三氮唑核苷注射液与三种抗生素的配伍实验

三氮唑核苷与青霉素、头孢唑啉、头孢拉定在生理盐水中配伍,经观察无物理变化,经连续4h的紫外扫描,吸收曲线和吸收值基本无改变。因此认为在临床上混合静滴是可行的.     

氮酮和薄荷醇对联苯苄唑体外经皮渗透性的影响

目的：研究透皮促进剂氮酮和薄荷醇对外用抗真菌药联苯苄唑体外经皮渗透性影响。方法：在离体透皮实验装置上进行透皮吸收试验和贮库效应的研究，采用正交函数分光光度法消除皮肤浸出物的吸收干扰。结果：1％氮酮明显促进联苯苄唑经皮渗透作用，并可明显缩短时滞而增加贮库效应。结论：氮酮对亲脂性极强的药物联苯苄唑的促透皮吸收作用较强，而薄荷醇无明显的促透作用，但可增加贮库效应。     

含服复方磺胺甲唑治疗咽炎

大多数临床医师在治疗咽喉部炎症时,用复方磺胺甲唑(复方新诺明)，一般都是以“口服，每次2片，1日2次”开处方。其实复方磺胺甲唑按其药理作用在治疗咽炎时，宜含服而不宜口服。含服时抑菌作用明显优于口服，且副作用少，理由如下。口服时，磺胺甲唑在经肠道吸收后，虽然在血中与血浆蛋白结合率较低，血中游离型浓度较高，但由于部分药物在肝脏中被乙酰化而失效，使药效降低。而含服时，复方磺胺甲唑在唾液中溶解，产生游离型磺胺甲基异唑，浓度较高。经吞咽使唾液中高浓度的磺胺甲基异唑在咽部被咽部粘膜吸收，使局部药物浓度增高，抑菌效力增强。另外，经吞咽后进入胃肠的磺胺甲基异唑仍可被吸收入血液循环从而增强药物的抑菌效果。     

紫外分光光度法测定三氮唑核苷及其注射液含量

<正> 三氮唑核苷,又名病毒唑,是目前临抗床常用的有效抗病毒新药。其含量测定多采用常量定氮法,操作繁琐复杂,测定时间较长。本文根据三氮唑核苷分子中含有共轭双键,在紫外区有特征吸收,经扫描发现其水溶液最大吸收波长为206nm,用于三氮唑核苷及其注射液的含量测定,尚未见报道。本法结果准确,操作简便,灵敏度高,稳定性好,取得较满意结果。一、仪器与试药UV-265FW分光光度计(日本岛津)三氮唑核苷对照品(比旋度-36.4含量99.98％)三氮唑核苷(900702 901015江苏盐城制药厂 901001上海第六制药厂)三氮唑核苷注射液(900801 900803江苏扬州制药厂,901029 90103(江苏兴化制药厂901119 901121 江苏泰州制药厂)二、紫外吸收光谱的测定     

他巴唑透吸收的研究

他马唑为一口抗甲亢药，经胃肠吸收后主要在肝脏代谢，且有较大的副作用，作者设想将其制成透皮吸收制剂，以其减少用药量和副作用，经实验证明，本药可透过离体免波，透过药量与时间和施药浓度有关，A zone可促进其透皮吸收，本实验采用UV法测定他巴唑的药物浓度。     

盐酸特拉唑嗪贴剂的制备及质量控制

目的：制备盐酸特唑嗪贴剂，研究其耐热，耐寒性，刺激性及透皮吸收性能，方法：以PVA制备盐酸特拉唑嗪贴剂，小鼠皮为模型皮肤，采用Franz扩散池分别进行药物经皮释放试验和渗透试验，并测定了人体透皮速率。结果：盐酸特拉唑嗪贴剂耐热和耐寒性质良好。对皮肤无刺激性。体外释放速率为13．52ug.cm^-2.h^-1，体外透皮速率为11．87ug.cm^-2.h^-1，人体平均透平速率为11．25ug.cm^-2.h^-1，结论：盐酸特拉唑嗪贴剂是一种有效的控释型外用制剂。     

三种抗真菌药的临床应用

１伊曲康唑１．１相关药物动力学特性伊曲康唑（Ｌｔｒａｃｏｎａｚｏｌｅ）为亲脂性三唑类抗真菌药。口服１００～２００ｍｇ，１．５～４ｈ达Ｃｍａｘ，Ｔ１／２２０ｈ，连服２～４周达稳态，Ｔ１／２可延长至３０ｈ，餐间服药可明显提高吸收。其作用机制是与细胞色素Ｐ...     

