Dissolution Improvement of Cisapride by Solid Dispersion with HPMC

To prepare a solid dispersion of cisapride with hydroxypropylmethyl cellulose(HPMC E5 LV) as carrier for the purpose of accelerating the in vitro drug release by means ofimproving the solubility of the model drug. Methods Alcohol and simulated gastric fluid (SGF) wereused to dissolve cisapride and HPMC in order to make the model drug dispersed homogeneously in thecarrier. The HPMC-cisapride solid dispersion was then obtained by conventional solvent evaporationmethod. Powder X-ray diffraction (XRD) was used to measure the diffraction peaks of pure carrier,pure cisapride, physical mixture of HPMC with cisapride (4:1), and HPMC-cisapride solid dispersion(4:1) to confirm the crystal existence. The solubility of pure drug and HPMC-cisapride soliddispersion was measured with water, SGF and simulated intestinal fluid (SIF) . The in vitro drugreleases of the sustained release tablet prepared with pure cisapride or HPMC-cisapride soliddispersion were investigated with water and SGF as media, respectively. Results No diffraction peakswere found by X-ray diffraction in the HPMC-cisapride solid dispersion (4:1), indicating that thedrug existed in an amorphous form at that drug-carrier ratio. Compared with the pure drug, thesolubilities of HPMC-cisapride solid dispersion are increased by 239.4% in SGF, 132.6% in water, and117.9% in SIF. According to the in vitro drug release, the sustained release tablet prepared withHPMC-cisapride solid dispersion had a faster drug release than did that prepared with pure drug. Thein vitro drug release profiles were found to comply with Higuchi's rule. Conclusion The in vitrodrug release of the sustained release tablet made by HPMC-cisapride solid dispersion is improvedowing to the increased drug solubility.

HPMC添加量及烧结温度对粉煤灰支撑体性能的影响

以燃煤电厂燃烧后的废弃物粉煤灰为原料,二氧化锰(MnO_(2))为烧结助剂,羟丙基甲基纤维素(HPMC)为粘结剂,通过滚压成型法和固态粒子烧结法制备单管式陶瓷膜支撑体,通过对原料的热稳定性、成品的纯水通量、抗折强度、微观形貌、晶相组成以及耐酸碱度进行表征,探究HPMC的添加量对于支撑体性能的影响。结果表明,HPMC的引入可以增强粉煤灰基支撑体泥料的粘性和塑性,在烧结温度为1 150℃,HPMC的添加量为2wt.%时,抗折强度为24.65 MPa、纯水通量为6 794.71 L/(m^(2)·h·MPa)、耐酸碱腐蚀性能优异且稳定。HPMC作为粘结剂在苛刻条件下仍然可以制备出低成本、效果优的粉煤灰基陶瓷膜支撑体,达到资源化利用的目的。

Cooperative effect of polyvinylpyrrolidone and HPMC E5 on dissolution and bioavailability of nimodipine solid dispersions and tablets

Solid dispersion(SD)systems have been extensively used to increase the dissolution and bioavailability of poorly water-soluble drugs.To circumvent the limitations of polyvinylpyrrolidone(PVP)dispersions,HPMC E5 was applied in the formulation process and scaling-up techniques,simultaneously.In this study,SD of nimodipine(NMP)and corresponding tablets were prepared through solvent method and fluid bed granulating one step technique,respectively.Discriminatory dissolution media were used to obtain reliable dissolution results.Meanwhile,the stability study of SDs was investigated with storage under high temperature and humidity conditions.Moreover,the solubility of SDs was measured to explore the effect of carriers.The preparations were characterized by DSC,PXRD,and FTIR.Dramatical improvements in the dissolution rate of NMP were achieved by the ingenious combination of the two polymers.Binary NMP/PVP/HPMC-SDs released steadily,while the dissolution of single NMP/PVP-SDs decreased rapidly in water.The fluid-bed tablets(FB-T)possessed a similar dissolution behavior to the commercial Nimotop TM tablets.The characterization patterns implied that NMP existed in an amorphous state in our SDs.Furthermore,the results of stability tests suggested a better stability of the binary SDs.A special cooperative effect of PVP and HPMC was discovered on dissolution characteristics of NMP SDs and tablets,which could be extended to other drugs henceforth.Finally,the bioavailability of FB-T was evaluated in beagle dogs with Nimotop TM as the reference,and the results showed a higher AUC 0–12h value for FB-T.

