Abstract
Aim: In the present study was to enhance the solubility of Tadalafil (TDF) by forming inclusion complexes with β-cyclodextrin (βCD) and further to enhance its dissolution rate by formulating orally disintegrating tablet (ODT) by direct compression technique.
Objectives: To performthe phase solubility studies, for to determine the ratio of drug: carrier ratio in the formation of complexes. Physico-chemicalcharacterizationof complexes byDSC and X-ray diffraction studies. To check the superiority of selected superdisintegrants [sodium starch glycolate (SSG), croscarmellose sodium (CCS), crospovidone (CPV)] in enhancing the dissolution rate of TDF. To fasten the onset of action and thereby increasing TDF’s bioavailability in comparison to its conventional tablets.
Methods: Standard calibration curve of TDF in pH 6.8 phosphate buffer was constructed by spectrophotometric method, drug-excipient compatibility was checked by FT-IR studies. All the Formulations were evaluated for pre- & post-compression studies. Accelerated stability studies up to 3 months were conducted for the optimized formulation, as per ICH guidelines.
Results and Discussions: polymers used in the study are compatible with TDF. Pre- & post- compression parameters were within the acceptable limits for all formulations. In vitro dissolution kinetic studies indicate the release of TDF from ODT increases with the increased concentration of superdisintegrants. The order of superdisintegrants in enhancing the dissolution rate of TDF is CPV>SSG>CCS. Formulation F6, had the highest dissolution efficiency at 5 min (DE5=39.55 %); first order dissolution rate constant (K1 =0.1052 min-1) with a regression coefficient (r2=0. 9844) and lesser time for 50% of drug release (t50=4 min), was considered as the optimal ODT. It passed the test for stability as per ICH guidelines.
Conclusion: The optimized TDF ODT with its 1:4 βCD complex was formulated by the direct compression technique, with 6% w/w CPV as superdisintegrant, which will fasten the onset of action and enhances the bioavailability of TDF in comparison to its conventional tablets.
References
Sharma S and G D Gupta. Formulation and characterization of fast dissolving tablet of Promethazine Theoclate. Asian J. Pharm. 2008; 2(1): 70-72.
Siddiqui NM, Garima G and Sharma PK. Fast dissolving tablets: preparation, characterization and evaluation. International Journal of Pharmaceutical Sciences Review and Research. 2010; 4(2): 87-96.
Velmurugan S and Vinushitha S Oral Disintegrating Tablets: An Overview. International Journal of Chemical and Pharmaceutical Sciences. 2010; 1(2): 1-12.
Guyot-Hermann A. M. The disintegration and disintegrating agent; S.T.P. Pharmaceutical Science: 1992, 2(6): 445-62.
P. Colombo, C. Caramella, U. Conte, A. La Manna, A. M. Guyot-Hermann, and J. Ringard. Disintegrating force and tablet properties. Drug Dev. Ind. Pharm 7: 135-153.
Hirani J. J., Rathod D. A., Vadalia K. R. Orally Disintegrating Tablet: A Review. Trop. J. Pharm. Res. 2009; 8(2): 161-72.
Hussar DA. New drugs of 2003. J Am Pharm Assoc. 2004; 44(2): 168-206.[View in PubMed]
Porst H, Padma-Nathan H, Giuliano F, Anglin G, Varanese L, Rosen R. Efficacy of tadalafil for the treatment of erectile dysfunction at 24 and 36 hours after dosing: a randomized controlled trial. Urology. 2003; 62(1): 121-126.[View in PubMed]
Padma-Nathan H. Efficacy and tolerability of tadalafil, a novel phosphodiesterase 5 inhibitors, in treatment of erectile dysfunction. Am J Cardiol. 2003; 92(9A): 19M-25M.[View in PubMed]
MalaniKetanAshokbhai, Dr.TejashSeresiya. International Journal of Pharma Sciences and Research. 2015; 6(6):991-1001.
Higuchi T, Connors KA.Phase-solubility techniques Adv Anal Chem Instr. 1965; 4: 117-122.
Hitendra S Mahajan, Swapnil R Bhagirath. Indian Journal of Novel Drug Delivery.2014, 6(1): 1-9.
Banker GS, Anderson NR, Lachman L, Liberman HA. The Theory and Practice of Industrial Pharmacy, 3rd ed. Mumbai: Varghese Publishing House; 1987, p: 293-4.
European Pharmacopeia 6th ed. Strasburg, France; 2007, p: 2435.
TanselComoglu, AysegulDogan, SelcukComoglu, and NursabahBasci. Formulation and evaluation of diclofenac potassium fast-disintegrating tablets and their clinical application in migraine patients.Drug Dev. Ind. Pharm. 2011; 37(3): 260-7.
Gautam Singhvi, Mahaveer Singh. Review: In vitro Drug Release Characterization Models. International Journal of Pharmaceutical Studies and Research.2011; 2(1): 77-84.
D.M. Brahmankar; Sunil. B. Jaiswal. Biopharmaceutics and Pharmacokinetics: A Treatise. 2nd ed. New Delhi: Vallabh Prakashan; 2009, p: 254-55.
Higuchi T, Connors KA. Phase solubility techniques, in: C.N. Reilly (Ed.), Advances in Analytical and Chemistry Instrumentation, vol. 4, Wiley Interscience, New York, 1965; pp. 117-212.
Loftsson T, Masson M, Brewster ME. Self-association of cyclodextrin and cyclodextrin complexes, J Pharm Sci. 2004; 93: 1091-99.[View in PubMed]
Mura P. Adragna E, Rabasco AM, Moyano JR. Perez-Mart?`nez JI, Arias MJ, Gines JM. Effects of the host cavity size and the preparation method on the physicochemical properties of ibuprofen-cyclodextrin systems. Drug Dev Ind Pharm. 1999; 25: 279-287.[View in PubMed]
Wasfy M. Obeidat and Al-Sayed A. Sallam. Evaluation of Tadalafil Nanosuspensions and Their PEG Solid Dispersion Matrices for Enhancing Its Dissolution Properties. AAPS-PharmSciTech.2014; 15(2): 364–374.
X, Joshi AA. Starches: A Versatile Source. Pharma Form. Qual. 2004; 6 (3): 48-50.
Rakesh Pahwa and Nisha Gupta. 2011; Vol. 2(11): 2767-80.
This work is licensed under a Creative Commons Attribution-NoDerivatives 4.0 International License.
Copyright (c) 2020 Array