三种常见致病菌耐药变迁及分析

观察综合医院４ａ间所分离的三种常见致菌耐药变化。结果表明，金黄色葡萄球菌青霉素、丁胺卡那霉素及苯唑青霉素耐药率呈逐年上升趋势，而对万古霉素、庆大霉素、氯霉素及头孢唑啉耐药率相对稳定；绿脓杆菌对羧苄青霉素、氯霉素耐药率也呈上升趋势，但对庆大霉素、多粘菌素耐药率呈下降趋势；克雷伯杆菌对庆大霉素、丁胺卡那霉素、氯霉素、氨苄青霉素、羧苄青霉及头孢唑啉的耐药在４ａ中均无明显变化。     

含服复方磺胺甲噁唑治疗咽炎

大多数临床医师在治疗咽喉部炎症时 ,用复方磺胺甲唑(复方新诺明 ) ,一般都是以“口服 ,每次 2片 ,1日 2次”开处方。其实复方磺胺甲唑按其药理作用在治疗咽炎时 ,宜含服而不宜口服。含服时抑菌作用明显优于口服 ,且副作用少 ,理由如下。口服时 ,磺胺甲唑在经肠道吸收后 ,虽然在血中与血浆蛋白结合率较低 ,血中游离型浓度较高 ,但由于部分药物在肝脏中被乙酰化而失效 ,使药效降低。而含服时 ,复方磺胺甲唑在唾液中溶解 ,产生游离型磺胺甲基异唑 ,浓度较高。经吞咽使唾液中高浓度的磺胺甲基异唑在咽部被咽部粘膜吸收 ,使局部药物…     

兰索拉唑在消化性溃疡病人中的药代动力学研究

目的在消化性溃疡病人中观察兰索拉唑的药代动力学的变化，进一步了解该药的代谢规律。方法选取经胃镜检查确诊为消化性溃疡的患者为试验组（Ｇ组，ｎ＝６）及健康志愿者为对照组（Ｃ组，ｎ＝６），口服兰索拉唑胶囊３０ｍｇ，定时取血通过高压液相方法测定血药浓度。利用３Ｐ８７药代动力学程序模拟药时曲线，计算药代动力学参数。结果兰索拉唑符合一房室模型。试验组中，５位患者的吸收速率常数Ｋα较对照组的Ｋα明显增加，吸收半衰期Ｔ１２α及达峰时间Ｔｍａｘ明显减少。血药浓度高峰Ｃｍａｘ有明显提高。而清除速率常数Ｋβ、清除半衰期Ｔ１２β也有较明显的差别，其表观分布容积Ｖ／Ｆ、清除率ＣＬ／Ｆ及血药浓度曲线下面积ＡＵＣ差别均不显著。１位幽门不全梗阻患者的药代动力学曲线表明吸收明显延迟。结论兰索拉唑口服后，分布广泛，代谢迅速。消化性溃疡患者应用时，其吸收速率和其排泄明显加快。血药浓度高峰明显增加，对于治疗该病可能具有重要的意义。     

Improvement of absolute bioavailability of normally poorly absorbed drugs: inducement of the intestinal absorption of streptomycin and gentamycin by lipid-bile salt mixed micelles in rat and rabbit

The effect of lipid—bile salt mixed micelles on the intestinal absorption of streptomycin and gentamycin was investigated in the loop of small and large intestine of rat. While bile salts micellar solutions did not enhance the absorption of aminoglycosides, their mixed micellar solutions including monoolein, oleic or lauric acid markedly enhanced their absorption. However, lecithin—bile salt mixed micellar solution did not affect the absorption. Pretreatment with mixed micellar solutions showed neither a direct action on the mucosal membrane nor a transient increase in permeability to aminoglycosides.Improvement of bioavailability in the rabbit was evaluated using various formulations and different routes of administration. In the rectal administration, not only mixed micellar solutions but also lyophilized mixed micelles powder improved bioavailability. The duodenal administration of mixed micellar solution, however, was not effective, indicating that enhanced absorption of drugs by mixed micelles may be more pronounced with rectal administration.     

干姜和白术挥发油提取工艺

目的研究干姜和白术挥发油的提取工艺。方法用共水回流冷凝法分别提取干姜和白术的混合挥发油、干姜挥发油以及白术挥发油 ,并将提取的挥发油经气相色谱 质谱 (GC MS)技术检测其主要成分。结果经GC MS分析 ,3种挥发油的主要成分一致 ,性质稳定。结论共水回流冷凝法对干姜和白术混合提取挥发油的工艺可行、简便 ,适合工业化生产     

基于分子对接技术的三元混合胶束对多西他赛的增溶效应及安全性

目的 为提高抗肿瘤药物多西他赛的水溶性,制备磷脂-胆酸钠-Soluplus?三元混合胶束包载多西他赛,结合分子对接仿真技术研究三元混合胶束的结构及形成机制.方法 采用薄膜分散法制备Soluplus?胶束、磷脂-胆酸钠二元混合胶束、磷脂-胆酸钠-Soluplus?三元混合胶束;采用芘荧光探针法测定不同胶束的临界胶束浓度值...     

