乳洁安缓释片的制备及体外释药

目的:研制乳洁安亲水凝胶缓释骨架片,进行体外释放度考察并解析其释药机制。方法:以羟丙基甲基纤维素(HPMC)为缓释骨架材料,通过正交设计优化处方,并考察释放介质黏度、pH值、溶出方法、转速及制片工艺等因素对缓释片体外释放度的影响。结果:正交设计获最优处方为A3B1C1,即HPMC作为亲水凝胶骨架材料,用量为40%,EC用量为10%,乳糖和MCC用量均为5%。药物体外释放行为符合Higuich方程。结论:该方法制得的缓释片具有良好的缓释效果,且制备工艺简单易行。     

烟酸凝胶骨架缓释片的处方工艺研究

目的:优化烟酸凝胶骨架缓释片处方工艺。方法:采用亲水凝胶骨架材料羟丙基甲基纤维素(HPMC)的2种型号K15M、E15-LV及辅料磷酸氢钙的处方用量为因素设计正交试验,以体外释放度为考察指标,优化烟酸凝胶骨架缓释片的处方,并进行批内和批间体外释放度验证试验。结果:优化处方为HPMC(K15M、E15-LV)分别为4%、40%,磷酸氢钙为25%。所制烟酸凝胶骨架缓释片可持续释药12h,批内释放均一性及批间重现性均良好。结论:所选烟酸凝胶骨架缓释片处方合理,工艺简单。     

齐墩果酸缓释片的研制及体外释放度考察

目的：制备齐墩果酸缓释片并考察其体外释放度。方法：以羟丙基甲基纤维素（HPMC）为缓释骨架材料，加淀粉和乳糖作填充剂。通过正交设计优化处方，并考察制剂大小，硬度，释放介质，pH及转速等因素对缓释片体外释放度的影响。结果：正交设计获最优处方为A2B3C1。即亲水凝胶骨架材料为HPMC（K4M），用量为30％。淀粉与乳糖的比例为1：1。药物体外释放行为符合Higuich方程。结论：该方法制得的缓释片具有良好的缓释效果。且制备工艺简单易行。     

青藤碱固体脂质纳米粒凝胶骨架缓释片的制备及处方优化

目的：制备青藤碱固体脂质纳米粒凝胶骨架缓释片,考察凝胶骨架缓释片处方因素对青藤碱固体脂质纳米粒体外释药行为的影响。方法：采用乳化蒸发-低温固化法制备青藤碱固体脂质纳米粒。以羟丙基纤维素（HPMC）为骨架材料制备青藤碱固体脂质纳米粒凝胶骨架缓释片,单因素考察吸附剂种类、骨架材料比例、PEG种类和骨架材料用量对缓释片体外释药的影响,正交试验进一步优化处方,并对释药模型进行拟合。结果：骨架材料比例和PEG种类是影响青藤碱固体脂质纳米凝胶骨架缓释片体外释药行为的主要影响因素,优化后的处方体外释放行为符合一级释药模型,释药方程为ln（1-M_t/M_∞）=-0.187 2 t+0.071 2（r=0.991 1）,累积释放度在12 h内可达90.15%。结论：优化后的青藤碱固体脂质纳米粒凝胶骨架缓释片制备工艺简单,重复性良好,在12 h内具有良好的体外缓释特征。     

非洛地平-美托洛尔缓释片处方优化及体外释放一致性评价

目的 优化非洛地平-美托洛尔缓释片的处方，并评价其与市售制剂体外释放的一致性。方法 采用HPLC测定非洛地平-美托洛尔缓释片中非洛地平及美托洛尔的释放度；以体外释放度为评价指标，重点考察了固体分散体、微丸以及片芯中关键处方因素对非洛地平/美托洛尔释放行为的影响，进一步优化处方。结果 微丸组成、微丸粒径、微丸衣膜中致孔剂用量、微丸增重以及片芯中阻滞剂用量均影响药物释放；处方优化后自制的非洛地平-美托洛尔缓释片与市售制剂在0.3% SDS水溶液、含0.3% SDS的pH 4.0的柠檬酸缓冲液、含0.3% SDS的pH 6.8的磷酸盐缓冲液、含0.3% SDS的0.1 mol·L^-1 HCl中的体外释放行为一致。结论 自制非洛地平-美托洛尔缓释片与市售制剂的体外释放行为一致。     

长春西汀海藻酸钠骨架片体外释药影响因素研究

目的以海藻酸钠为骨架材料 ,制备长春西汀控释骨架片 ,对影响其体外释放的多种因素进行了考察。方法以海藻酸钠为亲水骨架材料 ,粉末直接压片制备长春西汀控释片 ,采用《中华人民共和国药典》2 0 0 0年版二部收载的溶出度测定方法Ⅱ法 (桨法 ) ,测定药物在不同条件下的体外释放度 ,考察海藻酸钠用量及黏度 ,枸橼酸用量 ,释放介质离子强度和pH值对药物体外释放行为的影响。结果与结论海藻酸钠用量及黏度 ,枸橼酸用量 ,释放介质离子强度和pH值均对药物体外释放行为有显著影响。值得注意的是 ,通过调节处方中枸橼酸用量可以使释药行为达零级 ,这为制备长春西汀控释片提供指导 ,有进一步开发的价值。     

