AAPS PharmSciTech

, Volume 5, Issue 4, pp 63–68 | Cite as

Tablet formulation containing meloxicam and β-cyclodextrin: Mechanical characterization and bioavailability evaluation

  • Mamdouh M. Ghorab
  • Heba M. Abdel-Salam
  • Marwa A. El-Sayad
  • Mohammed M. Mekhel


The purpose of this research was to evaluate β-cyclodextrin (β-CD) as a vehicle, either singly or in blends with lactose (spray-dried or monohydrate), for preparing a meloxicam tablet. Aqueous solubility of meloxicam in presence of β-CD was investigated. The tablets were prepared by direct compression and wet granulation techniques. The powder blends and the granules were evaluated for angle of repose, bulk density, compressibility index, total porosity, and drug content. The tablets were subjected to thickness, diameter, weight variation test, drug content, hardness, friability, disintegration time, and in vitro dissolution studies. The effect of β-CD on the bioavailability of meloxicam was also investigated in human volunteers using a balanced 2-way crossover study. Phase-solubility studies indicated an AL-type diagram with inclusion complex of 1∶1 molar ratio. The powder blends and granules of all formulations showed satisfactory flow properties, compressibility, and drug content. All tablet formations prepared by direct compression or wet granulation showed acceptable mechanical properties. The dissolution rate of meloxicam was significantly enhanced by inclusion of β-CD in the formulations up to 30%. The mean pharmacokinetic parameters (Cmax, Ke, and area under the curve [AUC]0−∞) were significantly increased in presence of β-CD. These results suggest that β-CD would facilitate the preparation of meloxicam tablets with acceptable mechanical properties using the direct compression technique as there is no important difference between tablets prepared by direct compression and those prepared by wet granulation. Also, β-CD is particularly useful for improving the oral bioavailablity of meloxicam.


meloxicam β-CD tablet solubility bioavailability 


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  1. 1.
    Moyano JR, Ginés JM, Airas MJ, Rabasco AM. Study of the dissolution characteristics of oxazepam via complexation with β-cyclodextrin.Int J Pharm. 1995;114:95–102.CrossRefGoogle Scholar
  2. 2.
    Mukne AP, Nagarsenker MS. Triamterene-β-cyclodextrin systems: preparation, characterization and in vivo evaluation.AAPS Pharm Sci Tech. 2004;5:E19.CrossRefGoogle Scholar
  3. 3.
    Nalluri BN, Chowdary KPR, Murthy KVR, Hayman AR, Becket G. Physicochemical characterization and dissolution properties of nimesulide-cyclodextrin binary systems.AAPS Pharm Sci Tech. 2003;4:E2.CrossRefGoogle Scholar
  4. 4.
    Giordano F, Gazzaniga A, Bettinetti GP, La Manna A. The influence of water content on the binding capacity of β-cyclodextrin.Int J Pharm. 1990;62:153–156.CrossRefGoogle Scholar
  5. 5.
    Tasić LJ, Pintye-Hōdi K, Sabo-Revesz P. Evaluation of compression behavior of paracetamol tablets produced with β-cyclodextrin dispersions. Part II: Energy distribution study of tablets.Drug Dev Ind Pharm. 1997;23:1153–1158.Google Scholar
  6. 6.
    Naidu NB, Chowdary KP, Murthy KV, Satyanaryana V, Hayman AR, Becket G. Physicochemical characterization and dissolution properties of meloxicam-cyclodextrin binary system.J Pharm Biomed Anal. 2004;35(1):75–86.CrossRefGoogle Scholar
  7. 7.
    Baboota S, Agarwal SP. Inclusion complexation of meloxicam with β-cyclodextrin.Indian J Pharm Sci. 2002;64(4):408–411.Google Scholar
  8. 8.
    Nath BS, Shiva Kumar HN. A 2(3) factorial studies on factors influencing meloxicam β-cyclodextrin complexation for better solubility.Indian J Pharm Sci. 2000;Mar–Apr;62(2):129–132.Google Scholar
  9. 9.
    Baboota S, Agarwal SP. Effect of cyclodextrin complexation on the oral bioavailability of meloxicam. Paper presented at the 12th International Cyclodextrin Symposium; May 16–19, 2004; Montpellier, France.Google Scholar
  10. 10.
    Struengmann A, Freudensprung B, Klokkers K inventors. Pharmaceutical compositions of meloxicam with improved solubility and bioavailability. US patent 6284269. 2001.Google Scholar
  11. 11.
    Perissutti B, Rubessa F, Moneghini M, Voinovich D. Formulation design of carbamazepin fast-release tablets prepared by melt granulation.Int J Pharm. 2003;256:53–63.CrossRefGoogle Scholar
  12. 12.
    Shah D, Shah Y, Rampradhan M. Development and evaluation of controlled release dilitiazem hydrochloride microparticles using cross-linked poly(vinyl alcohol).Drug Dev Ind Pharm. 1997;23:567–574.CrossRefGoogle Scholar
  13. 13.
    Aulton ME. Pharmaceutical Technology. In:Pharmaceutics: The Science of Dosage Form Design. London, UK: Churchill Livingstone; 1988:600–616.Google Scholar
  14. 14.
    Martin A. Micromertics. In:Physical Pharmacy. Philadelphia, PA: Lea and Febiger, 1993:251–283.Google Scholar
  15. 15.
    Reddy KR, Mutalik S, Reddy S. Once-daily sustained-release matrix tablets of nicorandil: formulation and in vitro evaluation.AAPS Pharm Sci Tech. 2003;4:E61.CrossRefGoogle Scholar
  16. 16.
    FDA Center for Drug Evaluation and Research.Guidance for Industry: Dissolution Testing of Immediate Release Solid Oral Dosage Form. Rockville, MD: FDA: August 1997.Google Scholar
  17. 17.
    Higuchi T, Connors A. Phase-solubility techniques. In:Advances in Analytical Chemistry Instrumentation. Vol. 4, New York, NY: Wiley Interscience; 1965:117–211.Google Scholar
  18. 18.
    El-Shaboury MH. Physical properties and dissolution profiles of tablets directly compressed with β-cyclodextrin.Int J Pharm. 1990;63:95–100.CrossRefGoogle Scholar
  19. 19.
    Fenyresi E, Shirankura O, Szejtli J, Nagai T. Properties of cyclodextrin polymer as a tableting aid.Chem Pharm Bull (Tokyo). 1984;32:665–669.Google Scholar

Copyright information

© American Association of Pharmaceutical Scientists 2004

Authors and Affiliations

  • Mamdouh M. Ghorab
    • 1
  • Heba M. Abdel-Salam
    • 2
  • Marwa A. El-Sayad
    • 2
  • Mohammed M. Mekhel
    • 2
  1. 1.Department of Pharmaceutics, College of PharmacySuez Canal UniversityIsmailiaEgypt
  2. 2.Research Projects DepartmentMedical Union Pharmaceutical CoAbu Sultan-IsmailiaEgypt

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