Advances in Clinical and Experimental Medicine

Title abbreviation: Adv Clin Exp Med
JCR Impact Factor (IF) – 2.1
5-Year Impact Factor – 2.2
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Index Copernicus  – 161.11; MEiN – 140 pts

ISSN 1899–5276 (print)
ISSN 2451-2680 (online)
Periodicity – monthly

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Advances in Clinical and Experimental Medicine

2017, vol. 26, nr 9, December, p. 1319–1327

doi: 10.17219/acem/65507

Publication type: original article

Language: English

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Application of an anionic polymer in the formulation of floating tablets containing an alkaline model drug

Dorota Wójcik-Pastuszka1,B,C,D,E,F, Iwona Golonka1,B,C,D, Andrzej Drys1,C,D, Jobst B. Mielck2,E,F, Maria Twarda1,B,D, Witold Musiał1,A,B,C,D,E,F

1 Department of Physical Chemistry, Wroclaw Medical University, Poland

2 Institut für Pharmazie, Abteilung Pharmazeutische Technologie, Hamburg, Germany

Abstract

Background. Gastric residence time is the key factor affecting the bioavailability of active pharmaceutical ingredients absorbed mainly through the gastric mucous membrane and influencing the local activity of some drugs.
Objectives. The aim of this study was the development of a new composition of non-effervescent floating tablets and the evaluation of the effect of an anionic polymer and compressive force on the floating properties and release characteristics of tablets containing a model alkaline drug, chlorhexidine (CHX).
Material and Methods. Direct compression was applied to a polyacrylic acid derivative and sorbitol to fabricate the tablets. Drug release was analyzed using several kinetic models. The formulations floated on the surface of the fluid for 24 h. The values of the rate constants, statistical parameters, and half-release time (t0.5) were calculated.
Results. The diffusion coefficient n falls between 0.54 ±0.02 and 0.81 ±0.03 for most formulations. The floating time (FT) and floating lag time (FLT) were found to depend on the amount of polymer incorporated in the formulations. A high compressive force sustained the release of the drug but reduced the FT and FLT. Based on the FT and t0.5, it was determined that the C1 composition is the optimal formulation with FT >24 h and t0.5 between 113 ±2 and 144 ±13 min, depending on the drug release model.
Conclusion. The application of an anionic polymer results in a prolonged release of the drug from the tablets and allows them to float on fluid surfaces.

Key words

chlorhexidine, carbopol, floatation, kinetics of drug release

References (30)

