Download PDF
Drug Res (Stuttg) 2013; 63(11): 586-890
DOI: 10.1055/s-0033-1348258
Original Article
© Georg Thieme Verlag KG Stuttgart · New York

Formulation and Pharmacokinetics of Ketorolac Tromethamine Fast Dissolving Tablets

S. R. Mettu
1   Department of Pharmaceutics, Jyothishmathi Institute of Pharmaceutical Sciences, Andhra Pradesh, India
,
P. R. Veerareddy
2   Chaitanya College of Pharmacy Education and Research, Andhra Pradesh, India
› Author Affiliations
Further Information

Publication History

received 13 March 2013

accepted 28 May 2013

Publication Date:
18 June 2013 (online)

Also available at
    Permissions and Reprints

Abstract

Objective:

The current study is intended to develop the fast dissolving tablets of Ketorolac tromethamine using different superdisintegrants to improve the dissolution rate and absorption rate to produce the bioavailability enhancement and rapid onset of action.

Methods:

In this, Ketorolac tromethamine fast dissolving tablets were prepared using different superdisintegrants and evaluated for different physical parameters, in vitro dissolution studies and in vivo pharmacokinetics to demonstrate the bioavailability enhancement.

Results & Discussions:

From the in vitro drug release studies, in case of optimized formulation, the cumulative percent drug release in 15 min (Q15) was found to be 94.34±1.68 where as the conventional tablets showed 28.78±0.82 in 15 min. The initial dissolution rate and dissolution efficiency of optimized formulation was 6.29%/min and 53.43 but it was 1.92%/min and 14.03 in conventional tablets. From the in vivo pharmacokinetic evaluation, the optimized formulation showed peak plasma concentration (Cmax) as 1 248.39 ng/ml at 1 h Tmax, but they were found to be 988.22 ng/ml at 2 h Tmax, in case of conventional tablets. The area under the curve for the optimized and conventional tablets was 3 890.68 and 3 173.07 ng-h/ml.

Conclusion:

Hence the development of fast dissolving tablets using superdisintegrants was a good approach to improve the dissolution rate and absorption rate of Ketorolac tromethamine.

Key words

absorption rate - dissolution efficiency - in vitro drug release studies - initial dissolution rate - pharmacokinetic evaluation
 

  • References

  • 1 Charman WN. Lipids, lipophilic drugs, and oral drug delivery – some emerging concepts. J Pharm Sci 2000; 89: 967-978
    CrossrefPubMedGoogle Scholar
  • 2 Meyer MC. Bioavailability and bioequivalence of drugs. In: Swarbik J. (ed.). Encyclopedia of pharmaceutical technology. New York: Marcel Dekker; 1998: 33-58
    Google Scholar
  • 3 Hirani JJ, Rathod DA, Vadalia KR. Orally disintegrating tablets: a review. Trop J Pharm Res 2009; 8: 161-172
    PubMedGoogle Scholar
  • 4 Dobetti L. Fast-melting tablets: developments and technologies. Pharm Tech 2000; 12: 32-42
    PubMedGoogle Scholar
  • 5 Kaushik D, Dureja H, Saini TR. Mouth dissolving tablets: a review. Ind Drug 2004; 41: 187-193
    PubMedGoogle Scholar
  • 6 Vemula SK, Bontha VK, Garrepally P et al. Development and characterization of fast disintegrating tablets of terbinafine hydrochloride. J Pharm Res 2011; 4: 2273-2275
    PubMedGoogle Scholar
  • 7 Neduri K, Bontha VK, Vemula SK. Different techniques to enhance the dissolution rate of lovastatin: formulation and evaluation. Asian J Pharm Clin Res 2013; 6: 56-60
    PubMedGoogle Scholar
  • 8 Battu SK, Repka MA, Majumdar S et al. Formulation and evaluation of rapidly disintegrating feniverine tablets, effect of superdisintegrants. Drug Dev Ind Pharm 2007; 33: 1225-1232
    CrossrefPubMedGoogle Scholar
  • 9 Vemula SK, Veerareddy PR. Formulation and evaluation of ketorolac tromethamine tablets for time and pH dependent colon specific delivery. J Cur Pharm Res 2011; 8: 31-39
    PubMedGoogle Scholar
  • 10 Gohel M, Patel M, Amin A et al. Formulation design and optimization of mouth dissolve tablets of nimesulide using vacuum drying technique. AAPS Pharm Sci Tech 2004; 5: 1-6
    PubMedGoogle Scholar
  • 11 Narmada GY, Mohini K, Prakash B et al. Formulation, evaluation and optimization of fast dissolving tablets containing amlodipine besylate by sublimation method. Ars Pharm 2009; 50: 129-144
    PubMedGoogle Scholar
  • 12 Bi Y, Sunanda H, Yonezawa Y et al. Preparation and evaluation of a compressed tablet rapidly disintegrating in the oral cavity. Chem Pharm Bull 1996; 44: 2121-2127
    CrossrefPubMedGoogle Scholar
  • 13 Madan J, Sharma AK, Singh R. Fast dissolving tablets of Aloe vera gel. Trop J Pharm Res 2009; 8: 63-70
    PubMedGoogle Scholar
  • 14 Sammour OA, Hammad MA, Megrab NA et al. Formulation and optimization of mouth dissolve tablets containing Rofecoxib solid dispersion. AAPS Pharm Sci Tech 2006; 7: E1-E9
    PubMedGoogle Scholar
  • 15 Valleri M, Mura P, Maestrelli F et al. Development and evaluation of glyburide fast dissolving tablets using solid dispersion technique. Drug Dev Ind Pharm 2004; 30: 525-534
    CrossrefPubMedGoogle Scholar
  • 16 Vemula SK, Veerareddy PR. Formulation, evaluation and pharmacokinetics of ketorolac tromethamine time-dependent colon targeted drug delivery system. Exp Opin Drug Del 2013; 10: 33-45
    CrossrefPubMedGoogle Scholar
  • 17 Vemula SK, Bontha VK, Garrepally P. Development and characterization of fast disintegrating tablets of piroxicam. Inventi Impact: Pharm Tech 2010; 1: 169-173
    PubMedGoogle Scholar