Physicochemical and release properties of pellets coated with Kollicoat SR 30 D, a new aqueous polyvinyl acetate dispersion for extended release

Kollicoat^® SR 30 D is a new aqueous colloidal polyvinyl acetate dispersion used for extended release coatings. Kollicoat^® SR 30 D is stable against sedimentation, has a low viscosity (54 mPas) and a negative zeta potential of −23.2 mV because of the presence of the anionic surfactant, sodium dodecyl sulfate. Because of its low minimum film formation temperature (MFT = 18 °C), plasticizer addition and a thermal after-treatment (curing) of coated pellets was not required. Coated pellets showed no aging or curing effect. The rate of release could be easily adjusted by varying the coating level. A subcoating layer of the hydrophilic polymer, polyvinyl alcohol, between an ibuprofen-containing core and the Kollicoat^® SR coating prevented the diffusion of the lipophilic, low melting ibuprofen into the polymer coating during storage. The drug release from Kollicoat^® SR 30 D coated pellets was almost independent of the pH and ionic strength of release medium.     

挤出-滚圆和流化床包衣法制备硫普罗宁肠溶微丸的研究

目的应用挤出 滚圆法及流化床包衣制备硫普罗宁肠溶微丸，并对其性质进行考察。方法采用国产挤出 滚圆造粒机制备硫普罗宁微丸，采用L9(34)正交设计实验优化工艺条件；用微型流化床包衣设备，将微丸包肠溶衣，考察微丸的粉体学性质及不同包衣增重微丸的体外释放实验。结果制得的硫普罗宁微丸圆整度好，大小均匀。15%包衣增重的微丸体外释放比较理想。结论应用国产挤出 滚圆造粒机制备硫普罗宁微丸，工艺简便，制得的微丸质量好，采用适当的包衣工艺，可制得硫普罗宁肠溶微丸。     

挤出滚圆法制备葛根芩连微丸

目的制备能适合于工业化大生产具有较高载药量的葛根芩连微丸。方法采用挤出滚圆法制备葛根芩连微丸,对影响成球的4个关键参数水分比例、挤出速度、滚圆转速和滚圆时间进行筛选优化。结果制得的葛根芩连微丸载药量达70%、圆整度好、粒径分布窄,收率在90%以上。结论采用挤出滚圆法制备高载药量的葛根芩连微丸在工艺上是可行的,对中药微丸工业化大生产具有借鉴作用。     

基于QbD理念的盐酸坦索罗辛缓释胶囊的处方工艺研究

以盐酸坦索罗辛为模型药物,将QbD理念应用于其缓释微丸的开发。采用挤出-滚圆法制备含药丸芯,以流化床对含药丸芯进行包衣,制备肠溶缓释微丸。对参比制剂深入研究后确认产品的关键质量属性为pH 1.2介质中2 h的释放度及换成pH 7.2介质后继续溶出1 h、3 h的累积释放度。风险评估结果显示,对关键质量属性具有较高风险的因素为：丸芯中Eurdragit?誖NE30D的量（X1）、衣膜中Eudragit?誖L30D-55的比例（X2）、包衣增重（X3）。采用星点设计-效应面法对高风险因素进行效应分析,确定设计空间为X1：18.8%~21.0%,X2：15.0%~20.2%,X3：4.3%~6.1%,设计空间内产品符合预期且质量可控。     

高效液相色谱法测定盐酸可乐定脉冲释药微丸胶囊的含量

目的 建立盐酸可乐定脉冲释药微丸胶囊中盐酸可乐定的含量测定方法.方法 采用高效液相色谱法,色谱柱为Diamonsil C8柱(250 mm×4.6 mm,5μm),流动相为0.22%辛烷磺酸钠-甲醇-磷酸(500:500:1,用1 mol/L氢氧化钠溶液或磷酸调pH至3.0),流速为1.0mL/min,检测波长为220nm.结果 盐酸可乐定质量浓度在10.24～122.88 μg/L范围内与峰面积线性关系良好(r=0.9992);盐酸可乐定的平均回收率为99.73%,RSD=0.60%(n=9).结论 该法灵敏快速、准确可靠,可作为盐酸可乐定脉冲释药微丸胶囊中盐酸可乐定的含量测定方法.     

