PLC法测定血浆中喷昔洛韦浓度

目的 :建立泛昔洛韦人体内活性代谢产物—喷昔洛韦血浆浓度测定方法。方法 :采用C18反相色谱柱 ,以0 0 2mol·L-1高氯酸 -甲醇 (4 5 0∶8)为流动相 ,荧光检测波长为λex=2 70nm ,λem=375nm ,内标物为阿昔洛韦 ,血浆样品采用 6mol·L-1高氯酸液沉淀蛋白。结果 :喷昔洛韦血浆浓度在 0 12 5～ 16mg·L-1范围内 ,与面积呈良好的线性关系 (r=0 9998) ;本试验最低检测浓度为 0 0 5mg·L-1,日内及日间RSD均小于 8% ,喷昔洛韦的方法回收率大于 90 %。结论 :该方法简便、准确、灵敏 ,可用于泛昔洛韦人体药代动力学及生物利用度的研究     

天银胶囊的制备工艺研究

目的优选天银胶囊最佳制备工艺。方法以干膏收率及天麻素、总黄酮醇苷、萜类内酯含量为评价指标,进行正交试验;并进行制粒工艺研究。结果最佳提取工艺为：70℃时,70%乙醇提取2次,每次2.0h,第1次加12倍量乙醇,第2次加8倍量乙醇;制粒工艺：75%乙醇作润湿剂,干膏粉∶辅料为1∶1。结论该工艺合理可行,适用于天银胶囊的制备。     

泛昔洛韦缓释微丸体内测定方法的建立及药动学研究

目的：建立泛昔洛韦（FCV）缓释微丸体内血药浓度的测定方法并进行体内药动学研究。方法：以甲醇和0.02mol/L磷酸二氢钾（9∶91）为流动相,选择6条家犬口服泛昔洛韦缓释微丸375mg后,利用高效液相色谱法（HPLC）测定6条家犬的血药浓度并对其进行药动学的研究。结果：本法的线性范围为0.1-10μg/ml,r=0.9943,日内及日间RSD均小于10%。FCV缓释微丸在体内的代谢产物喷昔洛韦（PCV）的tmax为（4.80±0.84）h,Cmax为（2.61±1.37）mg/L,AUC0→∞为（25.59±7.58）mg/h/L,MRT为（9.85±2.47）h。结论：本方法简便快速,无干扰,重现性好,可用于泛昔洛韦在体内的药动学研究,并且通过本实验的体内测定方法得到了家犬体内的药动学参数。     

内窥镜辅助下乳房聚丙烯酰胺水凝胶取出术

目的探讨内窥镜辅助下取出隆乳术后注射物的整形修复的临床应用与操作要点。方法N2006年1月至2012年10月,应用内窥镜辅助取出聚丙烯酰胺水凝胶注射隆乳术后35例70侧。行双侧腋窝切口或乳晕切口,内窥镜直视下取出注射材料,21例I期放置乳房假体。结果随访1年,术后恢复良好,无明显包块,无包膜挛缩。所有患者术后乳房无明显注射物残留,无血肿及感染。结论采用内窥镜辅助下行注射隆乳术后注射物取出整形修复术,手术在直视下进行,去除注射物较彻底,创伤较小;I期假体置入无明显影响,术后效果好,无明显并发症发生,是值得推广应用的辅助技术。     

高效液相色谱法测定人血浆中喷昔洛韦浓度

目的:建立测定人血浆中泛昔洛韦人体内活性代谢物喷昔洛韦的高效液相色谱法。方法:血浆样品用10%三氯醋酸沉淀蛋白。色谱柱为Zorbax SB-C18柱(150mm×4.6mm,5μm),流动相为0.02mol.L-1磷酸二氢钾溶液(pH7.0)-甲醇-乙腈(90∶10∶0.1),流速为1.0mL.min-1,紫外检测波长为254nm。结果:血浆中内源性物质对样品测定无干扰。本方法线性范围为0.05~5mg.L-1(r=0.999 4),最低定量质量浓度为0.05mg.L-1,方法回收率为100.1%~101.5%,日内、日间RSD均小于7%。结论:本法简便、灵敏、准确,适用于泛昔洛韦药动学的研究。     

The synthesis of a new probe for PET imaging reporter gene HSV1‐tk: 2‐amino‐6‐[18F] fluoro‐9‐ (4‐hydroxy‐3‐hydroxymethylbutyl) purine (6‐[18F]fluoropenciclovir)

The one step radiosynthesis of 2‐amino‐6‐ [¹⁸F]fluoro‐9‐(4‐hydroxy‐3‐hydroxymethylbutyl) purine (6‐[¹⁸F]fluoropenciclovir) 6 is reported. Radiolabeled product 6‐[¹⁸F]fluoropenciclovir 6 was prepared by radiofluorination of compound 4 with [¹⁸F]KF and isolated by a silica Sep‐Pak cartridge. The radiochemical yield of compound 6 was 45–55% decay corrected (d.c.) in six runs with radiochemical purity >98% and the radiosynthesis time was 35–42 min from end of bombardment (EOB). Copyright © 2006 John Wiley & Sons, Ltd.     