  1. Kagan L, Hoffman A. Systems for region selective drug delivery in the GI tract: Biopharmaceutical considerations. Expert Opin Drug Deliv. 2008;5:681–692.
  2. Sood A, Panchagnula R. Design of controlled release delivery systems using a modified pharmacokinetic approach: A case study for drugs having a short elimination half-life and a narrow therapeutic index. Int J Pharm. 2003;261(1–2):27–41.
  3. Klausner EA, Eyal S, Lavy E, Friedman M, Hoffman A. Novel levodopa gastroretentive dosage form: In vivo evaluation in dogs. J Control Release. 2003;88:117–126.
  4. O’Reilly S, Wilson CG, Hardy JG. The influence of food on the gastric emptying of multiparticulate dosage forms. Int J Pharm. 1987;34:213–216.
  5. Sangekar S, Vadino WA, Chaudry I, Parr A, Beihn R, Digenis G. Evaluation of effect of food and specific gravity of tablets on gastric retention time. Int J Pharm. 1987;35(3):187–191.
  6. Khosla R, Feely LC, Davis SS. Gastrointestinal transit of non-disintegrating tablets in fed subjects. Int J Pharm. 1989;53(2):107–117.
  7. Natarajan R, Kaveri N, Rajndran NN. Formulation and evaluation of aceclofenac gastro retentive drug delivery system. Res J Pharm Biol Chem Sci. 2011;2(1):765–771.
  8. Rangapriya M, Manigandanm V, Natarajan R, Mohankumar K. Formulation and evaluation of floating tablets of pioglitazone hydrochloride. Int J Pharm Chem Sci. 2012;1(3):1048–1054.
  9. Baru CR, Vidyadhara S, Rao KVR, Prakash KV, Umashankar B. Formulation and evaluation of ibruprofen floating tablets. Int J Pharm Chem Biol Sci. 2012;2(4):472–481.
  10. Narendra C, Srinath MS, Babu G. Optimization of bilayer floating tablet containing metoprolol tartrate as a model drug for gastric retention. AAPS Pharm Sci Tech. 2006;7(2):E34.
  11. Sauzet C, Claeys-Bruno M, Nicolas M, Kister J, Piccerelle P, Prinderre P. An innovative floating gastro retentive dosage system: Formulation and in vitro evaluation. Int J Pharm. 2009;378:23–29.
  12. Rani SB, Hari VBN, Reddy BA, Punitha S, Devi P, Rajamanickam V. The recent developments on gastric floating drug delivery systems: An overveiw. Int J Pharm Tech Res. 2010;2(1):524–534.
  13. Jamil F, Kumar S, Sharma S, Vishvakarma P, Singh L. Review on stomach specific drug delivery systems: Development and evaluation. Int J Res Pharm Biomed Sci. 2011;2(4):1427–1433.
  14. Bijumol C, William H, Kurien J, Kurian T. Formulation and evaluation of floating tablets of theophylline. Hygeia J D Med. 2013;5(1):23–31.
  15. Jeganathan B, Prakya V. Preparation and evaluation of floating extended release matrix tablet using combination of polymethacrylates and polyethylene oxide polymers. Int J Pharm Pharm Sci. 2014;6(8):584–592.
  16. Russell TL, Beradi RR, Barmett JL, et al. Upper gastrointestinal pH in seventy-nine healthy, elderly, North American men and women. J Pharm Res. 1993;10(2):187–196.
  17. Council of Europe. European Pharmacopoeia Commission. Uniformity of mass of single-dose preparations (Chapter 2.9.5.). In: European Pharmacopoeia. 6th ed. Strasburg: Council of Europe;2007:278.
  18. Council of Europe. European Pharmacopoeia Commission. Friability of uncoated tablets, harmonised (Chapter 2.9.7.). In: European Pharmacopoeia. 6th ed. Strasburg: Council of Europe; 2009:1500.
  19. Council of Europe. European Pharmacopoeia Commission. Resistance to crushing of tablets (Chapter 2.9.8.). In: European Pharmacopoeia. 6th ed. Strasburg: Council of Europe; 2007:279.
  20. The United States Pharmacopoeial Convention Inc. The United States Pharmacopeia 31st ed. and The National Formulary 26th ed. (USP–NF). Rockville, MD: USP; 2007:2161–2162.
  21. Musial W, Voncina B, Pluta J, Kokol V. The study of release of chlorhexidine from preparations with modified thermosensitive poly-N-isopropylacrylamide microspheres. Sci World J. 2012;2012:1–8.
  22. Korsemeyer RW, Gurny R, Doelker E, Buri P, Peppas NA. Mechanism of solute release from porous hydrophilic polymers. Int J Pharm. 1983;15:25–35.
  23. Hixon AW, Crowell JH. Dependence of reaction velocity upon surface and agitation. Ind Eng Chem. 1931;23:923–931.
  24. Higuchi T. Mechanism of sustained-action medication. Theoretical analysis of rate of release of solid drugs dispersed in solid matrices. J Pharm Sci. 1963;52:1145–1149.
  25. StatSoft, Inc. STATISTICA (data analysis software system), v. 10. 2011. Available from www.statsoft.com.
  26. Asane GS, Nirmal SA, Rasal KB, Naik AA, Mahadik MS. Polymers for mucoadhesive drug delivery system: A current status. Drug Dev Ind Pharm. 2008;34:1246–1266.
  27. Elkheshen SA. Interaction of verapamil hydrochloride with carbopol 934P and its effect on the release rate of the drug and the water uptake of the polymer matrix. Drug Develop Ind Pharm. 2001;27(9):925–934.
  28. Bonacucina G, Martelli S, Palmieri GF. Rheological, mucoadhesive and release properties of carbopol gels in hydrophilic cosolvents. Int J Pharm. 2004;282:115–130.
  29. Musial W, Kokol V, Voncina B. Deposition and release of chlorhexidine from non-ionic and anionic polymer matrices. Chem Pap. 2010;64(3):346–353.
  30. Jones DS, Brown AF, Woolfson AD, Dennis AC, Matchett LJ. Examination of the physical state of chlorhexidine within viscoelastic, bioadhesive semisolids using Raman spectroscopy. J Pharm Sci. 2000;89(5):563–571.
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