FORMULATION AND EVALUATION OF MELOXICAM LIQUISOLID COMPACT
Keywords:
Meloxicam, Liquisolid compacts, PEG 400, Dissolution rateAbstract
Objective: The aim of the present research was to improve dissolution of poorly soluble meloxicam a BCS (Biopharmaceutical Classification System) Class-II drug by utilizing liquisolid technique. Different liquisolid (LS) compacts were prepared using a mathematical model to calculate the required quantities of powder and liquid ingredients to produce acceptably flow able and compressible admixture.
Methods: Liquisolid compact was prepared from; microcrystalline cellulose (Avicel PH 102) as carrier, colloidal silicon dioxide (Aerosil 200) and silica (cab-O-sil) as coating material, sodium starch glycol ate and cross povidon as super disintegrants, PVP-K25 and HPMC E5 as additives to increase loading capacity, polyethylene glycol 400, propylene glycol and tween 80 as liquid vehicles. The ratio of carrier to coating material was kept constant in all formulations at 25:1, this ratio was chosen after testing the ratios 5:1, 10:1, 15:1, 20:1 and 25:1. The ratio 25;1 give optimal results relative to other ratios.
The prepared LS compacts were evaluated for their tab letting properties. Fourier transform infrared (FTIR) analysis, differential scanning calorimetry (DSC), scanning electron microscope (SEM) and X-ray powder diffraction (XRPD) were performed.
Results: The tab letting properties of the liquisolid compacts was within the acceptable limits. The drug release rates of the selected formulas (LS-3, LS-3A, LS-3AP and LS-3AH) of prepared liquisolid compacts were distinctly higher as compared to directly compressed tablets, and marketed tablets.
The DSC, XRPD and SEM were suggested loss of meloxicam crystallinity upon liquisolid preparation indicating that even though the drug existed in a solid dosage form, it is held within the powder substrate in a solubilized, almost molecularly dispersed state, which may be contributed to the enhanced drug dissolution properties.
The FTIR spectra showed disappearance of the characteristic absorption band of meloxicam (3290 cm-1) in liquidsolid formulation which might be attributed to the formation of hydrogen bonding between the drug and liquid vehicle; this resulted in drug dissolution enhancement.
Conclusion: From this study it concludes that the LS technique is an effective approach to enhance the dissolution rate of meloxicam.
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References
Kapsi SG, Ayres. JW-Processing factors in development of solid solution formulation of itraconazole for enhancement of drug dissolution and bioavailability. Int J Pharm 2001;229:193—203.
Venkat B Yadav, Adhikrao V Yadav. Enhancement of solubility and dissolution rate of BCS class ii pharmaceuticals by nonaqueous granulation technique. IJPRD 2010;1:1-12.
DM Brahmankar, Sunil B Jaiswal. Methods for enhancement of bioavaibility Biopharmaceutics and pharmacokinetics Vallabh Prakhasan Delhi; 297-301.
Spireas S, Bolton M, Liquisolid systems and methods of preparing same. US Patent 1999;5:968, 550.
Spireas S. Liquisolid systems and methods of preparing same u s patent 2002;6:423, 339.
Baby DA, Saroj S, Sabitha M. Mechanisam of solubility of liquisolid formulation in nonvolatile solvent: a review. Int J Pharm Sci 2012;4 suppl 3:710-15.
Vittal G, Deveswaran R, Bharath S, Basavaraj BV, Madhavan V. Formulation and characterization of ketoprofen liquisolid compacts by Box-Behnken design. Int J Pharm Investigation 2012;2(3):150-6.
Shivhare Umesh D, Pardhni Dinesh M. Effect of non-volatile solvent on dissolution profile of carvedilol liquisolid compact. Res J Pharm Technol 2011;4(4):537-44.
Abdou M. In: HM Abdou (Ed.). Dissolution, bioavailability and bioequivalence. Easton, Mack Pub Co, PA; 1989. p. 53-72.
