EVALUASI DAN KARAKTERISASI KIT-KERING RADIOFARMAKA SIPROFLOKSASIN

EVALUASI DAN KARAKTERISASI KIT-KERING RADIOFARMAKA SIPROFLOKSASIN. Radiofarmaka 99mTc-siprofloksasin tersedia dalam bentuk kit-kering yang dikemas dalam dua flakon terpisah, masing-masing berisi ligan siprofloksasin laktat dan reduktor Sn-tartrat. Penyiapan radiofarmaka 99mTc-siprofloksasin dilakukan dengan menambahkan radionuklida 99mTc ke dalam larutan ligan siprofloksasin laktat diikuti dengan penambahan larutan reduktor Sn-tartrat. Untuk menjamin keberhasilan penyiapan dan penggunaan radiofarmaka ini diperlukan informasi tambahan bagi pengguna. Selain itu, penelitian ini dilakukan untuk memperoleh beberapa sifat fisikokimia dan biologis 99mTc-siprofloksasin yang dibuat dari kit-kering radiofarmaka siprofloksasin laktat. Pengujian kemurnian radiokimia dilakukan dengan cara instant kromatografi lapisan tipis (ITLC-SG) menggunakan aseton dan larutan diklorometan : metanol : amonium hidroksida : asetonitril (4:4:2:1) sebagai fase gerak. Ikatan protein plasma ditentukan secara in-vitro dengan metode pengendapan menggunakan larutan asam trikloro asetat (TCA) 5% dan lipofilisitas (P) 99mTc-siprofloksasin diketahui dengan menentukan koefisien partisinya dalam pelarut organik-air. Di samping itu, dilakukan juga pengujian pengaruh besarnya volume larutan Na99mTcO4 terhadap kemurnian radiokimia 99mTcsiprofloksasin. Dari hasil percobaan diperoleh bahwa sediaan 99mTc-siprofloksasin mempunyai kemurnian radiokimia 95,85 ± 2,10 %, ikatan protein plasma sebesar 58,35 ± 2,05 % dan lipofilisitas P = 0,024 ± 0,005. Pemakaian larutan Na99mTcO4 dengan volume lebih besar dari 2 mL memberikan kemurnian radiokimia lebih kecil dari 90 %. Dari hasil penyaringan 99mTc-siprofloksasin diperoleh rendemen penandaan sebesar 44,79 %. Penentuan stabilitas 99mTc-siprofloksasin dan kit-kering siprofloksasin dilakukan dengan melihat kemurnian radiokimianya. Radiofarmaka 99mTc-siprofloksasin masih dapat digunakan sampai 4 jam setelah penambahan teknesium-99m dengan kemurnian radiokimia 91,61 ± 1,60 %. Uji stabilitas kit kering siprofloksasin menunjukkan bahwa kit-kering tetap stabil sampai 5 bulan penyimpanan pada temperatur ± 4 oC.;

EVALUATION AND CHARACTERIZATION OF THE RADIOPHARMA-CEUTICAL LYOPHILIZED-KIT OF CIPROFLOXACIN. The 99mTc-ciprofloxacin radiopharmaceutical is available in the lyophilized-kit which is separately packed in two vials, ciprofloxacin lactate and Sntartrate, respectively. Preparation of 99mTc-ciprofloxacin was performed by adding 99mTc radionuclide into ciprofloxacin lactate solution, followed by addition of Sn-tartrate solution. The complement information was needed by user in order to assure the succesful preparation and utilization of this radiopharmaceutical. Meanwhile, this investigation was performed to obtaine the several physicochemical and biological characters of 99mTc-ciprofloxacin prepared from the radiopharmaceutical lyophilized-kit of ciprofloxacin lactate. The radiochemical purity was determined with instant thin layer chromatography (ITLC-SG) using aceton and solution of dichlorometane : methanol : ammonium hydroxide : acetonitrile : (4:4:2:1) as a mobile phases. The plasma binding protein of 99mTc-ciprofloxacin was investigated in-vitro by precipitation method using 5% of trichloro acetic acid solution, whereas the lipophilicity (P) was obtained by determination of octanol-water particion. Beside that, studies on the effect of volume of Na99mTcO4 solution to radiochemical purity of 99mTc-ciprofloxacin has been carried out. From the experiment, it was obtained that 99mTc-ciprofloxacin has 95.85 ± 2.10 % of radiochemical purity, the human plasma binding protein of 58.35 ± 2.05 % and the lipophilicity (P) = 0.024 ± 0.005. The volume more than 2 mL of Na99mTcO4 solution on the labelling of ciprofloxacin gave less than 90 % of radiochemical purity. The labelling efficiency of 44.79 % was obtained after filtration of 99mTc-ciprofloxacin. The stability test on 99mTc-ciprofloxacin and ciprofloxacin lyophilized-kit were performed by determining their radiochemical purities. The 99mTcciprofloxacin was still able to be used until 4 hours after labelling with radiochemical purity of 91.61 ± 1.60 %. The stability determination showed that the ciprofloxacin lyophilized-kit was remained stable 5 month of storage at 4 oC