蛇床子素固体分散体的制备与分析

应用聚乙烯吡咯烷酮(PVP)为载体,采用溶剂挥发法制备了蛇床子素(OSL)的固体分散体,测定了OSL原料药、固体分散体以及机械混合物的体外溶解度,并通过扫描电镜观察、红外光谱以及紫外光谱分析对固体分散体进行了研究,结果表明,OSL固体分散物的溶解度与OSL原料药和机械混合物相比有明显提高;OSL分子和载体分子之间未发生化学变化。     

姜黄素固体分散体的制备及体外评价

采用混合载体制备姜黄素固体分散体以提高姜黄素的溶解度和溶出度.实验采用溶剂法制备姜黄素固体分散体,以体外溶出度和饱和溶解度为评价指标,结合傅里叶红外光谱和差示扫描量热法,单因素试验筛选载体种类、单一载体与混合载体以及载药量,优化处方.最终处方为以尤特奇?聚丙烯酸树脂和羟丙基甲基纤维素为混合载体,姜黄素和两种载体的质量比例为1∶2∶2,此时姜黄素的溶出效果最佳.姜黄素以无定形态分散在载体中,姜黄素与载体间形成较强的相互作用,15 min的溶出度可到90%以上,饱和溶解度是原料药的9.7倍.实验结果表明,姜黄素三元固体分散体可提高姜黄素的溶解度和溶出度,为姜黄素制剂的研究提供了有效的实验参考.     

卡维地洛固体分散体的制备及其性质研究

为提高卡维地洛溶解度和溶出速率,采用固体分散技术,通过溶剂法,以PVP K30为载体,以药辅质量比(CAR∶PVP K30)、溶剂用量、溶剂蒸发的温度为考察因素,采用正交试验法,得出卡维地洛固体分散体制备的最佳工艺:药物与载体材料质量比1∶9,加入10 m L无水乙醇,蒸发溶剂的温度50℃。与卡维地洛原料药相比,按最佳工艺制备的卡维地洛固体分散体,60min溶出百分率从16.25%提高到98.04%。     

氟苯尼考PVPK30固体分散体的制备与表征

以聚维酮K30为载体,采用溶剂熔融法制备氟苯尼考固体分散体,用红外光谱法、显微鉴别法、差示热分析法和溶出速率法验证固体分散体,比较氟苯尼考原料、物理混合物和固体分散体的溶解度,并建立紫外法测定其含量.结果表明,氟苯尼考、混合物、固体分散体的差热曲线、红外光谱和溶出速率有很大区别,固体分散体可以显著提高药物的溶解度,在50.0～350.0 μg/mL浓度范围内吸收度与浓度间线形关系良好.氟苯尼考聚维酮K30固体分散体制备方法简单,质量可控,可以显著提高药物的溶解度,便于临床应用.     

黄芩苷固体分散体的研制

目的研制黄芩苷固体分散体,并对其进行考察。方法以PEG6000为载体,用溶剂法、熔融法、溶剂．熔融法、研磨法制备黄芩苷固体分散体,并通过紫外、红外、溶解度、溶出度的考察比较不同药物与载体的比例对固体分散体的影响。结果溶剂法即共沉淀法,药物与PEG6000的比例为1：8时的固体分散体最优。结论制备方法和药物与载体的比例都会影响黄芩苷-PEG6000固体分散体的质量。     

龙血竭总黄酮固体分散体的制备和性能表征

为制备龙血竭总黄酮(RDF)固体分散体,提高其溶出度,并对固体分散体进行表征,以聚乙烯比咯烷酮K30(PVP K30)和泊洛沙姆188(F68)为辅料,采用溶剂法制备了三相固体分散体,以体外溶出试验考察了固体分散体制备工艺,并以X射线衍射(XRD)、红外光谱(IR)、差示扫描量热法(DSC)及扫描电子显微镜法(SEM)等手段对固体分散体进行了性能表征.结果表明:以TFDB,PVP K30,F68质量比为181时制得固体分散体的溶出效果较好,药物和辅料间无相互作用力,药物溶出的改善主要归结于固体分散体中药物的粒径减小和F68的润湿与增溶作用.故采用三相固体分散体技术能显著提高龙血竭总黄酮的体外溶出度,为改善中药难溶性成分的溶出奠定了理论基础.     

聚乙二醇对葛根黄豆苷元体外溶出的影响

以聚乙二醇为载体材料,制备了葛根黄豆苷元固体分散体,采用紫外分光光度法测定其体外溶出度,分别研究了聚乙二醇的相对分子质量、药物和载体的比例和固体分散体的制备方法对药物溶出的影响.实验结果发现:固体分散体中药物的溶出度均高于原料药;药物的溶出度随聚乙二醇相对分子质量的增大而增大、随载体用量提高而增大;不同的固体分散体制备方法对药物的溶出度影响不大.     

