不同基质的吴藿降压滴丸中吴茱萸碱体外溶出研究

目的:比较不同基质的吴藿降压滴丸中吴茱萸碱体外溶出差异。方法:分别以泊洛沙姆-188、聚乙二醇(PEG)4000、PEG6000为基质,制备吴藿降压滴丸;测定各滴丸中吴茱萸碱的体外溶出度,绘制溶出曲线,求出累积溶出参数,并进行分析。结果:以泊洛沙姆-188、PEG4000、PEG6000为基质制备的滴丸中吴茱萸碱的溶出度分别为99.1%、95.2%、93.6%。以PEG4000、PEG6000为基质制备的滴丸中吴茱萸碱溶出速度较泊洛沙姆-188快,但吴茱萸碱溶出量较后者低。结论:泊洛沙姆-188、PEG类均为非离子型表面活性剂,对吴茱萸碱的溶出起增溶作用,泊洛沙姆-188增溶效果强于PEG类。     

泊洛沙姆固体分散体对穿心莲内酯溶出特性的影响

目的:考察泊洛沙姆固体分散体对难溶性药物穿心莲内酯体外溶出特性的影响。方法:以泊洛沙姆为载体材料,采用熔融法制备不同比例的穿心莲内酯-泊洛沙姆固体分散体,并考察其体外溶出特性。通过红外光谱和X射线衍射图谱研究药物在固体分散体的存在状态。结果:与穿心莲内酯空白药物相比,穿心莲内酯固体分散体在蒸馏水、pH1.2盐酸溶液与pH6.8磷酸盐缓冲液中溶出速率明显提高,载药固体分散体15min时累积释药量是穿心莲内酯空白药物的3.6倍;穿心莲内酯以微晶态高度分散于载体材料中。结论:以泊洛沙姆188为载体制备穿心莲内酯固体分散体,能有效提高难溶性药物的溶出速率。     

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。     

吲哚美辛-泊洛沙姆188固体分散体的制备

目的制备吲哚美辛-泊洛沙姆188固体分散体,提高吲哚美辛的溶出度。方法以泊洛沙姆188为载体,采用溶剂-熔融法制备固体分散体。用差示热分析(DTA)、扫描电子显微镜(SEM)考察药物在载体中的存在状态,并进行体外溶出度研究。结果吲哚美辛以微晶或无定形分散在载体中,药物的溶出度随载体比例增加而增加。结论制备的固体分散体吲哚美辛的溶出度和溶出速率显著提高。     

布渣叶总黄酮固体分散体的制备及体外溶出度测定

目的:采用固体分散体技术考察不同载体材料对布渣叶总黄酮提取物溶出度的影响.方法:选择不同种类的聚乙二醇、泊洛沙姆、聚乙烯吡咯烷酮为载体材料,与布渣叶总黄酮提取物按质量比1:4混合均匀,分别用熔融法和溶剂法制备固体分散体,以固体分散体中总黄酮、牡荆苷、异牡荆苷、水仙苷的90 min累积溶出度作为评价指标,比较不同载体制备的固体分散体的释药速率,并采用X射线衍射和红外光谱分析对其物相特征进行研究.结果:与布渣叶总黄酮提取物和物理混合物相比,以PEG和泊洛沙姆所制备的布渣叶提取物固体分散体中总黄酮、牡荆苷、异牡荆苷和水仙苷的体外溶出度与溶出速率均明显增加.其中以泊洛沙姆407为载体材料所制备的固体分散体中总黄酮体外溶出度最佳,90 min累积溶出度达到84%;以PEG 6000为载体材料所制备的固体分散体中牡荆苷、异牡荆苷、水仙苷体外溶出度最佳,90 min累积溶出度均达96%以上.结论:采用固体分散体技术,选择PEG 6000或泊洛沙姆407为载体制备布渣叶总黄酮提取物固体分散体,对提取物中脂溶性成分的溶出有明显改善作用.     

