Development of microbial trigger based oral formulation of Tinidazole and its Gamma Scintigraphy Evaluation: A promising tool against anaerobic microbes associated GI problems.
Tinidazole is a versatile anti-amoebic and anti-anaerobic drug used in treatment of intestinal infection. The aim of present study was to develop and evaluate a guar gum based novel target release Tinidazole matrix tablet in animal models and healthy human volunteer using Gamma Scintigraphy technique. Anti-anaerobic and anti-protozoal activity of the developed formulation was studied in vitro against Bacteroides fragilis and Dentamoeba fragilis. Tinidazole was successful radiolabelled with (99m)Tc-pertechnetate using stannous chloride as a reducing agent and stable up to 24h in normal saline and serum. Radiolabeled formulation was evaluated in 6 Newzealand white rabbits by gamma Scintigraphy in static manner up to 24h for its retention in gastrointestinal tract (GIT). Similar set of study was conducted in 12 healthy human volunteers for similar objective Scintigraphy images of healthy human volunteer showed retention of optimized formulations in stomach up to 60min, from where it moved to duodenum further and reached ileum in around 5h. However, initiation of drug release was observed from intestine at 7h. Complete dissociation and release of drug was observed at 24h in colon due to anaerobic microbial rich environment. Results drawn from Scintigraphy images indicate that radiolabeled (99m)Tc-Tinidazole tablet transit through upper part of GI without disintegration. Hence the developed matrix tablet may have a role in treatment of intestinal infection caused by anaerobic bacteria.
Department of nuclear medicine, INMAS-DRDO, Timarpur, Delhi 110054, India.
Braj Gaurav
BG
Sharma
Department of nuclear medicine, INMAS-DRDO, Timarpur, Delhi 110054, India.
Neeraj
N
Kumar
Department of nuclear medicine, INMAS-DRDO, Timarpur, Delhi 110054, India.
Dhruv Kumar
DK
Nishad
Dr. D. Y. Patil Institute of Pharmaceutical Sciences & Research, Pune, Maharashtra 411018, India.
Naveen K
NK
Khare
Department of nuclear medicine, INMAS-DRDO, Timarpur, Delhi 110054, India.
Aseem
A
Bhatnagar
D000328:Adult; D001421:Bacteria, Anaerobic / Q000187:drug effects*; D001424:Bacterial Infections / Q000188:drug therapy*; D001441:Bacteroides fragilis / Q000187:drug effects; D002626:Chemistry, Pharmaceutical; D016503:Drug Delivery Systems / Q000379:methods; D005685:Galactans / Q000648:ultrastructure; D005720:Gamma Rays; D041981:Gastrointestinal Tract / Q000382:microbiology*; D006801:Humans; D008297:Male; D008351:Mannans / Q000648:ultrastructure; D053149:Plant Gums; D011877:Radionuclide Imaging / Q000379:methods; D013607:Tablets / Q000627:therapeutic use; D014011:Tinidazole / Q000627:therapeutic use*; D055815:Young Adult
D005685:Galactans; D008351:Mannans; D053149:Plant Gums; D013607:Tablets; D014011:Tinidazole; C007894:guar gum
(99m)TC-pertechnatate; Bacteriodes fragilis; Gamma scintigraphy; Gastrointestinal tract; Guar gum; Matrix tablet; Tinidazole