Effect of HPMC on the Piezoresistivity of Smart Concrete Aggregate with Z Shape

Cement mortar with carbon fiber(CFc)and resin-cement mortar with carbon fiber(CFrc)were used as inner and outer cores of smart aggregate with Z shape,respectively,which was used as the basic perception units to prepare smart concrete aggregate with a mosaic structure(SAMS).The hydroxpropyl methylcellulose(HPMC)was taken into consideration to improve the properties of mortar;by using HPMC,the structure of SAMS was optimized and its mechanical and electrical properties were evaluated.The experimental results show that the toughness of mortar could be improved by the complex that formed by epoxy resin,and the effect of HPMC on the flexibility of CFc was greater than that on the flexibility of CFrc;the feasible designing indicates that the CFc-Z core and CFrc-Z core could be used as inner and outer cores of SAMS.When the proposed dosages of HPMC in inner and outer cores are 0.35wt%and 0.2wt%,respectively,it could give an effective prediction for the damage of concrete during the loading process.

EudragitS100与HPMC在茶碱缓释片中的应用比较与研究

EudragitS100(又称优特奇S100)是一完全人工合成的聚甲基丙烯酸酯系列聚合物之一。它具有在pH>7的环境下溶出的特性,因而可用于肠道一定位释放的肠溶包衣材料。另外,利用聚甲基丙烯酸酯制备口服制剂骨架片近来也得到应用,本文就把Eu-dragitS100与HPMC在茶碱缓释片中的应用作一下比较:

Association between the physical stability of flurbiprofen suspension and the interaction of HPMC/SDS

The anionic surfactant sodium dodecylsulfate(SDS) has improved the physical stability of flurbiprofen(FBP) suspension, which was suspended by 0.2%(w/v) hydroxypropylmethyl cellulose(HPMC, K4 M). Therefore, the physical stability of FBP suspensions and the interaction of HPMC/SDS were studied, and a certain association between them was revealed. The antisolvent precipitation method was used to prepare suspensions. The apparent drug concentration from different sites was evaluated to get the dispersion of drug actually. The process of flocculation and deflocculation with the addition of SDS was caught by analyzing the morphology of the suspended particles. The physical stability of the FBP suspensions was characterized mainly by measuring the re-dispersion time, the zeta potential and particle size. Meanwhile, conductivity measurements were carried out to obtain the characteristic concentrations of SDS in HPMC/SDS system. The viscosities, the abilities for improving the solubility and wettability of FBP in the separate and mixed HPMC/SDS solutions were also contrasted respectively. The suspensions prepared with HPMC/SDS possessed better physical stability. The suspensions were uniform when the concentration of SDS was between the critical adsorption concentration(CAC) and the polymer saturation point(PSP). After PSP, the uniformity became worse and worse until the SDS was enough to form a deflocculation state. Besides, the re-dispersion time of FBP suspensions was longest when the concentration of SDS around CAC and shorter by shorter after the critical micelle concentration(CMC). The article provided a new sight on the relation between the interaction of excipient matrix and pharmaceutical preparations.

Formulation of Domperidone Microspheres Using a Combination of Locally Extracted Chitosan and Hpmc as Polymers

Abstract： Commercially available domperidone -a D2 receptor antagonist- is an immediate release formulation which has never been formulated into microspheres for sustained release. The present work aims towards studying the effect of combination of a natural chitosan from an oyster shell of Mystilis edulis and HPMC （hydroxy propyl methyl cellulose） （spectracel 15 E） as polymer and tripolyphosphate as cross linking agent using wet gelation technique. The various polymer combination ratios for different batches were compared with a low molecular weight standard chitosan. The extracted chitosan - HPMC polymer combination ratios were chosen at ten levels： as batches B1, B2, B3, B4, B5, B6, B7, B8, B9, B10 for 1：1, 1：2, 2：1, 1：0, 0：1, 3：1, 1：3, 5：1, and 1：5 and 1：1 having 450：450, 300：600, 600：300, 900：0, 0：900, 675：225, 225：675, 750：150, 150：750, 450：450 mg respectively, while the quantity of domperidone and tripolyphosphate remained constant. B 11 and B 12 were formulated with standard chitosan and HPMC. The percentage yield of the formulated microspheres was determined and then evaluated for flowability, drug entrapment efficiency, drug release and mechanism of drug release by Fickian diffusion. The best batches of the domperidone loaded microspheres produced from the combination polymer were compared with the standard chitosan. The highest yields of microspheres were given by batches B12, B11, B10, and B4 with values of 50.1 ± 0.1%, 49.6 ± 0.1%, 46.6 ：± 0.1%, and 46.1 ± 0.0% respectively while the lowest yield were 23.3 ± 0.2% and 23.6 ± 0.2%. B5 and B6 and B9 did not yield any microsphere. The bulk density, tapped density, compressibility and Hausner＇s ratio of the microspheres showed good flowability and high percent compressibility. The drug entrapment efficiency showed that the entrapment ranged from 54.2 to 97.2, where the least entrapment was B4 （54.2 ± 0.1） and the highest B12 （97.2 ± 0.2）. The polymer surface of the microspheres as observed by SEM （scanning electron microscopy） was heterogeneous and porous which offers enhanced bioadhesivity. The dissolution study was used to determine the percentage drug release which ranged from 12.1% to 68.9% after 5 hours. Batches 1, 2, 3, 4, 7, and I 1 follow zero order kinetics via Fickian diffusion. The results indicate that microspberes of domperidone could be successfully formulated with a natural chitosan either alone or in combination with HPMC for sustained delivery of domperidone. Furthermore, the concentration of the natural polymer and HPMC employed in the formulation need to be carefully selected to enable the production of microspheres with the desired sustained release properties.

