Sri Aguswarini
PTPRR-PUSPIPTEK

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EVALUASI BIOLOGIS SENYAWA KOMPLEKS RENIUM-186 FOSFONAT SEBAGAI RADIOFARMAKA TERAPI PALIATIF KANKER TULANG Gunawan, Adang H.; Aguswarini, Sri; Abidin, Abidin; Karyadi, Karyadi; Bagiawati, Sri
Jurnal Radioisotop dan Radiofarmaka Vol 10 (2007): JURNAL PRR 2007
Publisher : Jurnal Radioisotop dan Radiofarmaka

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Abstract

EVALUASI BIOLOGIS SENYAWA KOMPLEKS RENIUM-186 FOSFONAT SEBAGAI RADIOFARMAKA TERAPI PALIATIF KANKER TULANG. Senyawa kompleks renium-186 fosfonat, 186Re-HEDP (hydroxyethylidienediphosphonate) dan 186Re-EDTMP (ethylenediaminetetramethylphosphonate), dewasa ini telah luas digunakan sebagai penghilang rasa nyeri tulang yang disebabkan oleh metastasis kanker prostat, payudara, paru-paru dan ginjal ke tulang. Penggunaan radiofarmaka tersebut merupakan pengganti penggunaan analgesik, hormon, kemoterapi, dan narkotik yang diketahui memberikan efek samping yang tidak diinginkan. Metode preparasi dan uji kualitas senyawa kompleks 186Re-HEDP dan 186Re-EDTMP telah dikembangkan untuk tujuan produksi komersial. Penentuan kemurnian radiokimia dengan kromatografi kertas dalam berbagai kepolaran pelarut menunjukkan kemurnian radiokimia diatas 90% sampai hari ketiga setelah proses penandaan dilakukan. Disamping itu hasil pengujian menunjukkan pula bahwa larutan senyawa kompleks bebas pirogen dan steril. Hasil uji pada binatang percobaan tikus putih menunjukkan kandungan senyawa kompleks di dalam darah mencapai puncaknya pada 5 menit setelah penyuntikan. Sedangkan ekskresi radiofarmaka kedua kompleks di dalam urin menunjukkan adanya keradioaktifan sekitar 41% dan 38,5 % dalam bentuk perenat, 186ReO4-, setelah 20 jam penyuntikan. Hasil biodistribusi dan pencitraan (imaging)menggunakan kamera gamma terhadap mencit dan tukus putih normal menunjukkan bahwa senyawa kompleks 186Re-HEDP dan 186Re-EDTMP terakumulasi cukup nyata di tulang. Kata Kunci : 186Re-HEDP , 186Re-EDTMP, kanker tulang, kemurnian radiokimia, biodistribusi. BIOLOGIC EVALUATION OF PHOSPHONATES COMPLEX LABELLED WITH RHENIUM-186 AS A BONE CANCER PALLIATIVE THEURAPEUTIC RADIOPHARMACEUTICAL. Currently, rhenium-186 phosphonate complexes are widely used as pain palliative agents due to bone metastasis caused by prostate , breast , lung and kidney cancers. Either 186Re-HEDP or 186Re-EDTMP has been used for replacing analgesic therapy, hormone therapy, chemotherapy and narcotic therapy . Preparation and quality control of 186Re-HEDP and 186Re-EDTMP complexes have been developed for commercial production purposes. Radiochemical purity was determined using paper chromatography and afforded maximum yielded for more than 90 % . Both complexes were stable for 3 days. Sterility and pirogenicity tests indicated that these compounds were sterile and pyrogen free. Rhenium-186 HEDP and 186Re-EDTMP complexes contents in the blood achieved optimum activity after 5 minutes post injection. Both complexes showed major renal clearance up to 41 % and 38,5 % as perrhenate ion within 20 hours post injection. Biodistribution pattern and gamma camera image of the injected complexes in rats were accumulated in the bone. Keywords : 186Re-HEDP, 186Re-EDTMP ,bone cancer, radiochemical purity, biodistribution.
UJI BIODISTRIBUSI DAN UJI PREKLINIS MIKROSFER GELAS-P-32 UNTUK PENGOBATAN KANKER Astuti, Laksmi Andri; Caniago, Djoharly; Pardede, Ratlan; Widjaksana, Widyastuti; Purwoko, Purwoko; Bagiawati, Sri; Setiyowati, Sri; Abidin, Abidin; Aguswarini, Sri
Jurnal Radioisotop dan Radiofarmaka Vol 6, No 2 (2003): Jurnal PRR 2003
Publisher : Jurnal Radioisotop dan Radiofarmaka

