THE DEVELOPMENT OF GLIBENCLAMIDE-SACCHARIN COCRYSTAL TABLET FORMULATIONS TO INCREASE THE DISSOLUTION RATE OF THE DRUG

ARIF BUDIMAN; PATIHUL  HUSNI; SHAFIRA; Tazyinul Q. Alfauziah

doi:10.22159/ijap.2019v11i4.33802

Authors

ARIF BUDIMAN Department of Pharmaceutical and Technology Formulation, Faculty of Pharmacy, University of Padjadjaran, Jatinangor 45363, Indonesia
PATIHUL HUSNI Department of Pharmaceutical and Technology Formulation, Faculty of Pharmacy, University of Padjadjaran, Jatinangor 45363, Indonesia
SHAFIRA Department of Pharmaceutical and Technology Formulation, Faculty of Pharmacy, University of Padjadjaran, Jatinangor 45363, Indonesia
Tazyinul Q. Alfauziah Department of Pharmaceutical and Technology Formulation, Faculty of Pharmacy, University of Padjadjaran, Jatinangor 45363, Indonesia

DOI:

https://doi.org/10.22159/ijap.2019v11i4.33802

Keywords:

Cocrystal, Tablet, Glibenclamide, Saccharin, Dissolution

Abstract

Objective: Cocrystallisation is a promising method in order to increase the solubility and dissolution of poorly water-soluble drugs. The aim of this study was to prepare, formulate and evaluate glibenclamide (GCM) cocrystal in direct compress tablet dosage form using saccharin (SAC) as the coformer.

Methods: GCM cocrystal with various stoichiometric ratios were prepared by the solvent drop grinding method. The co-crystal was characterized by a saturated solubility test and dissolution rate test, Fourier Transform Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), and Powder X-Ray Diffraction (PXRD). The tablet dosage form of GCM was formulated and evaluated compare with the conventional dosage form.

Results: The solubility and dissolution rate of GCM-SAC cocrystals increased significantly compared with pure GCM, especially for ratio of 1:2. The dissolution rate of cocrystal with ratio 1:2 increased by almost 91.9% compared with pure GCM. Based on the FTIR analysis, it showed the shifting of characteristic bands of GCM in the spectrum and there was no chemical reaction in GCM cocrystal. In PXRD measurement, the new crystalline peak was detected in the crystal habit of cocrystal compared with pure GCM and coformer. The new single melting of GCM-SAC cocrystal also was detected in DSC measurement. The tablets of GCM-SAC cocrystal were successfully prepared by direct compression method which rapidly disintegrated (1 min) and has higher dissolution compared with its pure form (32.36% greater than glibenclamide after 45 min).

Conclusion: The tablet dosage form of GCM cocrystal with SAC as coformer was successfully prepared, formulated and improved its solubility and dissolution rate.

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References

Chaturvedi AK, Verma A. Solubility enhancement of poorly water-soluble drugs by solid dispersion. Int J Pharm Sci Res 2012;3:26-34.

Sopyan I, Fudholi A, Muchtaridi M, Puspita Sari I. Simvastatin-nicotinamide co-crystal: design, preparation and preliminary characterization. Trop J Pharm Res 2017;16:297–303.

Ayoub M, Hasan A, El Nahas H, Ghazy FE. Enhancing oral bioavailability of carvedilol using solid dispersion technique. Int J Pharm Pharm Sci 2016;8:193-9.

Sola D, Rossi L, Schianca GPC, Maffioli P, Bigliocca M, Mella R, et al. Sulfonylureas and their use in clinical practice. Arch Med Sci AMS 2015;11:840-8.

Yalkowsky SH, Dannenfelser RM. Aquasol database of aqueous solubility. Coll Pharmacy, Univ Arizona, Tucson, AZ; 1992. p. 189.

Singh K, Kumar L, Prasad DN, Sharma S, Gupta GD. Fast dissolving tablet: a novel approach for the delivery of glibenclamide. Res Rev J Pharm Nanotechnol 2013;1:1–6.

Sajeev Kumar B, Saraswathi R, Venkates Kumar K, Jha SK, Venkates DP, Dhanaraj SA. Development and characterization of lecithin stabilized glibenclamide nanocrystals for enhanced solubility and drug delivery. Drug Delivery 2014;21:173–84.

Vaculikova E, Placha D, Pisarcik M, Jampilek J. Preparation of glibenclamide nanoparticles. 18th Int. Electron. Conf Synth Org Chem; 2014. p. 1–30.

