DEVELOPMENT OF MULTIPLE-UNIT MUCOADHESIVE SUSTAIN RELEASE MINI-TABLETS OF BOSENTAN

Authors

  • Tapan Kumar Panda School of Pharmaceutical Sciences, SOA University, Bhubaneswar, Odisha.
  • Debajyoti Das
  • Lalatendu Panighahi

Keywords:

Gelucire 4301, NaCMC, Burst release, Sylysia 350, Release modulator

Abstract

Objective: To formulate once daily capsule filled with multiple unit mucoadhesive sustain release (SR) mini tablets of bosentan prepared using combination gelucire 43/01 and hydroxypropyl methyl cellulose (HPMCK4M), sodium carboxymethyl cellulose (NaCMC) and chitosan to sustain drug release for 24 h.

Methods: The mini tablets were prepared by melt granulation technique using gelucire 43/01 as meltable hydrophobic release retardant. The polymers such as hydroxypropyl methylcellulose (HPMCK4M), sodium carboxymethyl cellulose (NaCMC) and chitosan were added as release modulators and mucoadhesives. The physical mixture of drug and excipient were subjected Fourier transform infrared (FT-IR) and differential scanning calorimetry (DSC) for evaluation of drug-polymer interaction. Mini tablets were evaluated for mucoadhesive strength, in vitro drug release, swelling index and percentage of hydration. The optimized mini tablets of formulation F23 were filled into zero sizes hard gelatin capsule.

Results: The release of bosentan from gelucire 43/01 based sustain release mini tablets extended drug release for 24 h with an initial burst release of more than 32 %. Incorporation of NaCMC, HPMCK4M and chitosan into the mini tablets controlled initial burst release with mucoadhesion.

Conclusion: Hence mini tablets prepared with a combination of gelucire 43/01 (release retardant) and NaCMC (release modulator and mucoadhesive polymer) filled into zero sizes hard gelatin capsule can be used to formulate once daily formulation of bosentan.

Downloads

Download data is not yet available.

References

Weber C, Schmitt R, Birnboeck H, Hopfgartner G, Eggers H, Meyer J, et al. Multiple-dose pharmacokinetics, safety, and tolerability of bosentan, an endothelin receptor antagonist, in healthy male volunteers. J Clin Pharmacol 1999;39:703-14.

Gabbay E, John Fraser J, McNeil K. Review of bosentan in the management of pulmonary arterial hypertension. Vasc Health Risk Manage 2007;3:887–900.

Aleksovski A, Dreu R, Gašperlin M, Planinšek O. Mini-tablets: a contemporary system for oral drug delivery in targeted patient groups. Expert Opin Drug Delivery 2015;12:65-84.

Dey NS, Majumdar S, Rao MEB. Multiparticulate drug delivery systems for controlled release. Trop J Pharm Res 2008;7:1067-75.

Sally AE, Abeer AK, Amal HE. Design and evaluation of gastro retentive levofloxacin floating mini-tablets-in-capsule system for the eradication of helicobacter pylori. Saudi Pharm J 2014;22:570–9.

Keerthi ML, Kiran RS, V Rao VUM, Sannapu A, Dutt AG, Krishna KS. Pharmaceutical mini-tablets, its advantages, formulation possibilities and general evaluation aspects: a review. Int J Pharm Sci Rev Res 2014;28:214-21.

Jain SK, Gupta A. Development of gelucire 43/01 beads of metformin hydrochloride for floating delivery. AAPS PharmSciTech 2009;10:1128-36.

Siripuram PK, Bandari S, Jukanti R, Veerareddy PR. Formulation and characterization of floating gelucire matrices of metoprolol succinate. Dissolution Technologies 2010;34-9. Doi.org/10.14227/DT170310P34

Jammula S, Patra CN, Swain S, Panigrahi KC, Nayak S, Dinda SC, et al. Design and characterization of cefuroxime axetil biphasic floating mini tablets. Drug Delivery 2015;22:125-35.

Wells JI, Aulton ME. Pharmaceutical pre-formulation. In: ME Aulton. Editor. Aulton’s pharmaceutics. The design and manufacture of medicines. Hungary: Elsevier; 2007. p. 355-7.

Margret C, Debjit M, Kumudhavalli C, Jayaker B. Formulation, design and development of bucco-adhesive tablets of verapamil HCl. Int J Pharm Technol 2009;1:1663-77.