山黄微丸的制备及质量控制研究

目的:研究山黄微丸的制备方法,建立测定山黄微丸中盐酸小檗碱和盐酸巴马汀含量的方法。方法:采用DLB-3型多功能制粒包衣机,离心-流化造丸法制得山黄微丸。采用HPLC法,C18柱,乙腈-0.1%磷酸=50∶50(每100 mL加0.1 g十二烷基磺酸钠)为流动相,检测波长为265 nm。结果:盐酸小檗碱在0.043 3μg~0.693 5μg之间线性关系良好。平均回收率为98.86%,RSD=1.98%。盐酸巴马汀在0.061 0μg~0.366 0μg之间线性关系良好,平均回收率为98.97%,RSD=1.88%。结论:离心-流化造丸法制得山黄微丸质量可控。     

Testosterone Pellet Implantation Practices: A Sexual Medicine Society of North America (SMSNA) Member Questionnaire

IntroductionThere has been renewed interest in the use of subcutaneous testosterone pellets for the treatment of hypogonadism since the introduction of Testopel in 2008 by Slate Pharmaceuticals (Durham, NC, USA). Manufacturer guidelines recommend using two to six pellets; however, in the clinical setting, this is deemed insufficient. This has produced a wide variety of testosterone pellet usage that is not fully understood.AimTo better understand subcutaneous testosterone pellet implantation practices among members of the Sexual Medicine Society of North America (SMSNA).MethodsA 19-item questionnaire was emailed to the 687 members of the SMSNA. Of the 19 questions, 17 were multiple choice and two required write-in responses. Usage patterns, satisfaction rates, and complication rates were investigated.Main Outcome MeasuresData regarding indications for initiating treatment with Testopel, initial dosage, follow-up of testosterone levels and dose titration, patient tolerance and satisfaction, technique of implantation, and procedural complications were collected.ResultsEighty-seven survey responses were received (12.9%). At initiation of Testopel therapy, 80.5% of respondents would implant at least 10 pellets, whereas only 4.6% would place six to seven pellets and 3.4% would implant fewer than six pellets. Many respondents would determine the starting dose based on some combination of baseline testosterone level and weight, although 24.1% described using a standard starting dose for all patients. All respondents would check testosterone levels within 3 months of initiating therapy, with the vast majority (72.4%) doing so at 1 month. Subsequent dosing of Testopel was not changed in most patients, with 41.4% and 26.4% of respondents reporting that 60% to 80% and 80% to 100% of patients, respectively, remained on their initial dose. Most respondents would re-implant pellets at a 3-month (21.8%) or 4-month (43.7%) interval. High patient satisfaction was described by respondents, with 56.3% finding patients to be satisfied “most times” and 34.5% “almost always.”ConclusionThis study provides insight into the usage of Testopel among members of the SMSNA. We found that the vast majority of specialists use at least 10 pellets at initial implantation, with limited need for subsequent dose adjustments, good durability of response, and high patient satisfaction and tolerability.     

微丸的研究进展

以微丸制剂为代表的多单元型给药系统因其特有的优越性,已成为缓控释制剂的主要发展方向。本文主要对微丸的形成机理、分类、制备工艺以及压片等相关方面作了较全面的介绍。     

GC法测定羚黄宝儿丸中麝香酮、冰片、丁香酚的含量

目的:建立GC法同时测定羚黄宝儿丸中麝香酮、冰片、丁香酚3种成分的含量。方法:采用直接进样GC法,色谱柱为DB-WAX毛细管柱(30.0 m×0.25 mm×0.25μm),FID检测器,载气为氮气,程序升温,柱流量为1.2 m L/min。结果:3种成分在均呈现良好的线性关系,精密度、重复性RSD均<3%,加样回收率在95%~106%。结论:直接进样GC法方法简便、灵敏、准确、重现性好,适用于羚黄宝儿丸中麝香酮、冰片、丁香酚的含量测定。     

安胃微丸抗胃溃疡作用

目的考察安胃微丸对慢性胃溃疡的治疗作用及对急性胃溃疡的保护作用。方法采用大鼠醋酸烧灼法、幽门结扎法和小鼠水应激法及消炎痛法 4种胃溃疡动物模型。结果安胃微丸对醋酸侵袭胃壁所致慢性胃溃疡有明显的治疗作用 ,对大鼠幽门结扎有一定保护作用 ,并能明显抑制胃酸及胃蛋白酶活性 ,对消炎痛引起的小鼠药物性胃溃疡有显著的抑制作用 ,并能抑制水浸应激性胃溃疡。并显示其有一定的镇痛作用。结论安胃微丸有很好的抗胃溃疡作用。