头孢呋辛酯片的制备及溶出因素的考察

采用固体分散技术与普通制粒相结合的方法制备难溶性药物——头孢呋辛酯片,考察影响其溶出的因素并进行处方筛选。选择聚乙烯吡咯烷酮（PVP）或泊洛沙姆作为载体,用溶剂法制备少量的固体分散体,与大量采用普通制粒方法的头孢呋辛酯颗粒相结合制成头孢呋辛酯片,并进行体外药物溶出度的测定。对影响药物溶出的因素：载体材料的种类和用量、崩解剂的加入方法、表面活性剂的加入等因素进行考察,最后利用正交实验进行处方筛选。结果表明,可以选择PVP作为载体制备少量固体分散体,并与普通制粒相结合制备头孢呋辛酯片,能有效提高头孢呋辛酯片的溶出度。     

头孢呋辛酯掩味颗粒剂的制备

采用明胶作为主要掩昧材料,利用固体分散技术制备头孢呋辛酯颗粒剂,并进行掩味效果及稳定性考察。结果表明,该制剂口感、长期稳定性良好,是理想的临床用药。     

头孢呋辛酯掩味方法及颗粒剂的稳定性研究

制备掩盖头孢呋辛酯苦味的混合物,并用其进一步制成头孢呋辛酯混悬颗粒剂。以Carbopol为载体材料,用溶剂挥发法制备掩味混合物：以口感有无苦味为评价指标,结合体外溶出实验,找出最佳处方;并对最终处方进行稳定性考察。以Carbopo 1934 PNF为载体材料制备的混合物可以掩盖头孢呋辛酯药物的苦味,且体外释放及稳定性均符合要求,其制成的颗粒剂质量合格。     

头孢呋辛酯制剂制备技术进展

头孢呋辛酯为临床上广泛使用的第二代口服头孢菌素。介绍了头孢呋辛酯制剂制备技术,包括微粉化技术和超临界流体技术,详细介绍了制粒技术和掩味技术。     

阿卡波糖固体分散体的制备及其溶出度测定

制备阿卡波糖疏水性固体分散体,延缓阿卡波糖的释放,为开发其缓释制剂奠定基础。采用溶剂法和熔融法,将阿卡波糖与不同种类的疏水性载体材料(十六醇、十八醇、硬脂酸、单硬脂酸甘油酯、乙基纤维素、白蜂蜡),分别按不同的比例制成固体分散体,用建立的HPLC方法测定制备的阿卡波糖固体分散体的溶出度。结果表明不同的疏水性载体材料与阿卡波糖制备的固体分散体,对阿卡波糖的释放均有阻滞作用,但以m(阿卡波糖)∶m(乙基纤维素)=1∶4制备的固体分散体药物释放最慢,缓释作用最强。     

水飞蓟素胶囊的制备工艺研究

实验运用溶剂-熔融法制备水飞蓟素固体分散体,并以制备的固体分散体为基础,以胶囊的溶出度为指标,通过单因素考察和正交试验,确定胶囊的处方及制备工艺的最佳工艺。得出最佳工艺条件是:以微晶纤维素为填充剂,固体分散体与微晶纤维素的比例1∶0.5,以L-HPC为崩解剂,固体分散体无水乙醇溶液配成的60%溶液的为粘合剂,微粉硅胶为润滑剂,粘合剂比例为5%,制备胶囊的溶出速率和累计溶出率最好。     

尼莫地平固体分散体的制备及评价

采用喷雾冷凝法制备了三批固体分散体,并对其质量进行考察,结果表明:该法制备的固体分散体,呈规则的粒径小于10μm的球形,绝大部分药物以无定型态分散在载体材料中;含量杂质符合现行版药典要求,60 min的溶出度能达到90%。因此,采用喷雾冷凝法制备固体分散体,能够解决尼莫地平溶出度低,生物利用度不高的问题,具有很好的应用前景。     

头孢呋辛酯及头孢呋辛钠合成工艺进展

头孢呋辛酯和头孢呋辛钠均为临床上广泛使用的第二代广谱头孢菌素类药物。介绍了头孢呋辛酯的合成工艺,详细介绍了头孢呋辛钠合成工艺及其回收工艺。     

头孢呋辛酯片处方工艺研究及溶出曲线一致性评价

由头孢呋辛酯,交联聚维酮、微晶纤维素、羟丙纤维素、二氧化硅和硬脂酸镁,制备了头孢呋辛酯片,并考察处方工艺与体外溶出曲线。采用干法制粒工艺,通过设计正交试验考察粘合剂羟丙纤维素用量（A）、崩解剂交联聚维酮用量（B）、润滑剂硬脂酸镁用量（C）,进行配方筛选,确定最佳处方为A1B2C2,与参比制剂进行4种介质的溶出曲线对比,发现3批样品批间稳定性好,且与参比制剂的溶出曲线一致。     

