Oral Dispersible System: A New Approach in Drug Delivery System

Dosage form is a mean used for the delivery of drug to a living body. In order to get the desired effect the drug should be delivered to its site of action at such rate and concentration to achieve the maximum therapeutic effect and minimum adverse effect. Since oral route is still widely accepted route but having a common drawback of difficulty in swallowing of tablets and capsules. Therefore a lot of research has been done on novel drug delivery systems. This review is about oral dispersible tablets a novel approach in drug delivery systems that are now a day''s more focused in formulation world, and laid a new path that, helped the patients to build their compliance level with the therapy, also reduced the cost and ease the administration especially in case of pediatrics and geriatrics. Quick absorption, rapid onset of action and reduction in drug loss properties are the basic advantages of this dosage form.     

甲磺酸伊马替尼联合VDLD化疗方案治疗急性淋巴细胞白血病患儿的长期随访研究

目的探究甲磺酸伊马替尼联合VDLD化疗方案治疗急性淋巴细胞白血病(ALL)患儿的应用价值。方法选取2015年5月~2018年6月收治的74例ALL患儿,按照治疗方案不同分组。对照组(37例)实施VDLD方案治疗,联合组(37例)实施甲磺酸伊马替尼+VDLD化疗方案治疗。对比两组疗效、不良反应发生率、随访1年无复发生存率(RFS)及治疗前、治疗2个疗程后血清B淋巴细胞刺激因子(BAFF)、增殖诱导配体(APRIL)水平。结果联合组总有效率(91.89%)高于对照组(72.97%)(P<0.05);联合组治疗2个疗程后血清BAFF、APRIL水平低于对照组(P<0.05);两组不良反应发生率、随访1年RFS对比无显著差异(P>0.05)。结论甲磺酸伊马替尼联合VDLD化疗方案治疗ALL,疗效确切,能显著降低血清BAFF、APRIL水平,且安全性高。     

美托洛尔用于老年COPD合并冠心病史治疗的临床疗效观察

目的:探讨美托洛尔(β1受体阻滞剂)用于老年COPD合并冠心病史治疗的临床疗效。方法:选取2018年6月—2019年6月在我院接受治疗的60岁以上(包括60岁)COPD合并冠心病史老年患者,分为对照组与观察组。对照组给予接受布地奈德福莫特罗粉吸入剂治疗,观察组在使用布地奈德福莫特罗粉吸入剂治疗的基础上口服琥珀酸美托洛尔缓释片治疗,观察对比两组治疗效果。结果:观察组临床治疗效果优于对照组,观察组住院时长以及并发症的发生率低于对照组(P<0.05),差异具有统计学意义。结论:老年COPD合并冠心病史接受美托洛尔治疗,可有效缩短住院时长、用药效果明显、有效提升用药安全性,值得临床推广。     

基于化学模式识别技术提升参威骨痹片的质量标准并监测其生产中质控指标的转移率变化

目的:提升参威骨痹片的质量标准,初步探索其质量控制指标成分在批间含量差异较大的原因。方法:采用HPLC建立参威骨痹片的指纹图谱,以Diamonsil C18(4. 6 mm×250 mm,5μm)为色谱柱,流动相乙腈(A)-0. 1%磷酸水溶液(B)梯度洗脱(0～5 min,10%A;5～15 min,10%～12%A;15～30 min,12%～26%A;30～43 min,26%～31%A,43～50 min,31%～40%A,50～70 min,40%～55%A;70～84 min,55%～72. 5%A),检测波长230 nm。以共有峰为自变量绘制正交偏最小二乘法-判别分析-变量重要性投影(OPLS-DA-VIP)图,将共有峰对该制剂各批次间指纹图谱差异的贡献度量化,寻找差异较大的色谱峰,结合相关文献,筛选出与参威骨痹片临床适应症相关的成分并进行其含量测定的专属性试验,最终选定质控指标。通过HPLC-二极管阵列检测器(DAD)同时对本品及其生产过程中间体中质控指标进行测定,检测波长236,276,230,322 nm,其他条件同HPLC指纹图谱检测方法。结果:HPLC指纹图谱共标定了26个共有峰,各批次样品指纹图谱与对照指纹图谱的相似度均≥0. 950。优选出马钱苷酸、龙胆苦苷、芍药苷、蛇床子素为参威骨痹片的质控指标,四者的平均质量分数分别为161. 02,401. 80,255. 54,80. 68μg·g-1。结论:所建立的指纹图谱及多指标定量分析方法稳定、可靠,可用于参威骨痹片的质量控制。原料药批间质控指标成分含量差异和生产过程中间体的质控方法不够完善是引起该制剂批间质控指标成分含量差异较大的主要原因。     

