Selective coating of cylindrical matrices with a central hole. I. An interpretation of the swelling process

Cylindrical matrices were prepared by compression either of polyvinyl alcohol 100000 or mixtures of the excipient and a drug (sodium salicylate or theophylline). To modify the cylindrical shape, a hole was bored in the centre of the flat surface through both sides of the matrices. Different swellable systems were obtained applying an impermeable coating to one, two or three surfaces of the perforated matrices. The swelling of the perforated matrices was modified according to the number and the position of the coated surfaces (selective coating) and the loaded drug. Pseudo-zero order kinetics were obtained when the interior hole was the only uncoated surface.     

芳香PET树脂母粒的研制

通过丙烯酸和丙烯酸正丁酯溶液共聚合，得到丙烯酸－丙烯酸正丁酯共聚物，该树脂与环氧氯丙烷反应后再与PET树脂切片继续反应，可使PET树脂切片表面形成聚丙烯酸酯自膨润型吸油网络结构，将表面具有聚丙烯酸酯自身膨润型吸油网络结构的PET树脂切片（简称为留香剂）在油溶性香精中浸泡，香精就被吸附在留香剂表面，即得到芳香PET树脂母粒。用SEM观察了母粒的表面结构形态。     

Clinical office anesthesia: The use of propofol for the induction and maintenance of general anesthesia

Ambulatory surgery has become routine for many plastic surgery procedures. Anesthesia techniques including general anesthesia by inhalation and intravenous infusion and the dissociative technique have all been used successfully for outpatient anesthesia. Propofol (Diprivan), a relatively new agent, has proven to be a safe and effective general anesthesia agent for outpatient surgery. We report on our experience with propofol as an induction agent and continuous drip for general anesthesia maintenance in 100 consecutive outpatient, plastic surgery procedures performed in an office facility. Assessment factors were recovery-room time, nausea and vomiting in the recovery room and at home, hallucinations, patients' recollection of anesthesia experience, and overall patient satisfaction.     

微量地塞米松与抗病毒药物合用对抗单疱病毒作用的影响

报告在组织培养中地塞米松对单纯疱疹病毒(HSV)的生长繁殖无影响,对无环鸟苷(ACV)和环胞苷(CC)的抗病毒作用亦无干扰。在动物实验中,微量地塞米松[0.001%,常用浓度(0.1%)的百分之一]并不恶化上皮型HSV角膜炎。同时证明有效抗病毒药物的合用,微量地塞米松仍保留有良好的消炎作用,能促进上皮型和实质层型单疱角膜炎的痊愈过程。     

非糖皮质激素的免疫抑制方案对同种异体移植胰岛的保护作用

目的　评价非糖皮质激素的免疫抑制方案对防止大鼠同种异体胰岛移植排斥反应的效果。方法　大鼠同种异体胰岛移植后 ,分别应用他克莫司 (FK5 0 6 ) 霉酚酸酯 (MMF)和FK5 0 6 MMF 泼尼松 (Pred)行免疫抑制治疗两周 ,并设对照组 ,动态观察受者血糖、胰岛素及C肽变化 ,并作移植部位的形态学检测。结果　FK5 0 6 MMF组和FK5 0 6 MMF Pred组与对照组相比 ,移植胰岛存活时间明显延长 ,移植后 2个月在受者肝汇管区可见较多形态完整的胰岛细胞。FK5 0 6 MMF组维持术后正常血糖、胰岛素及C肽的时间超过 6 0d ,而FK5 0 6 MMF Pred组与前者比较 ,分泌C肽较少 (P <0 .0 5 ) ,血糖维持在较高水平 (P <0 .0 1) ,胰岛素水平两组差异无显著性。FK5 0 6 MMF Pred组停药两周以后的血糖水平较用药期间、停药两周内有明显降低 (P <0 .0 5 ) ,胰岛素和C肽分泌有所增多 ,但差异无显著性。结论　应用FK5 0 6 MMF和FK5 0 6 MMF Pred均有很强的免疫抑制效应 ,但糖皮质激素对胰岛细胞有毒性作用。小剂量FK5 0 6与MMF联用对移植胰岛细胞有较强的保护作用。     

