高于饱和装填量时的平板混合药膜体系释放动力学模型

针对最一般的情况建立了Ｃｄ＞Ｃｓ时的混合药膜的释放动力学模型,用拉氏变换求得了解析解,该模型可通过相应简化而获得一些特定情况的解;用５－氟脲嘧啶／ＥＶＡＬ混合药膜体系的释放实验数据对所提出的模型进行了验证并与Ｈｉｇｕｃｈｉ模型进行了比较。结果表明：在中等装填量的情况下如：１５.５＜Ｃｄ＜１２３.６ｍｇ·ｃｍ(－３)时,本文模型与实验数据符合的很好,预测精度比Ｈｉｇｕｃｈｉ模型高,特别是在Ｃｄ＜１５．５ｍｇ·ｃｍ(－３)时;这两个模型均不能较好描述较高装填量的情况,如Ｃｄ＞２１０ｍｇ．ｃｍ(－３),这种情况我们在别处已经作过讨论（８,９）。     

Sustained Release of Amoxicillin from Chitosan Tablets

Sustained release systems in the forms of chitosan (CTS) tablet and extrude for releasing amoxicillin were studied. The degradation of amoxicillin in pH 1.2 was determined. The effects of particle sizes of chitosan on the dissolution profiles were investigated. The result showed that chitosan with the particle size less than 75 microm yielded the best controlled release pattern and it was comparable to that was obtained from the hydroxypropylmethylcellulose (HPMC) tablets. Moreover, the tablets containing chitosan with particle size less than 75 microm were able to provide a significantly improved sustained release profile of amoxicillin compared to the release profile of a commercial capsule. All release profiles of amoxicillin from the chitosan tablets could be described by first-order kinetics.     

马来酸氟吡汀缓释片的研制及体外释放特性考察

目的：采用羟丙甲基纤维素（HPMC）作为亲水凝胶骨架材料,制备马来酸氟吡汀缓释片,并考察其体外释放特性。方法：通过单因素试验,分剐考察了HPMC、乳糖用量对马来酸氟吡汀缓释片释放速率的影响;以体外释放度为评价指标优选处方的最佳组成和比例。结果：马来酸氟吡汀缓释片的释放速度随处方中HPMC含量增加而减慢,随乳糖用量增多而加快;释放介质对马来酸氟吡汀的释放速率也有明显影响,而释放度测定方法、转速对马来酸氟吡汀缓释片的释放速率无明显影响。结论：本品处方组成合理,制备工艺稳定。制备的马来酸氟吡汀缓释片,体外释药曲线显示有明显的缓释作用,属于零级释放。     

烟酸凝胶骨架缓释片的稳定性考察

目的：考察烟酸凝胶骨架缓释片贮存期间稳定性。方法：采用加速试验和长期试验方法，考察外观性状、含量和释放度。结果：密封包装条件下，36个月内外观性状、含量和释放度检查结果没有显著性变化。结论：该制剂密封条件下贮存，有效期可以定为2年。     

盐酸曲马多缓释片和胶囊剂的体外释放度对比研究

对盐酸曲马多缓释片和胶囊剂的体外释放模式及在不同ｐＨ条件下的体外累积释放度和释放速率进行对比研究。缓释片剂体外释放符合一级动力学模式,而缓释胶囊剂体外释放则符合Ｈｉｇｕｃｈｉ方程,二者在不同ｐＨ介质中的累积释放百分率及释放速率均有显著性差异（Ｐ〈０．０５）。表明两种盐酸曲马多缓释制剂体外释放模式存在差异。而且ｐＨ对二者的体外释放过程具有明显影响。     

氢溴酸高乌甲素亲水凝胶骨架片的制备及体外释放

目的为了减少给药次数,方便患者,并提高镇痛效果,制备氢溴酸高乌甲素亲水凝胶骨架片,优化制剂处方,并探讨释放机制。方法以羟丙甲纤维素(HPMC)为骨架材料,乳糖、微晶纤维素(MCC)、淀粉为填充剂,硬脂酸镁为润滑剂制备氢溴酸高乌甲素骨架片,考察各因素对药物释放度的影响,筛选优化处方,并拟合讨论其释放机制。结果 HPMC的用量及分子量,微晶纤维素和硬脂酸镁的用量对药物释放有显著影响。所制缓释片无突释现象,缓释周期12 h,根据拟合方程,药物释放符合一级释放模型,其释放既有扩散,又有骨架溶蚀。结论本方法制备的氢溴酸高乌甲素缓释片工艺简单,生产成本低,且具有良好的释放性能。     

