硫酸双氢链霉素中链霉素残留量的测定方法

目的 建立硫酸双氢链霉素中链霉素残留量的检验方法。方法 通过对1977版中国药典方法、2002版欧洲药典方法和24版美国药典方法做标准工作曲线，将实验结果进行分析后确定用国内、外药典方法的优点，根据硫酸双氢链霉素中链霉素残留量质量指标，建立硫酸双氢链霉素中链霉素残留量的检验方法。结论 此项检验方法完全适用于硫酸双氢链霉素中链霉素残留量的测定。     

硫酸双氢链霉素提取工艺的改进研究

硫酸双氢链霉素属于氨基糖苷类抗生素,硫酸双氢链霉素目前主要生产工艺是发酵液经过过滤,利用树脂两次吸附解析除杂,进行氢化反应后第三次用树脂除杂,再经活性炭脱色、RO浓缩、喷雾干燥后得到产品。该工艺的主要缺点为三次树脂除杂导致的排污量大,污水处理成本高,鉴于此,课题提出了一条新的工艺路线,用纳滤膜替代了第三次树脂除杂。论文验证了用纳滤膜工艺替代152树脂工艺可行性：对新工艺下关键质量属性进行了评估研究,得到了可行的工艺路线。通过论文的研究和实践,使企业在硫酸双氢链霉素绿色生产工艺上取得了新的突破。     

吸收度线性组合法测定硫酸阿托品滴眼液的含量

本文应用吸收度线性组合分光光度法，不经分离直接测定硫酸阿托品（Atropine Sulfate)滴眼液的含量。以239、258及275nm波长为测试点，分别在各点滴定硫酸阿托品和尼泊金乙酯混合液的吸收度，通过各点的线性组合，计算硫酸阿托品的含量，其回收率为99．66％（CV％＝0．66）。     

吸收度线性组合法测定硫酸阿托品滴眼液的含量

本文应用吸收度线性组合分光光度法,不经分离直接测定硫酸阿托品(Atropine Sulfate)滴眼液的含量。以239、258及275nm波长为测试点,分别在各点测定硫酸阿托品和尼泊金乙酯混合液的吸收度,通过各点的线性组合,计算硫酸阿托品的含量,其回收率为99.66%(CV%=0.66)。     

活性炭纤维吸附塔用于硫酸庆大霉素脱色的中试研究

设计了用于硫酸庆大霉素脱色工艺的活性炭纤维(ACF)吸附塔(径高比为1∶4),进行动态吸附脱色和活化再生的中试研究,并考察中试工艺对成品质量的影响.结果表明,选用具有较高比表面积(2 000 m2/g)的ACF、装填2 kg的吸附塔,活化再生45次后吸附能力仍能达到初始吸附能力的80％.采用本中试工艺和现有767型药用活性炭脱色工艺分别处理平均效价为2.5×105 u/ml的庆大霉素转盐液2.25 m3,中试工艺的活性炭纤维累积单耗3.56g/(1×109 u),所得产品符合中国药典2010年版,而现有工艺的活性炭平均单耗为1 kg/(1×109 u).     

分子量对海参岩藻聚糖硫酸酯在体内吸收的影响

目的 利用高温高压降解法制备两种不同分子量的岩藻聚糖硫酸酯,探究口服不同分子量的海参岩藻聚糖硫酸酯的吸收特性。方法 采用分子排阻凝胶色谱法、离子高效液相色谱法,检测海参硫酸多糖高温高压降解前后分子量、硫酸根含量的变化,并利用PMP柱前衍生-高效液相色谱法测定岩藻聚糖硫酸酯的单糖组成,以及大鼠血清中单糖的变化。结果 口服低分子量海参岩藻聚糖硫酸酯后,大鼠血清中岩藻糖和半乳糖的吸收速度和最大浓度明显高于中分子量岩藻聚糖组,血清中甘露糖、氨基葡萄糖的含量也显著上升,血清中氨基半乳糖的含量略有上升。而口服中、低分子量岩藻聚糖硫酸酯都能够降低血清中葡萄糖的含量。结论 分子量低于10 kDa的低分子量岩藻聚糖具有很好的体内的吸收率,适合于开发口服岩藻聚糖功能产品。     