Recurrent herpes labialis: efficacy of topical therapy with penciclovir compared with acyclovir (aciclovir)

This study compares the effects of topical acyclovir and penciclovir in the treatment of recurrent herpes labialis. The study patients were a population of 40 patients with in excess of five recurrences annually, and were separated into four homogeneous groups each of 10 subjects. The antiviral creams were used to achieve total lesional cover, every 2 h during waking hours. The effects on the time to lesion crusting and to resolution of pain, were assessed. The results not only confirmed that aciclovir is ineffective, but confirmed that penciclovir is effective, and that penciclovir is superior to aciclovir.     

脂质体对喷昔洛韦经小鼠皮肤渗透的影响

 目的　研究脂质体对喷昔洛韦经小鼠皮肤渗透的影响。方法　采用薄膜分散法制备喷昔洛韦脂质体,采用改进的Franz扩散池体外经皮渗透实验技术,以高效液相色谱法测定皮肤接收液中、血液和皮肤内药物浓度。结果　喷昔洛韦脂质体凝胶在皮肤中的渗透系数及药物滞留量明显大于喷昔洛韦乳膏;在体条件下,1%喷昔洛韦脂质体最大皮肤内浓度是 1%喷昔洛韦乳膏的1.51倍;18h后1%喷昔洛韦脂质体皮肤内浓度是1%喷昔洛韦乳膏的1.94倍。结论　脂质体对喷昔洛韦经小鼠皮肤的渗透具有显著影响。     

嘌呤药物的热解过程及其热分解动力学

目的研究嘌呤类药物的热解过程及非等温动力学。方法用红外光谱技术、加速稳定性试验方法和热重仪分析方法测定分解过程,用Ozawa法以及Coast-Redfern法和MKN法处理数据确定热分解函数。结果确定了阿昔洛韦(aciclovir,Acv)、喷昔洛韦(penciclovir,Pcv)热解过程和中间产物,得到热解动力学参数活化能Ea、指前因子A。结论加速稳定性试验与热重法的计算结果一致,喷昔洛韦的热稳定性大于阿昔洛韦;两者热解第一步具有相同的中间产物鸟嘌呤,且动力学方程相同:dα/dt=Ae^-Ea/RT2(1-α)^3/2,均为1.5级反应过程。     

Inhibition of the replication of the DNA polymerase M550V mutation variant of human hepatitis B virus by adefovir, tenofovir, L-FMAU, DAPD, penciclovir and lobucavir

Several nucleoside analogues (penciclovir, lobucavir, dioxalane guanine [DXG], 1-β-2,6-diaminopurine dioxalane [DAPD], L-FMAU, lamivudine) and acyclic nucleoside phosphonate analogues (adefovir, tenofovir) that are in clinical use, in clinical trials or under preclinical development for the treatment of hepatitis B virus (HBV) infections, were evaluated for their inhibitory effect on the replication of a la- mivudine-resistant HBV variant containing the methionine → valine substitution (M550V) in the polymerase nucleoside-binding domain. The antiviral activity was determined in the tetracycline-responsive HepAD38 and HepAD79 cells, which are stably transfected with either a cDNA copy of the wild-type pregenomic RNA or with cDNA containing the M550V mutation. As expected, lamivudine was much less (≈ 200-fold) effective at inhibiting replication of the M550V mutant virus than the wild-type virus. In contrast, adefovir, tenofovir, lobucavir, L-FMAU, DXG and DAPD proved almost equally effective against both viruses. A second objective of this study was to directly compare the antiviral potency of the anti-HBV agents in HepG2 2.2.15 cells (which are routinely used for anti-HBV drug-screening purposes) with that in HepAD38 cells. HepAD38 cells produce much larger quantities of HBV than HepG2 2.2.15 cells, and thus allow drug screening in a multiwell plate format. All compounds were found to be almost equally effective at inhibiting HBV replication in HepAD38 cells (as in HepG2 2.2.15 cells), except for penciclovir, which was clearly less effective in HepAD38 cells.