盐酸文拉法辛缓释胶囊的制备及体外释放试验简

目的研究盐酸文拉法辛缓释微丸的制备方法,并对其体外释药行为进行考察。方法用挤出滚圆造粒机制备盐酸文拉法辛微丸,用流化床进行微丸包衣,再填装胶囊;采用紫外分光光度法测定盐酸文拉法辛缓释胶囊的释放度。单因素试验考察包衣增重及致孔剂的量对缓释微丸释药行为的影响。结果采用挤出滚圆法制备的盐酸文拉法辛微丸,圆整度好,颗粒均匀。标准曲线方程△A=0．0044C＋0．0015,r=0．9998,盐酸文拉法辛的浓度在7～98μg·mL范围内呈良好的线性关系。包衣增重为12．5％～16．5％时,自制3批盐酸文拉法辛缓释胶囊的释放行为与原研产品一致,f2凶子分别为89．1、87．9、90．4。结论挤出滚圆法制备盐酸文拉法辛微丸工艺简便易行,制得的微丸重复性好,收率高。     

挤出-滚圆法制备盐酸文拉法辛缓释胶囊及体外释放性考察

目的制备盐酸文拉法辛缓释胶囊并考察其体外释药特性。方法采用挤出-滚圆法制备盐酸文拉法辛素丸,采用Eudragit NE30D水分散体作为成膜材料,流化床底喷法对素丸进行包衣,单因素考察对处方和工艺进行筛选和优化。结果挤出-滚圆法制备的丸芯粒度分布16～30目,缓释包衣增重为22%～30%时,与上市品(怡诺思)释放速率基本一致,4种包衣增重的f2值分别为68、78、71和50。结论该方法制备的盐酸文拉法辛缓释胶囊处方和制备工艺可靠,重现性好。     

茶碱脉冲式控释微丸的制备

目的：探讨茶碱脉冲式控释微丸的处方组成和制备工艺。方法：采用多层包衣的方法,以体外释药时滞和释药速率为指标,经正交试验设计,筛选较佳的处方组成和工艺。结果：制得的脉冲控释微丸体外释药时滞为６ｈ左右,在６－９ｈ内释药在７５％～９５％,稳定性良好。结论：采用多层包衣的能够制香合适的茶碱脉冲式控释微丸。     

阿替洛尔缓释微丸的制备和处方工艺研究

 目的 制备阿替洛尔缓释微丸,并对其体外释放行为进行研究.方法 采用挤出滚圆法制备载药丸芯,利用溶液层积法对载药丸芯进行缓释包衣.以圆整度和释放度为评价指标,对主要工艺参数:滚圆速度、滚圆时间和愈合时间;以及处方因素:微晶纤维素与主药的比例,丸芯粘合剂用量,以及缓释包衣增重进行考察.结果 所制得的缓释微丸在1、6、12、24 h的释放率分别为标示量的10%～15%,20%～45%,50%～75%,85%以上.释药行为符合零级动力学.结论 本研究处方工艺简便,重现性良好,适合工业化生产.     

双氯芬酸钠缓释微丸胶囊的制备

 目的 探讨双氯芬酸钠缓释微丸的制备工艺.方法 采用离心造粒法制备双氯芬酸钠缓释微丸,分别对影响微丸收率和释放的因素进行考察.结果 主药与辅料比例为1∶ 5,制备含药素丸,分别用聚丙烯酸树脂RL/RS 20∶ 1和7∶ 3对素丸进行包衣,再将两种包衣微丸等比例配混,即可达到释放度要求.结论 微丸制备工艺稳定,适于产业化放大.     

环胞素A植入微球的体外释放研究

目的:研究长效环胞素A(CyA)/PLA微球的体外释药特性.方法:以聚乳酸(PEA)为基质,采用乳化-挥发法制备CyA/PLA微球,采用HPLC法测定CyA/PLA微球中的含量,考察微球的体外释药性能.结果:CyA在5～80μg·mL<'-1>范围内呈线性,平均回收率为99.6%,RSD=1.12%(n=9).28 d的体外释药百分率为(65.32.4)%.结论:CyA/PLA微球体系具有一定的缓释性能.     

