FORMULATION AND IN VITRO EVALUATION OF ORLISTAT ORODISPERSIBLE TABLETS FOR ENHANCEMENT OF DISSOLUTION RATE
Keywords:Direct compression, Melt granulation method, Orlistat, Orodispersible tablets, Polyethylene glycol
Objective: The aim of the present study was to formulate the oro dispersible tablets (ODTs) of Orlistat (OST) by direct compression technique using melt granulation method.
Methods: Super disintegrants were used for the preparation of ODTs namely Crospovidone (CP), Croscarmellose sodium (CCS), Sodium starch glycolate (SSG). The powder mixture was subjected to pre compression evaluation like FTIR, Micromeritic, solubility studies and post-compression evaluation like friability, hardness, wetting time, dispersion time, disintegration time and in vitro dissolution rate.
Results: FTIR studies confirmed that there was no chemical interaction between the drug and excipients. Micromeritic studies revealed that the powder blend has good flow ability. The results of hardness and friability complied with the official standards. The solid dispersions (SDs) prepared in OST to PEG 6000 ratio of 1:2 were showed good solubility than other SDs and it was selected for formulation development. It was evident from the results that the increase in super disintegrants concentration decreases the wetting, dispersion and disintegration times and CP showed the best results than other super disintegrating agents.
Conclusion: The F4 formulation showed optimum drug release of 98.99 % at the end of 15 min when compared to the other formulations; it might be due to the presence of CP.
Keywords: Direct compression, Melt granulation method, Orlistat, Orodispersible tablets, Polyethylene glycol.Â
Wadhwani AR, Prabhu NB, Nandkarni MA, Amin PD. Patient compliant dosage form for roxithromycin. Indian J Pharm Sci 2004;66:670-3.
Bhoyar PK, Biyani DM, Umekar MJ. Formulation and characterization of the patient-friendly dosage form of ondansetron hydrochloride. J Young Pharm 2010;2:240-6.
Gohel MC, Jogani PD. A review of co-processed directly compressible excipients. J Pharm Pharm Sci 2005;8:76-93.
Banker GS, Anderson NRI. In: Lachman L, Liberman HA, Kanig JL, Editors. The theory and practice of industrial pharmacy. Mumbai: Varghese Publishing House; 1987. p. 293-9.
Malladi M, Jukanti R, Nair R, Wagh S, Padakanti HS, Mateti A. Design and evaluation of taste masked dextromethorphan hydrobromide oral disintegrating tablets. Acta Pharm 2010;60:267-80.
Abdelbary G, Prinderre P, Couani C, Taochim J, Reynier JP, Piccerelle P. The preparation of orally disintegrating tablets using a hydrophilic waxy binder. Int J Pharm 2004;278:423-33.
Fu Y, Yang S, Jeong SH, Kimura S, Park K. Orally fast disintegrating tablets: Developments, technologies, taste-masking and clinical studies. Crit Rev Ther Drug Carrier Syst 2004;2:433-76.
Badjugar BP, Mundada AS. The technologies used for developing orally disintegrating tablets: a review. Acta Pharm 2011;6:117-39.
Pabari RM, Ramtoola Z. Effect of a disintegration mechanism on wetting, water absorption, and disintegration time of orodispersible tablets. J Young Pharm 2012;4:15-63.
Klyankar P, Panzade P, Lahoti S. Formulation and optimization of orodispersible tablets of Qutiapine fumarate by a sublimation method. Indian J Pharm Sci 2015;77:26-73.
Subramanian S, Sankar V, Manakandan AA, Ismail S, Andhuvan G. Formulation and evaluation of Cetirizine dihydrochloride orodispersible tablet. Pak J Pharm Sci 2010;23:232-5.
Sarfraz RM, Khan HU, Mahmood A, Ahmad M, Maheen S, Sher M. Formulation and evaluation of mouth disintegrating tablets of atenolol and atorvastatin. Indian J Pharm Sci 2015;77:83-90.
Shukla D, Subhashis C, Sanjay S, Brahmeshwar M. Mouth dissolving tablets I: an overview of formulation technology. Sci Pharm 2009;76:309-26.
Pabari RM, Jamil A, Kelly JG, Ramtoola Z. Fast disintegrating crystalline solid dispersions of simvastatin for incorporation into orodispersible tablets. Int J Pharm Invest 2014;4:51-9.
Masareddy R, Kokate A, Shah V. Development of orodispersible Tizanidine HCl tablets using spray dried excipient bases. Indian J Pharm Sci 2011;73:392-6.
Prakash V, Maan S, Deepika, Yadav SK, Hemalata, Jogpal V. Fast disintegrating tablets: opportunity in drug delivery system. J Adv Pharm Technol Res 2011;2:223-35.
Swamy PV, Divate SP, Shirsand SB, Rajendra P. Preparation and evaluation of orodispersible tablets of Pheniramine maleate by the effervescent method. Indian J Pharm Sci 2009;71:151-4.
Shirsand SB, Suresh S, Jodhan LS, Swamy PV. Formulation design and optimization of fats disintegrating Lorazepam tablets by the effervescent method. Indian J Pharm Sci 2010;72:431-6.
Jcob S, Shirwaikar A, Nair A. Preparation, and evaluation of fast-disintegrating effervescent tablets of glibenclamide. Drug Dev Ind Pharm 2009;35:321-8.
Zidan AS, Aljaeid BM, Mokhtar M, Shehata TM. Taste-masked orodispersible tablets of cyclosporine self-nanoemulsion lyophilized with dry silica. Pharm Dev Technol 2015;20:652-61.
