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。     

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.     

离心造粒法制备奥美拉唑肠溶微丸

 目的 制备稳定性好的奥美拉唑肠溶微丸.方法 采用离心造粒法制备奥美拉唑肠溶素丸,采用羟丙基甲基纤维素与滑石粉包隔离层,使用Eudragit L30D-55包衣制得奥美拉唑肠溶微丸.结果 以羟丙基甲基纤维素及滑石粉包隔离后,提高了微丸的稳定性,而肠溶性包衣材料Eudragit L30D-55的使用,则使奥美拉唑微丸的释放度符合肠溶要求.结论 离心造粒法工艺简便易行,重现性好,药物溶出度好.     

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。     

葛根素肠溶纳米粒的制备及体外释放度研究

目的制备葛根素肠溶纳米粒,并对其体外释放度进行考察。方法采用离子交联法制备葛根素肠溶纳米粒,HPLC法测定药物的包封率及体外释放度,透射电镜考察纳米粒的表面形态,激光粒度分析仪测定粒径分布。结果制备的纳米粒,粒径较小,分布均一,包封率较高,理化性质合乎要求,并在pH7.2的磷酸盐缓冲液中释放达到70%以上。结论葛根素肠溶纳米粒体外释药良好,能达到良好肠溶效果。     

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.     

离心制粒工艺制备微晶纤维素空白微丸的研究

目的：考察微日纤维素（MCC）以离心制粒工艺制备微丸时的颗粒形成机理和影响因素，优化工艺参数。方法：采用不同批次间颗粒性质比较的方法，考察并确定影响离心制粒工艺的处方和工艺因素，通过均匀设计，优化MCC处方成丸的工艺参数。以优化条件制备微丸，与市售空白丸芯进行颗粒物理性质比较。结果：粘合剂用量、主机转速、粘合剂加入速度和滚圆时间对MCC处方的颗粒结聚影响较大。经多元线性回归，获得了这些因素与微丸收率、均匀度、微丸粒径间的定量关系，颗粒增长主要受物料含水量的制约，以优化工艺参数制备的微丸颗粒物理性质，与市售MCC空白丸芯相比无较大差异。结论：水性辅料以离心制粒工艺制备微丸切实可靠。     

布地奈德结肠靶向脉冲片的制备及体外释放度研究

目的　制备治疗溃疡性结肠炎药物布地奈德的结肠靶向脉冲片 ,并考察其体外释放特性。方法　采用粉末直接压片法制备速释片芯 ,以EudragitL为材料 ,喷雾包衣法制备结肠靶向脉冲片 ,紫外分光光度法进行体外溶出度测定。结果　按照优化后的处方所制备的脉冲片的体外释药时滞为 (6 .18± 0 .15 )h。结论　本脉冲片达到设计要求 ,体外试验满足结肠靶向和脉冲释药效果。     

盐酸二甲双胍壳聚糖-海藻酸钠缓释微囊的制备及性能研究

目的 制备盐酸二甲双胍壳聚糖-海藻酸钠缓释微囊并探索其性能.方法 以壳聚糖和海藻酸钠为囊材,利用复凝聚法将盐酸二甲双胍微囊化.以微囊的药物包封率为制备工艺优化指标,用转篮法测定其体外溶出速率.结果 通过正交实验得出微囊的最佳制备工艺条件为:壳聚糖浓度0.2%,成囊pH 4.5,成囊温度45℃,搅拌速度200r/min.微囊的溶出释放性能实验显示,该载药微囊的累积释放速度远低于市售缓释片剂,在20h左右达到75%左右的最高累积释放值.结论 以最佳制备工艺条件制备含药微囊重现性好、工艺稳定、吸水溶胀性好,体外溶出实验显示具有较好的缓释作用.     