葡萄糖注射液在灭菌锅中的位置对其杂质吸收度的影响

葡萄糖灭菌时间过长,灭菌温度过高,可引起葡萄糖脱水,分解成5-羟甲基糠醛,其聚合物呈淡黄色,使葡萄糖颜色变黄,杂质吸收度增大,故我国药典1985年版规定了葡萄糖注射液在284nm波长处吸收度为0.32以下来控制其质量。据报道影响杂质吸收度的因素有灭菌压力、温度、时间、溶液的pH等。经过实验,我们选择了最佳条件:pH3.8～4.0,灭菌条件115℃,40mim。每批按药典葡萄糖项下进行检查,结果发现有时杂质吸收度合格,小于0.32,有时大于0.32,为说明这种情况,我们作了以下实验。     

硫酸沙丁胺醇控释胶囊释放度的HPLC测定

目的建立HPLC测定硫酸沙丁胺醇控释小丸胶囊释放度的方法.方法采用腈基键合硅胶柱(Spherisorb CN 25cm×4.6mm);以水-0.05mol/ml醋酸铵-异丙醇(30∶65∶5)为流动相;流速为2ml/min;检测波长为276nm.结果线性范围为0.48～19.20μg/ml,r=1.000;回收率为95.3%～99.5%,RSD<1.31%(n=6).结论本方法快捷、简便、准确,适合于本品释放度的检测.     

硫酸庆大霉素微囊霜剂的制备及体外透皮吸收的研究

本文研究了庆大霉素微囊霜剂制备及吸收过程。实验结果表明，庆大霉素微囊霜剂对家兔的皮肤刺激性小，比庆大霉素霜具有缓释、长效的功能，为临床用于Ⅱ度、深Ⅱ度烧烫伤及小面积创伤提供了一个较为理想的剂型。     

硫酸庆大霉素缓释片的制备及其体外释放度的试验研究

目的制备硫酸庆大霉素缓释片。方法以HPMC、丙烯酸树脂及十八醇作为辅料,采用湿颗粒制备硫酸庆大霉素缓释片。结果本品在2、4和6h的释放量限度分别为45%~70%、60%~85%与80%以上。结论硫酸庆大霉素缓释片在酸性溶液中具有显著的缓释作用。     

Liquid chromatographic analysis of dihydrostreptomycin sulfate

The analysis of dihydrostreptomycin sulfate using a column packed with base deactivated reversed phase silica gel and ultraviolet detection at 205 nm is described. The mobile phase consists of an aqueous solution containing 4 g/l of sodium sulfate, 1.5 g/l of sodium octanesulfonate, 100 ml/l of acetonitrile and 50 ml/l of a 0.2-M phosphate buffer at pH 3.0. The method allows separation of streptidine, dihydrostreptomycin B, streptomycin, dihydrostreptomycin and deoxydihydrostreptomycin, as well as some other components which were not identified. The total time of analysis is 55 min. The effects of the different chromatographic parameters on the separation were also investigated. A number of commercial samples were analyzed using this method.     

The influence of absorption enhancers on nasal absorption of acyclovir.

The objective of this work was to increase the nasal absorption of acyclovir by using absorption enhancers. Acyclovir was selected as a model drug. A rat in situ nasal perfusion technique was utilized in the investigation to examine the rate and extent of absorption of acyclovir. In vitro enzymatic drug degradation study was carried out with rat nasal washings. Various experimental conditions such as nasal perfusion rate, pH of the perfusion medium and concentrations of absorption enhancers such as sodium deoxycholate, hydroxypropyl beta-cyclodextrin, sodium caprate, sodium tauroglycocholate and EDTA were optimized. Nasal absorption of acyclovir was pH dependent. Initial absorption rate constants were determined by the plot of log% remaining amount of drug in perfusate vs time. It was found maximum at pH 7.4 and decreased at lower and higher pH conditions. In in vitro enzymatic degradation study, no measurable degradation was observed during first week. The extent of drug absorption was increased via absorption enhancers. In vivo studies were carried out for the optimized formulation in rabbits and the pharmacokinetics parameters of nasal solution were compared with oral solution. Hydroxypropyl beta-cyclodextrin appeared to be more effective for enhancing the nasal absorption of acyclovir than the other absorption enhancers. The order of increasing absorption of acyclovir caused by the enhancers was hydroxypropyl beta-cyclodextrin>sodium deoxycholate>sodium caprate>sodium tauroglycocholate>EDTA.     