淫羊藿素-泊洛沙姆188固体分散体的制备及溶出度研究

目的:制备淫羊藿素-泊洛沙姆188固体分散体以提高淫羊藿素的溶出度。方法:以泊洛沙姆188为载体,采用熔融法制备固体分散体。通过体外溶出度比较,考察了载体泊洛沙姆188的用量(淫羊藿素-泊洛沙姆188质量之比为5∶1、3∶1、2∶1、1∶1、1∶3、1∶5、1∶7、1∶9、1∶11、1∶13、1∶15、1∶17、1∶19、1∶27、1∶31)、熔融温度(60、70、80℃)、冷却温度(-20、0、20℃)对固体分散体中淫羊藿溶出度的影响;同时比较了淫羊藿素原料药及其物理混合物、固体分散体的体外溶出度以证实固体分散体的形成。结果:所制固体分散体的淫羊藿素溶出度在一定程度上随载体比例增加而增加,当淫羊藿素与载体之比为1∶17~1∶27时淫羊藿素在120min时的溶出度均在90%以上;熔融温度、冷却温度经综合分析后分别确定为60、0℃;在溶出30 min时,固体分散体的溶出度是物理混合物的1.5倍。结论:制备的固体分散体显著提高了淫羊藿素的溶出度。     

盐酸小檗碱泊洛沙姆188固体分散体的制备

目的:制备盐酸小檗碱泊洛沙姆188固体分散体。方法:采用熔融法制备固体分散体,考察药物和载体的比例、熔融温度、冷却温度对溶出率的影响,比较固体分散体和物理混合物的溶出率的区别。结果:药物和载体比例达到1∶1时,载体的量足够使药物分散均匀;熔融温度对溶出率影响不大;冷却温度对溶出率影响较大,0℃时溶出率最快。与物理混合物相比,固体分散体将盐酸小檗碱的溶出率提高了近1倍。结论:盐酸小檗碱泊洛沙姆188固体分散体提高了盐酸小檗碱的体外溶出率。     

三元固体分散体提高利多卡因溶解度研究（英文）

使用熔融法制备利多卡因-泊洛沙姆固体分散体以提高利多卡因的溶解度及溶出度。以利多卡因(LIC)作为模型药物,分别使用泊洛沙姆188 (P188)和泊洛沙姆407 (P407)作为单一及混合载体,制备三元及二元固体分散体并进行比较。使用DSC、XRD、SEM及FTIR进行一系列表征,通过溶出度试验研究固体分散体的溶出特性,药物以晶体形式存在于载体中,药物溶出度及溶解度结果较原料药均有明显提高。相溶解度研究显示出药物与载体呈AL型曲线,有分子相互作用的存在。此外,还考察了固体分散体在不同相对湿度下的长期稳定性,稳定性测试结果表明三元及二元利多卡因-泊洛沙姆固体分散体在不同湿度下,6个月内保持稳定。研究结果表明,混合泊洛沙姆三元固体分散体可以显著提高难溶性利多卡因的溶出度和溶解度。     

不同因素对去甲斑蝥素—泊洛沙姆407缓释制剂体外释放度的影响

目的：了解溶出介质温度、转盘速度及泊洛沙姆407浓度对去甲斑蝥素／泊洛沙姆407缓释制剂释放动力学的影响。方法：采用紫外分光光度法,对去甲斑蝥素在不同情况下的体外释放度进行考察。结果：去甲斑蝥素随泊洛沙姆407凝胶的溶解而逐步释放,随着介质温度升高、转盘速度加快及辅料浓度的降低,去甲斑蝥素释放度相应增加。结论：去甲斑蝥素从泊洛沙姆407中的释放速度与介质温度、转蓝速度呈线性正相关,而与泊洛沙姆407的浓度呈线性负相关。     

