Preparation and in vitro evaluation of slow release ketoprofen microcapsules formulated into tablets and capsules.

Ketoprofen powder was encapsulated with Eudragit RL/RS polymer solutions in isopropanol-acetone 1:1, using a simple and rapid method. Microcapsules were prepared using Eudragit solutions with different RL/RS ratios. The encapsulation process produces free-flowing microcapsules with good drug content and marked decrease in dissolution rate. The retardation in release profile of ketoprofen from microcapsules was a function of the polymer ratio employed in the encapsulation process. In vitro release of ketoprofen from microcapsules either filled in gelatin capsules or compressed into tablets, using calcium sulphate as diluent, confirmed the efficiency of the encapsulation process for preparing prolonged release medication. A capsule formulation with optimum sustained-release profile was suggested.     

Spray-dried microspheres containing ketoprofen formulated into capsules and tablets

In this study, microspheres were prepared by a spray-drying technique using solutions of ketoprofen and two polymers, cellulose acetate butyrate (CAB) and hydroypropylmethylcellulose phthalate (HPMCP), in different weight ratios. Different total concentrations were used in the feed solutions: 3, 6 and 9% w/v. The spray-dried microparticles were characterized in terms of shape (SEM), size (light scattering method), production yield and encapsulation efficiency. They were formulated into capsules; tablets were prepared by direct compression of the microparticles mixed with maltose and, in some cases, hydroypropylmethylcellulose (HPMC). In vitro release studies were performed both at acidic and neutral pHs. The spray-drying process of solutions of ketoprofen with polymeric blends of cellulose derivatives leads to microparticles which, depending on their final formulation (capsules or tablets), can give a rapid or prolonged drug release. The formulations here described can be proposed for the oral administration of NSAIDs.     

酮洛芬微丸缓释片的制备及体外释放度考察

目的:制备一种酮洛芬缓释片剂。方法:采用挤出-滚圆法制备酮洛芬微丸,用Eudragit?RS 30D和Eudragit?RL30D包衣。再将包衣微丸与酮洛芬原药压片,最终制成酮洛芬缓释片。结果:体外释放度实验显示,制备的酮洛芬缓释片在2h内能释药30%,剩余70%药物在随后的10 h内缓慢释放。结论:用本方法制备酮洛芬缓释片,工艺简便,易于操作。     

Preparation and in vitro evaluation of modified release ketoprofen microsponges

Microsponges containing ketoprofen and Eudragit RS 100 were prepared by quasi-emulsion solvent diffusion method. The effects of different mixing speeds, drug-polymer ratios, solvent-polymer ratios on the physical characteristics of the microsponges as well as the in vitro release rate of the drug from the microsponges were investigated. All the factors studied had an influence on the physical characteristics of the microsponges. In vitro dissolution results showed that the release rate of ketoprofen was modified in all formulations.     

酮洛芬缓释胶囊剂制备工艺正交设计实验及其体外释放特性研究

采用小丸包衣工艺,利用正交设计实验对胶囊的处方、工艺进行筛选与优化,制备酮洛芬缓释胶囊,并测定其释放特征。结果表明:以优选的处方和工艺制备的缓释胶囊,体外释药缓释特征明显,持续释药达12h以上。该缓释胶囊处方合理,工艺简单,适合于工业化生产。     

Formulation and in vitro evaluation of ketoprofen fast-dissolving tablets

Drugs exhibiting satisfactory absorption from the oral mucosa or intended for immediate pharmacological action can be advantageously formulated as orally fast-disintegrating tablets (FDTs or ODTs). Therefore, taste masking of active ingredients becomes essential in these systems because the drug is entirely released in the mouth. Despite advances in the FDT technologies, formulation of drugs with a bitter taste is still a challenge, especially when the amount of drug is high. In this study, a new solution is being developed to incorporate higher doses of a model bitter taste drug; ketoprofen, without affecting the fast-disintegrating properties of the formulation. The unpleasant taste of the active drug usually masked by adding flavoring ingredients and sweeteners to improve taste and palatability but in this study a novel approach of using a polymer; Eudragit EPO and a granulation procedure of this polymer with the active drug was applied to mask the bitter taste of ketoprofen. In order to produce ketoprofen FDT formulations, a two-stepped procedure was followed; granulation process with the taste-masking agent (Eudragit EPO) and then direct compression (F3 and F4). In F1 and F2 formulations, granulation process was not implemented in order to observe the effect of application method of Eudragit EPO. As well as observing the effect of taste-masking agent, crospovidone and sodium starch glycolate were used in different concentrations (2, 4 and 8wt%) to examine the influence of superdisintegrants on FDT properties. All the FDTs containing 30?mg ketoprofen (F1, F2, F3 and F4) were evaluated by means of in vitro quality control tests.     