颜料、颜料制剂及填料

201211050用于化妆品、油墨、涂料的水分散性固体颜料分散体： 用于水性组合物的固体颜料分散体包括颜料和乙氧基醇。这种固体颜料分散体适合以较小的剪切力直接加入到水性组合物中,并作为着色剂使用。该颜料分散体的制备方法包括：加热乙氧基醇和颜料的混合物,然后冷却该混合物,从而制得固体颜料分散体。     

A DSC study of curative interactions. I. The interaction of ZnO,sulfur, and stearic acid

The interaction between combinations of sulfur, stearic acid, and ZnO were studied by differential scanning calorimetry in the absence of rubber. The only reaction observed was between ZnO and stearic acid. A small amount of zinc stearate formed as soon as the stearic acid melted, but the solid product blocked further reaction, which was only completed at 154°C. Water played a major role in the reaction, and in the presence of water, the reaction went to completion at lower temperatures. Sulfur, too, affected the temperature of the ZnO/stearic acid reaction. The preparation of zinc stearate by a number of routes was investigated.     

Effect of Dispersants on the Rheological Behavior of Zirconia-Wax Suspensions

Three types of fatty acids-namely, stearic acid, oleic acid, and 12-hydroxystearic acid-were used as dispersants for stabilization of highly concentrated zirconia-wax suspensions. Rheological properties such as viscosity and yield stress of the suspensions were determined over a temperature range of 65°-85°C. Experimental results indicated that better suspension stabilization was achieved when the 12-hydroxystearic acid was used. Adsorption behavior revealed a greater affinity at the solid/liquid interface that occurred for the 12-hydroxystearic acid than for stearic acid or oleic acid. This observation suggests that the adsorption of 12-hydroxystearic acid may lead to a better packing (or surface concentration) of the acid molecules onto the solid surface than others and also results in a better suspension fluidity and processability. Attractive interparticle interaction was estimated quantitatively by using the Vold model and resulting analysis showed a linear correlation between the yield stress and the attractive potential for the suspensions.     

Influence of Powder Agglomerates on the Structure and Rheological Behavior of Injection-Molded Zirconia–Wax Suspensions

Surface-modified zirconia powders with 20% to 100% of the particle surface area covered with stearic acid was blended with 50 vol% of an organic wax vehicle for rheological study. These fractions of surface coverage gave rise to different degrees of powder agglomeration. A further adsorption of the wax on partially modified particle surfaces was examined, which was likely to exhibit different degrees of solid surface-wax affinity depending upon whether the particle surfaces were "bare" or "premodified." The rheological behavior of the suspensions revealed that the shear viscosity as well as the yield stress increased appreciably with decreased fractions (or surface coverage) of the pre-adsorption. The observed suspension rheology due to incomplete surface modification can be accounted for by the formation of agglomerates which suppress suspension flowability to a significant extent. The formation of the agglomerates alters the suspension structure by reduction of the maximum solid concentration (φ_max) that is attainable for a given powder. This change in suspension structure (decrease in φ_max) leads to a restriction of particle mobility, reflected as a linear function of the yield stress of the suspensions.     

头孢呋辛酯的合成研究

利用7-氨基头孢烷酸(7-ACA)合成头孢呋辛酯,同时对合成过程及关键点进行优化。首先7-ACA在甲醇和水的混合溶剂中低温水解,生成D-7-ACA,不经分离,直接进行7-位酰化反应,经结晶分离干燥后得到关键中间体去氨甲酰基头孢呋辛酸(DCC),收率可达84.8%,再经过与氯磺酸异氰酸酯(CSI)反应完成C-3位的氨甲酰化改造,得到头孢呋辛酸的溶液,结晶分离干燥后,收率可达91.4%,最后与1-溴乙基乙酸酯缩合得到头孢呋辛酯,收率可达93.8%,总合计收率达72.7%。该工艺具有高收率、低成本、易操作等特点,极具有工业化生产价值。     

Development of a continuous process for enol esters of fatty acids

A continuous process for the production of iso-propenyl stearate from stearic acid and propyne was developed. The reaction proceeds at elevated pres-sures and temperatures (∼550 psig and 400 F, respec-tively) in about l0 min. A slower, second reaction produces stearic anhydride from the isopropenyl stearate. A recovery section was devised, wherein the liquid product stream is chilled, recovered as flakes, and extracted with a solvent, e.g. Skelly B. Reaction studies were scaled-up from 10 to 40 lb feed/hr using triple pressed stearic acid and MAPP® gas (AIRCO, Inc., Montvale, NJ), a commercially available gas con-taining a nominal 1/3 propyne, 1/3 propadiene, and 1/3 stabilizing, saturated hydrocarbons. The acid and propyne are reacted in the presence of zinc stearate in a continuous stirred tank reactor (CSTR). The reac-tion is “finished” in a short tubular reactor. Data are presented on the effect of pressure, temperature, catalyst level, dwell in the reactors, and solvent ratio during extraction. The product is about 92% iso-propenyl ester, contaminated with unconverted stearic acid and by-product stearic anhydride.     

