Labeling of new formulation of tin-sucralfate freeze-dried kit with technetium-99m and its biological evaluation

The present investigation deals with a simple preparation of new formulation of tin-sucralfate freeze-dried kit (F.D.K.), to be directly labeled with 99mTc at optimal pH value of 7.0. The lyophilized form containing 100 mg sucralfate and 11.3 mg dihydrated stannous chloride. Other optimal pH values of the preparation were found to be from 4.0 to 11.0. The range of sucralfate amount studied (50-500 mg) not affected the radiochemical purity of the labeled complex. The radiochemical purity and the stability of the labeled preparation that assessed by filtration were more than 95%. 99mTc sucralfate was radiochemical stable up to a specific activity of 1,000 mCi per gram which was more stable than earlier published value (700 mCi per gram) without any radiolytic decomposition. The biological behavior of 99mTc-pertechnetate was evaluated in two groups of animals, the first group (neither fasted nor ulcerated) and the second group (fasted and ulcerated mice). The data of organ distribution of 99mTc-sucralfate in ulcerated fasted mice showed that more than 99% of the administered dose was accumulated in the stomach (87.92%) and intestine (11.43%). The radioanalytical results together with the in vivo-biological behavior of the labeled preparation demonstrate it's stability, efficacy and usefulness in medical applications for the detection of gastrointestinal ulcers. (author)