固体分散技术提高黄芩提取物溶出度的研究

目的：通过制备固体分散体，提高黄芩提取物的溶出度。方法：采用熔融法和溶剂法，制备聚乙二醇4000（PEG4000），聚乙二醇6000（PEG6000），聚乙烯吡咯烷酮K30（PVPK30）3种载体材料及不同比例条件下的固体分散体。通过比较原药材、固体分散体、机械混合物的溶出性能，从而确定制备的最佳方法和最佳比例。结果：不同载体不同比例的固体分散体均能提高药物的溶出度，且载体比例越大，药物的溶出越快，3种载体的增溶效果依次为PVPK30〉PEG4000〉PEG6000。结论：以PVP为载体，采用溶剂法所制备的药物/载体比例为1：6的固体分散体能显著提高黄芩提取物的溶出速率。     

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。     

硝苯地平固体分散体制备工艺的研究

目的利用固体分散技术将硝苯地平制成固体分散体,提高其体外溶出速率。方法分别以聚乙二醇6000(PEG6000)、聚乙二醇4000(PEG4000)、聚乙烯吡咯烷酮K30(PVPK30)、泊洛沙姆188(Pluronic F68)等为载体,用熔融法、溶剂法、溶剂-熔融法和喷雾干燥法制备硝苯地平固体分散体。采用差热分析法(DTA)分析药物在固体分散体中的存在状态,并进行体外溶出度试验。结果各种固体分散体均能加快药物的溶出速率,并且随着载体在固体分散体中的比例增大,溶出速率增大。DTA分析显示硝苯地平在PVPK30的固体分散体中以微细结晶存在。结论将硝苯地平制成固体分散体能显著提高硝苯地平的体外溶出速率。     

硝苯地平固体分散体制备工艺的研究

目的利用固体分散技术将硝苯地平制成固体分散体,提高其体外溶出速率。方法分别以聚乙二醇6000(PEG6000)、聚乙二醇4000(PEG4000)、聚乙烯吡咯烷酮K30(PVPK30)、泊洛沙姆188(Pluronic F68)等为载体,用熔融法、溶剂法、溶剂-熔融法和喷雾干燥法制备硝苯地平固体分散体。采用差热分析法(DTA)分析药物在固体分散体中的存在状态,并进行体外溶出度试验。结果各种固体分散体均能加快药物的溶出速率,并且随着载体在固体分散体中的比例增大,溶出速率增大。DTA分析显示硝苯地平在PVPK30的固体分散体中以微细结晶存在。结论将硝苯地平制成固体分散体能显著提高硝苯地平的体外溶出速率。     

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。     

洛伐他汀固体分散体的制备及体外溶出特性比较

目的：利用固体分散技术制备洛伐他汀固体分散体，增加其溶出速率。方法：以不同比例的聚乙烯吡咯烷酮（PVPk-30）、聚乙二醇6000（PEG6000）为载体，采用溶剂法和熔融法制成洛伐他汀固体分散体，测定其溶出速率，并采用差示扫描量热（DSC）法、显微照相技术鉴别药物在固体分散体中的存在状态。结果：两种固体分散体均能提高洛伐他汀溶出速率，在药物载体比例大于1：5时效果较好；洛伐他汀固体分散体中晶型消失，分散在载体中。载体为PVPK30所制固体分散体的溶出速率总体优于载体PEG6000。结论：固体分散体能加速洛伐他汀溶出速率。     

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。     

氨苯砜固体分散体的制备与溶出度测定

目的制备氨苯砜固体分散体，增大氨苯砜溶出度。 方法以聚乙二醇6000(PEG 6000)为载体，采用熔融法，按照不同比例制备固体分散体，并进行体外溶出度研究。结果体外溶出实验表明分散体的溶出速率明显快于原料药及物理混合物，且载体比例越大，药物溶出越快。结论将氨苯砜制备成固体分散体，可以增大其溶出度，有利于提高其剂型的生物利用度。     

环孢素固体分散体的制备及溶出研究

目的: 提高难溶性药物环孢素(CsA)的溶出速率.方法: 选择聚乙二醇(PEG4000)和聚乙烯吡咯烷酮(PVPK30)两种载体,分别以溶剂熔融法和溶剂法制备CsA固体分散体;建立HPLC法检测固体分散体的体外溶出度,并考察不同载体、不同比例及溶出介质、桨法转速对CsA溶出速率的影响.对溶出度结果用Weibull分布模型进行拟合,计算体外溶出参数T50和Td,并进行方差分析.结果: 使用HPLC法测定CsA的体外溶出量准确、稳定、可靠、载体无干扰.制备成的固体分散体能显著提高CsA的体外溶出速率,PVPK30载体的固体分散体的溶出速率明显快于PEG4000载体的固体分散体.溶出介质对药物溶出没有明显影响.结论: CsA: PVPK30为1: 6的固体分散体具有良好的体外速释作用.     

