盐酸地尔硫卓控释微丸的研究

采用包衣法制备含有速释和缓释两部分的地尔硫控释微丸。体外溶出试验表明，微丸在最初１ｈ溶出主药２０％之后以缓慢平稳的速度持续释药，其释药曲线与对照制剂恬尔心缓释胶囊接近，零级释药速率常数为７．２５％／ｈ。其释药速度受介质ｐＨ的影响，但受转速的影响较小。控释微丸在４０℃、相对湿度７５％时贮存３个月，质量稳定。     

雷公藤双层片的制备工艺研究

目的：以丙烯酸树脂Ⅱ为主要材料，研究雷公藤双层片制备工艺。方法：分别对双层片速释部分、缓释部分进行辅料筛选，通过正交设计试验，以体外溶出度测定优化处方和工艺。结果：处方优选为速释部分：雷公藤浸膏15g，淀粉适量，碳酸钙10g：缓释部分：雷公藤浸膏35g，PEG600017．5g，糊精52．5g，丙烯酸树脂Ⅱ10．5g。雷公藤双层片在2，5，10h药物释放分别达到20％-40％，40％-65％，75％以上。结论：本处方合理、工艺可行，适于雷公藤双层片的制备，产品缓释性能良好。     

离子强度对丙基甲基纤维素骨架片释药的影响

目的：探讨溶出介质的离子强度对难溶性药物的丙基甲基纤维素（HPMC）骨架片释药的影响。方法：以甲氧苄胺嘧啶、卡马西平、磺胺甲恶唑和茶碱4种难溶性药物为模型药物，测定5种不同离子强度介质（水、0．20％氯化钠溶液、0．50％氯化钠溶液、0．90％氯化钠溶液和1．80％氯化钠溶液）下的药物释放度和溶出参数。结果：难溶性药物的HPMC骨架片释药随着其溶出介质离子强度的增加而减慢。结论：释药速率与离子强度之间存在较好的线性负相关关系。     

豆豉溶栓酶肠溶片剂的制备及体外释放度

采用均匀设计优化豆豉溶栓酶肠溶片片芯的制备工艺。结果表明，按优化处方经工艺过程制得的片芯酶活性损失仅6％。包肠溶衣后的制品在0．1mol／L盐酸中2h平均累积释放率为2．1％；在0．2mol/L磷酸钠缓冲液（pH6．8）中，23．4min累积释药50％，45min释药86．3％，释药规律符合Weibull分布模型。     

尼群地平口服定时释药片的成型工艺考察

目的：研究尼群地平口服定时释药片的成型工艺。方法：以崩解时间为指标筛选片芯处方、工艺。应用薄膜包衣技术，采用羟丙基甲基纤维素（HPMC）为成膜材料，巴西棕榈蜡和蜂蜡混合物为阻滞剂制备尼群地平口服定时释药片，并考察巴西棕榈蜡和蜂蜡混合物用量、比例、片芯增重量、不同pH溶出介质和转篮转速对定时释药的影响。结果：经过筛选确定片芯处方为每片含尼群地平10mg，微晶纤维素（MCC）81mg，低取代羟丙基纤维素（L-HPC）9mg，硬脂酸镁0．5％；包衣混悬液处方为5％HPMC，3．5％巴西棕榈蜡，1．5％蜂蜡，0．5%PEG4000，0．5％吐温-80，89％水。结论：巴西棕榈蜡和蜂蜡混合物用量与比例，包衣层厚度，是影响定时释药的主要因素。巴西棕榈蜡和蜂蜡混合物用量越多，释药时滞越长；混合物总量不变，蜂蜡用量增大，释药时滞变长；包衣层厚度越厚，释药时滞变长。     

6种阿莫西林胶囊及片剂的溶出度比较

本文采用分光光度法测定了6个厂家阿莫西林的3种胶囊以及3种片剂（普通片、速溶片、可溶片）的体外溶出度，方差分析表明，6个厂家的产品在45min时的累积溶出量无显著性差异（P＞0．05）；胶囊剂与片剂之间的溶出速率有极显著性差异（P＜0．01）。尤其是速溶片及可溶片的初始溶出速度比普通片剂及胶囊剂快。初始释药速率依次为F＞E＞D＞A＞B＞C厂。     

