槲皮素聚维酮固体分散体的研制

目的制备槲皮素聚维酮固体分散体,以提高槲皮素的水溶性。方法以聚乙烯吡咯烷酮(PVP)为载体,采用溶剂法制备槲皮素的固体分散体;分别测定槲皮素原料药、固体分散体以及机械混合物在水中的溶解度,并对其进行红外、紫外光谱分析。结果槲皮素固体分散物在水中的溶解度与槲皮素原料药和机械混合物相比有明显提高;槲皮素分子与载体PVP分子之间未发生化学变化,槲皮素只是以超微结构分散于载体中。结论PVP可用作槲皮素固体分散体的载体,并可提高槲皮素的水溶性。     

二氢杨梅素—聚乙二醇固体分散体的制备

目的:制备二氢杨梅素(DMY)-聚乙二醇6000(PEG6000)固体分散体,以提高二氢杨梅素的水溶性。方法:以PEG6000为载体,采用熔融法制备DMY的固体分散体,测定DMY对照品、固体分散体以及机械混合物的溶解度,并通过红外光谱和紫外光谱对固体分散物进行分析。结果:DMY固体分散体的溶解度明显提高且比DMY提高了52倍。结论:DMY固体分散体的水溶性大大增强,且分子结构未改变。     

不同相对分子质量聚乙二醇对槲皮素的增溶作用

目的　研究不同相对分子质量聚乙二醇对槲皮素的增溶作用。方法　分别用聚乙二醇 4 0 0 0 ,6 0 0 0 ,10 0 0 0 (PEG40 0 0 ,PEG60 0 0 ,PEG10 0 0 0 )为载体 ,采用熔融法制备槲皮素固体分散体 ,测定槲皮素原料药、固体分散物以及机械混合物的溶解度 ,以红外光谱和紫外光谱分析固体分散物。结果　槲皮素固体分散物中槲皮素的溶解度 (48.78,78.39,81.35 mg.L-1)比槲皮素 (12 .75 mg.L-1)以及相同质量比机械混合物 (12 .86 ,13.15 ,13.2 8mg.L-1)的溶解度有明显提高。结论　不同相对分子量聚乙二醇可以不同程度增加槲皮素的溶解度。     

蛇床子素—聚乙二醇固体分散体的特性及有关分析方法研究

目的建立固体分散体中蛇床子素的分析方法、考察其有关特性。方法应用聚乙二醇6000(PEG6000)为载体,采用熔融法制备了蛇床子素(Osthole,OSL)的固体分散体,测定了OSL原料药、固体分散物以及机械混合物的体外溶出度,通过扫描电镜观察、红外光谱及紫外光谱分析对固体分散物进行了研究。结果及结论OSL固体分散物的溶出度与OSL原料药和机械混合物相比有明显提高;OSL以超细态分散于载体中,OSL分子和载体分子之间未发生化学变化。     

瑞格列奈固体分散体的制备及体外溶出

目的制备瑞格列奈的固体分散体,提高瑞格列奈的体外溶出度。方法以聚乙二醇6000(polyethylene glycol 6000,PEG6000)作为载体,采用溶剂-熔融法制备不同处方的瑞格列奈固体分散体,进行溶出度考查。采用红外光谱、差示扫描量热(differential scanning calorimetry,DSC)与X-射线衍射(X-ray diffraction,XRD)对瑞格列奈固体分散体进行物相分析。结果与瑞格列奈原料和物理混合物相比,固体分散体可显著提高瑞格列奈的体外溶出度,物相鉴定表明,瑞格列奈大部分以无定形状态分散于PEG6000中,提高了药物的体外溶出度。结论制备瑞格列奈的PEG6000固体分散体能显著提高药物的体外溶出度,可满足速释制剂的要求。     

索法酮固体分散体的制备及体外溶出特性

目的:制备索法酮固体分散体并考查其体外溶出特性.方法:以PEG 2000、PEG 4000和PEG 6000为载体,采用熔融法制备固体分散体,与物理混合物比较体外溶出度.结果:PEG 4000和PEG 6000制得的固体分散体的体外溶出度高于PEG 2000,均高于物理混合物.载体比例越大,体外溶出越快.结论:以PEG为载体,采用熔融法可制得体外溶出较快的索法酮固体分散体.     