核磁共振法测定非离子表面活性剂 HLB 值的研究 2.几种混合体系 HLB 值的测定与计算

本文应用核磁共振法(NMR)测定了几种混合体系的 HLB 值与混合体系中各组分的 HLB 值。实验结果表明,混合体系中各组分在核磁共振图谱中的积分曲线高度也具有加和性。混合体系的 HLB 值是体系中各组分 HLB 值的加权平均值。因此,对混合体系的 HLB 值可以应用 NMR 法直接测定,也可应用 NMR 法测定各组分的 HLB值,通过计算求得,计算值与实测值完全一致。     

Preparation and <Emphasis Type="Italic">in vitro</Emphasis> evaluation of povidone-sodium cholate-phospholipid mixed micelles for the solubilization of poorly soluble drugs

Mixed micelles made of polyvinylpyrrolidone (PVP), sodium cholate, and phospholipids were prepared to improve the solubility of poorly water-soluble drugs. Sylibin, a drug used in treating liver diseases, was incorporated into the mixed micelles. The formulation of sylibin containing PVP-sodium cholate-phospholipid mixed micelles with an optimized composition (PVP/sodium cholate/phospholipid/silybin = 3:3:4:1∼2 by weight) was obtained based on the study of pseudoternary phase diagrams. The critical micelle concentration was used to evaluate the micellar stability towards dilution. The results showed that addition of PVP to sodium-cholate-phospholipid mixed micelles increased stability. The solubility of sylibin in PVP-sodium cholate-phospholipid mixed micelles was higher than that in pure water or in sodium cholate-phospholipid mixed micelles. In a stability study, we found that PVP-sodium cholate-phospholipid mixed micelles showed good stability. After 3 months storage at 40°C, just 2.6% sylibin was lost with only minor changes of the particle size when compared to a reference formulation containing sodium cholate and phospholipid mixed micelles. In addition, the developed formulation significantly improved in vitro drug release. The time required to release 50% sylibin (t50%) from sodium cholate and phospholipid mixed micelles was 326 h, while the t50% from PVP-sodium cholate-phospholipid mixed micelles was only 51.1 h. Our results suggest that these mixed micelles might have significant potential application to the biomedical field.     

头孢噻肟钠注射液与4种注射液配伍稳定性考察

目的 探讨头孢噻肟钠注射液与4种常见注射液的配伍稳定性,以期为头孢噻肟钠注射液的临床合理利用提供一定的参考。方法 建立了头孢噻肟钠高效液相含量测定方法,考察了其与氨茶碱注射液、维生素B6注射液、地塞米松磷酸钠注射液和奥硝唑注射液配伍后含量、外观和溶液pH值的变化。结果 头孢噻肟钠注射液与地塞米松磷酸钠注射液配伍4 h 内外观、pH 值和含量均无明显变化。头孢噻肟钠与氨茶碱注射液配伍后,1 h时配伍溶液出现氨味,4 h时氨味更浓,含量也发生明显变化。头孢噻肟钠与维生素B6注射液配伍pH值虽无明显变化,但含量在2 h内就明显降低。头孢噻肟钠与奥硝唑注射液配伍后,2 h溶液外观发生了变化,在4 h时溶液变成了粉红色,含量明显降低。结论 头孢噻肟钠可与地塞米松磷酸钠注射配伍使用,与维生素B6注射液和氨茶碱注射液不宜配伍使用,若必须与奥硝唑配合,宜在配伍后1 h 内滴注完毕。     

Replacement of an NH(3) by an iminoether in transplatin makes an antitumor drug from an inactive compound

To investigate the modifications of antitumor activity and DNA binding mode of transplatin after replacement of one nonleaving group NH(3) by an iminoether group, trans-[PtCl(2)(Z-HN=C(OMe)Me)(NH(3)] and trans-[PtCl(2)(E-HN=C(OMe)Me)(NH(3)] complexes (differing in the Z or E configuration of iminoether, and abbreviated mixed Z and mixed E, respectively), have been synthesized. In a panel of human tumor cell lines, both mixed Z and mixed E show a cytotoxic potency higher than that of transplatin, the mean IC(50) values being 103, 37, and 215 microM, respectively. In vivo mixed Z is more active and less toxic than mixed E in murine P388 leukemia and retains its efficacy against SK-OV-3 human cancer cell xenograft in nude mice. In the reaction with naked DNA, mixed Z forms monofunctional adducts that do not evolve into intrastrand cross-links but close slowly into interstrand cross-links between complementary guanine and cytosine residues. The monofunctional mixed Z adducts are removed by thiourea and glutathione. The interstrand cross-links behave as hinge joints, increasing the flexibility of DNA double helix. The mixed Z, transplatin, and cisplatin interstrand cross-links, as well as mixed Z monofunctional adducts are not specifically recognized by HMG1 protein, which was confirmed to be able to specifically recognize cisplatin d(GpG) intrastrand cross-links. These data demonstrate that the DNA interaction properties of the antitumor-active mixed Z are very similar to those of transplatin, thus suggesting that clinical inactivity of transplatin could not depend upon its peculiar DNA binding mode.     