奥美拉唑胃溶速释片的制备及处方研究

目的：制备奥美拉唑胃溶速释片，并考察其处方工艺。方法：采用羟丙纤维素为囊材、喷雾干燥法制备奥美拉唑微囊，再与抗酸剂碳酸氢钠和氢氧化镁混合压片。建立HPLC法测定奥美拉唑微囊的包封率及其片剂在模拟胃酸介质中的溶出度，并考察片剂对溶出介质pH的影响，进行处方筛选研究。结果：每片胃溶速释片最优处方：奥美拉唑40mg，碳酸氢钠350mg，氢氧化镁600mg，囊心物与囊材的用量比为1：2。微囊包封率为92．54％。片剂最大溶出度为75％，奥美拉唑在数分钟内快速溶出，其溶出介质的pH在3．5以上至少可维持30分钟。结论：该制剂在溶出介质中能快速释放奥美拉唑，其中微囊可延缓药物溶出，而抗酸剂可以提高胃内pH值，从而减少奥美拉唑在胃酸性环境的降解。     

时间控制型结肠定位释药片体外释放的影响因素

以美沙拉嗪为模型药物，制备含不同有机酸的片芯，依次包内隔离层（HPMC）、胃溶衣层（丙烯酸树脂Ⅳ）、外隔离层（HPMC）和肠溶衣层（HPMCP），制得时间依赖型结肠定位释药片。考察了有机酸种类、用量及内隔离层和胃溶衣层增重对片剂释放时滞的影响。结果表明，片芯含琥珀酸50mg、内隔离层和胃溶衣层增重分别为1．2％和12％的片剂，在模拟胃肠液中的时滞约5h,6h累积释放达85％以上。     

尼莫地平固体分散体在速释制剂中的溶出性质(英)

为了提高难溶性药物尼莫地平的溶出度,并在此基础上研制出其速释制剂,本研究选用PVP（k30）为载体制备了尼莫地平的固体分散体及机械混合物,比较了二者体外药物溶出度及药物的结晶形态,并考查了共沉淀物的稳定性。进而进行了尼莫地平速释片剂处方的筛选,并按最优处方制备了胶囊剂。比较了自制速释胶囊剂与市售片剂的释药情况。体外实验结果表明,固体分散体对尼莫地平溶出度的提高大大优于机械混合物,5分钟的释药量,前者为89％,而后者仅为45％。X-射线衍射实验表明,尼莫地平在以PVP为载体的固体分散体中是以非晶体形式存在,并且在室温并密封于玻璃瓶中放置一年后仍无结晶出现。本研究制备的片剂和胶囊剂都具有速释性质,而以胶囊剂为优,说明压片压力可能影响溶出。速释胶囊的释药速率大大高于市售普通片剂。     

瑞格列奈二甲双胍缓释片的制备

目的设计并制备瑞格列奈二甲双胍双层片。方法以释放度为指标筛选优化处方。结果以羟丙基纤维素（HPMC）及乙基纤维素（EC）为缓释层辅料,以氯化钠（NaCl）及包衣粉为速释层辅料制备了双层片。缓释层及速释层均可获得良好的溶出行为。结论瑞格列奈二甲双胍双层片的制备工艺简单可行。     

Synthesis,characterization and evaluation of deacetylated xanthan derivatives as new excipients in the formulation of chitosan-based polyelectrolytes for the sustained release of tramadol