工业硬脂酸高温色泽检测方案的建立

通过两种目前在用的硬脂酸高温色泽检测方案的详述,比较了两种检测方案,并通过数据分析,发现试验方案二更适合高温色泽项目的检测,即在200℃空气浴中加热2 h后,在色度计上,以去离子水为空白,检测高温融化后的硬脂酸液体的色泽,读出相应的色号,从而定量测试硬脂酸的高温条件下的色泽,进而控制硬脂酸的质量。     

In vitro and in vivo release of cefuroxime axetil from bioactive glass as an implantable delivery system in experimental osteomyelitis

The aim of this study was to evaluate the characterisation, in vitro and in vivo biocompatibility and antimicrobial activity of bioactive glass (BG) impregnated with an antibiotic. The BG was prepared by normal glass melting procedures as a controlled release device to treat experimental osteomyelitis. The study design was for prospective in vivo experimental study. Two sets of porous bioactive glass ceramic blocks (9 mm × 4 mm × 4 mm and 20 mm × 9 mm × 9 mm) were fabricated using bioactive glass powder and subsequently antibiotic cefuroxime axetil (CFA) (55 and 125 mg on an average) was impregnated in these two sets of blocks, respectively. Osteomyelitis was produced in the right tibia of the rabbits according to the model of Norden. After thorough in vitro characterization of the porous blocks [including X-ray diffraction (XRD), Fourier-transformed infra-red spectroscopy (FTIR), thorough chemical analysis by inductively coupled plasma-atomic emission spectra (ICP-AES) and field-emission scanning electron microscopy (FESEM)] and in vitro elution of the said drug, in vivo test was carried out with rabbit species split into two groups: (a) animals treated with CFA impregnated bioactive glass and (b) parenteral [intra muscular (IM)] administration of CFA. Histological, radiological and drug concentration in bone and serum (measured by HPLC) in both groups were carried out. HPLC technique was used for determination of concentration both in vitro and in vivo. Fabricated porous struts showed amorphous microstructure without formation of any crystallite. The elution of said drug was stopped after 6 days in vitro. Histological studies at 3 and 6 weeks revealed formation of well-developed lamellar bone and havarsian canal. Radiological evaluation pointed out disappearance of sequestrum and existence of newly formed bony specules. Concentration of cefuroxime axetil in bone and serum showed highest value on day 21 which reduced marginally by day 42 and these values were higher than minimum inhibitory concentration (MIC) against Staphylococcus aureus (known pathogen for chronic osteomyelitis). It could be concluded that the biodegradable antibiotic carrier system developed in this study proved to be an effective therapeutic approach toward an experimental model of osteomyelitis. Based particularly on the in vivo results of the study, this cefuroxime axetil incorporated bioactive glass blocks can be successfully used in clinical cases of osteomyelitis in veterinary as well as human orthopaedic surgery.     

Stearic Acid Modified Stearyl Alcohol Oleogel: Analysis of the Thermal,Mechanical and Drug Release Properties

The present study delineates the effect of stearic acid on the properties of stearyl alcohol oleogel. Herein, a series of oleogels were prepared by mixing different proportions of fatty alcohol (Stearyl alcohol; gelator) and fatty acid (stearic acid; co‐gelator). The characterization of the oleogels was done by thermal, macro‐scale stress relaxation, drug release, and antimicrobial studies. The oleogels were formed by the self‐assembly of stearyl alcohol/stearic acid. Thermal studies indicated that the stearic acid alters the crystal morphology, polymorphic transition and rate of crystallization of stearyl alcohol. The firmness of the oleogels with higher stearic proportion was better, which was due to the formation of a rigid network structure of stearyl alcohol in the presence of stearic acid. The release of ciprofloxacin hydrochloride, model drug, from the oleogels was better from the oleogels with higher stearic acid content. The release of the drug from the oleogels was Fickian diffusion‐mediated; except the oleogel with the highest stearic acid proportion. The antimicrobial study showed that the drug loaded oleogels were able to resist the growth of Escherichia coli, model microbe.