维生素C缓释包衣片的研究

目的：　制备维生素Ｃ缓释包片,考察自制的渗透型丙烯酸树脂与Ｅｕｄｒａｇｉｔ ＲＳ／ＲＬ的一致性及包衣片的稳定性。方法：分别以自制的渗透型丙烯酸树脂和标准样品为薄膜包衣材料,制备维生素Ｃ缓释包衣片,以体外溶出试验,考察二者的缓释性能及所得包衣缓释片的稳定性。结果：转蓝法测定药物溶出度表明,用Ｅｕｄｒａｇｉｔ ＲＬ和ＲＳ包衣的缓释片,其释药速度有明显的差别,但在１０ｈ 内均以零级动力学过程连续释药;自制的ＲＬ和ＲＳ产品达到了国外同类产品的应用性能要求。结论：自制的渗透型缓释材料与标准样品ＥｕｄｒａｇｉｔＲＳ／ＲＬ 基本一致;维生素Ｃ缓释包衣片能延缓药物氧化、增加片剂的稳定性     

硝苯地平缓释微丸的体外释药机制

目的 考察自制硝苯地平缓释微丸的体外释药机制。方法 按中国药典(2000版)浆法，进行体外释放度测定，累积释放度数据经计算机处理。结果 本自制硝苯地平缓释微丸为亲水性凝胶骨架制剂，体外释放机制包括药物扩散和骨架溶蚀两种作用。结论 自制硝苯地平缓释微丸体外缓释，有进一步开发的价值。     

盐酸多西环素牙周用微球温敏性凝胶的制剂学研究简

目的构建盐酸多西环素牙周用微球温敏性凝胶缓释系统。方法通过乳化一交联固化法制备盐酸多西环素羧甲基壳聚糖微球（DXY-CMCTS-MS）。采用壳聚糖和卢．甘油磷酸钠（β-GP）制备凝胶。用扫描电镜和光学显微镜观察微球表面形态;体外动态透析法测定释药性能。结果制备的DXY—CMCTS—MS形态圆整,粒径分布较为均匀,平均粒径约25μm,载药量18．9％,包封率64．6％。DXY微球凝胶在室温下为自由流动的液体,37℃的平均凝胶时间为（1．1±0．3）min,明显低于凝胶剂的凝胶时间。微球凝胶复合载体的释药速度明显低于微球剂,体外释药曲线符合Higuchi拟合方程。结论盐酸多西环素微球温敏凝胶复合载体的处方和制备工艺可行,作为牙周用缓释制剂值得进一步研究。     

挤出-滚圆法制备枸橼酸莫沙必利骨架缓释微丸

目的制备枸橼酸莫沙必利骨架缓释微丸,研制枸橼酸莫沙必利新剂型。方法采用挤出-滚圆法制备枸橼酸莫沙必利骨架缓释微丸,考察润湿剂用量、挤出速度及滚圆速度对释放度的影响,并通过加速试验考察制剂的稳定性。结果枸橼酸莫沙必利骨架缓释微丸的释药动力学符合Higuchi方程,制剂稳定性良好。结论本方法制备枸橼酸莫沙必利骨架缓释微丸工艺可靠,质量可控。     