This paper addressed the application of deacetylated xanthan (XGDS) and chitosan (CTS) as a mixture blend forming hydrophilic matrices for Tramadol (TD) sustained release tablets. XGDSs derivatives were obtained by alkaline treatment of xanthan gum (XG) with various degrees of deacetylation (DD). The obtained products were characterized in terms of structural, thermal and physicochemical properties. Different tablet formulations containing CTS/XGDSs were prepared by direct compression method and compared to CTS/XG tablets. Flow properties of powder mixtures and pharmaceutical characteristics were evaluated. The dissolution test of TD was realized under simulated gastric and intestinal conditions to achieve drug release more than 24 h. All developed tablets were found conforming to standard evaluation tests. It was shown that CTS/XGDSs matrices ensure a slower release of TD in comparison with CTS/XG based formulations. Meanwhile, increasing DD resulted in a decrease of drug release. In addition, TD release from XGDS matrices was faster at pH (6.8) than at acidic pH (1.2). The matrix tablets based on CTS/XGDS4 (DD = 98.08%) were selected as the best candidates compared to the other systems in prolonging drug release. The optimal formulation was found to release 99.99% of TD after 24 h following a non-Fickian type.     

对高效硝苯地平微丸在人体内的生物利用度研究

本文对６名健康志愿受试者口服硝苯地平微丸胶囊和常规片剂的药动学进行了交叉比较；并介绍了一种简单、快速、准确的高效液相方法检测硝苯地平的血药浓度。结果表明与常规片剂相比．硝苯地平微丸胶囊的相对生物利用度为１７２％。     

Cryptotanshinone ameliorates renal ischaemia–reperfusion injury by inhibiting apoptosis and inflammatory response

Cryptotanshinone (CTS) is a natural compound from the Chinese herb Salvia miltiorrhiza. Previous studies demonstrated that CTS possesses anti‐apoptotic and anti‐inflammatory properties. However, its effects and underlying mechanism on renal ischaemia reperfusion (IR) injury remain unknown. In the present study, we investigated the effects of CTS on renal IR injury and its potential underlying mechanisms. Mice were randomized into four groups as follows: (a) sham operation + vehicle, (b) sham operation + CTS, (c) IR + vehicle, (d) IR + CTS. The CTS‐treated group were injected intraperitoneally with CTS (10 mg/kg/d) for 7 days prior to IR operation. Renal IR injury was induced by clamping the bilateral renal artery for 30 minutes followed by 24 hours of reperfusion. The mice were then killed to collect the serum and the kidneys for analysis. The results of the present study showed that CTS pretreatment significantly attenuates IR‐induced renal functional and morphological injuries, which was accompanied with inhibition of cell apoptosis and inflammatory response. Moreover, the phosphorylation of p38 mitogen‐activated protein kinase (MAPK) and the activation of nuclear factor‐κB (NF‐κB) signalling were inhibited by CTS. Therefore, CTS could be a useful therapeutic agent in the fight against renal IR injury.     

硝苯地平缓释片的制备及体外释放研究

目的制备具有良好释放性能的硝苯地平（NF）缓释片。方法将NF制备成固体分散体后,再以羟丙甲纤维素（HPMC）为骨架材料制备成缓释片,对固体分散体载体及骨架材料用量进行考察。结果随着聚乙烯吡咯烷酮用量的增加NF固体分散体溶出速率加快,所制备的缓释片体外释放缓慢、完全。结论固体分散技术可用于难溶性药物NF缓释片的制备。     

流化床制粒法制备速释硝苯地平片及其体外溶出度研究

目的:研制具有速释性的硝苯地平(NFP)片并考察其体外溶出度。方法:对NFP原料药先进行微粒化,再加入辅料采用流化床制粒,经压片、包衣制备NFP片。依据2005年版《中国药典》溶出度第2法及高效液相色谱法测定NFP的累积溶出度,并与2种市售NFP片进行比较。结果:所制NFP片为薄膜衣片,其中NFP粒径小于15μm;其10、60min时累积溶出度分别约为85%、99%,而市售样品1约为30%、78%,市售样品2约为70%、93%。结论:采用流化床法制备NFP片方法简单,工艺可行,所制制剂具有速释作用,优于市售片。     

The physicodynamic properties of mucoadhesive polymeric films developed as female controlled drug delivery system