Epidemiology, diagnosis and management of mixed mania

The presence of depressive symptomatology during acute mania has been termed mixed mania, dysphoric mania, depressive mania or mixed bipolar disorder. Highly prevalent, mixed mania occurs in at least 30% of bipolar patients. Correct diagnosis is a major challenge. The DSM diagnostic criteria, the most widely adopted clinical convention, require a complete manic and complete depressive syndrome co-occurring for at least 1 week. However, recent alternative categorical and dimensional studies of manic phenomenology have shown that there are certain depressive symptoms or constellations that have special clinical importance when describing mixed states, such as depressed mood and anxiety symptomatology that do not overlap with manic symptoms. Patients with mixed mania are over-represented in the subgroup with severe and treatment-resistant symptoms. The course and prognosis of mixed mania are worse than that of pure manic forms in the medium and long term, with higher recurrence rates, higher frequency of co-morbid substance abuse and greater risk of suicidal ideation and attempts. Moreover, mixed manic episodes are usually associated with increased depression during follow-up, greater risk of rapid cycling course and higher prevalence of physical co-morbidities, principally related to thyroid function. All these factors are very relevant to selection of treatment. There are three crucial steps in the treatment of mixed mania--making the correct diagnosis, starting treatment early, and considering not only the acute state but also maintenance treatment and the patient's long-term outcome. Although challenging, acute mixed episodes are treatable. To date there have been no controlled studies devoted exclusively to treatment of mixed mania, and the only controlled data available therefore derive from sub-analyses of randomised clinical trials. Both short-term and maintenance treatments of patients with mixed mania require experience and usually involve the combination of different treatments. As a general rule, there is some consensus about discontinuing antidepressants during mixed mania. Olanzapine, aripiprazole or valproate semisodium (divalproex sodium) are first-line drugs for mild episodes; severe episodes of mixed mania usually require treatment with a combination of valproate semisodium or lithium plus an antipsychotic, preferably an atypical agent. Carbamazepine is also useful for the treatment of mixed mania. High-dose medications are sometimes needed to control the episode, and time to remission is usually longer than in pure mania. Importantly, patients with mixed manic episodes have more adverse events of psychopharmacological treatment. In some cases, electroconvulsive therapy is required.     

丙泊酚mPEG-PLA/普朗尼克混合胶束的制备和性质(英文)

采用生物相容性聚合物胶束材料聚乙二醇-聚乳酸(mPEG-PLA)和普朗尼克P105(P105),构建了全新的混合胶束体系,用于提高难溶性麻醉药—丙泊酚的溶解度。相对于单纯由mPEG-PLA构建的载药胶束,该载药混合胶束能有效提高药物溶解度。最优化处方为mPEG-PLA:P105:丙泊酚=10:4:5(w/w/w),粒径约为90nm,多分散指数为0.2左右。载药混合胶束中游离药物浓度显著低于市售品脂肪乳(P<0.05)。此混合胶束于4oC条件下放置6个月,其粒径、多分散指数、游离药物浓度和载药量均无明显变化,说明4oC条件下该体系在6个月内是稳定的。混合胶束在各时间点的体外释放百分率显著高于市售品脂肪乳,这可能有利于更快发挥药效。睡眠/苏醒试验结果表明,混合胶束、单一胶束以及市售品脂肪乳的翻正反射消失时间和恢复时间没有显著性差异(P>0.05)。上述结果表明该混合胶束有望成为静脉给药系统应用于临床。     

注射用盐酸头孢甲肟在5%转化糖注射剂中的稳定性

目的考察注射用盐酸头孢甲肟在5%转化糖注射剂中的稳定性。方法分别于25、37℃条件下,采用双波长分光光度法测定24 h内5%转化糖注射剂中盐酸头孢甲肟的含量,观察配伍液外观并测定pH值和微粒数。结果在25℃条件下,配伍液中盐酸头孢甲肟含量6 h内无明显变化,配伍液外观、pH值无明显变化,微粒数符合规定;但在37℃条件下,盐酸头孢甲肟含量4 h内下降19.43%,配伍液颜色加深,pH值有一定程度上升。结论 5%转化糖注射剂可以用作注射用盐酸头孢甲肟的稀释剂,但应注意环境温度对配伍液稳定性的影响。