Merchant HA, Shoaib HM, Tazeen J, Yousuf RI. Once-daily tablet formulation and in vitro release evaluation of cefpodoxime using hydroxypropyl methylcellulose: a technical note. AAPS PharmSciTech 2006;7:E178-83.

Bourne DW. Pharmacokinetics. In: Banker GS, Rhodes. Ed. Modern Pharmaceutics. 4th Edition. Marcel Dekker Inc, New York; 2002. p. 67–92.

Higuchi T. Mechanism of sustained action medication. J Pharm Sci 1963;52:1145–9.

Korsmeyer RW, Gurny R, Docler E, Buri P, Peppas NA. Mechanism of solute release from porous hydrophilic polymers. Int J Pharm 1983;15:25–35.

Perioli L, Ambrogi V, Giovagnoli S, Maurizio R, Paolo B, Carlo R. Mucoadhesive bilayered tablets for the buccal sustained release of flurbiprofen. AAPS PharmSciTech 2007;8:54.

Patra CN, Pandit HK, Singh SP, Devi MV. Applicability and comparative evaluation of wet granulation and direct compression technology to Rauwolfia serpentina root powder: a technical note. AAPS PharmSciTech 2008;9:100-4.

Bahl D, Hudak J, Bogner RH. Comparison of the ability of various pharmaceutical silicates to amorphized and enhance dissolution of indomethacin upon co-grinding. Pharm Dev Technol 2008;13:255–69.

Swain S, Behera UA, Beg S, Sruti J, Patro CN, Dinda SC, et al. Design and characterization of enteric-coated controlled release mucoadhesive microcapsules of rabeprazole sodium. Drug Dev Ind Pharm 2013;39:548-60.

Mankala SK, Korla AK, Gade S. Development, and evaluation of aceclofenac-loaded mucoadhesive microcapsules. J Adv Pharm Technol Res 2011;2:245–54.

Chauhan B, Shimpi S, Mahadik KR, Paradkar A. Preparation and evaluation of floating risedronate sodium-Gelucire 43/01 formulations. Drug Dev Ind Pharm Pharm 2005;31:851-60.

Shaikh R, Singh TRR, Garland MJ, Woolfson ADW, Donnelly RF. Mucoadhesive drug delivery systems. J Pharm Bioallied Sci 2011;3:89–100.

Patra CN, Padhy S, Sen T, Bhattacharya S, Swain S, Jammula S, et al. Formulation development and evaluation of SR matrix tablets of stavudine. Indian J Pharm Educ Res 2013;47:214-20.

Swain S, Jammula S, Patra CN, Beg S, Rao MEB, Dinda SC. Formulation design, optimization, characterization and in vivo pharmacodynamic study of enteric coated mucoadhesive microcapsules of esomeprazole magnesium. Drug Delivery Lett 2015;5:86-9.

El-Nahas HM, Hosny KM. Chitosan-based floating microspheres of trimetazidine dihydrochloride; preparation and in vitro characterization. Indian J Pharm Sci 2011;73:397-403.

Bueno VB, Bentini R, Catalani LH, Petri DFS. Synthesis and swelling behavior of xanthan-based hydrogels. Carbohydr Polym 2013;92:1091–9.

Patra CN, Padhy S, Sen T, Bhattacharya S, Swain S, Jammula S, et al. Formulation development and evaluation of sr matrix tablets of stavudine. Indian J Pharm Educ Res 2013;47:214-20.

Gu JM, Robinson JR, Leung SH. Binding of acrylic polymers to mucin/epithelial surfaces: structure-property relationships. Crit Rev Ther Drug Carrier Syst 1998;5:21–67.

Das S, Samanta A, Bose A. Design, development and evaluation of fluconazole topical gel. Asian J Pharm Clin Res 2015;8:132-5.

Published

01-10-2016

How to Cite

Panda, T. K., D. Das, and L. Panighahi. “DEVELOPMENT OF MULTIPLE-UNIT MUCOADHESIVE SUSTAIN RELEASE MINI-TABLETS OF BOSENTAN”. International Journal of Pharmacy and Pharmaceutical Sciences, vol. 8, no. 10, Oct. 2016, pp. 235-41, https://mail.innovareacademics.in/journals/index.php/ijpps/article/view/13859.

Issue

Section

Original Article(s)