聚乙醇酸与羟丙基甲基纤维素用于远端胰腺切除模型术后缝合的有效性和安全性评估

目的探讨应用聚乙醇酸(polyglycolic acid,PGA)与羟丙基甲基纤维素(hydroxypropyl methylcellulose,HPMC)复合材料在远端胰腺切除术后缝合中的有效性和安全性。方法选用36只健康成年比格犬,将其随机均分为观察组和对照组,每组各18只行远端胰腺切除手术。观察组实验犬使用PGA+HPMC复合材料进行切口加固;对照组实验犬使用NEOVEIL进行切口加固。术前、术后3 d及解剖前,分别对各组实验犬进行血常规检测。设置2周、4周、8周观察周期,每个观察点各6只动物进行心肝脾肺肾组织学检查、硬组织切片病理诊断等评估,并进行安全性评价。结果观察组和对照组实验犬在术前血常规检测比较差异无统计学意义。重复测量方差分析结果显示,不同时间点的白细胞计数(WBC)(F=14.875,P=0.001)、平均红细胞血红蛋白浓度(MCHC)(F=5.049,P=0.009)、中性粒细胞百分比(Neu%)(F=4.794,P=0.011)、红细胞计数(RBC)(F=6.591,P=0.002)、血红蛋白(HGB)(F=8.154,P=0.001)、红细胞比容(HCT)(F=5.281,P=0.007)、血小板计数(PLT)(F=6.560,P=0.014)、红细胞分布宽度变异系数(RDW-CV)(F=33.950,P=0.039)、淋巴细胞百分比(Lym%)(F=3.299,P=0.043)均值存在差异,但观察组和对照组组间无统计学差异,且时间与组别交互作用对其无显著影响,表明两组实验犬均出现了炎症反应或手术应激。两组实验犬在术后8周的硬组织病理切片评分中,观察组和对照组实验犬的炎症与坏死相关评分、纤维化、修复等相关评分和总分方面差异均无统计学意义(P>0.05)。两组实验犬在术后8周的解剖中,均未发现心肝脾肺肾等器官有明显的损伤,也未发现缝合材料残留、胰液渗漏或胰瘘等情况,表明两组缝合材料均已完全被吸收代谢,且切口愈合良好不会对内脏器官造成不良影响。结论PGA与HPMC是一种有效和安全的术后缝合材料,具有良好的生物可降解性、生物相容性、缝合强度和创面愈合质量,可以在远端胰腺切除术后缝合中与传统的可吸收性加固材料相媲美,为其在临床上的应用提供了科学依据。

阿司匹林HPMC骨架片药物释放因素研究

目的 :考察影响阿司匹林亲水性骨架片体外释药的各种因素。方法 :以羟丙基甲基纤维素 (HPMC)为骨架材料 ,用粉末直接压片法制备缓释骨架片 ,并考察HPMC用量、粘度、粒度、制片方法、压片压力、片子大小及其它辅料对阿司匹林HPMC骨架片体外释药的影响。结果 :阿司匹林HPMC骨架片的体外释药均符合Higuchi方程。HPMC的用量、粘度和粒度、制法、片子大小对阿司匹林的释放速率均有显著性影响。湿法制片的释药比干法慢。阿司匹林的释药速率随HPMC粒度的减小、粘度和片子的增大而减慢。对压片压力影响的研究结果表明 ,阿司匹林HPMC骨架片的硬度范围不同时 ,影响有所不同。淀粉 ,PVP ,EC ,MCC的加入 (每片HPMC含量不变 )均加快阿司匹林的释放速率 ,且加入量不同时 ,释放速率间具显著性差异。结论 :HPMC用量、粘度和粒度、制片方法。