卡维地洛固体分散体的制备与溶出度测定

目的：制备卡维地洛固体分散体,增加其溶解度和溶出速度。方法：以聚乙烯吡咯烷酮（PVP）、聚乙二醇－6000（PEG－6000）为载体,溶剂法和溶剂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;且载体比例愈小,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,为难溶于水药物提高生物利用度开辟一条途径。     

尼群地平固体分散片的制备及其体外溶出度的测定

目的 制备尼群地平(NT)固体分散体片，提高其溶出度：方法 以聚乙烯吡咯烷酮(PVPk30)为载体，用溶剂法制备NT固体分散体；显微镜观察和差示热分析(DTA)鉴别药物在载体中的状态；制备普通片和固体分散体片，测定溶出度，并与市售国产片相比。结果 DTA曲线表明药物在固体分散体中以非晶体状态存在，其体外溶出速率明显提高，20min的累计释放率为73．2％，而普通片及市售国产片分别为22．5％和21．7％。结论 NT制成固体分散体片能明显增加NT的体外溶出度。     

卡维地洛固体分散体的初步研制

目的:制备卡维地洛固体分散体并考察其体外溶出度。方法:以聚乙二醇(PEG)、聚乙烯吡咯烷酮(PVP)的混合物(2∶1、1∶2)为载体,采用溶剂熔融法和共沉淀法制备载体与药物不同比例的固体分散体并比较其体外溶出度。结果:药物溶出度随载体比例增加而增加;载体与药物比例越小,固体分散体与药物原料粉之间溶出度差异越显著;PEG∶PVP(1∶2)所制分散体体外溶出行为较优,以3、10、30、60min时溶出百分率进行比较,固体分散体是药物原料粉的3～8倍。结论:所制卡维地洛固体分散体能增加药物体外溶出度。     

格列喹酮固体分散体的制备及溶出度测定

目的:制备格列喹酮固体分散体并考察其体外溶出性。方法:以聚乙烯吡咯烷酮K30(PVP)、聚乙二醇6000(PEG)为载体,溶剂熔融法和溶剂法制备格列喹酮固体分散体,并与原料药比较体外溶出度。结果:载体比例越大,药物溶出愈快。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者。格列喹酮-PVP固体分散体(1∶7)10min内体外溶出度达到70%以上,优于格列喹酮原料药。结论:成功制备了格列喹酮固体分散体。     

Solid dispersion adsorbates for enhancement of dissolution rates of drugs

Amalgamation of solid dispersion and melt adsorption technologies was utilized for enhancing the dissolution rate of poorly soluble drugs. Glibenclamide was employed as a model drug. PEG6000 and Gelucire44/14 were used as hydrophilic carriers for the preparation of solid dispersions, and lactose was utilized as an adsorbent for the preparation of solid dispersion adsorbates. A high dissolution rate of solid dispersion adsorbates was observed when compared to solid dispersions alone and one of the marketed products.     

缬沙坦固体分散体的制备及体外溶出度研究

目的采用冷冻干燥法制备缬沙坦（Valsartan）速释固体分散体（SD）来提高其体外溶出度。方法分别以羟丙甲基纤维素（HPMC）、聚乙二醇6000（PEG6000）、聚乙烯吡咯烷酮k30（PVPk30）为载体,十二烷基硫酸钠（SDS）为表面活性剂来制备不同比例的缬沙坦固体分散体,通过测定体外溶出度,来选择最优辅料及比例,结果当以PEG6000载体,SDS为表面活性剂时,且药物：PEG6000：SDS=1：5：1％时药物呈现了很好的水溶性。结论在5min时即可溶出90％以上,很大程度上提高了缬沙坦的体外溶出度。     

Optimization for glimepiride dissolution enhancement utilizing different carriers and techniques