巴洛沙星生物黏附片的制备及体外释药考察

目的：制备巴洛沙星生物黏附片,考察其体外释药行为,并测定其与大鼠离体胃、小肠组织的黏附力.方法：以羟丙基甲基纤维素（HPMCK15M）和甲壳胺（CS）为生物黏附材料和骨架材料,乳糖为稀释剂制备生物黏附片;以0.1 mol·L^-1盐酸溶液（pH 3.0）500mL为溶剂,浆法（转速50 r·min^-1）测定2,8,18,24 h时的释放度.以自制黏附力测定装置测定、比较巴洛沙星生物黏附片及巴洛沙星Ⅱ片对大鼠离体胃、小肠组织的黏附力.结果：巴洛沙星生物黏附片体外释放符合设计要求,其与大鼠离体胃、小肠组织的黏附力明显大于普通片,且与肠的黏附力大于与胃的黏附力.结论：该处方设计及制备工艺合理,能够满足设计要求.     

萘普生缓释微囊的制备及其体外释药研究

目的 对以壳聚糖和海藻酸钠为囊材,通过复凝聚法将萘普生微囊化的制备工艺和体外释药进行研究.方法 以微囊的药物包封率为制备工艺优化指标,得出成囊的最佳制备工艺条件.结果 最佳工艺条件为:搅拌速度500 r·min-1,pH4.0,壳聚糖浓度3%,反应温度50℃.结论 以最佳制备工艺条件制备了可生物相容,自然降解无毒的载药微囊,重现性好,工艺稳定,同时体外溶出实验表明,该微囊具有较好的缓释作用.     

阿司匹林多单元肠溶片的制备及体外溶出度考察

目的：研制阿司匹林多单元肠溶微丸片。方法：采用阿司匹林粉末包衣先制备肠溶包衣微粒,再与适量辅料混合后直接压片制备肠溶阿司匹林微粒片,并对影响其质量的关键因素进行了考察。结果：制备的微粒片溶出度符合阿司匹林肠溶制剂质量的标准要求。     

盐酸帕罗西汀肠溶缓释片的制备及体外释放研究

目的制备盐酸帕罗西汀肠溶缓释片,并对其体外释放度进行考察。方法采用HPMC K100LV和HPMC K4M作为骨架材料,以水乳糖为填充剂制备盐酸帕罗西汀缓释片芯,再使用Eudragit L30D-55包肠溶衣,制成盐酸帕罗西汀肠溶缓释片,并采用f_2相似因子法评价自制制剂和参比制剂在释放介质中的体外释放行为。结果体外释放度实验显示,自制制剂和参比制剂的f_2相似因子值大于50。结论制备的盐酸帕罗西汀肠溶缓释片的释药行为与参比制剂的体外释放行为相似。     

氧化苦参碱缓释胶囊的制备及体外释放特性研究

目的制备氧化苦参碱24h缓释胶囊并对其体外释放特性进行研究。方法采用流化床包衣法,先将氧化苦参碱与聚乙烯吡咯烷酮溶于85%乙醇中,喷于空白丸芯制成含药微丸,再以乙基纤维素水分散体（Surelease）作为主要包衣材料进行包衣,得微丸装胶囊。建立体外分析方法并进行体外释药模型拟合。结果该缓释胶囊的释药符合Higuchi方程,具有缓释制剂的体外溶出特征。结论苦参碱缓释胶囊制备工艺简单,释药稳定,具备优良缓释制剂的特征。     

吲达帕胺缓释胶囊的制备及体外释放度考查

目的:制备吲达帕胺缓释胶囊及考查体外释放特性。方法:以空白丸芯、柠檬酸三乙酯、滑石粉、硬脂酸镁、胶体二氧化硅、聚维酮K30等为骨架材料制备吲达帕胺缓释胶囊;采用高效液相色谱法建立含量测定方法,通过释放度试验评价缓释效果。结果:本品在0.01 mol/L盐酸溶液中可持续释药24 h,其释放规律符合Higuchi方程;前12 h平均累计释放度与时间呈良好线性关系,3批样品与进口吲达帕胺缓释片释放曲线基本一致。结论:本品处方合理,制备工艺简单,体外缓释效果明显。     

TJ0711盐酸盐缓释片的制备及体外释放特性考察

目的:研制TJ0711盐酸盐混合骨架缓释片,并评价其体外释放特性。方法:研究了HPMC的黏度和用量,十八醇、CMC-Na的用量对药物释放的影响,并通过正交试验设计对片剂的处方进行优化。结果:正交设计所得最优处方为十八醇、HPMC K4M、CMC-Na的用量分别为片重的20%,40%,10%。药物体外释放良好,符合Higuchi模型(Q=33.909t1/2-20.263,r=0.996 2),持续释药达12 h。结论:经正交优化的TJ0711盐酸盐缓释片处方可行。     

阿莫西林缓释片的制备及体外释放度的研究

目的 研制阿莫西林缓释片，并对其体外释放度进行了考察。方法 以聚乙二醇6000为固体分散体载体，先将阿莫西林制备成固体分散体，增加阿莫西林在水中的溶出度，再以羟丙甲基纤维素为骨架材料，以水为牯合剂，采用湿法制粒压片，制备阿莫西林缓释片，并进行体外释放度试验。结果 该片在1、2、3、6和8h体外释放度控制在30％～45％、45％～65％、60％～80％、75％～95％和90％以上，药物的体外释放模式符合Highuchi方程。结论 研制缓释片的缓释效果良好。     