瑞格列奈片的处方工艺及溶出度研究

目的:考察瑞格列奈片的处方优化策略,为该药的片剂开发提供参考.方法:采用单因素试验和正交实验的方法,对瑞格列奈片处方中的粘合剂、崩解剂、增溶剂等多种辅料进行选择,并对片剂的性能和溶出等进行考察.结果:通过单因素考察,崩解剂选择为交联PVP XL、PVP-K30作为黏合剂、泊洛沙姆188为增溶剂.多因素正交考察将处方确定为瑞格列奈2mg,微晶纤维素60mg,泊洛沙姆188为1mg,30％的PVP K30水溶液适量,交联PVP XL 10mg.溶出和片剂性能检测结果显示,优化后的处方能满足瑞格列奈的制剂要求.结论:瑞格列奈2mg,微晶纤维素60mg,泊洛沙姆188为1mg,30％的PVP K30水溶液适量,交联PVP XL 10mg可作为瑞格列奈的制剂处方,可达到工艺效果.     

800 mg Darunavir tablets prepared by hot melt extrusion

Darunavir (TMC 114) is a protease inhibitor used in the therapy of HIV-1. The aim of this study was to formulate 800?mg of Darunavir in a single unit dosage form, with suitable mechanical properties and dissolution behavior, using a corotating twin screw extruder. In preliminary investigations, extrudates of 1?mm diameter were prepared to evaluate the extrusion and dissolution behavior of Darunavir. Two different poloxamers (188 and 407) were used to modify the dissolution properties of Darunavir, and a higher solubilization for poloxamer 188 was observed. Furthermore, a zero order drug release from pure Darunavir extrudates was found which was modulated by the extrudate diameter. Extrudates of 13?mm diameter were cut into tablets containing 800?mg of Darunavir. Due to the lower specific surface area in comparison to the 1?mm extrudates, an addition of solubilizing agent was required to obtain the desired dissolution profiles. Therefore, the influence of Mannitol and poloxamer 188 was investigated in different formulations. The formulations exhibited acceptable extrusion behavior and dissolution properties.     

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。     

Effect of poloxamer on the dissolution of felodipine and preparation of controlled release matrix tablets containing felodipine

The effects of poloxamer and HPMC on the dissolution rate of felodipine were investigated and a felodipine controlled release tablet was developed by increasing the water solubility of felodipine and using swelling polymer to control release rate. Milling of felodipine slightly increased the dissolution rate of felodipine when compared with physical mixture. XRD results indicated that felodipine remained in the crystalline form even after co-milling with poloxamer. Improved dissolution rates after co-milling with HPMC and poloxamer were due to both solubilization effect of polymer and milling. The effect of poloxamer on dissolution rate was more significant than that of HPMC. Based on increased solubility of felodipine in the presence of poloxamer, it was concluded that the improved dissolution rate of felodipine was mainly due to a high local concentration of poloxamer around felodipine. Controlled release felodipine tablets were prepared using poloxamer as a solubilizing agent and Carbopol as a controlled release matrix.     

Solubility enhancement of desloratadine by solid dispersion in poloxamers

The present study investigates the possibility of using poloxamers as solubility and dissolution rate enhancing agents of the poorly water soluble drug substance desloratadine that can be used for the preparation of immediate release tablet formulation. Two commercially available poloxamer grades (poloxamer P 188 and poloxamer P 407) were selected, and solid dispersions (SDs) containing different weight ratio of poloxamers and desloratadine were prepared by a low temperature melting method. All SDs were subjected to basic physicochemical characterization by thermal and vibrational spectroscopy methods in order to evaluate the efficiency of poloxamers as solubility enhancers. Immediate release tablets were prepared by direct compression of powdered solid dispersions according to a General Factorial Design, in order to evaluate the statistical significance of two formulation (X(1) - type of poloxamer in SD and X(2) - poloxamer ratio in SD) and one process variable (X(3) - compression force) on the drug dissolution rate. It was found that desloratadine in SDs existed in the amorphous state, and that can be largely responsible for the enhanced intrinsic solubility, which was more pronounced in SDs containing poloxamer 188. Statistical analysis of the factorial design revealed that both investigated formulation variables exert a significant effect on the drug dissolution rate. Increased poloxamer ratio in SDs resulted in increased drug dissolution rate, with poloxamer 188 contributing to a faster dissolution rate than poloxamer 407, in accordance with the results of intrinsic dissolution tests. Moreover, there is a significant interaction between poloxamer ratio in SD and compression force. Higher poloxamer ratio in SDs and higher compression force results in a significant decrease of the drug dissolution rate, which can be attributed to the lower porosity of the tablets and more pronounced bonding between poloxamer particles.     