奥美拉唑肠溶微丸胶囊的制备

目的制备奥美拉唑肠溶微丸胶囊。方法采用流化床包衣技术,在空白丸芯上依次包以主药层、隔离层和肠溶层,制备成奥美拉唑肠溶微丸,并对其处方和工艺进行优化,将肠溶微丸装入普通胶囊制成奥美拉唑肠溶微丸胶囊。结果将奥美拉唑、羟丙基甲基纤维素(5 mPa.s)、无水碳酸钠、聚山梨酯-80、二甲基硅油和水混合制成主药层包衣溶液,以无水碳酸钠作为隔离层的碱性调节剂,EUDRAGITL30D-55作为肠溶包衣材料,自制的3批奥美拉唑肠溶微丸胶囊在人工肠液中45 min的释放度分别为(98.0±1.2)%、(95.3±4.0)%和(94.3±1.8)%。结论以肠溶微丸技术制备奥美拉唑肠溶胶囊,工艺可行,重复性良好,质量稳定可靠。     

吲哚美辛缓释胶囊的制备及释放度研究

目的：以壳聚糖和海藻酸钠为载体制备吲哚美辛缓释胶囊,考究壳聚糖对吲哚美辛的缓释作用。方法：复凝聚法制备微囊型颗粒,再将颗粒装入胶囊壳制得胶囊;通过发迹制粒时壳聚糖的深度考究壳聚糖对吲哚美辛的缓释作用;用转法研究所制胶囊的体外释放度。结果：壳聚糖组吲哚美辛胶囊的体外释放度较对照组降低,且深度越高降低越明显。结论：与吲哚美辛普通胶囊相比,所制胶囊确实具有缓释作用。     

Radioprotection,pharmacokinetic and behavioural studies in mouse implanted with biodegradable drug (amifostine) pellets

PURPOSE: We evaluated the use of a subcutaneously (s.c.) implantable, biodegradable pellet as a drug delivery system for the radioprotector amifostine. MATERIALS AND METHODS: Mice were implanted s.c. with either the custom-made biodegradable amifostine drug pellet or the placebo pellet without amifostine, exposed to cobalt-60 gamma-radiation (bilateral, 1 Gy min(-1), 7-16 Gy), and the 30-day survival rate was monitored. The non-irradiated mouse was used for pharmacokinetic and behavioural tests. RESULTS: Significant radioprotection (85-95% survival) at 10 Gy was observed in the three-amifostine pellet implanted group 3-5 h after implantation. LD50/30 was 7.97, 8.74 and 16.64 Gy for the control, three-placebo pellet (dose reduction factor, DRF=1.10, p<0.01), and three-amifostine pellet (DRF=1.79, p<0.01) groups respectively in mouse exposed to radiation 2h after implantation. Radioprotection at 12 Gy was observed up to 4h after s.c. amifostine administration and up to 3h after implantation. Pharmacokinetic data revealed that the three-amifostine pellet group had sustained blood WR-1065 levels at 2 h after implantation, in contrast to the reported sharp peak at 30 min for s.c. administration. Although locomotor activity was significantly reduced (p<0.01) in the amifostine pellet group, the onset of the locomotor decrement was delayed as compared with groups that received 400 and 750 mg kg(-1) s.c. amifostine. CONCLUSIONS: Amifostine in biodegradable implant was effective. The radioprotection observed was comparable between conventional s.c. administration of the drug and implantation. Pharmacokinetic data and locomotor activity suggest that the implantation was beneficial though radioprotection data warrants formulation improvements in implants.     

Radioprotection,pharmacokinetic and behavioural studies in mouse implanted with biodegradable drug (amifostine) pellets

