Journal of Pharmaceutical Investigation

The Korean Society of Pharmaceutical Sciences and Technology (한국약제학회)
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Dissolution Rate Improvement of Tinidazole Tablets using PEO and HPMC

PEO와 HPMC를 이용한 티니다졸 정제의 용출율 개선

  • Published : 2009.02.20
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Abstract

A novel polymeric tablet of Tinidazole was formulated to treat Helicobacter pylori and Giardia lambria more efficiently, It was possible to reduce hepatotoxicity by controlling the release of Tinidazole after peroral administration. A gastric retentive formulation made of naturally occurring carbohydrate polymers and containing Tinidazole was tested in vitro for swelling and dissolution characteristics. Tinidazole tablets containing various concentration of either PEO or HPMC were prepared by the wet granulation method. In vitro release of Tinidazole at pH 1.2 and pH 6.8 buffer solutions was observed at $37^{\circ}C$ by using a KP dissolution method and an UV (313 nm) spectrophotometer. Compared to a commercial Tinidazole tablet, in vitro release of Tinidazole at both pH 1.2 and pH 6.8 buffer solutions significantly decreased as the concentration of PEO or HPMC in the tablet increased up. And the gastric retentive formulation hydrated and swelled back to about 50% of its original size in 30 min. Thus, it was possible to control the release of Tinidazole by changing the content of PEO or HPMC in the tablet, thereby manipulating the release rate and the retention of Tinidazole.

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References

  1. Antonio, A., Adriana, M. V., Edgard, F.C and Joaquim, M, Effect of different types of fundoplication on the gastric emptying of liquids and gastric compliance in rats, J. Pediatric Surgery, 40, 1551-1556 (2005) https://doi.org/10.1016/j.jpedsurg.2005.06.006
  2. Emmanuel, B.S., Michel, A., Simon, R., Sophie, H., Guillaume, S., Eric L. and Philippe, D, Modalities in Performing Capsule Endoscopy : Does it Influence Gastric Retention? Gastrointestinal Endoscopy, 61, AB160 (2005) https://doi.org/10.1016/S0016-5107(05)00891-6
  3. Joon Yun, A., Patrick, Y.L. and Kimberly, A.B., Clinical benefits of hydration and volume expansion in a wide range of illnesses may be attributable to reduction of sympathovagal ratio, Medical Hypotheses, 64(3), 646-650 (2005) https://doi.org/10.1016/j.mehy.2004.07.014
  4. Torrado, S., Prada, P. and Palooma M, de la Torre and Torrado, S., Chitosan-poly(acrylic) acid Polyionic complex: in vivo study to demonstrate prolonged gastric retention Biomaterials, 25(5), 917-923 (2004) https://doi.org/10.1016/S0142-9612(03)00579-9
  5. John, D., Smart, R.G., Riley, J.T., Simon, A., Young, F.C., Hampson, J. A. D., Grant, Kelly., Peted, W.D. and William, R.W, The retention of 14C-labelled Poly(acrylic acids) on gastric and oesophageal mucosa: an in vitro study. European Journal of Pharmaceutical Sciences, 20(1), 83-90 (2003) https://doi.org/10.1016/S0928-0987(03)00175-1
  6. J. E. F. Reynolds, Martindale-The Extra pharmacopoeia, Royal Pharmaceutical Society, London (1996)
  7. P. F. L. Boreham, R. E. Philips and R. W. Shepard, The sensitivity of Giardia intestinalis to drug in vitro, J. Antimicrob. Chemoth., 14, 449-461 (1984). https://doi.org/10.1093/jac/14.5.449
  8. D. R. Hill, R. Pohl and R.D. Pearson, Giardia lambria: A Culture method for determining parasite viability, Am. J. Trop. Med. Hyg., 35, 1129-1133 (1986) https://doi.org/10.4269/ajtmh.1986.35.1129
  9. P. H. Katelaris, A. Naeen and M. J. G. Farthing, Activity of metronidazole, azithromycin and 3-benzimidazoles on Giardia lambria Growth and attachment to a human intestinal-cell line, alimentary Pharmacol. Ther., 8, 187-192 (1994) https://doi.org/10.1111/j.1365-2036.1994.tb00277.x
  10. Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed., McGraw Hill, New York, pp. 957-960 (1996)
  11. S. Pyorala, S. Soback, V.Rainio, P. Silvennoinen and M. Nokelainen, Pharmacokinetics of single-dose administration of Tinidazole in unweaned calves, Am. J. Vetrinary Res., 55, 831-834 (1994)
  12. H. Salomies and J. P. Salo, An HPLC study of tinidazole hydrolysis, Chromatographia, 36, 79-82 (1992) https://doi.org/10.1007/BF02263842
  13. E. M. Sarkiala, S. E. A. Asikainen, A. Kanervo, J. Junttila and H. R. Jousimiessomer, The efficacy of Tinidazole in naturally-occuring periodontitis in dog-bacteriological and clinical results, Veterinary Microb., 367, 273-288 (1993) https://doi.org/10.1016/0378-1135(93)90094-N
  14. E. M. Sarkiala, Treatment of Perioontitis in dogs with Tinidazole, J. Small Animal practice, 34, 90-94 (1993) https://doi.org/10.1111/j.1748-5827.1993.tb02617.x
  15. L. Jokipii and A. M. M. Jokipii, Treatment of Giardiasis: Com-parative evaluation of ornidazole and Tinidazole as a single oral dose, Gastroenterology, 83, 399-404 (1982)
  16. P. Speelman, Single-dose Tinidazole for the treatment of giardasis, Antimicrob. Agents Chemother., 27, 227-229 (1985) https://doi.org/10.1128/AAC.27.2.227
  17. Snoeck, V., Huyghebaert, N., Cox, E., Vermeire, A., Saundeers, J., Remon, J. P., Verschooten, F. and Goddeeris, B.M., Gastrointestinal transit time of nondisintegrating radioopaque pellets in suckling and recently weaned piglets. Journal of Controlled Release, 94(1), 143-153 (2004) https://doi.org/10.1016/j.jconrel.2003.09.015