Improvement of Dissolution Rate of Chlorzoxazone by Solid Dispersion Technique and Development of Buccal Patch
DOI:
https://doi.org/10.6000/1929-5030.2013.02.02.9Keywords:
Solid dispersions, pluronic F127, chlorzoxazone, dissolution studies, buccal patchAbstract
Chlorzoxazone (CLZ) is insoluble in water. Its half life is 1.1 hr, dose is 250 mg and has first pass metabolism. Formation of solid dispersions of CLZ with pluronic F127 will enhance the bioavailability of the drug. Phase-solubility studies revealed AL type of curves, indicating the ability of pluronic F127 to disperse with CLZ and significantly increase in solubility. The solid dispersions of CLZ was carried out with pluronic F127 by different methods and characterized by in vitro drug release, drug content, FTIR, DSC, XRD. All the solid dispersions showed dissolution improvement compare to pure drug. These techniques revealed distinct loss of drug crystallinity in the formulation accounting for enhancement in dissolution rate. The stability study for solid dispersions indicated, all formulations were stable. Methods showing best in vitro drug release profile were selected in further development of mucoadhesive buccal patches. A buccal patch has been developed using mucoadhesive polymers HPMC K4M and carbapol 974. The developed patches were evaluated for the physicochemical, mechanical and drug release characteristics. The optimized patches showed good mechanical and physicochemical properties to withstand environment of oral cavity. The in-vitro permeation study showed that patches could deliver drug to the oral mucosa for a period of 8 hrs. The results indicate that suitable bioadhesive buccal patches with good permeability could be prepared. The batches FH4 and FC4 showed 79.65% and 79.93% permeated through goat mucosa membrane in 8 hrs. The stability study for buccal patch revealed that all batches were stable.References
[1] Amidon G, lennernas H, Shah V, Crison J. A theoretical basic for a bio pharmaceutic drug classification: the correlation of in vitro drug product dissolution & in vivo bioavailability. Pharm Res 1995; 12(3): 26-31. http://dx.doi.org/10.1023/A:1016212804288
[2] Emami J. In vitro - In vivo correlation: from theory to applications. J Pharm Pharmaceut Sci 2006; 9(2): 169-89.
[3] Susana A, Breda A, Kairuz J, Manzo R, Olivera M. Solubility behavior and biopharmaceutical classification of novel highsolubility ciprofloxacin and norfloxacin pharmaceutical derivatives. Int J Pharm 2009; 371: 106-13. http://dx.doi.org/10.1016/j.ijpharm.2008.12.026
[4] Guneri T, Taneri F, Ertan G. Studies on sustained release matrix systems of chlorzoxazone. Acta Pharmaceutica Turcica 2005; 47: 39-51.
[5] Karthikeyan V, Vaidhyalingam, Yuvaraj G, Rajesh K. Simultaneous estimation of paracetamol, chlorzoxazone and aceclofenac in pharmaceutical formulation by HPLC method. Int J ChemTech Res 2009; 1(3): 457-60.
[6] Jalali M, Valizadeh H, Shadbad M, Adibkia K, Mohammadi G. Cogrinding as an approach to enhance dissolution rate of a poorly water-soluble drug (gliclazide). Powder Tech 2010; 197: 150-58. http://dx.doi.org/10.1016/j.powtec.2009.09.008
[7] Lewis D, Udupa N, Atin K. Solid dispersions: a review. Pak J Pharm Sci 2009; 22(2): 234-46.
[8] Shin S-C, Cho C-W. Physicochemical characterization of piroxicam-poloxomer solid dispersion. Pharm Dev Tech 1997; 2(4): 403-407. http://dx.doi.org/10.3109/10837459709022639
[9] Goddeeris C, Van den Mooter G. Free flowing solid dispersions of the anti-HIV drug UC 781 with poloxamer 407 and a maximum amount of TPGS 1000: investigating the relationship between physicochemical characteristics and dissolution behavior. Eur J Pharm Sci 2008; 13-18.
[10] Saritha A, Shastri N. Preparation, physico chemical characterization of solid dispersions of tenoxicam with poloxamer. J Pharm Sci Tech 2010; 2(9): 308-11.
[11] Cappello B, Giannini L, Mensitieri G, Miro A, Quaglia F, Russo R. Cyclodextrin-containing poly(ethylene oxide) tablets for the delivery of poorly soluble drugs: potential as buccal delivery system. Int J Pharm 2006; 319: 63-70. http://dx.doi.org/10.1016/j.ijpharm.2006.03.031
[12] Mario J, Becirevic-Lacan M. Influence of hydroxypropylcyclodextrin complexation on piroxicam release from buccoadhesive tablets. Eur J Pharm Sci 2004; 21: 251-60. http://dx.doi.org/10.1016/j.ejps.2003.10.029
[13] Gill B, Kaur T, Kumar S, Gupta G. Formulation and evaluation of glimepiride solid dispersion tablets. Asian J Pharm 2010; 4(3): 212-18. http://dx.doi.org/10.4103/0973-8398.72121
[14] Burgalassi S, Panichi L, Saettone M. Development and in vitro/ in vivo testing of mucoadhesive buccal patches releasing benzydamine and lidocaine. Int J Pharm 1996; 133: 1-7. http://dx.doi.org/10.1016/0378-5173(95)04392-6
[15] Vishnu Y, Chandrasekhar K, Ramesh G, Rao Y. Development of mucoadhesive patches for buccal administration of carvedilol. Curr Drug Deliv 2007; 4: 27-39. http://dx.doi.org/10.2174/156720107779314785
[16] Luana P, Valeria A, Fausta A, Maurizio R, Stefano G, Marinella C, Carlo R. Development of mucoadhesive patches for buccal administration of ibuprofen. J Control Rel 2004; 99: 73-82. http://dx.doi.org/10.1016/j.jconrel.2004.06.005
[17] Noha A, Fatma A, Boraie N, Mortada L. Mucoadhesive buccal patches of miconazole nitrate: in vitro/in vivo performance and effect of ageing. Int J Pharm 2003; 264: 1- 14. http://dx.doi.org/10.1016/S0378-5173(03)00371-5
[18] Salamat-Miller N, Chittchang M, Johnston T. The use of mucoadhesive polymers in buccal drug delivery. Adv Drug Del Rev 2005; 57: 1666-91. http://dx.doi.org/10.1016/j.addr.2005.07.003
[19] Sudhakar Y, Kuotsu K, Bandyopadhyay A. Review buccal bioadhesive drug delivery - a promising option for orally less efficient drugs. J Control Rel 2006; 114: 15-40. http://dx.doi.org/10.1016/j.jconrel.2006.04.012
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Published
2013-05-31
How to Cite
Jagdale, S., Hable, A., Chabukswar, A., & Kuchekar, B. (2013). Improvement of Dissolution Rate of Chlorzoxazone by Solid Dispersion Technique and Development of Buccal Patch. Journal of Applied Solution Chemistry and Modeling, 2(2), 145–157. https://doi.org/10.6000/1929-5030.2013.02.02.9
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