灯盏花素缓释片的制备及体外释放度研究

目的以羟丙甲基纤维素为骨架材料制得灯盏花素缓释片,并对释药机制进行探讨。方法进行体外释放度试验,研究体外释放度测定方法,以及辅料和加速稳定性试验对释放度的影响。结果制得的灯盏花素缓释片体外释放度测定结果符合缓释片质量标准中的释放度标准要求。体外释放符合一级释药动力学规律。结论制备灯盏花素缓释片缓释效果明显．方法简单,适于工业化生产。     

烟酸缓释骨架片的制备及体外释放度考察

目的 :制备烟酸缓释骨架片并考察其体外释放度。方法 :以国外上市 Niaspan R○ 作为对照 ,考察了 4种型号的羟丙基甲基纤维素 (HPMC)对释放性能的影响 ,并比较了缓释片在水、0 .1mol/ L 盐酸及 p H6 .8磷酸盐缓冲液三种介质中的释放度。结果 :用 Higuchi方程拟合发现 ,自制片和对照片均具有典型的缓释性能 ,而且自制片和对照片的释放度没有差别。结论 :自制的烟酸缓释骨架片工艺简单易行 ,释放度亦符合要求。     

丁螺环酮缓释片的制备及其体外释放度的研究*

目的：研制丁螺环酮缓释片的最佳处方并考察其释放度。方法：以丁螺环酮为模型药物，新型载体材料聚已内酯（PCL）和羟丙基甲基纤维素（HPMC）为骨架材料，湿法制粒压制丁螺环酮缓释片，测定药物的体外释放度，以拟合方程的相关系数r，T25，T50，Td和T80等质量评价指标来进行处方筛选。结果：根据初步筛选的最佳处方制备的缓释片释放曲线符合Higuchi方程，24h释药超过90％。结论：以PCL和HPMC为骨架材料，能制备出释药24h的丁螺环酮缓释片。     

硝苯地平缓释胶囊的制备及释放度测定

目的 研制硝苯地平24h缓释胶囊并进行体外释放度测定。方法 采用流化床包衣法，将硝苯地平与聚乙烯吡咯烷酮溶于90％乙醇喷于空白丸芯制成固体分散体含药小丸．以含有致孔剂的乙基纤维素水分散体（Surelease）作为包衣材料进行包衣，得小丸装胶囊。对各处方缓释胶囊进行释放度测定，筛选最佳处方并进行体外释药模型拟合。结果 按最佳处方制得的胶囊中药物体外释放行为良好。胶囊体外释药行为符合一级动力学方程 结论 硝苯地平缓释胶囊达到了缓释制剂要求。     

辛伐他汀-烟酸双层缓释片的制备及其体外质量评价

目的 制备辛伐他汀(SVT) -烟酸(NA)双层缓释片并进行体外质量评价.方法 分别通过正交实验和单因素实验,筛选NA缓释层与SVT常释层处方,确定最佳处方组成并制备SVT-NA双层缓释片,测定缓释片中NA与SVT的含量.以国内已上市NA缓释片为参比制剂,测定自制双层缓释片中NA的释放度,计算释放度相似因子(f2),并进行方程拟合.按照中国药典2010版中SVT普通片溶出度测定条件,测定自制双层缓释片常释层中SVT的溶出度.结果 自制双层缓释片中NA的释放度与市售NA缓释片相似(f2＞75),其释放行为符合Higuchi方程;常释层中SVT 30 min内的累积溶出度＞98％,符合中国药典有关规定.结论 SVT-NA双层缓释片处方组成合理,制备工艺稳定,重现性良好,有望开发成为新的复方制剂.     

Preparation and in vitro evaluation of polylactic acid-mitomycin C microcapsules

Abstract

An emulsion method was developed for the incorporation of water-soluble mitomycin C into polylactic acid biodegradable microcapsules. With an average particle size of about 95 μm, microcapsules with a desired loading of from 3.65 to 13.80 per cent were prepared. These microcapsules, which contained both crystalline and finely dispersed drug particles, showed a dose-dependent drug release pattern with microcapsules of higher drug loading having a faster release rate than those of lower drug loading. Effective sterilization of the microcapsules for parenteral use was achieved by ⁶⁰Co γ-ray irradiation, which did not affect the microcapsule structure, release rate or drug stability. Mitomycin C showed dose-dependent antiproliferative activity against the growth of the K562 human erythroleukaemia cells. The microencapsulated dosage form of mitomycin C was found to enhance the drug's activity through sustained drug release. In experiments where drug concentrations in the cell medium were reduced according to the drug's biological half-life, the microcapsule systems showed a distinct advantage over the non-capsulated dose for the kinetic inhibition of K562 cell growth.