黄连总生物碱胃内漂浮缓释片处方组成的研究

目的：研究黄连总生物碱胃内漂浮缓释片的处方组成及影响因素。方法：以体外释放度为指标,筛选黄连总生物碱胃内漂浮缓释片的处方组成,采用单因素试验法,考察处方中HPMC、海藻酸钠、碳酸氢钠三个因素对其体外释放度的影响。结果：黄连总生物碱胃内漂浮缓释片较优的处方组成为HPMC13.4%,海藻酸钠26.6%,硬脂酸镁5.4%,硬脂酸42%,碳酸氢钠10.6%,HPMC与碳酸氢钠的用量显著影响黄连总生物碱胃内漂浮缓释片的体外释放度。结论：HPMC与海藻酸钠以1：2配伍使用作为片剂亲水凝胶骨架时,其体外释放度良好,且两者具有交互作用。     

愈创甘油醚缓释片的研究

目的研究1天给药2次的愈创甘油醚骨架型缓释片。方法以HPMC为骨架材料,采用正交试验设计,考察HPMC的不同型号和不同用量对释放度的影响,筛选出最佳处方。结果体外释放度实验表明,缓释片比普通片释药时间延长,其体外释放行为符合Higuchi(r=09915)方程。结论该缓释片处方工艺简单,适合工业化生产;缓释效果明显。     

愈创甘油醚缓释片的研究

目的 研究1天给药2次的愈创甘油醚骨架型缓释片。方法 以HPMC为骨架材料，采用正交试验设计，考察HPMC的不同型号和不同用量对释放度的影响，筛选出最佳处方。结果体外释放度实验表明，缓释片比普通片释药时间延长，其体外释放行为符合Higuclli(r=0．9915)方程。结论 该缓释片处方工艺简单，适合工业化生产；缓释效果明显。     

枸橼酸钾凝胶骨架缓释丸体外释放的影响因素研究

目的 自制枸橼酸钾凝胶骨架缓释丸,考察影响其体外释放度的处方和工艺因素。方法 实验采用硫酸铜比色法测定枸橼酸钾含量,研究不同型号、不同黏度的HPMC、丸剂大小及压力大小对药物释放的影响。结果 该缓释微丸的体外释放度与美国药典对枸橼酸钾缓释片体外释放度的相关要求相符。结论 该剂型可以作为缓释片的替代剂型用于相关疾病的治疗。     

血塞通脉冲控释片的处方优化

目的:优化血塞通脉冲控释片的处方。方法:采用单因素试验考察片芯崩解剂种类、片芯崩解剂用量、包衣液组成和包衣增重百分率对药物累积释放率的影响;采用正交试验考察片芯崩解剂用量、包衣液组成、包衣增重百分率对释药时滞时间的影响,优化血塞通脉冲控释片的处方。结果:最佳处方为片芯崩解剂用量为15%,包衣增重百分率为9%,包衣液组成为Eudragit L100∶EC=1.5∶1(m/m);在该处方条件下,血塞通脉冲片的体外释药时滞为6 h左右,然后迅速脉冲式释药。结论:所选处方合理,制备的血塞通脉冲控释片能达到设计要求,体外试验可达到脉冲释药时滞效果。     

响应面法优化富马酸喹硫平缓释片处方

目的:优化富马酸喹硫平缓释片处方。方法:以累积释放度综合评分作为响应值,采用3因素3水平的响应面法,确定富马酸喹硫平缓释片处方中羟丙甲纤维素(HPMC)的黏度、用量与枸橼酸钠、乳糖的用量,并探讨其体外释药机制。结果:骨架材料选择HPMC K15M,考虑到实际操作便利确定其用量为13.5%,枸橼酸钠用量为9.5%,乳糖用量为14%。缓释片体外释放符合Higuchi方程,释药机制为扩散和溶蚀并存的双重机制。结论:筛选所得的富马酸喹硫平缓释片处方工艺稳定可行,有一定的缓释作用。     

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。     

Alginate-diltiazem hydrochloride beads: optimization of formulation factors,in vitro and in vivo availability

Alginate beads containing diltiazem hydrochloride (DTZ) were prepared by the ionotropic gelation method. The effects of various factors (alginate concentration, additives type, calcium chloride concentration and curing time) on the efficiency of drug loading were investigated. The formulation containing a mixture of 0.8% methylcellulose (MC) and 4% alginate cured in 2% calcium chloride for 6 h was chosen as the best formula regarding the loading efficiency. The release rate of DTZ from various beads formulations was investigated. The release of drug from alginate beads followed two mechanisms; by diffusion and relaxation of the polymer at pH 1.2, whilst diffusion and erosion are at pH 6.8. The in vitro release of DTZ from MC-alginate beads showed an extended release pattern which was compared with that from commercially available sustained-release (Dilzem SR) and fast release tablets (Dilzem). Thermal analysis revealed that the drug was molecularly dispersed in the beads matrix. Although the release characteristics of DTZ from Dilzem SR and MC-alginate beads were completely different, the bioavailability of DTZ in dogs was comparable as measured by AUC, MRT and relative bioavailability. The absolute bioavailability of MC-alginate beads and Dilzem SR was 88 and 93%, respectively.     