In Vitro and in Vivo Evaluation of Whole and Half Tablets of Sustained-Release Adinazolam Mesylate

The mechanism of release from sustained-release adinazolam mesylate tablets was assessed by the Higuchi equation and by analysis of drug release profiles through 60% released using the Peppas equation. Computed values of the diffusional exponent, n, ranged from 0.59 to 0.66. Values of n in this range are consistent with a mixed mechanism of release, with diffusion of drug through the hydrated polymer matrix and relaxation of this matrix being the principal processes controlling release. The rate of in vitro drug release was increased for half tablets relative to whole tablets and is attributed to an increase in the surface to volume ratio of half tablets of about 16%. This increase in surface-to-volume ratio of half tablets was reflected by an increase in the constant, k, from the Peppas equation of 20–23% and by an increase in the slope of Higuchi plots of 12–18% for four lots of tablets. In vivo/in vitro relationships from two bioavailability studies were thoroughly evaluated. Using either a linear or a quadratic relationship, an in vivo/in vitro correlation exists for sustained-release adinazolam mesylate tablets.     

采用多元定时释药技术制备雷公藤胃漂浮缓释胶囊的研究

目的:采用多元定时释药技术制备雷公藤胃漂浮缓释制剂.方法:采用挤出滚圆法,以90%十八醇为助漂剂制得空白胃漂浮微丸.使用流化床包衣设备,制备载药胃漂浮微丸.再以低取代羟丙基纤维素作为内溶胀层材料,以乙基纤维素水分散体作为外控释层材料进行包衣制备胃漂浮定时释药包衣微丸.等量称取控释层包衣增重分别为0%,8%,12%,15%,22%的包衣微丸,混均装入硬胶囊中,即得雷公藤胃漂浮缓释胶囊.结果:当溶胀层处方及用量固定后,通过控制控释层的厚度,可使包衣微丸在预期的不同时间定时释药.将几种控释层增重不同的包衣微丸混合后制成雷公藤胃漂浮缓释胶囊,在溶出介质中,均立即起漂,包衣微丸8 h漂浮率大于80%,并于不同时间依次释药,从而在整体上呈现出一种缓释特征.结论:采用多元定时释药技术制备而成的雷公藤胃漂浮缓释胶囊具有良好的漂浮性能和缓释特性.     

芪月降脂片制剂处方的优化

[目的 ]优化芪月降脂片的制剂处方 .[方法 ]采用正交设计和多指标综合评分法对已筛选出的药剂辅料进行处方优化 .[结果 ]最佳制剂处方为糖粉 50 g ,辅料X 50g ,微晶纤维素 75g .[结论 ]该处方合理 ,成型性好     

关于中成药口腔崩解片开发应用的思考

通过对口腔崩解片的特点及主要制备工艺的分析,结合当前中成药工业的现状及具体实际,认为口腔崩解片可以应用于中成药制剂的开发。     

Bioavailability and Pharmacokinetics of a New Sustained-Release Potassium Chloride Tablet

The bioavailability of a new sustained-release potassium chloride (KC1) tablet, designed for once-a-day dosing, was compared to a KC1 elixir using urinary excretion data. The study utilized 25 male volunteers dosed in a crossover design in a dietary/activity-controlled environment. The regimens consisted of a total of 80 mEq of potassium in three equally divided doses of elixir every 6 hr and a single 80-mEq dose using four 20-mEq sustained-release (SR) tablets. The mean time to maximum rate of potassium urinary excretion was 2.2 hr for the first elixir dose and 5.5 hr after the SR tablet (P < 0.01), thereby supporting the prolonged-release properties of this formulation. After correction for baseline urinary potassium excretion, the mean total 24-hr urinary potassium excretion was 42.18 mEq for the elixir and 40.41 mEq for the SR tablet. The results indicate that the absorption pattern from the SR tablet is equal to three doses of KC1 elixir dosed 6 hr apart.     

新药甲磺酸帕珠沙星的手性拆分

目的：建立新药甲磺酸帕珠沙星手性拆分的方法。方法：运用AD手性柱法和流动相添加剂法，考察了不同条件下对分离的影响。结果：运用这两种方法，甲磺酸帕珠沙星都可以达到基线分离，相同条件下，柱温越低，拆分因子越大。结论：在分离甲磺酸帕珠沙星时，流动相添加剂法要优于手性柱法。