FORMULATION DESIGN AND EVALUATION OF MUCOADHESIVE BUCCAL TABLETS OF NITROGLYCERIN
Keywords:Nitroglycerin, Swelling index, In vitro drug release Mucoadhesion, Ex vivopermeation
Objective: The main objective of present investigation is to prolong drug action and enhance bioavailability.
Methods: The tablets were prepared using Carbopol 934 in varying concentration with secondary polymers like HPMC K4M, HPMC K15M and sodium alginate by direct compression method. The compatibility studies like TLC and FTIR spectroscopy were carried out. The tablets were evaluated for hardness, thickness, weight variation, friability and drug content and concluded that all these parameters were in acceptable range of pharmacopoeial specification. The tablets were furtherevaluated for their mucoadhesive characteristics such as surface pH, swelling index, ex vivo residence time, mucoadhesive strength, ex vivo permeation,in vitro drug release and also for the effect of Carbopol concentration on mucoadhesive parameters.
Results: The surface pH of the tablet was 6.48 to 6.75 which fall in the range of salivary pH and all the tablet of batch C containing sodium alginate as secondary polymer showed ex vivo residence time of 10 to 12.30 hrs indicated good mucoadhesive capacity of tablet. The buccal tablets showed good swelling up to 8 hrs maintaining the integrity of polymers. The formulation (C3) showed better control of drug release and able to release entire amount of drug in 12 hrs than the other formulations. All the formulations of batch C & A except A1 followed zero order kinetics and all other formulations of batch B and A1 formulation followed Hixson-Crowell model.The â€˜n' value of all the formulations was found to be more than 0.89 indicating that the drug release followed Super case II transport type of release mechanism due to the erosion of the polymer. All the tablets showed good mucoadhesive strength in the range of 21.87 to 26.26.Ex vivopermeation studies of the optimized formulation C3 revealed that percent drug permeated through sheep buccal mucosa was 38.294 % for 8 hrs. The slopes of the basic in vitro data suggests that drug permeates across the membrane but slowly as the mucosa offers barrier to the transportation of the drug.
Conclusion: Hence Carbopol 934 and Sodium alginate polymers can be used to prepare mucoadhesive buccal tablets of nitroglycerin having prolonged therapeutic effect with enhanced bioavailability.
Prasanth VV, Sirisha M, Sam T Mathew, RinkuMathapan. Buccal tablet as Mucoadhesive drug delivery:an over view. J Pharm Res 2011;4(3):706-09.
Shivam T, Nishiprakash J. Buccal Control Drug Delivery System:A Review. Int J of Pharm Sci and Res 2011;2(1):27-38.
Pankil Gandhi A, Dr. Patel MR,Dr. Patel KR, Dr. Patel NM. A review article on mucoadhesive buccal drug delivery system. Int J of Pharm Res and Development 2011;3(5):159-73.
Patil SB, Murthy RSR, Mahajan HS, Wagh RD, Gattani SG. Mucoadhesive polymers:means of improving drug delivery. J Pharm Times 2006;38(4):25-8.
Mythri G, Kavitha K, Rupesh Kumar M, Jagadeesh Singh Sd. Novel Mucoadhesive Polymers â€“A Review. J of Applied Pharm Sci 2011;1(8):37-42.
Borgaonkar PA, Virsen TG, Hariprasanna RC, Najmuddin M. Formulation and in vitro evaluation of buccal tablets of loratadine for effective treatment of allergy. Int J of Res in Pharmacy and Chemistry 2011;1(3):551-59.
Leon Lachaman, Herbert A, Liberman. The theory and practice of Industrial Pharmacy. 3rdedition;1987:455.
Banker GS, Rhodes CT. Modern pharmaceutics. 2nd ed. vol. 40. Newyork:Marcel Dekker Inc;1990;40:416-417.
Berner B, Cowles VE. Case studies in swelling polymeric gastric retentive tablets. J Expert Opin Drug Deliv 2006;3(4):541-8.
Gupta A, Garg S, Khar RK. Measurement of bioadhesive strength of mucoadhesive buccal tablets:Design of an in vitro assembly. J Indian Drug 1993;30:152-5.
AgaiahGoud B, Kumara Swamy S, Praveen Kumar V. Formulation and evaluation of bioadhesivebuccal tablets of simvastatin. J of Adv Pharm Sci 2011;1(1):29-38.
Satishbabu BK, Srinivasan BP. Preparation and evaluation of buccoadhesive films of atenolol. Indian J Pharm Sci 2008;70(2):175-9.
Patel VM,PrajapatiBG, Patel HV, Patel KM. Mucoadhesive bilayer tablets of Propranolol Hydrochloride. J AAPS Pharm Sci Tech 2007;8(3):E77.
Bhanja SB, Ellaiah P, Martha SK, Kar RK, Panigrahi BB. Buccoadhesive Drug Delivery System of Captopril:Formulation and In Vitro Evaluation. J Pharm Res 2010;3(2):335-40.
Mumtaz AM, Ch'ng HS. Design of a dissolution apparatus suitable for in situ release study of triamcinolone acetonide from bioadhesivebuccal tablets. Int J Pharm 1995;121:129-39.
Rao YM, Vishnu YV, Chandrasekhar K, Ramesh G. Development of Mucoadhesive patches for buccal administration of Carvedilol. J Current Drug Delivery 2007; 4:27-39.