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本文在Cumming等人1985年报道的基础上报道以硝基甲烷和丙酮为原料合成HM-PAO、meso和dl HM-PAO的分离、~(99m)Tc标记、冻干品药盒的制备,以及初步动物实验。MP(meso)148—149℃,(dl)127—129℃;元素分析(meso或dl)误差小于0.2％;MS(meso或dl)272(M~+);IR(meso或dl)3310(OH);UV(meso或dl)λ_(max)203.2nm;NMR(meso)δ0.78(6H,S,CH_3-C—CH_3),δ3.31(2H,q,-CH-),(dl)δ0.79(6H,S,CH_3-C-CH_3),δ3.14(2H,q,-CH-)。用HPLC方法鉴定meso和dl HM-PAO。HM-PAO的定量方法是紫外分光光度法(测量范围5—46μg/ml)。Sn(Ⅱ)的含量测定用电位滴定法(测量范围10—100μg)。HM-PAO冻干品药盒的pH、Sn(Ⅱ)含量,以及澄明度均合格。标记率大于90％(由两个薄层层析系统和一个纸层析系统测定)。初步动物实验采用meso和dl混合的HM-PAO。小鼠体内分布实验结果显示静脉注射之后,脑立即摄取~(99m)Tc-HM-PAO(6.56％D/g),并在脑内稳定停留至少1小时(4.13％D/g)。药物动力学模型拟合显示~(99m)Tc-HM-PAO在小鼠体内符合二室模型。血清除很快(Tα/λ=47.3min)。家兔γ照像的结果与小鼠体内分布实验结果一致,显像效果良好。
In this paper, Cumming et al reported in 1985 on the basis of nitromethane and acetone synthesis of HM-PAO, meso and dl HM-PAO separation, ~ (99m) Tc labeled, lyophilized kit preparation, and Preliminary animal experiments. MS (meso or dl) 272 (M ~ +); IR (meso or dl) 3310 (mso) OH); UV (meso or dl) λ max (max) 203.2 nm; NMR (meso) δ 0.78 (6H, s, CH 3 3- C-CH 3) ) δ 0.79 (6H, s, CH 3-C-CH 3), δ 3.14 (2H, q, -CH-). The meso and dl HM-PAO were identified by HPLC method. The quantitative method for HM-PAO is UV spectrophotometry (measuring range 5-46 μg / ml). The Sn (II) content was determined by potentiometric titration (measuring range 10-100 μg). HM-PAO freeze-dried product kit pH, Sn (Ⅱ) content, and clarity are qualified. Labeling rate> 90% (as determined by two thin layer chromatography systems and one paper chromatography system). Preliminary animal experiments using meso and dl mixed HM-PAO. The results of in vivo distribution in mice showed that immediately after intravenous injection, the brain ingested 99mTc-HM-PAO (6.56% D / g) and remained stable in the brain for at least 1 hour (4.13% D / g). Pharmacokinetic model fitting showed that ~ (99m) Tc-HM-PAO conformed to a two-compartment model in mice. Serum was removed rapidly (Tα / λ = 47.3 min). Rabbit γ-ray results and the distribution of the mice in vivo experimental results consistent, good imaging results.