Formulation and Evaluation of Orodispersible Tablets Containing Co-Crystals of Modafinil
Abstract
Background: Modafinil is a CNS stimulant used to treat Narcolepsy, sleepiness and other disorders related to sleep. It is a BCS class II drug having poor aqueous solubility.
Objective: This study was aimed to formulate and evaluate orodispersible tablets of containing co-crystals of Modafinil for the improvisation of critical attributes of the product such as dissolution rates, solubility and oral bioavailability.
Methods: Co-crystals were prepared by dry grinding method using Sodium acetate, Nicotinic acid, Benzoic acid, Urea and Succinic acetate as co-formers. Tablets were compressed by using direct compression method using SSG, Crospovidone, and Croscarmellose sodium as super disintegrants in different concentration.
Results: Pre-formulation studies were performed and evaluation of prepared co-crystals revealed that Co-crystals formulated with sodium acetate showed best results. The manufactured orodispersible tablets were evaluated for different parameters including weight variation, hardness, thickness, friability, drug content, In-vitro disintegration and In-vitro dissolution studies. Formulation F2 shows significant change in dissolution rate and also helped to increase the solubility of poorly water soluble drugs and both of them i.e. solubility and percentage of drug release are the key factors to exhibit the efficiency of the drug. Formulation of co-crystal with sodium acetate in 1:1 ratio showed highest drug content (97.97%), while Benzoic acid in ratio 1:2 showed least drug content (56.48%).
Conclusion: According to the result obtained, an orodispersible tablet containing co-crystals of modafinil enhances the dissolution rate, solubility and hence increases the therapeutic efficacy and could be considered convenient oral delivery systems to enhance the drug bioavailability.
Keywords: Co-crystal, Oro-dispersible, Sodium acetate, Narcolepsy, Sleepiness
Keywords:
Co-crystal, Oro-dispersible, Sodium acetate, Narcolepsy, SleepinessDOI
https://doi.org/10.22270/jddt.v12i5-S.5634References
Schultheiss N, Newman A. Pharmaceutical cocrystals and their physicochemical properties. Cryst Growth Des. 2009;9(6):2950-2967. doi:10.1021/cg900129f
Kuang W, Ji S, Wang X, Zhang J, Lan P. Relationship between crystal structures and physicochemical properties of lamotrigine cocrystal. Powder Technol. 2021;380:18-25. doi:10.1016/j.powtec.2020.11.039
Bolla G, Nangia A. Pharmaceutical cocrystals: Walking the talk. Chem Commun. 2016;52(54):8342-8360. doi:10.1039/c6cc02943d
Shan N, Perry ML, Weyna DR, Zaworotko MJ. Impact of pharmaceutical cocrystals: The effects on drug pharmacokinetics. Expert Opin Drug Metab Toxicol. 2014;10(9):1255-1271. doi:10.1517/17425255.2014.942281
Hickey MB, Peterson ML, Scoppettuolo LA, et al. Performance comparison of a co-crystal of carbamazepine with marketed product. Eur J Pharm Biopharm. 2007;67(1):112-119. doi:10.1016/j.ejpb.2006.12.016
Qiao N, Li M, Schlindwein W, Malek N, Davies A, Trappitt G. Pharmaceutical cocrystals: An overview. Int J Pharm. 2011;419(1-2):1-11. doi:10.1016/j.ijpharm.2011.07.037
Tomaszewska I, Karki S, Shur J, Price R, Fotaki N. Pharmaceutical characterisation and evaluation of cocrystals: Importance of in vitro dissolution conditions and type of coformer. Int J Pharm. 2013;453(2):380-388. doi:10.1016/j.ijpharm.2013.05.048
Gerrard P, Malcolm R. Mechanisms of modafinil: a review of current research. Neuropsychiatr Dis Treat. 2007;3(3):349–364.
Lindsay SE, Gudelsky GA, Heaton PC. Use of modafinil for the treatment of attention deficit/hyperactivity disorder. Ann Pharmacother. 2006;40(10):1829–1833.
Panzade P, Shendarkar G, Shaikh S, Rathi PB. Pharmaceutical Cocrystal of Piroxicam : Design , Formulation and Evaluation Pharmaceutical Cocrystal of Piroxicam : Design , Formulation and Evaluation. Tabriz Univ Med Sci. 2017;7(3):399-408. doi:10.15171/apb.2017.048
Mohan G, Kuriachan MA. Formulation and Evaluation of Orodispersible Tablet of Esomeprazole. 2018;(3).
Kiran NR, Palanichamy S, Rajesh M, et al. Formulation and Evaluation of Orodispersible Piroxicam Tablets. 2010;2(10):615-621.
Cocrystal F. Superior Solubility and Dissolution of Zaltoprofen via Pharmaceutical Cocrystals. 2019;16(3):310-316. doi:10.4274/tjps.galenos.2018.15013
Latif S, Abbas N, Hussain A, et al. Development of paracetamol-caffeine co-crystals to improve compressional, formulation and in vivo performance. Drug Dev Ind Pharm. 2018;44(7):1099-1108. doi:10.1080/03639045.2018.1435687
Shewale S, Shete AS, Doijad RC, Kadam SS, Patil VA, Yadav A V. Formulation and solid state characterization of nicotinamide-based co-crystals of fenofibrate. Indian J Pharm Sci. 2015;77(3):328-334. doi:10.4103/0250-474X.159669
Poonuru R, Cheruku R, Juluri P, et al. Original Article formulation and evaluation of orodispersible tablets of lamotrigineusing discrete super disintegrants and coprocessed excipients. 2020;12(6).
Abed KK, Hussein AA, Ghareeb MM, Abdulrasool AA. Formulation and Optimization of Orodispersible Tablets of Diazepam. 2010;11(1):356-361. doi:10.1208/s12249-010-9387-y
Rampure M, Shirsand SB, Deshpande R. Formulation and Evaluation of Orodispersible tablets of Alfuzosin. 2010;(January).
Basu B, Bagadiya A. Formulation and evaluation of fast dissolving tablets of cinnarizine using superdisintegrant blends and subliming material. 2011;2(4). doi:10.4103/2231-4040.90885
P. Hyma ds, k. Jyothi. Formulation and evaluation of orodispersible tablets of naproxen sodium by direct compression method . 2021;11(09).
Panhale DP, Bachhav RS, Gondkar SB. Formulation and Evaluation of Orodispersible Tablets of Apremilast by Inclusion Complexation using β -Cyclodextrin. 2021;55(1). doi:10.5530/ijper.55.1s.42
Sirmour D. The formulation and evaluation of mouth dissolving tablet Levocetirizine by using synthetic Superdisintegrants. 2020;5(1):1-11. doi:10.22270/hjhs.v5i1.47
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