氢溴酸加兰他敏缓释片的研制

目的研制氢溴酸加兰他敏缓释片并建立释放度测定方法。方法用正交设计优选处方，以单硬脂酸甘油酯、Eudragit L100-55为主要缓释材料，考察其用量及滑石粉用量对缓释片的影响。用紫外．可见分光光度法测定主药含量，并根据《中国药典》2005年版释放度测定方法，建立了体外释放度测定方法。结果氢溴酸加兰他敏缓释片在24h内呈现良好的缓释特征，释药行为符合Higuchi方程，制备工艺及释放度测定方法简单易行。结论该氢溴酸加兰他敏缓释片处方设计合理，可进一步研究开发。     

氢溴酸加兰他敏缓释片的研制

目的研制氢溴酸加兰他敏缓释片并建立释放度测定方法。方法用正交设计优选处方,以单硬脂酸甘油酯、Eudragit L100-55为主要缓释材料,考察其用量及滑石粉用量对缓释片的影响。用紫外-可见分光光度法测定主药含量,并根据《中国药典》2005年版释放度测定方法,建立了体外释放度测定方法。结果氢溴酸加兰他敏缓释片在24 h内呈现良好的缓释特征,释药行为符合Higuchi方程,制备工艺及释放度测定方法简单易行。结论该氢溴酸加兰他敏缓释片处方设计合理,可进一步研究开发。     

Effect of Processing Methods and Heat Treatment on the Formation of Wax Matrix Tablets for Sustained Drug Release

The objective of this study was to evaluate the effects of processing methods and heat treatment on matrix formation and subsequent drug release from wax matrix tablets for controlled release. Phenylpropanolamine hydrochloride (PPA) and Compritol® were processed with appropriate diluent(s) using either dry blending (DB), wet granulation (WG), partial melt granulation (PMG), or melt granulation (MG). Then the tablets were heat-treated at 80°C. Particle size distribution and compressibility, along with drug release, tablet micro-morphology, wettability, porosity, and tortuosity were investigated. The drug release was different for the four processing methods even though the tablet formulation was identical. Heat treatment further retarded drug release and its effect was related to the previous manufacturing processes. Scanning Electron Microscopy (SEM) showed that heat treatment redistributed the wax and formed a film-like structure covering drug and excipients. The contact angle of tablets made from DB, WG, and PMG methods increased after heat treatment, while that of tablets made from DB, WG, and PMG methods increased after heat treatment, while that of tablets made from MG remained constant. Tablet tortuosity calculated from drug release rate constants increased dramatically after heat treatment. Drug release from the wax tablets with or without heat treatment was best described by the Higuchi equation. Different processing methods produced different matrix structures that resulted in different drug release rates. Heat treatment retarded drug release mainly by increasing tortuosity of the matrix. Contact angle measurement and SEM analysis indicated that heat treatment caused the wax to melt, redistribute, coat the drug and diluents, and form a network structure.     

美托拉宗缓释片的制备和释药机制的研究

目的 制备美托拉宗缓释片并探讨其释药机制.方法从处方和工艺两个方面考察了各因素对药物释放行为的影响.在单因素考察的基础上,采用羟丙甲基纤维素(HPMC)4000 cps作为骨架材料HPMC 5 cps作为致孔剂,制备美托拉宗缓释片.通过正交设计,以2、4、7 h的药物释放度为评价指标,优化最佳处方.结果HPMC的用量和...     

Relationship Between Polymer Viscosity and Drug Release from a Matrix System

Pharmaceutical Research -     

Formulation and Evaluation of Dextromethorphan Hydrobromide Sustained Release Tablets

Sustained release (SR) matrix tablets of dextromethorphan hydrobromide were prepared by wet granulation using hydroxypropyl methyl cellulose (HPMC-K-100 CR) as the hydrophilic rate controlling polymer. The effect of the concentration of the polymer and different fillers on the in vitro drug release rate was studied. The studies indicated that the drug release can be modulated by varying the concentration of the polymer and the fillers. A complete cross-over bioavailability study of the optimized formulation of the developed sustained tablets and marketed immediate release tablets was performed on six healthy male volunteers. The extent of absorption of drug from the SR tablets was significantly higher than that for the marketed dextromethorphan hydrobromide tablet because of lower elimination rate and longer half-life.     

