appl Pharm 2010;2:7-12.
Ladan AN, Gurinder S, Gaurav S, Kimia FK. Solid dispersion: methods and polymers to increase the solubility of poorly soluble drugs. J Appl Pharm Sci 2012;2:170-5.
Sweta KS, Vijay S, Kamla P. Formulation and evaluation of taste masked rapid release tablets of sumatriptan succinate. Int J Pharm Pharm Sci 2012;4:168-74.
Bajpai M, Singh DCP, Bhattacharya A, Singh A. Design and in vitro evaluation of compression-coated pulsatile release tablets of losartan potassium. Indian J Pharm Sci 2012;74:101â€“6.
Mafalda CS, JoÃ£o AL, Ana VC, Sandra OS, Helena RA, Paulo CC. Determination of flow properties of pharmaceutical powders by near infrared spectroscopy. J Pharm Biomed Anal 2010;52:484-92.
Ashwini R, Bushetti SS, Archana Giri. Design and evaluation of compression coated formulations for an anti-inflammatory drug based on modified okra mucilage. J Appl Pharm Sci 2012;2:238-45.
Poluri K, Suvarnala S, Puttugunta S, Govada KB, Pinnamraju DN. Formulation development and evaluation of fast disintegrating tablets of lamotrigine using the liquid-solid technique. Int J Pharm Investig 2014;4:207â€“14.
Harshal AP, Rachana D. Development and evaluation of gastro retentive floating tablets of an antidepressant drug by thermoplastic granulation technique. Beni-Seuf Univ J Appl Sci 2014;3:122-32.
Dettmar PW, Hampson FC, Farndale A, Strugala V, Sykes J, Jolliffe IG. Alginate rafts and their characterisation. Int J Pharm 2005;294:137â€“47.
Basak SC, Jayakumar RBM, Lucas MKP. Formulation and release behaviour of sustained release ambroxol hydrochloride HPMC matrix tablet. Indian J Pharm Sci 2006;68:594-8.
Suvakanta D, Padala NM, Lilakanta N, Prasanta C. Kinetic modelling on drug release from controlled drug delivery systems. Acta Poloniae Pharm Drug Res 2010;67:217-23.