乌拉地尔HPMC骨架片的研制及释放度的考察

以HPMC为骨架材料 ,采用湿法制粒 ,制备了乌拉地尔缓释片。以体外释放度试验研究了缓释片的释药机理及影响因素。结果表明 :乌拉地尔HPMC骨架片的释放符合Higuchi方程 ,其释药速度受到许多因素的影响 ,如HPMC的型号、HPMC的用量、附加剂。

国产HPMC作为盐酸普萘洛尔缓释骨架片基质的研究

以盐酸普萘洛尔为模型药物，考察了影响羟丙基甲基纤维素（ＨＰＭＣ）亲水凝胶骨架片体外释药的各种因素，并对国产（ＲＴ系列）和进口（Ｍｅｔｈｏｃｅｌ）的产品在理化性质、片剂制备工艺及缓释效果等方面进行了比较。结果表明，药物／ＨＰＭＣ比值、ＨＰＭＣ粘度和粒度以及溶出介质中的电解质均对骨架片的体外释药有较大影响，而压片压力和稀释剂溶解性的影响则并不显著。国产高粘度ＨＰＭＣ可用于制备盐酸普萘洛尔缓释骨架片，其缓释效果与进口品相近。

不同pH的溶出介质对HPMC骨架片释药的影响

目的 探讨溶出介质的pH对难溶性药物的HPMC骨架片释药的影响。方法 以甲氧苄胺嘧啶、卡马西平、磺胺甲恶唑和茶碱四种难溶型性药物为模型药物 ,测定四种pH缓冲溶液介质 (pH1.0 ,pH4 .0 ,pH6 .0 ,pH7.5 )下的药物的溶解度和释放度。结果 难溶性药物的HPMC骨架片释药随着其溶解度的增加而加快。结论 难溶性药物HPMC骨架片释药的差异主要与药物在不同pH的溶出介质中的溶解度有关。

尼莫地平HPMC骨架片的药物释放影响因素研究

选用HPMC为骨架材料，将难溶于水的尼莫地平制成缓释骨架片，考察HPMC的粘度、羟丙基和甲氧基含量、用量、粒径、辅料和释放介质的pH对尼莫地平缓释片的体外释药速率的影响。结果表明：尼莫地平缓释骨架片的体外释放行为近似零级释放。HPMC用量、粘度、粒径和释放介质的pH均对体外释放行为有明显影响；同一粘度HPMC甲氧基不同对释放速率影响不明显；辅料乳糖的加入能使释药速率加快，而微晶纤维素和十二烷基硫酸钠的加入在本实验范围内影响不明显。

温敏性PAC/HPMC水凝胶的制备与性能研究

以醚-羟丙甲基纤维素(HPMC),聚阴离子纤维素(PAC)和氯化铝为原料,通过物理方法制备了一系列热缩型温敏性PAC/HPMC水凝胶,并对凝胶强度、溶胀动力学、耐盐性和温敏性进行了研究.结果表明:PAC/HPMC水凝胶强度受到HPMC用量和相对分子质量影响.在研究范围内,当HPMC的2.0%水溶液黏度为4 Pa.s,加入量为0.10%时所制备的凝胶强度最大;与纯PAC凝胶相比,PAC/HPMC凝胶在去离子水中的平衡溶涨率有显著提高;PAC/HPMC凝胶的溶胀率随着NaCl溶液浓度的增加而减小,PAC/HPMC凝胶在相同浓度NaCl溶液中的溶涨率高于纯PAC凝胶;HPMC的存在使PAC/HPMC凝胶具有了温敏性,由于HPMC与PAC分子间存在协同效应,PAC/HPMC凝胶的LCST比HPMC的相应温度低.

HPMC胶囊壳对干粉吸入剂性能的影响

目的 :筛选新型的干粉吸入剂用胶囊壳。方法 :以HPMC胶囊壳和明胶胶囊壳进行对照 ,考察不同条件下胶囊壳稳定性、不同条件下胶囊壳内粉体性质 ,并进行碎片发生率实验。结果 :HPMC胶囊壳的稳定性、对粉体的保护能力均优于明胶胶囊壳 ,且碎片发生率低于明胶胶囊壳。结论 :HPMC胶囊壳与明胶胶囊壳相比 。