Ahmed IS, Shamma RN, Shoukri RA. Development and optimization of lyophilized orally disintegrating tablets using factorial design. Pharm Dev Technol 2013;18:935-43.
Hitendra SM, Vilas SJ. Formulation and evaluation of mouth dissolving tablets of azithromycin dihydrate and chloroquine by melt granulation. Int J PharmTech Res 2014:6:1616-23.
Sree GPB, Siva SN, Swetha M, Gupta VRM, Devanna N, Madiha S. Formulation and evaluation of orodispersible tablets of levocetirizine by melt granulation technology. Der Pharm Lett 2013;5:107-15.
Abdul M, Purushotham RK. Novel chewable tablet-in-tablet dosage form of Orlistat and Venlafaxine hydrochloride: development and evaluation. J Appl Pharm Sci 2015;5:91-7.
Rakesh P, Mona P, Prabodh CS, Dhirender K, Sanju N. Orally disintegrating tablets-friendly to pediatrics and geriatrics. Arch Appl Sci Res 2010;2:35-48.
Shailaja T, Latha K, Alkabab AM, Sasibhushan P, Uhumwangho MU. Formulation and evaluation of orodispersible tablets of metoprolol tartrate with natural and synthetic super disintegrants. Int J Pharm Pharm Sci 2012;4:148-52.
Rafah KM, Laith HS, Muyad AS. Formulation and in-vitro evaluation of orodispersible tablet. Int J Pharm Sci Res 2015;6:689-96.
Karan M, Gurpreet A, Inderbir S, Sandeep A. Lallemantia reylenne seeds as super disintegrant: Formulation and evaluation of nimesulide orodispersible Tablets. Int J Pharm Invest 2011;1:192-8.
Solanki SS, Dahima R. Formulation, and evaluation of aceclofenac mouth dissolving tablets. J Adv Pharm Technol Res 2011;2:128-31.
Chandira RM, Venkataeswarlu BS, Kumudhavalli MV. Formulation and evaluation of mouth dissolving tablets of the etoricoxib. Pak J Pharm Sci 2010;23:178-81.
Nilesh J, Suman M, Jitendra B, Surendra J. Effect of super disintegrants on the formulation of taste masked fast disintegrating ciprofloxacin tablets. Int Curr Pharm J 2012;1:62-7.
Kondo K, Niwa T, Ozeki Y, Ando M, Danjo K. Preparation and evaluation of orally rapidly disintegrating tablets containing taste-masked particles using one-step dry-coated tablets technology. Chem Pharm Bull 2011;59:1214-20.
Okuda Y, Irisawa Y, Okimoto K, Osawa T, Yamashita S. A new formulation for orally disintegrating tablets using a suspension spray-coating method. Int J Pharm 2009;382:80-7.
Zhi J, Melia AT, Eggers H, Joly R, Patel IH. Review of limited systemic absorption of orlistat, a lipase inhibitor, in healthy human volunteers. J Clin Pharmacol 1995;35:1103-8.
Mancini MC, Halpern A. Pharmacological treatment of obesity. Arq Bras Endocrinol Metabol 2006;50:377-89.
Padwal R, Li SK, Lau DC. Long-term pharmacotherapy for obesity and overweight. Cochrane Database of Systematic Rev 2004;3: CD004094.
Torgerson J, Hauptman J, Boldrin M, SjÃ¶strÃ¶m L. XENical in the preparation of diabetes in the obese subjects (XENDOS) study: a randomized study of orlistat as an adjunct to life style changes for the prevention of type 2 diabetes in obese patients. Diabetes Care 2004;27:155-61.
Elkhodairy KA, Hassan MA, Afifi SA. Formulation and optimization of orodispersible tablets of flutamide. Saudi Pharm J 2014;22:53-61.
Shah D, Shah Y, Rampradhan M. Development and evaluation of controlled release diltiazem hydrochloride microparticles using cross-linked poly (vinyl alcohol). Drug Dev Ind Pharm 1997;23:567-74.
Cooper J, Gunn C. Powder flow and compaction. In: Carter SJ. Editors. Tutorial Pharmacy. New Delhi: CBS Publishers and Distributors; 1986. p. 211-33.
Venkateswarlu K, Shanthi A. Formulation, and evaluation of glipizide matrix. IOSR J Pharm Biol Sci 2012;2:17-23.
Khan KA. The concept of dissolution efficiency. J Pharm Pharmacol 1975;27:48-9.
Tejvir K, Bhawandeep G, Sandeep K, Gupta GD. Mouth dissolving tablets: a novel app to drug delivery. Int J Curr Pharm Res 2011;3:1-7.
Venkateswarlu Kambham. In-vitro stability testing of syrup dosage form for hepatitis. Am J Phytomed Ther 2013;1:491-7.
Raymond CR, Paul JS, Marion EQ. Handbook of pharmaceutical excipients. 6th ed. London: Pharmaceutical press; 2009.
K Vijayabhaskar, Kambham Venkateswarlu, SB Thirumalesh Naik, R Kiran Jyothi, G Nethra Vani, KB Chandrasekhar. Preparation and in-vitro evaluation of ranitidine mucoadhesive microspheres for prolonged gastric retention. Br J Pharm Res 2016;10:1-12.
Thirumalesh Naik SB, Venkateswarlu Kambham, Chandrasekhar KB. Formulation and in-vitro evaluation of orodispersible tablets of olanzapine for the improvement of dissolution rate. J Chem Pharm Res 2016;8:177-81.
Thirumalesh Naik SB, Venkateswarlu Kambham, Chandrasekhar KB. Formulation and evaluation of Oxybutynin chloride extended release matrix tablets. Indo Am J Pharm Res 2016;6:4179-84.