Purpose : We evaluated the use of a subcutaneously (s.c.) implantable, biodegradable pellet as a drug delivery system for the radioprotector amifostine. Materials and methods : Mice were implanted s.c. with either the custom-made biodegradable amifostine drug pellet or the placebo pellet without amifostine, exposed to cobalt-60 γ-radiation (bilateral, 1 Gy min -1, 7-16 Gy), and the 30-day survival rate was monitored. The non-irradiated mouse was used for pharmacokinetic and behavioural tests. Results : Significant radioprotection (85-95% survival) at 10 Gy was observed in the three-amifostine pellet implanted group 3-5 h after implantation. LD 50/30 was 7.97, 8.74 and 16.64 Gy for the control, three-placebo pellet (dose reduction factor, DRF=1.10, p <0.01), and three-amifostine pellet (DRF=1.79, p <0.01) groups respectively in mouse exposed to radiation 2h after implantation. Radioprotection at 12 Gy was observed up to 4h after s.c. amifostine administration and up to 3h after implantation. Pharmacokinetic data revealed that the three-amifostine pellet group had sustained blood WR-1065 levels at 2 h after implantation, in contrast to the reported sharp peak at 30 min for s.c. administration. Although locomotor activity was significantly reduced (p <0.01) in the amifostine pellet group, the onset of the locomotor decrement was delayed as compared with groups that received 400 and 750 mg kg -1 s.c. amifostine. Conclusions : Amifostine in biodegradable implant was effective. The radioprotection observed was comparable between conventional s.c. administration of the drug and implantation. Pharmacokinetic data and locomotor activity suggest that the implantation was beneficial though radioprotection data warrants formulation improvements in implants.     

星点设计-效应面法优化琥珀酸美托洛尔缓释微丸处方

目的：通过星点设计-效应面法优化琥珀酸美托洛尔（ MS）缓释微丸处方工艺。方法采用蔗糖丸芯,以乙基纤维素为包衣材料,模型药物MS为致孔剂,通过流化床底喷工艺制备MS缓释微丸。以致孔剂比例和包衣增重为考察因素（自变量）,微丸1,4,8,12,16 h的释放度为考察指标（因变量）,采用两因素五水平星点设计对处方进行优化。根据自变量和因变量数据,进行数学方程拟合并描绘效应面,选择最佳处方工艺进行验证实验。结果与结论数学方程拟合结果表明二项式方程拟合度较高。根据效应面优化的最佳自变量范围可知,致孔剂比例为16％～18％,包衣增重为20％～25％。优化的缓释微丸药物释放度1 h达到9．15％,消除了释放初期的迟滞相,且能够在较长时间内维持良好的缓释作用。通过星点设计-效应面法优化的MS缓释微丸处方工艺稳定可行。     

左旋布比卡因在下颌阻生智齿拔除术中麻醉效果及术后镇痛作用研究

 目的 观察左旋布比卡因在下颌阻生智齿拔除术中的麻醉效果及术后镇痛作用.方法 选择需拔除双侧下颌阻生智齿34例,采用交叉试验方法,分别使用0.5%左旋布比卡因及2%利多卡因进行下齿槽神经麻醉,观察麻醉药起效时间.采用VAS评分法对两组麻醉效果进行评定,并对术后患者服用镇痛药(芬必得胶囊)情况进行记录.结果 0.5%左旋布比卡因及2%利多卡因麻醉药起效时间分别为(6.59±2.20)min和(4.40±1.43)min,两组差异具有统计学意义(P<0.05);左旋布比卡因组术中VAS评分低于利多卡因组,两组差异具有统计学意义(P<0.05);左旋布比卡因组术后服用镇痛药人数为3人,明显少于利多卡因组16人,差异具有统计学意义(P<0.01).结论 采用左旋布比卡因行下齿槽神经阻滞麻醉拔除下颌阻生智齿,术中麻醉有效,术后镇痛作用较好.     

盐酸二甲双胍肠溶微丸胶囊的制备及其释放度测定

 目的 制备盐酸二甲双胍肠溶微丸胶囊,并测定其释放度.方法 采用丸芯喷雾上药法,筛选微丸处方,并通过溶出度试验考察其释放度.结果 以空白丸芯(600～700 μm)400 g;盐酸二甲双胍800 g;HPMC(6 cps)40 g;水2 500 ml为优选处方,所制备的微丸在规定的酸性介质中几乎不释放,而在磷酸盐缓冲液中则释放80%以上.结论 该片剂制备工艺简单易行,能达到肠溶的目的,可降低或消除盐酸二甲双胍在临床上使用的不良反应.