Phenoporlamine hydrochloride is a novel compound that is used for the treatment of hypertension. The purpose of this study was to develop a sustained release tablet for phenoporlamine hydrochloride because of its short biological half-life. Three floating matrix formulations of phenoporlamine hydrochloride based on gas forming agent were prepared. Hydroxypropyl methylcellulose K4M and Carbopol 971P NF were used in formulating the hydrogel drug delivery system. Incorporation sodium bicarbonate into matrix resulted in the tablet floating over simulated gastric fluid for more than 6 h. The dissolution profiles of all tablets showed non-Fickian diffusion in simulated gastric fluid. Moreover, release of the drug from these tablets was pH-dependent. In vivo evaluations of these formulations of phenoporlamine hydrochloride were conducted in six healthy male human volunteers to compare the sustained release tablets with immediate release tablets. Data obtained in these studies demonstrated that the floating matrix tablet containing more Carbopol was capable of sustained delivery of the drug for longer periods with increased bioavailability and the relative bioavailability of formulation (containing 25% Carbopol 971P NF, 8.3% HPMC K4M) showed the best bioequivalency to the reference tablet (the relative bioavailability was 1.11 ± 0.19).     

Diffusion transport in interpolyelectrolyte matrix systems based on chitosan and Eudragit L100

With a view to the development of new controlled drug delivery systems, the formation of an interpolyelectrolyte complex (IPEC) between chitosan (CTS) and Eudragit L100 (L-100) has been studied. The structure of this IPEC is such that two maxima are observed in the curves of IPEC swelling in the media with different pH values. The release of a model drug (ibuprofen) from IPEC-based tablets is significantly retarded, and this delay can be controlled by changing the molecular weight of CTS in the IPEC composition. __________ Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 39, No. 12, pp. 44–46, December, 2005.     

Sexually Transmitted Diseases and Reproductive History in Women with Experience of Casual Travel Sex Abroad

Background: The objective of this study was to determine whether the frequency of sexually transmitted diseases (STDs) and some reproductive events in women with experience of casual travel sex (CTS) abroad with previously unknown male partners differed when compared to women lacking such experience.
Methods: Nine hundred and ninety-six women seeking contraceptive advice from two family planning clinics and a youth clinic were studied. Two hundred and seventy-six of these women (27.7%) admitted experience of CTS.
Results: Among current STDs, only the prevalence of cervical human papilloma virus infection was significantly higher in women with a history of CTS when compared to the comparison (COMP) group (11.2% vs. 0.7%). A history of gonorrhea, genital chlamydial infection, and genital warts was reported significantly more often in women with, rather than without, CTS ( p =0-.005). Women who had experienced CTS had a lower rate of childbirth, but higher rates of legal abortion and pelvic inflammatory disease than did females in the COMP group.
Conclusion: The study shows that women with experience of CTS belong to a group at high risk for acquisition of STDs. This increased risk, with the exception of genital warts, was attributed to sexual risk taking in general, not merely to traveling abroad.     

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.     

Methods for the practical determination of the mechanical strength of tablets-From empiricism to science

This review aims to awake an interest in the determination of the tensile strength of tablets of various shapes using a variety of direct and indirect test methods. The United States Pharmacopoeia monograph 1217 (USP35/NF30, 2011) has provided a very good approach to the experimental determination of and standards for the mechanical strength of tablets. Building on this monograph, it is hoped that the detailed account of the various methods provided in this review will encourage industrial and academic scientists involved in the development and manufacture of tablet formulations to take a step forward and determine the tensile strength of tablets, even if these are not simply flat disc-shaped or rectangular. To date there are a considerable number of valid test configurations and stress equations available, catering for many of the various shapes of tablets on the market. The determination of the tensile strength of tablets should hence replace the sole determination of a breaking force, because tensile strength values are more comparable and suggestions for minimum and/or maximum values are available. The review also identifies the gaps that require urgent filling. There is also a need for further analysis using, for example, Finite Element Method, to provide correct stress solutions for tablets of differing shapes, but this also requires practical experiments to find the best loading conditions, and theoretical stress solutions should be verified with practical experiments.