Abstract
Taste masked sublingual film of buspirone hydrochloride (BH) was developed with the objectives of taste masking, fast disintegration, increased dissolution and better patient compliance. The film was formulated using Polyox WSR N-10, polyvinyl pyrolidone (PVP) K-30 and propylene glycol as a plasticizer. Taste masking was obtained by ternary complexation between BH, β-cyclodextrin and PVP K-30. Optimized batch contained 3 % w/v of Polyox WSR N-10, 2 % w/v PVP K-30 and propylene glycol (20 % weight of Polyox WSR N-10). The optimized formulation also contained BH: β-CD (1:1.5 molar ratio), BH: sucralose (1:0.5 ratio) and 0.15 ml orange flavour. This batch was evaluated for % elongation, tensile strength, in vitro disintegration time and in vitro dissolution studies. In-vitro permeation studies employing rabbit sublingual mucosa, indicated higher drug permeability at the ventral surface than at the bottom surface of the mouth. In-vivo absorption studies in rabbits revealed that 50.27 ± 5.24 % of BH was absorbed sublingually from film within 5 min. The kinetics of in vivo drug absorbed from sublingual film in human volunteers indicated that there is no significant difference between ex vivo and in vivo data obtained for the drug absorption. The formulation, subjected to stability studies at 25 °C/60 % RH for 2 months, showed good stability indicating suitable packaging and storage conditions.
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References
Aloisio C, Oliveira AG, Longhi M (2014) Solubility and release modulation effect of sulfamerazine ternary complexes with cyclodextrins and meglumine. J Pharm Biomed 100:64–73
Artusi M, Santi P, Colombo P (2003) Buccal delivery of thiocolchicoside: in vitro and in vivo permeation studies. Int J Pharm 250:203–213
Avery JK, Avery N (2002) Oral development and histology. Thieme Stuttgart, New York
Bala R, Pawar P, Khanna S, Arora S (2013) Orally dissolving strips: a new approach to oral drug delivery system. Int J Pharm Investig 3:67–76
Beckett AH, Triggs EJ (1967) Buccal absorption of basic drugs and its application as an in vivo model of passive drug transfer through lipid membranes. J Pharm Pharmacol 19:Suppl:31S–41S
Bhyan B, Jangra S (2012) Formulation and evaluation of fast dissolving sublingual films of Rizatriptan Benzoate. Int J Drug Dev Res 4:133–143
British Pharmacopoeia (2010) The stationery office on behalf of the medicines and healthcare products regulatory agency (MHRA). British Pharmacopoeia, London, pp 313–314
Challa R, Ahuja A, Khar RK (2005) Cyclodextrins in drug delivery: an updated review. AAPS PharmSciTech 6:329–357
Dahiya M, Sumit SA (2009) A review on mouth dissolving films. Curr Drug Deliv 6:469–476
Ghosh T, Pfister W (2005) Drug delivery to oral cavity molecules to market. Marcel Dekker, New York
Indian Pharmacopoeia 6 (2010) The Indian Pharmacopoeia Commission. Indian Pharmacopoeia, Ghaziabad, p 938
Koland M, Sandeep VP, Charyulu NR (2010) Fast dissolving sublingual films of ondansetron hydrochloride: effect of additives on in vitro drug release and mucosal permeation. J Young Pharm 2:216–222
Mady FM, AbouTaleb AE, Khaled KA, Yamasaki K, Iohara D, Ishiguro T, Hirayama F, Uekama K, Otagiri M (2010) Enhancement of the aqueous solubility and masking the bitter taste of famotidine using Drug/SBE-b-CyD/povidone K30 complexation approach. J Pharm Sci 99:4285–4294
Marques MC, Loebenberg R, Almukainzi M (2011) Simulated biological fluids with possible application in dissolution testing. Dissolution Technol 18(3):15–28
Mashru RC, Sutariya VB, Sankalia MB, Parikh PP (2005) Development and evaluation of fast dissolving film of salbutamol sulphate. Drug Dev Ind Pharm 31:25–34
Mishra R, Amin A (2009) Formulation development of taste masked rapidly dissolving films of cetirizine hydrochloride. PharmTech (USA) 33:48–56
Mura P, Faucci MT, Betinetti GP (2001) The influence of polyvinylpyrrolidone on naproxen complexation with hydroxypropyl-ß-cyclodextrin. Eur J Pharm Sci 13:187–194
Ong CM, Heard CM (2009) In vitro permeation of quinine across sublingual mucosa. Int J Pharm 366:58–64
Prasad D, Chauhan H, Atef E (2014) Amorphous stabilization and dissolution enhancement of amorphous ternary solid dispersions: combination of polymers showing drug-polymer interaction for synergistic effects. J Pharm Sci 103:3511–3523
Rajitha K, Kumar SY, Adukondalu D, Gannu R, Rao MY (2009) Formulation and evaluation of orally disintegrating tablets of buspirone. Int J Pharm Sci Nanotechnol 1(4):327–334
Sayed S, Ibrahim HK, Mohamed MI, El-Milligi MF (2013) Fast-dissolving sublingual films of terbutaline sulfate: formulation and in vitro/in vivo evaluation. Mol Pharm 10:2942–2947
Sean CS (2001) Martindale the complete drug reference. Pharmaceutical Press, London
Sohi H, Sultana Y, Khar RK (2004) Taste masking technologies in oral pharmaceuticals : recent developments and approaches. Drug Dev Ind Pharm 30:429–448
Szejtli J, Szente L (2005) Elimination of bitter, disgusting tastes of drugs and foods by cyclodextrins. Eur J Pharm Biopharm 61:115–125
Taupitz T, Dressman JB, Buchanan CM, Klein S (2013) Cyclodextrin-water soluble polymer ternary complexes enhance the solubility and dissolution behaviour of poorly soluble drugs. Case example: itraconazole. Eur J Pharm Biopharm 83:378–387
United States Pharmacopeia 31/NF (2008) The official compendia of standards. In: Asian (ed) United States Pharmacopeia Convention Inc. United States Pharmacopeia, Rockville, p 1576
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All authors (R. Mishra, A. Sharma, T. Mehta, and M. Gohel) declare that they have no conflict of interest. The authors would like to acknowledge Nirma University, Ahmedabad for providing facilities for conduct of the study.
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Mishra, R., Sharma, A., Mehta, T. et al. Formulation and characterization of ternary complex of sublingual film of buspirone hydrochloride. Journal of Pharmaceutical Investigation 45, 359–366 (2015). https://doi.org/10.1007/s40005-015-0193-0
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DOI: https://doi.org/10.1007/s40005-015-0193-0