杨梅素固体分散体的制备以及体外溶出试验

目的运用固体分散技术制备杨梅素固体分散体并提高其体外溶出速率。方法选用PEG6000和PVPK30为载体,采用溶剂法和溶剂-熔融法制备杨梅素固体分散体,采用紫外分光光度法进行含量测定,并进行溶解度、体外溶出试验。结果两种载体的固体分散体均能增加药物的溶解度和溶出速率,杨梅素在载体中以高度分散状态存在。结论以PVPK30为载体的杨梅素固体分散体体外溶解度和溶出速率明显提高。杨梅素固体分散体能显著提高杨梅素的溶出速率。     

卡维地洛固体分散体的制备及其体外溶出度的测定

目的 :制备卡维地洛固体分散体 ,提高其溶解度和溶速率。方法 :以聚乙烯吡咯烷酮 (PVP)、聚乙二醇 -6000(PEG -6000)为载体 ,以溶剂法和熔融法制备固体分散体 ,并进行体外溶出度研究。结果 :载体比例越大 ,药物溶出愈快 ;载体比例愈小 ,差异愈显著。载体为PVP所制固体分散体的体外溶出行为总体优于载体为PEG -6000的固体分散体。结论 :本试验所制卡维地洛固体分散体能加速体外溶出 ,提高生物利用度 ,可用于制备高效制剂     

(噁)丙嗪固体分散体的制备

目的:制备噁丙嗪固体分散体.方法:以聚乙二醇(PEG 6000)为载体,采用熔融法制备噁丙嗪固体分散体,桨法测定体外溶出度,X-射线衍射法分析结构状态.结果:噁丙嗪-PEG 6000固体分散体是一种简单低共熔混合物,噁丙嗪以超细结晶状态分散在PEG载体中.1:5,1:7,1:9,1:11比例固体分散体的标示含量均在98%～106%范围.与原料药及物理混合物相比,固体分散体的溶出速度和程度均显著增加(P＜0.01);且随着载体比例的逐渐增大,固体分散体的药物溶出加快.结论:以PEG 6000为载体制备的噁丙嗪固体分散体体外溶出迅速,可用于制备速效、高效的噁丙嗪口服制剂.     

冬凌草甲素固体分散体的制备及溶解性能研究

目的采用固体分散技术,提高冬凌草甲素的体外溶解性能。方法分别以聚乙二醇6000（PEG6000）、聚乙烯吡咯烷酮K30（PVPK30）为载体,制备冬凌草甲素固体分散体。采用紫外分光光度法进行含量测定,差示热分析法鉴别药物在载体中的存在状态,并进行溶解度、体外溶出速率实验。结果两种载体的固体分散体均能增加药物的溶解度和溶出速率,冬凌草甲素在载体中以高度分散状态存在。结论以PVPK30为载体制备的冬凌草甲素固体分散体体外溶解度和溶出速率明显提高。     

Preparation and characterization of solid dispersions of Quercetin with PEG4000

Objective To enhance the solubility,quicken the speed of digesting and absorption,and increase the bioavailability of quercetin(3,3',4',5,7-pentahydroxyflavone).Methods A series of Quercetin-PEG4000 solid dispersions were prepared by fusion method.The configuration and property of solid dispersion were characterized by solubility tests,dissolution tests,FTIR spectra,differential scanning calorimetry(DSC)and microphotograph.Results 1.According to solubility tests the the mass ratio of quercetin to PEG4000 affected strongly on the solubility of solid dispersions,on the whole,the relation of the solubility of solid dispersions to the mass ratio presented linear relationship.The preparation temperature had little effect on the solubility of solid dispersions.The surface-active agent,polysorbate80 increased strongly the solubility of solid dispersions.2.According to the dissolution tests,the mass ratio of quercetin to PEG4000 affected strongly on the dissolution of solid dispersions,the preparation temperature had little effect on the dissolution of solid dispersions.The surface-active agent,polysorbate80 increased strongly the dissolution of solid dispersions,and after addition polysorbate80,the dissolution of solid dispersions was two times of the dissolution of solid dispersions without polysorbate80.3.According to the DSC results,except that a little of quercetin molecular existed as crystalline state in the solid dispersion with the mass ratio was qu:PEG=1:2,quercetin existed as amorphous phase in other mass ratio solid dispersion.4.According to the FTIR spectra and microphotograph results,the relation of quercetin and PEG4000 was mainly physical mixing in quercetin-PEG4000 solid dispersion.Quercetin was just like solute in solution,and PEG4000 was just like solvent in solution.The force between quercetin and PEG4000 was mainly hydrogen bonding,so the biological activity of quercetin would not be influenced greatly after the formation solid dispersion.Conclusions These results suggest that quercetin existed mainly as amorphous phase in solid dispersion;the solubility and the dissolution in water were increased obviously after formation the solid dispersion.     