吡罗昔康片溶出度考察

目的考察不同厂家吡罗昔康片在不同pH值溶出介质中的体外溶出情况。方法采用中国药典溶出度第二法装置、转速50、75 r·min^-1、溶出介质均为900 ml。UV法测定吡罗昔康溶出度。结果在pH6.8磷酸盐缓冲液中各厂家吡罗昔康片的溶出在20 min达到70%以上,在pH1.2盐酸溶液中,基本达到《中华人民共和国药典》（2005年版）的规定（既45 min溶出度分别≥70%）;在pH4.5醋酸盐缓冲液60 min达到70%以上,在水中90 min时只达64%。结论在四种溶出介质中溶出差异显著,在水中溶出达不到要求。不同厂家及同一厂家的不同批次溶出差异显著。     

过程分析比较不同厂家盐酸吡格列酮片的溶出度

目的建立过程分析盐酸吡格列酮片溶出度的方法,比较同一厂家制剂溶出度的一致性及不同厂家盐酸吡格列酮片的溶出度。方法桨法,以(9→1000)盐酸溶液为溶出介质,转速75r.min-1,光纤药物溶出度实时测定仪检测3个厂家盐酸吡格列酮片的溶出度。结果A厂和C厂生产的盐酸吡格列酮片溶出度曲线一致性很好;B厂的溶出度曲线差异较大。结论利用光纤药物溶出仪实时、在线、过程监测的特点,计算机平台全面直观地反映各厂盐酸吡格列酮片的溶出度,为全面评价药物内在质量和生物等效性提供参考。     

不同厂家枸橼酸他莫昔芬片的体外溶出度考察

目的:考察国内4个厂家生产的枸橼酸他莫昔芬片的体外溶出度,为临床选用用药提供参考。方法:采用中国药典2010年版中规定的桨法测定溶出度,紫外分光光度计测定溶液吸光度,吸收系数法计算他莫昔芬浓度。利用Excel软件计算累积溶出百分率,并对各厂家之间的溶出度进行比较分析。结果:4个厂家枸橼酸他莫昔芬片的体外溶出度均达到中国药典规定的要求,但各厂家的溶出表现存在一定差异。结论:不同厂家枸橼酸他莫昔芬片的溶出表现存在一定差异,应予关注。     

国产替米沙坦片与进口对照片溶出曲线对比

目的国产替米沙坦片与进口替米沙坦片溶出曲线的对比。方法本试验采用ZRS-6智能溶出试验仪,以磷酸盐缓冲溶液(pH7.4)为溶出介质,分别测定了替米沙坦进口对照片与国产片的溶出曲线。结果及结论国产替米沙坦片与进口片在磷酸盐缓冲溶液(pH7.4)中溶出完全,且两者溶出曲线基本一致。     

不同厂家格列美脲片溶出度的比较

考察了在不同pH的溶出介质中,不同厂家格列美脲片的体外溶出情况。采用中国药典2005年版溶出度第二法装置、转速50r/min、溶出介质900ml。结果显示,在水、pH 1.2盐酸、pH 6.8磷酸盐缓冲液和pH 7.8磷酸盐缓冲液中,各厂家格列美脲片的溶出度有显著性差异。