芦丁缓释骨架片释药机制影响因素考察

目的：考察芦丁缓释骨架片释药机制的影响因素。方法：以羟丙基甲基纤维素(HPMC)为骨架材料制备缓释骨架片，利用Peppas经验式释放指数n值，评价HPMC、微晶纤维素(MCC)、可压性淀粉用量对芦丁缓释骨架片体外释药机制的影响。结果：释药速率随HPMC含量增高而减慢，MCC和可压性淀粉的加入均加快芦丁释药速率。结论：HPMC、MCC、可压性淀粉的用量对释药机制均有影响，以HPMC用量影响较大。     

布洛芬缓释片的人体生物等效性研究

目的:研究布洛芬缓释片在健康人体内的药动学及其相对生物利用度,以评价其与布洛芬缓释胶囊的生物等效性。方法:18名男性志愿者,随机分为2组,分别口服布洛芬缓释片(受试制剂)与布洛芬缓释胶囊(参比制剂)后,采用高效液相色谱法测定血药浓度,用3p97药动学程序拟合,计算药动学参数。结果:受试制剂与参比制剂Cmax分别为(25.43±0.78)、(26.87±0.66)μg·mL-1,tmax分别为(3.67±0.52)、(3.83±0.75)h,AUC0~24分别为(181.20±5.12)、(187.58±5.29)μg·h·mL-1,AUC0~∞分别为(184.34±5.35)、(191.19±4.87)μg·h·mL-1,MRT分别为(6.51±0.73)、(6.80±0.48)h;受试制剂的相对生物利用度为103.7%。结论:与参比制剂比,布洛芬缓释片有较好的缓释效果。     

尼莫地平缓释胶囊的释放度与其普通片的溶出度比较

目的　在相同介质中将尼莫地平缓释胶囊的释放度与普通片的溶出度作比较。方法　利用ZRS 8C型药物智能释放仪 ,采用转篮法 ,溶出介质为 0 5 5 %的十二烷基硫酸钠水溶液 ,溶出杯内温度为 ( 37± 0 5 )℃ ,转速为 5 0± 1r/min ,分别在不同的时间点取样 ,在波长为 36 0nm处测定吸收度 ,计算出释放度和溶出度。结果　尼莫地平缓释胶囊在 6 0min的累积释放率为 4 4 17% ,而普通片的累积溶出率达到了 90 91%。结论　尼莫地平缓释胶囊与普通片相比 ,血药浓度明显平稳 ,从而使药效延长 ,达到了提高人体生物利用度的目的     

米诺环素亲水凝胶型缓释骨架片的制备及体外释放度考察

目的:制备米诺环素亲水凝胶型缓释骨架片并考察其体外释放度。方法:采用粉末直接压片工艺制备缓释片;采用紫外分光光度法测定其释放度,同时考察羟丙基甲基纤维素(HPMC)的不同规格、用量以及不同释药条件对药物释放速率的影响。结果:所制制剂为黄色片剂,检查项符合2005年版《中国药典》中的相关规定。试验确定了以HPMCK100为缓释骨架材料,处方用量为32%;不同释放介质与释放装置对药物的释放均有显著影响。释放规律符合Higuchi方程。结论:该制剂处方工艺简单,体外释放度测定方法准确易行,制剂具有明显的缓释效果。     

硫酸伪麻黄碱凝胶骨架型缓释片的制备与释放度试验

目的 研制硫酸伪麻黄碱缓释片并对其释放度的影响因素进行考察，方法 以羟丙甲纤维者（HPMC）为骨架材料制备硫酸伪麻黄碱凝胶骨架型缓释片，采用紫外分光光度法测定体外硫酸伪麻黄碱，并对缓释片进行释放度试验，结果 HPMC用量增加时释放速度变慢。磷酸氢钙用量增加时片削可压性得以改善．结论 该制刺缓释效果良好。     

盐酸安非他酮缓释片人体药代动力学研究

目的:研究国产盐酸安非他酮缓释片在中国健康人体内的药代动力学特征.方法:19名健康男性志愿者单剂量口服300mg盐酸安非他酮缓释片,采用HPLC法测定血浆中盐酸安非他酮浓度,并用3P97软件统计处理.结果:盐酸安非他酮供试缓释片药-时曲线符合二室模型,其Cmax为(221.08±64.42)μg·L-1;tmax为(2.95±0.78)h,t1/2为(16.78±5.26)h;AUC0-48为(1758.4±323.7)μg·L-1·h;AUC0-∞为(1969.2±351.4)μg·L-1·h.结论:为临床合理用药提供了参考资料.     

骨架片在缓释给药系统中应用

本文研究的主要内容是骨架片作为一种有效的缓释给药系统的基本信息。骨架片是用来调节药物释放最常用的方法。骨架片受到广泛的欢迎,而且是治疗的首选,因为它能提高患者的顺应性,减少药物剂量和副作用,还能增加安全性。不同的聚合物材料能够被用来设计出适宜的释放曲线,并提供一个可行的和一致性的生产模式。     

硫酸锌缓释片研究

用高分子亲水性胶体作为主要骨架材料制备了硫酸锌骨架型缓释片SR-1 SR-2,用普通片C-T作对照,测定了SR-l、SR-2及C-T片的体外溶出累计百分率。用溶出速度参数T50作比较,SR-1,SR-2的缓释作用分别为普通片的4.7倍和2.8倍。锌含量测定采用锌试剂(zincon)紫外分光光度方法。