Shah SR, Parikh RH, Chavda JR, Sheth NR. Application of plackett–burman screening design for preparing glibenclamide nanoparticles for dissolution enhancement. Powder Technol 2013;235:405–11.

Dhillon N, Midha K, Nagpal M, Pahwa R. Formulation, optimization and characterization of solid dispersion of glibenclamide. Pharm Methods 2015;6:1–10.

Tabbakhian M, Hasanzadeh F, Tavakoli N, Jamshidian Z. Dissolution enhancement of glibenclamide by solid dispersion: solvent evaporation versus a supercritical fluid-based solvent-antisolvent technique. Res Pharm Sci 2014;9:337–50.

Saifee M, Zarekar S, Rao VU, Zaheer Z, Soni R, Burande S. Formulation and in vitro evaluation of solid-self-emulsifying drug delivery system (SEDDS) of glibenclamide. Am J Adv Drug Delivery 2013;1:323-40.

Azharshekoufeh L, Shokri J, Barzegar Jalali M, Javadzadeh Y. Liquigroud technique: a new concept for enhancing the dissolution rate of glibenclamide by a combination of liquisolid and co-grinding technologies. BioImpacts BI 2017;7:5-12.

Budiman A, Megantara S, Raraswati P, Qoriah T. Solid dosage form development of glibenclamide with increasing the solubility and dissolution rate using cocrystallization. Int J Appl Pharm 2018;10:181-6.

Budiman A, Megantara S, Apriliani A. Solid dosage form development of glibenclamide-aspartame cocrystal using the solvent evaporation method to increase the solubility of glibenclamide. Int J Appl Pharm 2019;11:150-4.

Siswandi S, Rusdiana T, Levita J. Virtual screening of co-formers for ketoprofen co-crystallization and the molecular properties of the co-crystal. J Appl Pharm Sci 2015;5:78–82.

Hickey MB, Peterson ML, Scoppettuolo LA, Morrisette SL, Vetter A, Guzmán H, et al. Performance comparison of a co-crystal of carbamazepine with marketed product. Eur J Pharm Biopharm 2007;67:112–9.

Hiendrawan ST, Veriansyah BA, Widjojokusumo ED, Soewandhi SN, Wikarsa S, Tjandrawinata RR. Simultaneous cocrystallization and micronization of paracetamol-dipicolinic acid cocrystal by supercritical antisolvent (SAS). Int J Pharm Pharm Sci 2016;8:89-98.

Rajurkar VG, Sunil NA, Ghawate V. Tablet formulation and enhancement of aqueous solubility of efavirenz by solvent evaporation Co-Crystal technique. Med Chem 2015;2:S2-002.

Savjani JK, Pathak C. Improvement of physicochemical parameters of acyclovir using cocrystallization approach. Brazilian J Pharm Sci 2016;52:727–34.

Bhowmik D, Yadav R, Jayakar B, Kumar KPS. Formulation and evaluation of the oral tablets ibuprofen. Pharma Innov 2012;1:32-43.

Rajbhar P, Sahu AK, Gautam SS, Prasad RK, Singh V, Nair SK. Formulation and evaluation of clarithromycin co-crystals tablets dosage forms to enhance the bioavailability. Pharma Innov 2016;5:5-13.

Ansel HC, Popovich NG, Allen LV. Pharmaceutical dosage forms and drug delivery systems. Lippincott Williams and Wilkins; 1995.

Banerjee ND, Singh M. Formulation and evaluation of compression coated tablets of cefpodoxime proxetil. Int J Pharma Sci Res 2013;4:104–12.

Panzade P, Shendarkar G, Shaikh S, Rathi PB. Pharmaceutical cocrystal of piroxicam: design, formulation and evaluation. Adv Pharm Bull 2017;7:399–408.

Sopyan I, Fudholi A, Muchtaridi M, Sari IP. Co-crystallization: a tool to enhance the solubility and dissolution rate of simvastatin. J Young Pharm 2017;9:183-6.

Trask AV, Motherwell WS, Jones W. Solvent-drop grinding: green polymorph control of cocrystallization. Chem Comm 2004;7:890-1.

Basavoju S, Boström D, Velaga SP. Indomethacin–saccharin cocrystal: design, synthesis and preliminary pharmaceutical characterization. Pharm Res 2008;25:530-41.

Rodríguez Hornedo N, Nehm SJ, Jayasankar A. Cocrystals: design, properties and formation mechanisms. In: Swarbrick J. editor. Encycl. Pharm. Technol. Vol. 1. 3rd edition, New York: Informa Healthcare USA, Inc; 2007. p. 615–35.