甲硝唑缓释片处方优化研究

目的优化甲硝唑缓释片的处方。方法采用正交试验设计,以体外累积释放度为指标,以羟丙基甲基纤维素(HPMC)的规格、HPMC和乳糖的用量为考察因素,筛选甲硝唑缓释片的最佳处方。结果最佳处方为HPMC的规格为K4M、HPMC 20%、乳糖10%;优化后所制制剂可持续释药12 h。结论甲硝唑缓释片处方合理,具有良好的缓释效果。     

Evaluation of alginate based mesalazine tablets for intestinal drug delivery.

The aim of this study was to develop the alginate based mesalazine tablets for intestinal delivery. Sodium alginate is a biocompatible, natural polymer with pH-sensitive gel-forming ability. Matrix tablets were prepared with two types of sodium alginate of different amounts. The in vitro release characteristics of mesalazine from alginate tablets were compared with those of the commercial product (Salofalk). X-ray imaging was used to monitor the tablets throughout the gastrointestinal system. Although alginate tablets gave a faster release in an acidic medium compared with the commercial product (Salofalk), the cumulative amount of released drug of the optimum formulation was found to be almost the same as that of the commercial product at the end of 4 h. The alginate type and amount in the matrices played an important role in basic media. The release of the optimum formulation containing low viscosity alginate was found to be almost identical to that of the commercial product in acidic and basic media. Tablets were visualized to determine whether they were located in the terminal ileum or cecum for 3-6 h. Mesalazine-alginate matrix tablet formulations can deliver the drug to the small and large intestine. Thus, the alginate matrix system may be a promising system for the treatment of Crohn's disease involving both the ileum and large intestine.     

复方缬沙坦双层片的处方筛选及优化

目的:优选由硝苯地平缓释层与缬沙坦速释层组成的双层片处方。方法:先制备硝苯地平固体分散体,以丙烯酸树脂Eudragit NE30D为缓释骨架材料,采用正交试验设计优选处方;然后以缬沙坦在30 min的释放度为评价指标优化速释层的处方。结果:硝苯地平缓释层的最佳处方为Eudragit NE30D(以聚合物干重计)3.0%,乳糖为40%,磷酸氢钙为35%;缬沙坦速释层的最佳处方为乳糖18%、微晶纤维素40%、羧甲基淀粉钠6%、十二烷基硫酸钠10%。结论:正交试验优化的双层片处方良好,达到了设计要求。     

茶碱缓释片的制备及其初步稳定性考察

目的：考察茶碱羟丙基甲基纤维素（HPMC）骨架片的制备方法及其初步稳定性。方法：以HPMC为骨架材料,采用湿颗粒法制备茶碱缓释片,考察了HPMC用量、HPMC黏度及释放介质pH值对药物体外释放行为的影响,以及光照、高温及高湿度对茶碱缓释片稳定性的影响。结果：HPMC用量和黏度显著影响茶碱释药速率,释放介质pH值对茶碱释药速率影响较小。光照、高温及高湿度不影响茶碱缓释片的含量及释放度。结论：通过使用合适黏度的HPMC及调节HPMC用量可获得具有理想释药行为的茶碱缓释片,且其稳定性良好。     

In vitro characterization and release study of Ambroxol hydrochloride matrix tablets prepared by direct compression

A series of either hydrophilic or hydrophobic polymers were used to prepare controlled release Ambroxol hydrochloride (AMX) matrix tablets by direct compression. Both the compatibility and flow properties of AMX/polymer mixtures were investigated. The effect of the amount and type of polymer on the physical properties and in vitro drug release was studied and compared to commercially available Ambroxol(?) SR capsules. A kinetic study of the release profile of AMX from the prepared matrix tablets was performed. All excipients used in the study were compatible with the model drug. AMX/drug mixtures containing sodium alginate (NA) and hydroxypropylmethyl cellulose (HPMC) showed better flow properties than other polymers used in the study. The in vitro drug release studies showed that matrix tablets formulae containing 10% HPMC (S7) or a combination of 30% NA and 5% HPMC (Ah) exhibited a higher ability to control the release of AMX. The kinetic study revealed that a diffusion controlled mechanism prevailed except when carbopol was used. Formula Ah followed a non-fickian diffusion mechanism similar to Ambroxol(?) SR capsules. Both formulae S7 and Ah could be considered as potential candidates for formulation of AMX controlled release matrix tablets.