对乙酰氨基酚HPMC骨架片药物释放影响因素研究

目的：考察影响对乙酰氨基酚亲水性骨架片体外释药的各种因素。方法：以羟丙基甲基纤维素（ＨＰＭＣ）为骨架材料，用湿颗粒法将对乙酰氨基酚制成缓释片考察ＨＰＭＣ的用量、粘度、粒度、制法、压片压力、片子大小及其它辅料对对乙酰氨基酚ＨＰＭＣ骨架片体外释药的影响。结果：对乙酰氨基酚ＨＰＭＣ骨架片的体外释药均符合Ｈｉｇｕｃｈｉ方程。ＨＰＭＣ用量和粒度、制法、片子大小对对乙酰氨基酚的释放速率均有显著性影响。湿法制片的释药比干法压片慢。对乙酰氨基酚的释药速率随ＨＰＭＣ粒度的减小和片子的增大而减慢。ＨＰＭＣ的粒度及不同浓度乙醇作湿润剂对对乙酰氨基酚的释放速率影响不大。对压片压力影响的研究结果表明，对乙酰氨基酚ＨＰＭＣ骨架片的硬度范围不同时，影响有所不同。淀粉，ＰＶＰ，ＭＣＣ的加入（每片ＨＰＭＣ含量不变）均减慢对乙酰氨基酚的释放速率，加入量的影响在本实验范围内无显著差异。ＥＣ加入量多时（８０ｍｇ·片－１），对乙酰氨基酚释放速率显著加快。结论：ＨＰＭＣ用量和粘度，制备工艺，片剂大小及其辅料为影响对乙酰氨基酚骨架片释放速率的主要因素。

稀释剂对HPMC骨架片释药的影响

目的 探讨稀释剂对难溶性药物的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 口 恶 唑和茶碱四种难溶型性药物为模型药物 ,测定三种相同剂量的稀释剂 (糊精、乳糖和磷酸氢钙 )时药物的释放度。结果 甲氧苄胺嘧啶、卡马西平、磺胺甲 口恶 唑的释药速率为糊精 >乳糖 >磷酸氢钙 ;而茶碱的释药速率为糊精≈乳糖 >磷酸氢钙。

神经网络多目标同步优化HPMC缓释片处方

目的 通过建立BP神经网络模型,预测HPMC缓释片中药物释放;并和优化算法结合实现缓释片处方的多目标同步优化。方法 选取溶解度为难溶到略溶的5种药物(别嘌醇,甲氧苄氨嘧啶,阿昔洛韦,替硝唑,对乙酰氨基酚)作为模型药物,压制HPMC骨架片,并进行体外释放情况考察,考察52个处方中药物的溶解度、含药量、HPMC的量、HPMC的固有黏度、辅料的量、黏合剂的浓度、溶出仪的转速对药物释放情况的影响。将各因素作为神经网络的输入,药物的累计释放量作为输出,对网络进行训练,建立BP神经网络模型,并和优化算法相结合实现以对乙酰氨基酚、甲氧苄氨嘧啶、米诺地尔、氧氟沙星为模型药物,在不同的含药量、不同转速的条件下对处方进行优化。结果 利用神经网络预测药物的释放,训练处方和测试处方的实测值和预测值能很好吻合,4个优化处方的释放值均和目标值很接近。结论 神经网络可用于预测不同药物不同处方组成的HPMC缓释片中药物的释放,并能同步优化HPMC缓释骨架片的处方。

添加HPMC对无麸质大米面包品质的影响

水稻是全球主导的粮食作物之一,作为无麸质食品的主要原料倍受青睐。但水稻中缺乏面筋蛋白,在发酵过程中难以形成持气性较好的网孔结构,所以很难获得理想的面包类发酵产品。本论文探讨了采用HPMC为面筋替代物制作无麸质大米面包的可行性,并研究了HPMC对大米面包品质的影响,从而为无麸质大米面包的制作奠定基础,为大米资源的广泛应用开辟新的途径。结果表明,当添水量提高到100%110%时,4%的HPMC可以作为面筋替代物,用以改善大米面团的品质,烘焙出优质、理想的无麸质大米面包,但其淀粉体外消化率和整体感官评价却受到影响。最后认为,应该把无麸质大米面包看作为一类新型的焙烤食品,不一定要完全适用小麦面包的评价体系。

盐酸二甲双胍HPMC骨架片的实验研究

用HPMC为骨架材料 ,用湿法制粒 ,将水溶性药物盐酸二甲双胍制成缓释骨架片 ,考察了HPMC的用量、粘度、粘合剂种类如乙醇、乙基纤维素、丙烯酸树脂等对药物体外释放速率的影响。通过正交实验设计方法进行处方筛选及实验研究制成盐酸二甲双胍缓释片。结果表明盐酸二甲双胍缓释片的体外释放行为均符合Higuchi方程 (Q =2 8.6 3t1/2 +12 .6 1,r =0 .995 3) ;处方中粘合剂种类和HPMC用量对该缓释片的释药速率有显著性影响 。