Fahmy RH, Kassem MA, Enhancement of famotidine dissolution rate through liquisolid tablet formulation: In Vitro and in vivo evaluation. Eur J Pharm Biopharm 2008;69(3):993-1003.
Qureshi S. Tablet testing in encyclopedia of pharmaceutical technology.3rd ed, Informa Healthcare USA, Inc 2007;3:3707-16.
Nicholas G. Sustained released dosage forms in Lachman L, Lieberman H and Kanig J, The Theory and practice of industrial pharmacy.3rd ed Lea & Febiger; 1986. p. 430-56.
Pratlkkumar A Patel, Vandana B Patravale. Commercial telmisartan tablets: acomparative evaluation with innovator brand micardis. Int J Pharm Sci Res 2010;1(8):282-92.
Javadzadeh Y, Asnaashari S, Nokhodchi A. Liquisolid technique as a tool for enhancement of poorly water soluble drugs and evaluation of their physicochemical properties. Acta Pharm Sin B 2007;57(1):99-109.
El-Gizawy SA. Effect of formulation additives in the dissolution of meloxicam from liquisolid tablets. Egypt J Biomed Sci 2007;25:143-58.
Liberman HA, Ringer MM, Banker GS. Pharmaceutical Dosage Form: Disperse system, 2ndedn, Marcel Dekker Inc, New York; 2005;1:216-8.
Rajendarn A, Basu K. Crystal modification of dipyridamole using different solvents and crystallization conditions. Int J Pharm 2006;321:27–34.
Sathesh PR, Sathya CV, Juturu Thimmasetty. Solubility of meloxicam in mixed solvent systems. Ethiop Pharm J 2007;25:23-8.
Rowe C, Sheskey J, Weller J. Handbook of Pharmaceutical Excipients. Fourth ed, Amer. Pharma Asso, Chicago; 2003. p. 108–11, 161–4, 355–61, 407–66.
Fahim JS, Sachin LT, Umesh BK. Design and development of liquisolid compact of candesartan cilexetil to enhance dissolution. J Pharm Res 2013;7:381-8.
Hassan MA, El-Saghir HM. Enhancement of dissolution and the anti-inflammatory effect of nimesulide using liquisolid compact for oral application. Bull Pharm Sci 2011;34(1):1-8.
Chuahan Pankaj V, Patel Hiren K, Bhavana A Patel, Kunal N Patel, Poras A Patel. Liquisolid technique for enhancement of dissolution rate of ibuprofen. Int J Pharm Res Sci 2012;1(2):268-80.
Gubbi S, Jarag R. Formulation and characterization of
atorvastatin calcium liquisolid compacts. Asian J
Pharm Sci 2010; 5(2):50-60.
Saleem MA, Sumanji Bala. Formulation and evaluation of meloxicam solid dispersion incorporated topical gel. Int J Pharm Biosci 2010;1:3.
Sayyad FJ, Tulsankar SL, Kolap UB. Design and development of liquisolid compact of candesartan cilexetil to enhance dissolution. J Pharm Res 2013;7(5):381-8.
McCauley JA, Brittain HG. Thermal methods of analysis, in: HG Brittain (ed.), Physical characterization of pharmaceutical solids. Drugs Pharm Sci 1995;70:223-50.
Mura P, Faucci MT, Parrini PL. Effect of grinding with microcrystalline cellulose and cyclodextrins on the ketoprofen physicochemical properties. Drug Dev Ind Pharm 2001;27(2):119-28.
Bhaumik B patel. Formulation and evaluation of liquisolid compact. An overview. Der pharm let; 2011.
Kapure VJ, Pande VV, Deshmukh PK. Dissolution enhancement of rousvastatin calcium by liquisolid compact technique. J Pharm 2013. p. 1-9.
Yala P, Srinivasan S, Mahalingan K, Alladi S, Zalaki S. Solubility
enhancement of a model etricoxib drug using liquisolid compacts. Int J Bio-Pharm Res 2012;3(4):577-85.
Kapoor D, Sharma S, Patel M, Vyas RB, Chaitali Lad. Solubility
enhancement and dissolution improvement-liquisolid technique. J Drug Delivery Ther 2013;3(6):155-61.