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Abstract

ABSTRAKUJI BIODISTRIBUSI DAN UJI PREKLINIS MIKROSFER GELAS-P-32 UNTUK PENGOBATAN KANKER.Radiofarmaka telah  menunjukkan  manfaat lebih unggul dan spesiflk biladibandingkan dengan teknik pelayanan kesehatan lain, terutama untuk keperIuan diagnosis dan terapi beberapa penyakit  mematikan seperti kanker. Mikrosfer gelas-P-32 ( P-32 GMS ) adalah  salah  satu sediaan  baru  radiofarmaka untuk terapi  dengan cara  radiasi  interna beberapa penyakit  kanker ganas  seperti  penyakit  kanker  hati. Mikrosfer  gelas-P-32 ini  disiapkan  dengan  cara  mengira diasikan mikrosfer gelas-P31dengan neutron di reaktor nuklir, kemudian sediaan disuntikkan ke daerah yang terkena kanker Untukmemudahkan  penyuntikan  pada  sediaan  ini  perlu ditambahkan larutan pensuspensi, yaitu campuran dari PVP 16 %, dekstrose 50% dan salin. Mengingat ukuran mikrosfer ini spesiflk yaitu 40-60 J.Ull  maka pemilihan jamm suntik perIu dilakukan agar P-32 GMS yang diinjeksikan maksirnal bisa masuk ke daerah sasaran, dan mikrosfer tidak mengalami kerusakan karena gesekan dengan permukaan dalam  jarum. Ujibiodistribusi perIu dilakukan untuk melihat apakah P-32 GMS yang telah diinjeksikan terak1.lmulasike daerah penyuntikan  atau  terdistribusi  ke organ - organ lain yang  tidak dikehendaki, Hewan percobaan yang dipakai  adalah  mencit dengan penyuntikan dilakukan  pada otot  paha  kanan. Hasil biodistribusi pada I, 3dan  24 jam  setelah  injeksi  menunjukkan 100% aktivitas P-32 GMS terakumulasi di daerah penyuntikan.Hasil biodistribusi pada 5 jam setelah penyuntikan menunjukkan adanya penimbunan  aktivitas di organ lambung selain penimbunan aktivitas di daerah penyuntikan, namun hal ini diduga karena terjadi kontaminasi akibat kesalahan kerja .Kata Kunci : Radiofarmaka, , Mikrosfer gelas, P-32,  iradiasi, uji biodistribusi , kanker. ABSTRACTBIODISTRIBUTION AND PRECLINICAL TEST OF P-32 GLASS MICROSPHERESFOR CANCER THERAPY. The superiority of  radiophannaceutical compare to the  other  techniques off medical services, especially for diagnosis and  therapy  of  several deadly diseases such as cancer, shows that this technique is more specific and accurate. P-32-Glass microsphere (P-32 GMS) is one of theradiophannaceuticals developed reccntly for therapy using  interrnal  radiation  method  for several malignant cancers, such as hepatic canccr. 111cP-32 GMS was prcpared by irradiating P-31 GMS with neutron at a nuclear reactor, then the preparation was injected to the cancerous infected  area. To make easy  injection, it needs suspension agent that was including PVP, dextrose and saline with a composition of 16% PVP - 50%dextrose - saline as 2 : 3 : 3 (v/v/v). As microsphere size should be maintained at 40-60 11m, the injectionneedle was selected properly in order to remain the particle size of P-32 GMS unchanged  when  the frictionoccurs between microspheres and the inside surfaces of the needle. The injection  needle  used  was needle produced  by BD with a typical size of 20 GI Tw. Biodistribution  studies were carried out after I, 3, 5 and24 hour of injection. Experimental results  for 1, 3 and 24 hour post -injection studies showed  that 100%activity of  P-32 GMS was accumulated  at  the  injected  area. For 5 hour post-injection study, accumulation of  P-32 GMS activity was also found at stomach besides the injected area, but it was presured as working error. Keywords: Radiophannaceutical , glass microspheres ,P-32,  biodistribution, , cancer.    
Uji Klirens dan Uji Pirogenitas sebagai Bagian dari Penentuan Mutu Biologi Sediaan 90Y-EDTMP Sulaiman, Sulaiman; Aguswarini, Sri; Karyadi, Karyadi; Chairuman, Chairuman; Setiawan, Gatot; HG, Adang; Subur, M.
Jurnal Kefarmasian Indonesia VOLUME 8, NOMOR 2, AGUSTUS 2018
Publisher : Pusat Penelitian dan Pengembangan Biomedis dan Teknologi Dasar Kesehatan

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.22435/jki.v8i2.352

Abstract

Cancer is one of the causes of death in Indonesia and even the world. Nuclear medicine techniques with radiopharmaceuticals and SPECT are one of the ways to treat cancer, but their use in Indonesia is not yet popular. Radiopharmaceuticals marked with radionuclide emitting beta (β) radiation are proven to be used for cancer therapy, one that has been developed in PTRR-BATAN is 90Y-EDTMP. Yttrium-90 is used in nuclear medicine by utilizing β radiation (E max 2.28 MeV). The β energy which is produced from the decay process of 90Y radionuclides to 90Zr can kill cancer cells. This study aimed to provide information about the substances biological effects so that preventive measures can be taken to protect humans. This study conducted evaluation of the 90Y-marked radiopharmaceutical (90Y produced from a 90Sr / 90Y generator which is 90Y-EDTMP) encompasses clearance test, pyrogen test, and dose safety test in experimental animals. The clearance test utilized mice, the pyrogen test utilized rabbits, and the dose safety test utilized mice. The results of the clearance test showed that 90Y-EDTMP compound which was excreted in 192 hour was 49.70% through urine and 14.59% through feces. The total excretion of 90Y-EDTMP within 192 hours was 64.57%. Based on the results of clearance tests with calculations, 90Y of 90Sr / 90Y generators in 90Y-EDTMP dosage form had 84.2 hours of half-life, 36.5 hours of an effective half-life and 52.7 hours of a residence time. Pyrogen test results showed pyrogen-free. The 90Y-EDTMP dose safety test showed that the dose is safe and not deadly. The development of 90Y-EDTMP is expected to be improved to produce radiopharmaceuticals for cancer therapy in order to make a real contribution in public health services.