FORMULATION AND EVALUATION OF BUOYANT TABLETS OF KETOCONAZOLE

GHOSH  T.; S.  BHARATH; NAIK  R.; B.V.  BASAVARAJ; R.  DEVESWARAN

doi:10.22159/ijap.2019v11i2.31318

Authors

GHOSH T. Department Pharmaceutics, Faculty of Pharmacy, M.S. Ramaiah University of Applied Sciences, Bangalore, Karnataka http://orcid.org/0000-0001-8470-3966
S. BHARATH Department of Pharmaceutics, Faculty of Pharmacy, M.S. Ramaiah University of Applied Sciences, Bangalore, Karnataka
NAIK R. Department Pharmaceutics, Faculty of Pharmacy, M.S. Ramaiah University of Applied Sciences, Bangalore, Karnataka
B.V. BASAVARAJ Department of Pharmaceutics, Faculty of Pharmacy, M.S. Ramaiah University of Applied Sciences, Bangalore, Karnataka
R. DEVESWARAN Department of Pharmaceutics, Faculty of Pharmacy, M.S. Ramaiah University of Applied Sciences, Bangalore, Karnataka

DOI:

https://doi.org/10.22159/ijap.2019v11i2.31318

Keywords:

Buoyancy, Gastro-retentive drug delivery, Ketoconazole, Optimization design

Abstract

Objective: The primary objective of the present work was to formulate the gastro-retentive delivery system of ketoconazole (ktz) for its extensive absorption in the stomach.

Methods: The solubility and dissolution of antifungal ktz were reported to be higher in the stomach than in the intestinal pH conditions because of its dibasic pKa values 6.51 and 2.94. Thus the development of target buoyant tablets using Hydroxy Propyl Cellulose (HPC) and Xanthan gum (Xg) as polymers along with the effect of citric acid and sodium bicarbonate as an effervescent causing agent of floatation properties and drug release profile was investigated. The formulation optimization was carried out by using a central composite design using Design Expert software by taking HPC, Xanthan gum and sodium bicarbonate as independent variables and floating lag time, in vitro drug release profile as dependent variables respectively.

Results: The optimized formulation of ktz buoyant tablets could be developed. The amount of HPC and Xg was found to significantly influence all in vitro response parameters. The results of pre-compression and post-compression parameters of all the formulations were found to be within the standard limits. The optimized formulation exhibited floating lag time of 160 secs with sustained drug release over a period of 12 h in simulated stomach pH condition.

Conclusion: Buoyant tablets of ktz with sustained drug release over a period of 12 h in simulated stomach conditions for enhanced drug absorption could be successfully developed.

Downloads

Download data is not yet available.

Author Biography

GHOSH T., Department Pharmaceutics, Faculty of Pharmacy, M.S. Ramaiah University of Applied Sciences, Bangalore, Karnataka

Assistant Professor

Department Of Pharmaceutics

Faculty OF Pharmacy

References

Gilbert SB, Christopher TR. Modern Pharmaceutics. 4th ed. Marcel Dekker Inc publishing; 2005. p. 501-5.

Kumar R, Patil S, Patil MB, Patil SR, Paschapur MS. Design and in vitro evaluation of oral floating matrix tablets of aceclofenac. Int J ChemTech Res 2009;1:815-25.

Ponchel G, Irache JM. Specific and non-specific bioadhesive particulate system for oral delivery to the gastrointestinal tract. Adv Drug Delivery Rev 1998;34:191-219.

Lenaerts VM, Gurny R. Gastrointestinal tract-physiological variables affecting the performance of oral sustained release dosage forms. In: Lenaerts V, Gurny R. eds. Bioadhesive Drug Delivery System. Boca Raton, FL: CRC Press; 1990.

Rednick AB, Tucker SJ. Sustained release bolus for animal husbandry. US patent 3507952; 1970.

Davis SS, Stockwell AF, Taylor MJ. The effect of density on the gastric emptying of single and multiple unit dosage forms. Pharm Res 1986;3:208-13.

Fix JA, Cargill R, Engle K. Controlled gastric emptying. III. Gastric residence time of a non-disintegrating geometric shape in human volunteers. Pharm Res 1993;10:1087-9.

Kedzierewicz F, Thouvenot P, Lemut J, Etienne A, Hoffman M, Maincent P. Evaluation of peroral silicone dosage forms in humans by gamma-scintigraphy. J Controlled Release 1999;58:195-205.

Groning R, Heun G. Oral dosage forms with controlled gastrointestinal transit. Drug Dev Ind Pharm 1984;10:527-39.

Groning R, Heun G. Dosage forms with controlled gastrointestinal passage studies on the absorption of nitro-furantion. Int J Pharm 1989;56:111-6.

Villafuerte RL, Quirino BT, Jimenez MI. Sustained delivery of captopril from floating matrix tablets. Int J Pharm 2008;362:37-43.

Debajyoti R, Amresh KP. Designing and in vitro studies of gastric floating tablets of tramadol hydrochloride. Int J Appl Pharm 2010;2:12-6.

Devendra KB, Peeyush B, Akash Y, Sarita K. Development and characterization of floating tablets of captopril using natural polymers. Pharma Res 2009;1:213-22.

Rosa M, Zia H, Rhodes T. Dosing and testing in vitro of a bioadhesive and floating drug delivery system for oral application. Int J Pharm 1994;105:65-70.

Shreeraj HS, Jayvadan KP, Nirav VP. Formulation and evaluation of effervescent floating tablet of Levofloxacin against H. pylori infection. Der Pharm Sin 2010;1:232-44.

Bolai P, Senthil A, Mohd JQ, Nahlah EI. A review of helicobacter pylori infection diseases, antibiotic resistance and diagnosis. Asian J Pharm Clin Res 2018;11:566-71.

Formulation and in vitro evaluation of salbutamol sulphate and theophylline extended-release tablets using modified polymers. Int J Pharm Pharm Sci 2018;10:67-71,

Ain S, Kumar B, Pathak K. Development and characterization of controlled release famotidine matrix tablets containing complexes. Int J Appl Pharm 2017;9:38-46.