Dinesh M, Umesh D, Vijay B, Kishor P. Liquisolid technique for enhancement of dissolution properties of carvedilol. Scholars Research Library. Der Pharm Lett 2010;2(5):412-27.
Martin A, Bustamante P, Chun A. "Micromeritics" in Martin's Physical Pharmacy and Pharmaceutical Sciences, P J Sinko, Ed Lippincott Williams & Wilkins, Philadelphia, Pa, USA, 5th edition; 2006. p. 533-60.
Shangraw R. Compressed tablets by direct compression in pharmaceutical dosage forms: Tablets. H A Lieberman, L Lachman, and J B Schwartz, Eds, Marcel Dekker, New York: NY, USA, 2nd edition; 1989. p. 195-245.
Pan N, Chen H, Chen L. Enhancement of dissolution and bioavailability of piroxicam in solid dispersion systems. Drug Dev Ind Pharm 2000;26:989-94.
Indian pharmacopoeia, Gov of India, Ministry of health and family welfare, Delhi: controller of India: New Delhi, India; 2007. p. 662-3, 1471-2.
Patel K, Upadhyay H. An evaluation of microcrystalline cellulose and lactose excipients using an instrumented single station tablet press. Int J Pharm 1994;110:203-10.
Petrovick R, Jacob M. Influence of adjuvents on the in vitro dissolution of hydrochlorothiazide from hard gelatin capsules. Int J Pharm 1991;76:49-53.
Manoj S, Kumbhar, Priti S Mujgond, Naresh H Choudhary, Meera C Singh. Enhancement of solubility and dissolution rate of escitalopram oxalate by liquisolid compact technology. Int J Pharm Chem Sci 2013;2(2):730-7.
Gubbi S, Jarag R. Liquisolid technique for enhancement of dissolution properties of bromhexine hydrochloride. Res J Pharm Technol 2009;2(2):382-6.
Noyes AA, Whitney WR. The Rate of solution of solid substances in their own solutions. J Am Chem Soc 1997;19:930-4.
Seedher N, Bhatia S. Solubility enhancement of Cox-2 inhibitors using various solvent systems. Am Association Pharm Sci 2003;4(3):1-4.
Amrit B Karmarkar. Effect of Ceolus K G-802 on the dissolution rate of fenofibrate liquisolid tablets: preformulation and formulation development studies. Drug Discoveries Ther 2010;4(6);493-8.
Petrovick PR, Jacob M, Gaudy D, Bassani VL. Influence of adjuvents on the in vitro dissolution of hydrochlorothiazide from hard gelatin capsules. Int J Pharm 1994;110(3):203-10.
Sabale M, Grampurohit D, Gaikawad D, Gadhave V. Liquisolid technique for enhancement of dissolution properties of fenofibrate. Int J Pharm Sci Res 2012;3(5):1481-6.
Nagabandi V, Tadikonda R. Formulation development and evaluation of liquisolid systems to improve the dissolution rate of ketoprofen. Int J Biomed Res 2011;2(10):530-41.
Indrajeet D Gonjara, Amrit B Karmarkar, Avinash H Hosmania. Evaluation of in vitro dissolution profile comparison methods of sustained release tramadol hydrochloride liquisolid compact formulations with marketed sustained release tablets. Digest J Nanomatericals Biostructures 2009;4(4):651-61.
Vajir S. Enhancement of dissolution rate of poorly water-soluble diclofenac sodium by liquisolid technique. Int J Pharm Chem Sci 2012;1(3):989-1000.
Gandhi KJ, Sawant AR, Nagpure SV, Deshmane SV, Biyani KR. Formulation development, charecterization and evaluation of liquisolid tablet containing piogliltazone HC1. Int J Pharm 2013;3(1):122-30.
Cairns D. Chemistry of acids and bases, in: D Cairns (Ed.), Essentials of Pharmaceutical Chemistry.2nd ed., Pharmaceutical Press: London; 2003. p. 1–27.