特异性COX-2抑制剂保护骨关节炎软骨的临床观察

目的探讨特异性COX-2抑制剂对骨关节炎的关节软骨保护作用的临床研究。方法门诊选取膝关节骨关节炎患者80例,随机分为特异性COX-2抑制剂组和维骨力对照组,各40例,单盲给药。应用平均Womac关节炎指数评分和平均OA严重程度指数评定两组用药前后临床症状改善情况及使用血清软骨代谢标志物蛋白聚糖与型胶原和关节MRI进行检测关节软骨结构与功能的改变情况,并作统计学分析。结果经12个月治疗观察,特异性COX-2抑制剂组的平均Womac关节炎指数评分和平均OA严重程度指数在前3个月改善明显优于维骨力对照组(P<0.01),但在治疗12个月后,两组差异不显著(P>0.05);治疗12个月后特异性COX-2抑制剂组的软骨代谢指标蛋白聚糖和型胶原及关节MRI均显示组内变化显著(P<0.01),而与维骨力组对比结果无显著性差异(P>0.05)。结论特异性COX-2抑制剂对骨关节炎的软骨有保护和促进修复作用,兼有抗炎与保护软骨双重疗效,它是一类既能改善关节炎症状又能改善关节软骨结构的药物,值得临床广泛应用。同时本研究为其在临床应用和进一步研究此类药物提供了更好的理论基础和依据。     

Effect of chronic oral domperidone therapy on gastrointestinal symptoms and gastric emptying in patients with parkinson's disease

This study investigated whether domperidone could improve gastrointestinal symptoms in patients with Parkinson's disease who were receiving levodopa therapy. A total of 11 patients were studied. Following a baseline gastric emptying test, patients were treated with a starting dose of domperidone 20 mg p.o. q.i.d. A follow-up gastric emptying test was repeated at least 4 months after starting domperidone therapy. At the beginning and at each 3-month follow-up visit, symptoms of nausea, vomiting, anorexia, abdominal bloating, heartburn, regurgitation, dysphagia, and constipation were evaluated and scored on a scale of 0–3. The overall mean follow-up period was 3 years. Compared with their baseline evaluation, patients experienced a significant improvement in all symptoms (p < 0.05) except dysphagia and constipation. Gastric emptying of an isotope-labeled solid meal was significantly faster, with a baseline result of 60.2 ± 6.4% retention of isotope 2 h after the meal compared with 37.0 ± 2.2% retention during domperidone therapy (p < 0.05). Patients' global assessment of Parkinson's disease remained stable or improved. Serum prolactin was elevated in all patients after domperidone therapy (p < 0.05). Domperidone therapy significantly reduces upper gastrointestinal symptoms and accelerates gastric emptying of a solid meal, but does not interfere with response to antiparkinsonism treatment.     

Retrograde air insufflation in MRI: A technical note

Retrograde air insufflation was employed to distend the colon and the ileum in 18 patients and five volunteers for magnetic resonance examination. Good and moderate marking of the ileum was obtained in 18 cases. The colon was nearly completely distended in every case. Intraluminal tumor, mural thickening, and extraluminal lesion were outlined by intraluminal air and surrounding air-distended bowel. This study shows that retrograde air insufflation is a useful method to mark the colon and most parts of the ileum.     

可逆性胆硷酯酶抑制剂二甲氨基甲酸-5-二氢吲哚酯的合成

为了深入研究催醒宁类化合物的结构与抑酶活性的关系,设计合成了-系列1-,3-或5-位不同取代的二氢吲哚类衍生物(中间体和终产物共24个新化合物)。中间体1,3-二甲基-5-烷氧基-2-二氢吲哚酮(A)的C₃烷化。采用相转移催化方法进行;反应中还分离到三个副产物(Ⅶ～Ⅸ)。初筛结果表明:这些化合物大多有较强的抑酶活性;1,3-或5-位取代基的改变均明显影响其活性。     

抗棘球蚴药物研究:3-取代苯基-5-取代-1,2,4-噁二唑的合成

合成了3-取代苯基-5-取代-1,2,4-(口恶)二唑类化合物50个,经感染棘球蚴的小鼠初筛,部分化合物对棘球蚴有不同程度的作用,化合物13、28和30对棘球蚴的囊重抑制率分别为70、75.6和71.6%,其中化合物13对棘球蚴的生发层有损害作用。