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흰쥐에서의 신규 항암제 BR-28702-2 의 체내동태
용철순(Chul Soon Yong),이신웅(Shin Woong Lee),전철수(Chul Soo Jun),채희상(Hee Sang Chai),신원섭(Won Sup Shin),백우현(Woo Hyun Paik) 한국응용약물학회 1995 Biomolecules & Therapeutics(구 응용약물학회지) Vol.3 No.2
The purpose of this study was to determine pharmacokinetic parameters of BR-28702-2, a new antineoplastic agent which is the conjugate of nucleotide and phospholipid, and to compare them with those of ara-C. Male rats were cannulated in the left femoral vein and received a single i.v. bolus dose of either BR-28702-2 or ara-C. BR-28702-2 was also administered i.p, and plasma samples were analyzed by reversedphase HPLC. The t_(½(β)) of ara-C(1.22 hr.) was significantly smaller than that of BR-28702-2(4.420 hr.). The absolute bioavailability of BR-28702-2 after i.p. injection was 1.125%. This lower bioavailability, together with previous reports that marked antineoplastic activity was observed when given i.p., indicates that BR-287022 would act as a depot system to release active moieties. Further works, therefore, need to be done to characterize active metabolites.
단순 포진 바이러스 감염 생쥐에 대한 아데닌 아라비노사이드와 그의 프레드니손 결합화합물인 BR-8702-AP 의 항바이러스 효과
신현종,백우현,채희상,신원섭 한국응용약물학회 1993 Biomolecules & Therapeutics(구 응용약물학회지) Vol.1 No.1
The therapeutic effectiveness of adenine arabinoside(ara-A) and its conjugate of prednisone(BR-8702-AP) was compared in Herpes simplex Virus Type 1 (HSV-1) infected BALE/c mice. The BALB/C mouse was infected with HSV-1(700 PFU/mouse) intranasally. Among mice infected intranasally with virus, a mortality rate of 100% was observed. On the oral administration of non-toxic doses of ara-A or BR-8702-AP(125 mg /kg/day) for 5 consecutive days 2 hours after virus infection, the ara-A was highly effective in reducing mortality to 0% (P<0.001) and BR-8702-AP was also effective in reducing mortality to 15% (P<0.01). In this model infection, the virus was first replicated in the lung and transmitted to the brain. Both ara-A and BR-8702-AP did not inhibit the viral replication in the lung, but they inhibited the viral transmission to the brain. However, the BR-8702-AP was less effective than the ara-A to prevent transmission of virus to brain. Therefore, the reduced mortality due to ara-A or BR-8702-AP therapy was associated with inhibition of viral transmission to brain.
용철순,이신웅,전철수,채희상,신원섭,백우현 영남대학교 약품개발연구소 1995 영남대학교 약품개발연구소 연구업적집 Vol.5 No.-
The purpose of this study was to determine pharmacokinetic parameters of BR-28702-2, a new antineoplastic agent which is the conjugate of nucleotide and phospholipid, and to compare them with those of ara-C. Male rats were cannulated in the left femoral vein and received a single i.v. bolus dose of either BR-28702-2 or ara-C. BR-28702-2 was also administered i.p. and plasma samples were analyzed by reversed-phase HPLC. The t_(L/2(β)) of ara-C(1.22 hr.) was significantly smaller than that of BR-28702-2(4.420 hr.). The absolute bioavailability of BR-28702-2 after i.p. injection was 1.125%. This lower bioavailability, together with previous reports that marked antineoplastic activity was observed when given i.p., indicates that BR-28702-2 would act as a depot system to release active moieties. Further works. therefore, need to be done to characterize active metabolites.