The influence of enteral feedings on sustained-release theophylline absorption

In a randomized, crossover study the influence of enteral feedings (Ensure) on the absorption of theophylline from a sustained-release preparation (Theo-24) was evaluated. Six healthy, male subjects, age 22 to 37 years, participated. In phase 1 the subjects received a single oral dose of Theo-24 6 mg/kg with 100 ml of water at 8:00 A.M. In phase 2, they received 100 ml boluses of Ensure hourly, beginning 3 hours prior to the oral dose and continuing for a total of 1000 ml. In phase 3, subjects received a single 30-minute intravenous infusion of an equivalent dose of aminophylline. After each dose, serial blood samples were collected for 72 hours. No statistically significant differences in area under the curve (AUC infinity 0) (126.0 vs 127.3 micrograms hr/ml), maximum concentration (3.80 vs 4.08 micrograms/ml), or time to peak plasma level (13 vs 11 hrs) were found between phases 1 and 2. Mean AUC infinity 0 for the intravenous phase (161.4 micrograms hr/ml) was significantly higher than the AUC for either oral study (p less than 0.05). The mean bioavailability was 81% for phase 1 and 80% for phase 2. Percent absorbed versus time plots revealed no difference in rate of absorption between treatments. We conclude that short-term administration of the enteral feeding. Ensure does not influence the absorption of theophylline when administered as the sustained-release product Theo-24.     

The influence of food on the oral absorption of bevantolol

The bioavailability of bevantolol was compared in 12 healthy volunteers given single doses of the drug as the HCl salt after an overnight fast, or 15 minutes before or after a standardized breakfast in a nonblind, randomized crossover design. Bevantolol was rapidly absorbed in all three treatment groups, with maximum concentrations (Cmax) observed at 1.0, 0.9, and 1.8 hours for the fasting, before breakfast, and after breakfast groups, respectively. Time to Cmax was significantly longer than fasting only when bevantolol was given after breakfast. Food ingestion did not significantly affect Cmax, total of absorbed drug, or the drug elimination rate. Since food only slightly decreases the drug absorption rate and has no measurable effect on the extent of drug absorption, the relationship of bevantolol administration to meals is not expected to influence therapeutic efficacy.     

Influence of polyethylene glycol 400 on the gastrointestinal absorption of ranitidine

Purpose. To investigate the effect of co-administered polyethylene glycol 400 (PEG 400), a pharmaceutical excipient previously shown to accelerate small intestinal transit, on the absorption characteristics of ranitidine from the gastrointestinal tract. Methods. Ten healthy male volunteers each received, on two separate occasions, an immediate-release pellet formulation of ranitidine (150 mg) encapsulated within a hard gelatin capsule and a liquid preparation consisting of 150 ml orange juice (control) or 150 ml orange juice containing 10 g PEG 400 (test). The liquid preparations were also radiolabelled with indium-111 to allow their transit through the gastrointestinal tract to be followed using a gamma camera. On a further occasion an intravenous injection of ranitidine (50 mg) was administered. Blood samples were taken over a 12 h period on each study day to allow a ranitidine plasma and subsequent absorption rate profile to be generated for each oral formulation. Urine was collected for 24 h and assessed for PEG 400 concentration. Results. The absolute bioavailability of ranitidine from the pellet formulation was significantly reduced by 31% (from 51% to 35%) and small intestinal liquid transit time was significantly shortened by 37% (from 226 min to 143 min) as a consequence of PEG 400 in the test preparation. PEG 400 also affected the rate of ranitidine absorption, with major differences noted in the mean absorption time and C_max parameters. The appearance of double peaks were less evident in the ranitidine pharmacokinetic profiles in the presence of PEG 400, and little or no correlation was observed between the absorption of ranitidine and PEG 400. Conclusions. These results clearly demonstrate that PEG 400 adversely influences the gastrointestinal absorption of ranitidine. This in turn has ramifications for the use of PEG 400 as a pharmaceutical excipient in oral formulations.