The present work is a comparative study that matches between carriers and techniques used to prepare solid mixtures with glimepiride. The study is directed towards elucidation of the most promising carrier capable of highly improving drug dissolution along with the most successful technique used for drug formulation. Mixtures were tested for drug content and dissolution. The most optimum formulae were characterized by DSC, IR and XRPD. Kinetic treatment of dissolution data was performed for physical and co-ground mixtures, solid dispersions and their adsorbates, triple solid dispersions and their adsorbates, microwave generated or treated solid dispersions. Results revealed that enhancing effect mostly reached maximum with ternary solid dispersion adsorbate (TSDads). The latter technique demonstrated a dramatic increase in drug dissolution rate which was reflected in the shortest half-life for most carriers at variable degrees. The highest dissolution rate was attained with pregelatinized starch and decreased to variable degrees with remaining carriers. Differences were ascribed to chemical nature as well as relative water solubility of carriers. The combined effects of incorporating surfactants, polymers and adsorbents to glimepiride contributed together to improve wetting, reduce crystallinity and caused substantial increase in the surface area which made TSDads the most promising technique for enhancing dissolution of glimepiride.     

Dissolution behaviour of nalidixic acid solid dispersions using water soluble dispersion carriers

The oral bioavailability of nalidixic acid (NA) is low due to its poor solubility and slow dissolution. Solid dispersions of NA containing varying concentrations of polyvinylpyrrolidone (PVP), beta-cyclodextrin (BCD) and sodium starch glycolate (SSG) were prepared by solvent evaporation technique in an attempt to improve dissolution rate of NA. Physical characterization of NA, physical mixtures (PM) and solid dispersions were investigated by a variety of analytical methods including scanning electron microscopy (SEM), infrared (IR) spectroscopy and powder X-ray diffraction (XRD). SEM was useful in the verification of possible nalidixic acid inclusion in the dispersion system by studying its surface and shape characteristics of different samples. IR analysis demonstrated no strong interaction between the drug and the carrier exists in the solid dispersions. The degree of crystallinity of nalidixic acid decreased and also differed with the dispersion systems of different carriers. Disolution studies indicated that the dissolution rate and percent dissolution efficiency (DE) were significantly increased in the solid dispersions compared with drug alone. The relative potency of the carriers to enhance the dissolution rate of nalidixic acid was in the order: BCD > PVP > SSG. The dissolution rate of the drug in the solid dispersions was faster when the ration of the drug to carrier was smaller. F-test suggests that first order model may be used for explaining the kinetics of drug release from all the solid dispersion systems.     

盐酸胺碘酮固体分散体的制备及溶出度测定

目的制备盐酸胺碘酮固体分散体,测定其体外溶出度,同时与普通胶囊剂的体外溶出度比较。方法以聚乙二醇6000(PEG6000)为载体,溶剂熔融法制备盐酸胺碘酮固体分散体,用紫外分光光度法测定体外溶出度。结果盐酸胺碘酮固体分散体的体外溶出度比普通胶囊剂显著提高。结论成功制备了盐酸胺碘酮固体分散体。     

The characterization and dissolution performances of spray dried solid dispersion of ketoprofen in hydrophilic carriers

Solid dispersion is one of the most promising strategies to improve oral bioavailability of poorly soluble API. However, there are inconsistent dissolution performances of solid dispersion reported which entails further investigation. In this study, solid dispersions of ketoprofen in three hydrophilic carriers, i.e. PVP K30, PVPVA 6:4 and PVA were prepared and characterized. Physical characterization of the physical mixture of ketoprofen and carriers shows certain extent of amorphization of the API. This result is coinciding to evaluation of drug–polymer interaction using ATR-FTIR whereby higher amorphization was seen in samples with higher drug–polymer interaction. XRPD scanning confirms that fully amorphous solid dispersion was obtained for SD KTP PVP K30 and PVPVA system whereas partially crystalline system was obtained for SD KTP PVA. Interestingly, dissolution profiles of the solid dispersion had shown that degree of amorphization of KTP was not directly proportional to the dissolution rate enhancement of the solid dispersion system. Thus, it is concluded that complete amorphization does not guarantee dissolution enhancement of an amorphous solid dispersion system.     

长春西汀固体分散体的制备及体外溶出特性

目的:制备长春西汀固体分散体,提高其溶出速度和程度。方法:以泊洛沙姆188(F68)为载体,用溶剂-熔融法制备固体分散体;差热分析、X-射线粉末衍射分析以鉴别药物在载体中的存在状态;并考察载体的用量、溶出介质和转速对药物体外溶出特性的影响。结果:长春西汀的固体分散体中药物部分以分子状态分散,部分以微晶分散。固体分散体VIN-F68(1∶6,w/w)的溶出参数t50t、d与相应物理混合物、原料药粉末和市售片剂间差异存在显著性(P<0.01),溶出介质和转速的选择对药物的溶出有一定影响。结论:长春西汀的固体分散体能显著提高药物的溶出速度和程度。