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。     

毛冬青缓释胶囊的制备

目的 制备膜控释毛冬青缓释微丸胶囊并研究其体外释药性能。方法 用乙基纤维素等辅料包衣材料,以PEG1000为致孔剂,经薄膜包衣制备毛冬青缓释微丸胶囊,并以体外释放度试验来评价。结果 实验表明体外释药符合Higuchi方程,Q=18．415t^1/2 29．649(r=0．9874)。结论 毛冬青缓释微丸具有较好的释药性能,为一种较理想的口服缓释剂型,制备工艺可行。     

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。     

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     

A simple method for preparing radioactive capsules in colon transit study

Colon transit study is currently performed by delivering technetium-99m or indium-111 labelled activated charcoal to the colon in a methacrylate-coated capsule (coated capsule). However, the coating procedure is complicated and methacrylate has not been approved by the Food and Drug Administration. Therefore, a simpler method is needed for the clinical routine use of colon transit study. In this study, we used a commercial empty enteric capsule and a coated capsule for the measurement of colon transit time. We compared the in vitro stability and in vivo scintigraphy of 99mTc-labelled activated charcoal in the coated capsule and the enteric capsule to evaluate the possibility of clinical usage of the enteric capsule for colon transit time study. Activated charcoal powder was mixed with 49mTc-diethylene triamine pentaacetic acid (DTPA) and vaporized to dryness. The dry 99mTc-DTPA activated charcoal was loaded into the coated capsule and the enteric capsule. In vitro stability study was performed by immersing these capsules in a colourless buffer of variable pH which mimicked the conditions in the stomach and the small bowel. Capsule disruption was determined. Colon transit scintigraphy with 99mTc-DTPA charcoal was performed in five normal volunteers using these two capsules. The in vitro stability of these two types of capsule was similar and the colon transit scintigraphy findings were almost identical. Most capsules dissolved in the ascending colon and very few in the terminal ileum. It is concluded that enteric capsule is a suitable alternative to coated capsule for measurement of colon transit.     

复方非洛地平/酒石酸美托洛尔渗透泵控释片的研制

目的制备复方非洛地平/酒石酸美托洛尔渗透泵控释片,并优选最佳处方。方法采用高效液相色谱法测定不同处方制剂累积释药百分率,建立体外评价方法,并通过相似因子和正交设计筛选出最佳处方。结果 渗透泵片的片芯处方、包衣增重是影响释药的主要因素。优化的处方为15 mg聚氧乙烯、45 mg NaCl、11%包衣增重。结论按优化处方制备的渗透泵控释片符合零级释放特征,且两种药物释放同步。     

A simple method for preparing radioactive capsules in colon transit study

Colon transit study is currently performed by delivering technetium-99m or indium-111 labelled activated charcoal to the colon in a methacrylate-coated capsule (coated capsule). However, the coating procedure is complicated and methacrylate has not been approved by the Food and Drug Administration. Therefore, a simpler method is needed for the clinical routine use of colon transit study. In this study, we used a commercial empty enteric capsule and a coated capsule for the measurement of colon transit time. We compared the in vitro stability and in vivo scintigraphy of ^99mTc-labelled activated charcoal in the coated capsule and the enteric capsule to evaluate the possibility of clinical usage of the enteric capsule for colon transit time study. Activated charcoal powder was mixed with ^99mTc-diethylene triamine penta-acetic acid (DTPA) and vaporized to dryness. The dry ^99mTc-DTPA activated charcoal was loaded into the coated capsule and the enteric capsule. In vitro stability study was performed by immersing these capsules in a colourless buffer of variable pH which mimicked the conditions in the stomach and the small bowel. Capsule disruption was determined. Colon transit scintigraphy with ^99mTc-DTPA charcoal was performed in five normal volunteers using these two capsules. The in vitro stability of these two types of capsule was similar and the colon transit scintigraphy findings were almost identical. Most capsules dissolved in the ascending colon and very few in the terminal ileum. It is concluded that enteric capsule is a suitable alternative to coated capsule for measurement of colon transit. Received 14 December 1999 and in revised form 14 March 2000