槲皮素PVP固体分散体的制备及物相鉴定

目的用溶剂法制备槲皮素-PVP固体分散体并考察其溶出特性并对物相进行鉴定。方法采用溶剂法制备槲皮素-PVP固体分散体,通过溶出实验对槲皮素溶出率的测定研究固体分散体的溶出性质,利用差热分析（Differentialscanning calorimetry,DSC）、红外光谱分析（Infrared spectroscopy,IR）、粉末X衍射（X-ray powder diffractometry,PXRD）、扫描电镜（Scanning electron microscopy,SEM）等方法对其进行物相鉴定。结果槲皮素-PVP固体分散体的溶出速率相对其物理混合物有了明显的改善; 溶解实验显示固体分散体中槲皮素的溶解度有了显著的提高;热差分析及粉末X衍射结果表明固体分散体中槲皮素呈非结晶形式;扫描电镜下固体分散体中无槲皮素晶体。结论采用溶剂法制备槲皮素-PVP固体分散体可显著提高槲皮素的溶解度及溶出速度。     

Experimental and mesoscale computational dynamics studies of the relationship between solubility and release of quercetin from PEG solid dispersions

The flavonol quercetin is potentially clinically relevant for its antimicrobial, beneficial cardiovascular effects, cancer treatment amongst others. However, its successful therapeutic application is severely curtailed by its poor water solubility and poor absorption following oral administration. In this study, solid dispersions of quercetin in poly(ethylene glycol) (PEG) at various compositions demonstrated an increase in the solubility, however with time, dissolution profiles show a decrease in dissolved flavonol concentration. The mechanism by which this decrease in solubility occurs was studied experimentally as well as by computational mesocscale particle dynamics simulations. The results suggest that phase separation of the polymer and flavonol during release from the solid dispersion is responsible for the time-dependent decrease in dissolved quercetin. It is suggested that the increase in release of quercetin in a PEG solid dispersion would only be beneficial if it were administered at the site of absorption, e.g. rectal administration, to ensure absorption prior to phase separation. The solid dispersions presented here would greatly improve the pharmaceutical availability of the flavonol at the site of absorption. Computational mesoscopic modeling was successfully applied to study the solid dispersions and corroborate experimental findings.     

间尼索地平固体分散体的研制

目的:将难溶性药物间尼索地平制备成固体分散体,以增加其溶解度及体外溶出度。方法:以泊洛沙姆为载体,共沉淀法制备间尼索地平固体分散体。采用差示扫描量热分析(DSC)方法鉴别药物在载体中的存在状态,并进行溶解度和体外溶出度研究。结果:DSC显示间尼索地平与泊洛沙姆形成了低共熔物,间尼索地平原料药及其与泊洛沙姆不同比例的固体分散体(1∶3、1∶5、1∶7)的溶解度分别为0.89、4.50、15.35、23.03mg·L-1,120min时的累积溶出百分率分别为26.80%、38.57%、41.38%、45.92%,固体分散体的溶出度高于同比例的物理混合物。结论:以泊洛沙姆为载体制备间尼索地平固体分散体,可增加药物的体外溶出度和溶解度。     

托伐普坦固体分散体的制备及体外溶出特性考察

目的 采用固体分散技术提高难溶性药物托伐普坦的体外溶出度。方法 选用聚维酮K_29/32为载体材料,以溶剂蒸发法制备托伐普坦固体分散体。采用差示扫描量热法(DSC)、X-射线粉末衍射法(XRPD)对所得固体分散体进行鉴定, 并进行溶解度、体外溶出实验。结果 固体分散体的DSC 图谱及X-射线粉末衍射确定了托伐普坦以无定形态分散在载体中, 体外溶解实验表明其溶出较原料药、物理混合物均有明显提高。结论 将托伐普坦与PVP K_29/32制成固体分散体,其分散状态发生了改变,溶出性能明显提高。     

磷脂固体分散体对槲皮素溶出促进作用的研究

目的研究磷脂固体分散体对槲皮素溶出的促进作用。方法用溶剂法制备了不同比例的槲皮素的磷脂固体分散体 ,与其相应的物理混合物及槲皮素的PVP或PEG4 0 0 0 (1∶1)固体分散体并进行了溶出的对比研究。结果所制得固体分散体均可改善槲皮素的溶出 ,而质量比为 1∶1的槲皮素 磷脂固体分散体的溶出促进作用最为显著。DSC和X射线粉末衍射的研究表明 ,在质量比为1∶1的槲皮素 磷脂固体分散体中 ,槲皮素以无定形的状态分散于载体磷脂中 ,其熔点吸热峰消失。结论槲皮素溶出度的增大与其无定形的存在状态、磷脂对其的润湿作用以及磷脂在水中可形成脂质体有关     

盐酸溴己新固体分散体制备及体外溶出实验

目的制备盐酸溴己新（BH）固体分散体并研究其体外溶出度。方法以聚乙烯吡咯烷酮（PVP）为载体,采用喷雾干燥法制备难溶性药物盐酸溴己新固体分散体,并进行体外溶出实验。结果制备成的固体分散体能显著提高盐酸溴己新的体外溶出速率,PVPk-15载体的固体分散体溶出较PVPk-30载体的固体分散体快。随着PVPk-15载体比例增加,固体分散体的溶出先增大后减小,BH-PVPk-15为1∶5时的固体分散体具有良好的体外速释作用。结论将盐酸溴己新制成固体分散体能明显提高其溶解度及体外释放速率。