微波照射法制备药物-高分子固体分散体

利用微波技术制备无有机溶剂残留的固体分散体.以布洛芬为模型药物,聚乙烯吡咯烷酮为载体,采用微波照射法制备布洛芬固体分散体,利用体外溶出度试验,傅里叶变换红外光谱法和扫描电镜进行验证.结果表明以微波照射法制备的布洛芬固体分散体能够显著提高其体外溶出度,120min内布洛芬的累积溶出度可达94％.通过扫描电镜观察及红外光谱对固体分散体进行测定发现:经微波照射后发生强烈的聚集,应该存在着药物-聚合物的相互作用,使布洛芬以非晶形状态或分子态分散在载体中.该方法符合设计要求,且制备方法简便可行.     

HPMCAS/PVP K30胡椒碱双载体无定型固体分散体的制备及其体外溶出测定

为提高胡椒碱(Piperine,Pip)的体外溶出,本文对Pip的双载体无定型态固体分散体制备技术进行研究。将醋酸羟丙基甲基纤维素琥珀酸酯(HPMC-AS)的3种异构体(HPMC-AS-HF、HPMC-AS-MF、HPMCAS-LF,分别简称为HF、MF和LF)和聚乙烯吡咯烷酮PVP K30(K30)按一定比例混合作为载体,并通过超饱和测试测定其对Pip溶液超饱和度的影响。使用溶剂法制备Pip双载体无定型态固体分散体,并运用差示扫描量热法(DSC)和红外光谱(IR)对Pip双载体固体分散体进行表征。实验结果显示K30/HF、K30/LF、K30/MF 3种组合均对Pip有一定的增溶作用,HF与MF可以提高溶液的超饱和度。当双载体固体分散体载药量为10%时,其溶出速度和稳定性按比例顺序为K30/HFK30/MFK30/LF。当MF/HF比例为1∶1或4∶1时效果最佳。随着MF占比增大,双载体固体分散体的溶出速度加快,稳定性下降。因此,双载体无定型态固体分散体对于维持胡椒碱的超饱和作用和提高体外溶出度都有显著效果。     

乌索酸固体分散体的制备与分析

采用聚乙烯吡咯烷酮(PVP-K30)作为载体,用溶剂法制备乌索酸(UA)固体分散体,以提高制剂中UA的溶出度;建立高效液相色谱(HPLC)法测定固体分散体的体外溶出度,并进行红外和紫外光谱分析,鉴别药物在载体中的存在状态.研究结果表明,HPLC法测定UA的溶出度准确可靠、稳定、无载体的干扰;选择PVP-K30作为载体制备成固体分散体,能显著地提高UA的体外溶出速度.     

微米级单分散苯乙烯-甲基丙烯酸共聚物微球的制备

以聚乙烯吡咯烷酮为分散稳定剂、偶氮二异丁腈为引发剂、醇或醇/水混合物为分散介质，用分散共聚合方法制备了微米级苯乙烯-甲基丙烯酸共聚物微球。研究了功能单体用量、介质的溶解度参数、分散剂用量及温度对共聚反应速率、转化率、共聚物微球的粒径和粒径分布的影响。结果表明，功能单体用量增加，聚合速率变慢，粒径增大；介质的溶解度参数增大，聚合速率增大，转化率提高，粒径减小；分散剂用量增大，聚合速率及转化率的变化不大，粒径减小；反应温度升高，聚合速率和转化率提高，粒径增大，粒径分布变宽。     

表面涂覆活性凝胶聚合物暂堵剂的研究与应用

以聚乙烯醇、骨胶和苯甲酸为固相材料,采用具有表面活性的单体和丙烯酰胺、丙烯酸钠进行共聚得到的活性聚合物对粉状固体表面进行包覆,通过有机硅改性处理得到一种水溶性暂堵剂WRP,测试了暂堵剂的悬浮性、水溶性以及抗温性能,通过驱替实验测试了暂堵和解堵性能。实验结果表明,该暂堵剂水溶率大于95%,可耐260℃高温,悬浮分散性能好,在岩心中注入8倍孔隙体积的0.4%暂堵剂后,暂堵率与水驱解堵率均大于95%,突破压力高达6.2 MPa。并将其应用于赵凹油田的安2117井进行了现场实验,加入暂堵剂后压力上升6.3 MPa,达到暂堵效果和解堵效果,实现了裂缝的暂堵转向。     

Co－W－C固溶体比矫顽磁力

模拟硬质合金Ｃｏ基胶结相的成分制备了二元Ｃｏ－Ｗ、Ｃｏ－Ｃ固溶体和三元Ｃｏ－Ｗ－Ｃ固溶体模拟合金，探讨了固溶成分影响比矫顽磁力Ｈｓｃ的规律．结果表明，Ｗ和Ｃ的固溶可分别提高和降低其Ｈｓｃ，影响程度随固溶度增加而加剧；由于Ｃ对Ｈｓｃ的影响较Ｗ更为强烈，导致Ｃｏ－Ｗ－Ｃ固溶体模拟合金的Ｈｓｃ低于纯Ｃｏ．     

