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Stomach-specific anti-H. pylori therapy; part III: effect of chitosan microspheres crosslinking on the gastric residence and local tetracycline concentrations in fasted gerbils.
Int J Pharm. 2004 Mar 19; 272(1-2):99-108.IJ

Abstract

The main objective of the present study was to examine the effect of chemical crosslinking of chitosan microspheres on the gastric residence and local tetracycline concentrations following oral administration in fasted gerbils. Radioiodinated [125I] glyoxal-crosslinked chitosan microsphere suspension in deionized distilled water was administered for the gastric residence studies. At different time points, the animals were sacrificed and the radioactivity in tissues and fluids was measured. Stomach tetracycline concentrations were determined using tritiated-[3H]-tetracycline-loaded crosslinked chitosan microspheres. The radioactivity, measured with a liquid scintillation analyzer, was used to determine the microgram of drug per gram of tissues or fluids. After 2 h in the fasted stomach, approximately 10% of the non-crosslinked chitosan microspheres remained. On the other hand, 17% of the crosslinked chitosan microspheres remained in the fasted stomach after the same time period. The microspheres were predominantly found in the colon after 6 h of administration. There was no detectable radioactivity in the plasma, urine, small intestine, liver, and kidneys. Tetracycline concentration profile in the stomach from the crosslinked microsphere formulation was higher than that of the aqueous solution and the non-crosslinked microsphere formulation. While the area-under-the-curve (AUC(0.5-->10 h)) for tetracycline solution and non-crosslinked chitosan microspheres was 447.3 and 358.2 microg h/g of tissue, respectively, the AUC(0.5-->10 h) for the crosslinked chitosan microspheres was 868.9 microg h/g of tissue. The drug was predominantly found in the colon and urine after 6 h of administration. Results of this study show that chitosan microspheres prepared by chemical crosslinking provide a longer residence time in the fasted gerbil stomach than either tetracycline solution or microspheres prepared by ionic precipitation.

Authors+Show Affiliations

Department of Pharmaceutical Sciences, School of Pharmacy, Northeastern University, Boston, MA 02115, USA. Radi71@yahoo.comNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

15019073

Citation

Hejazi, Radi, and Mansoor Amiji. "Stomach-specific anti-H. Pylori Therapy; Part III: Effect of Chitosan Microspheres Crosslinking On the Gastric Residence and Local Tetracycline Concentrations in Fasted Gerbils." International Journal of Pharmaceutics, vol. 272, no. 1-2, 2004, pp. 99-108.
Hejazi R, Amiji M. Stomach-specific anti-H. pylori therapy; part III: effect of chitosan microspheres crosslinking on the gastric residence and local tetracycline concentrations in fasted gerbils. Int J Pharm. 2004;272(1-2):99-108.
Hejazi, R., & Amiji, M. (2004). Stomach-specific anti-H. pylori therapy; part III: effect of chitosan microspheres crosslinking on the gastric residence and local tetracycline concentrations in fasted gerbils. International Journal of Pharmaceutics, 272(1-2), 99-108.
Hejazi R, Amiji M. Stomach-specific anti-H. Pylori Therapy; Part III: Effect of Chitosan Microspheres Crosslinking On the Gastric Residence and Local Tetracycline Concentrations in Fasted Gerbils. Int J Pharm. 2004 Mar 19;272(1-2):99-108. PubMed PMID: 15019073.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Stomach-specific anti-H. pylori therapy; part III: effect of chitosan microspheres crosslinking on the gastric residence and local tetracycline concentrations in fasted gerbils. AU - Hejazi,Radi, AU - Amiji,Mansoor, PY - 2003/09/18/received PY - 2003/12/01/revised PY - 2003/12/01/accepted PY - 2004/3/17/pubmed PY - 2004/7/29/medline PY - 2004/3/17/entrez SP - 99 EP - 108 JF - International journal of pharmaceutics JO - Int J Pharm VL - 272 IS - 1-2 N2 - The main objective of the present study was to examine the effect of chemical crosslinking of chitosan microspheres on the gastric residence and local tetracycline concentrations following oral administration in fasted gerbils. Radioiodinated [125I] glyoxal-crosslinked chitosan microsphere suspension in deionized distilled water was administered for the gastric residence studies. At different time points, the animals were sacrificed and the radioactivity in tissues and fluids was measured. Stomach tetracycline concentrations were determined using tritiated-[3H]-tetracycline-loaded crosslinked chitosan microspheres. The radioactivity, measured with a liquid scintillation analyzer, was used to determine the microgram of drug per gram of tissues or fluids. After 2 h in the fasted stomach, approximately 10% of the non-crosslinked chitosan microspheres remained. On the other hand, 17% of the crosslinked chitosan microspheres remained in the fasted stomach after the same time period. The microspheres were predominantly found in the colon after 6 h of administration. There was no detectable radioactivity in the plasma, urine, small intestine, liver, and kidneys. Tetracycline concentration profile in the stomach from the crosslinked microsphere formulation was higher than that of the aqueous solution and the non-crosslinked microsphere formulation. While the area-under-the-curve (AUC(0.5-->10 h)) for tetracycline solution and non-crosslinked chitosan microspheres was 447.3 and 358.2 microg h/g of tissue, respectively, the AUC(0.5-->10 h) for the crosslinked chitosan microspheres was 868.9 microg h/g of tissue. The drug was predominantly found in the colon and urine after 6 h of administration. Results of this study show that chitosan microspheres prepared by chemical crosslinking provide a longer residence time in the fasted gerbil stomach than either tetracycline solution or microspheres prepared by ionic precipitation. SN - 0378-5173 UR - https://www.unboundmedicine.com/medline/citation/15019073/Stomach_specific_anti_H__pylori_therapy L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378517303006677 DB - PRIME DP - Unbound Medicine ER -