Advances in Clinical and Experimental Medicine

Title abbreviation: Adv Clin Exp Med
JCR Impact Factor (IF) – 2.1
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ISSN 1899–5276 (print)
ISSN 2451-2680 (online)
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Advances in Clinical and Experimental Medicine

2013, vol. 22, nr 1, January-February, p. 41–45

Publication type: original article

Language: English

Pharmacokinetic Study of Hydroxypropylmethylcellulose Microparticles Loaded with Cimetidine

Badanie farmakokinetyczne mikrocząsteczek hydroksypropylometylocelulozy wypełnionych cymetydyną

Rozina Kousar1,2,B, Mahmood Ahmad1,A, Ghulam Murtaza2,C,D, Shujaat A. Khan2,B, Sabiha Karim3,E,F, Izhar Hussain2,E,F

1 Faculty of Pharmacy & Alternative Medicine, the Islamia University of Bahawalpur, Punjab, Pakistan

2 Department of Pharmaceutical Sciences, COMSATS Institute of Information Technology, Abbottabad, Pakistan

3 University College of Pharmacy, University of Punjab, Lahore, Pakistan


Objectives. The objective of this study was to assess the pharmacokinetic behavior of floating hydroxypropylmethylcellulose microparticles loaded with cimetidine (FMC) prepared using the non-solvent addition coacervation technique.
Material and Methods. Based on the physico-chemical characteristics of three formulations (FMC1, FMC2 and FMC3), FMC2 having a 1:3 ratio of cimetidine:HPMC was found optimum. For in vivo analysis, a new HPLC analytical method was developed and validated. The optimized formulations were subjected to in vivo studies to calculate the various pharmacokinetic parameters for developed optimized microparticulate formulation FMC3. The developed floating microparticles of cimetidine were further evaluated by in vivo experimentation.
Results. The bioavailability parameters were found as: Cmax 1508.79 ± 37.95 ng/ml, Tmax 3.67 ± 0.17 h and AUC 14366.19 ± 377.64 ng h /mL.
Conclusion. For prolonged drug release in the stomach, developed floating microparticles of cimetidine (FMC3) may be used, thereby improving the bioavailability and patient compliance.


Cel pracy. Ocena zachowania farmakokinetycznego pływających mikrocząstek hydroksypropylometylocelulozy wypełnionych cymetydyną (FMC), przygotowanych za pomocą techniki koacerwacji przez dodanie nierozpuszczalnika.
Materiał i metody. Na podstawie właściwości fizykochemicznych trzech preparatów (FMC1, FMC2 i FMC3) stwierdzono, że preparat FMC2 mający stosunek cymetydyny:HPMC 1:3 był optymalny. W analizie in vivo opracowano i zweryfikowano nową metodę analityczną HPLC. Zoptymalizowane związki badano in vivo w celu obliczenia parametrów farmakokinetycznych zoptymalizowanego preparatu FMC3 w postaci mikrocząstek. Opracowane pływające mikrocząstki cymetydyny oceniano dalej za pomocą doświadczeń in vivo.
Wyniki. Parametry biodostępności były następujące: 1508,79 Cmax ± 37,95 ng/ml, 3,67 ± 0,17 Tmax h AUC 14366,19 ± 377,64 ng h / ml.
Wnioski. Do przedłużonego uwalniania leku w żołądku opracowano pływające mikrocząstki cymetydyny (FMC3), które mogą być stosowane w celu poprawy biodostępności i stosowania się do zaleceń lekarskich przez pacjenta.

Key words

microparticles, hydroxypropylmethylcellulose (HPMC), cimetidine, pharmacokinetics, human plasma, HPLC method.

Słowa kluczowe

mikrocząstki, hydroksypropylometyloceluloza (HPMC), cymetydyna, farmakokinetyka, osocze ludzkie, metoda HPLC.

References (11)

  1. Kousar R, Khan SA, Ahmad M, Aamir MN, Murtaza G: Preparation and in vitro characterization of microparticles loaded with cimetidine: Analysis of dissolution data using DDSolver. Bull Chem Soc Ethiop, Submitted for Publication.
  2. Murata H, Kawano S, Tsuji S, Kamada T, Matsuzawa Y, Katsu K: Gastric acid suppression by combination therapy of ecabet sodium and cimetidine compared with cimetidine alone for gastric ulcer. J Gastroenterol Hepatol 2003, 18, 1029–1033.
  3. Yoshimatsu K, Ishibashi K, Yokomizo H, Umehara A, Yoshida K, Fujimoto T, Atanabe K, Otani T, Matsumoto A, Osawa G, Ogawa K: Can the survival of patients with recurrent disease after curative resection of colorectal cancer be prolonged by the administration of cimetidine? Gan Kagaku Ryoho 2006, 33,1730–1732.
  4. Ahmad M, Ahmad T, Sultan RA, Murtaza G: Pharmacokinetic study of nifedipine in healthy adult male human volunteers. Trop J Pharm Res 2009, 8, 385–391.
  5. Rasool F, Ahmad M, Khan HMS, Akhtar N, Murtaza G: The effect of binders on the bioavailability of ofloxacin tablets in animal model. Acta Pol Pharm-Drug Res 2010, 67, 185–189.
  6. Murtaza G, Ahmad M, Madni MA, Asghar MW: A new reverse phase HPLC method with fluorescent detection for the determination of salbutamol sulfate in human plasma. Bull Chem Soc Ethiop 2009, 23, 1–8.
  7. Rasool F, Ahmad M, Murtaza G, Khan HMS, Khan SA: Comparative bioavailability and pharmacokinetics of investigational eudragit® FS based colonic tabletted microparticles and marketed sustained release tablets of metoprolol. Accepted for publication in Trop J Pharm Res in 2011.
  8. Khan SA, Ahmad M, Murtaza G, Aamir MN, Rehman NU, Kousar K, Rasool F, Akhtar M: Low viscosity hydroxypropylmethylcellulose coated nimesulide floating microparticles. Trop J Pharm Res 2010, 9, 293–299.
  9. Rasool R, Ahmad M, Murtaza G, Khan HMS, Khan SA: Comparative dissolution study of metoprolol tartrate loaded PLGA (50:50) and PLGA (75:25) Microparticles. Asian J Chem 2011, 23, 3815–3818.
  10. Moreno RA, Oliveira C, Brum JL, Sverdloff CE, Domingues CC, Borges DC, Oliveira RA, Borges NC: Cimetidine quantification in human plasma by high-performance liquid chromatography coupled to electrospray ionization tandem mass spectrometry. Application to a comparative pharmacokinetics study. J Bioanal Biomed 2009, 1, 5–13.
  11. Kanto J, Allonen H, Jalonen H, Mantyla R: The effect of metoclopramide and propantheline on the gastrointestinal absorption of cimetidine. J Clin Pharmac 1981, 11, 629–631.