NaCl-NH4Cl-H2O三元水盐体系在高原大气压下的相平衡研究

通过湿渣法测定了水中NH4Cl和NaCl的溶解度数据,同时研究了三元水盐体系NaCl-NH4Cl-H2O在25℃时的固液相平衡关系。采用Pitzer模型计算了该三元水盐体系相平衡溶解度,比较了计算值和实验值,结果基本吻合。并从定量的角度描述了θNaNH4和ΨNaNH4Cl各以±10%变动时,对体系溶解度的影响。     

丹参酮固体分散物的研究

应用聚乙烯吡喀烷酮（PVP）为载体,采用喷雾干燥制备了丹参酮（Tanshinone TAN)的固体分散物。测定了TAN原料药、固体分散物以及机械混合物的体外溶出度,并通过X－射线衍射、扫描电观察、以及用红光光谱和紫外光谱分析对固体分散物进行了研究。结果表明,TAN固体分散物的溶出度与TAN原料药和机械混合物相比有显著提高;TAN以超细态分散于载体中;TAN分子和载体分子之间未发生化学反应。     

Effects of drug-polymer dispersions on solubility and <Emphasis Type="Italic">in vitro</Emphasis> diffusion of artemisinin across a polydimethylsiloxane membrane

Artemisinin(ART) is a sesquiterpene lactone with an endo-peroxide bridge that is thought to be responsible for its antimalarial activity.It has low oral bioavailability because of aqueous insolubility,which leads to local toxicity at the site of aggregation.The present work focused on increasing its solubility and evaluating its permeation across a model membrane to mimic transdermal delivery that bypasses the hepatic metabolism.For this purpose,physical mixtures(PM),solid dispersions(SD) and lyophilized dispersions(LD) with different drug-polymer ratios(1:0.5,1:1,1:2,1:4 and 1:9) were prepared using the hydrophilic polymer polyvinylpyrrolidone(PVP).Drug-polymer dispersions were characterized using X-ray diffraction(XRD) and Fourier transform infrared spectroscopy(FTIR).Solubility was measured in three solvents:de-ionized water,phosphate buffered saline(PBS) and methanol.The toluene-water partition coefficient was evaluated and compared with the literature and calculated logP values.In vitro diffusion of ART was studied across a polydimethylsiloxane membrane from a saturated solution of drug-polymer dispersions.XRD patterns showed a gradual decrease in crystallinity of ART with increasing polymer concentration,while FTIR confirmed no interactions between ART and PVP.Solubility was increased up to 4-,5-and 8-fold for LD in water,PBS and methanol,respectively.The logP for toluene-water was 2.65 ± 0.3,which is in good agreement with literature and calculated logP values.Permeation was enhanced,which is attributed to the decrease in crystallinity and increase in wettability of the drug.The ART flux was significantly higher than that of pure ART(0.12 ± 0.01) with increasing PVP concentration for SD and LD formulations.In conclusion,drug-polymer dispersions with PVP improve the pharmaceutical properties of ART in the order LD>SD>PM.     

Preparation of Latex Film with Macropores and Their Applications in Pigment Dyeing

Aiming at improving the permeability of the pigment dyed fabrics,two kinds of hydrophilic polymers(polyvinyl pyrrolidone(PVP),and polyethylene glycol(PEG)were fed into the styrene-butyl acrylate(St-BuA)copolymer latex binder respectively to prepare films with macropores.The effects of the post-added polymers on the latex film formation process and film structures were studied and the performance of the dyed fabrics was evaluated.It was found that the drying process could still be divided into three stages even after the addition of PVP and PEG.And the water evaporation rate during the first and last stage remained the same as usual.However,after the addition of PVP,the onset of the second stage was delayed to high volume fraction,and PVP formed into spherical dispersion phase with 300 nm in diameter.It provided a great deal of interface between the latex polymer and the PVP phase,which led to an increase in the water evaporation rate during the second stage.A different case was found after the feeding of PEG.Firstly,the first stage ended at low volume fraction and a decreased evaporation rate was observed in the second stage.Secondly,the PEG dispersion appeared as finger-like structure in the transmission electron microscopy(TEM)images with 9μm in length.After rinsing,pores were found only in the films formerly containing PVP or PEG,and the shapes and the sizes were closely correlated with the initial morphologies of the PVP or PEG domains.However,the shade of color,the abrasion fastness,and the permeability of the dyed fabric were independent of the type of the post-added hydrophilic polymer.