羧甲基纤维素钠助悬性能的研究

本文对羧甲基纤维素钠(CMC—Na)的流变学性质及在不同条件下的助悬性能进行了研究。实验表明:CMC—Na水溶液呈假塑性流动,其流变学特性符合经验或(Ωη’)q=Ωη’,logη”和浓度间呈线性关系。乙醇可增大CMC—Na水溶液的表观粘度。当混悬剂中固体分散相含量较高时,应用一定浓度的CMC—Na可呈现触变性.适当的Ca~(2+)可增强触变性.这可能是由于Ca~(2+)在相邻吸附了CMC—Na的颗粒间起架桥作用所致。二价金属离子的这种架桥作用既可能增强触变性,又可能促进结块。     

羧甲基纤维素钠的配伍研究

本文研究了羧甲基纤维素钠与硫酸新霉素,硫酸庆大霉素及醋酸洗必泰的配伍问题。结果表明,两者配伍后可产生沉淀,并影响制剂的粘性及上述抗生素的抑菌效价。     

羧甲基纤维素钠胶浆制备方法的比较

羧甲基纤维素钠胶浆制备方法的比较印嘉骏（江苏武进中医院，江苏２１３１６１）ＣＯＭＰＡＲＩＳＯＮＯＦＰＲＥＰＡＲＡＴＩＯＮＯＦＣＡＲＢＯＸＹＭＥＴＨＹＬＣＥＬＬＵＬＯＳＥＳＯＤＩＵＭＭＵＣＩＬＡＧＥ￥ＹＩＮＪｉａ－Ｊｕｎ（ＷｕｊｉｎＨｏｓｐｉｔａｌｏｆ...     

羧甲基纤维素钠胶浆制备方法的改进

目的:解决羧甲基纤维素钠胶浆配制过程中溶胀慢、易结块问题.方法:将羧甲基纤维素钠分散于羟苯乙酯醇溶液和适量的甘油中,再进行配制.结果:改进法简化了配制操作过程,缩短了胶浆的放置时间,减少了药品的污染.结论:改进法可作为医院配制该制剂的有效方法,具有很好的实用应用价值.     

比色法测定2%羧甲基纤维素钠滴眼液含量

根据羧甲基纤维素钠水解产物与蒽酮在酸性条件下生成蓝绿色,其浓度与比色吸收值在一定范围内成正比的原理,采用比色法测定羧甲基纤维素钠滴眼液含量。该方法简便,尤其适用于医院快速分析,经回收试验。平均回收率为99.76%.     

药用辅料羧甲基纤维素钠物理表征参数研究

目的：对不同来源的羧甲基纤维素钠物理质量属性进行评价。方法：借鉴中药化学指纹图谱的概念,由松密度、振实密度、粒径＜50 μm百分比、粉体粒度分布宽度、粉体粒度分布范围、豪斯纳比、 休止角、颗粒间空隙率、卡尔指数、干燥失重、吸湿性11个指标作为羧甲基纤维素钠的物理表征参数, 并对其进行评价;构建了可压性参数(参数指数、参数轮廓指数和良好可压性指数),预测辅料的压缩特性。结果：不同来源或同一型号不同批次的羧甲基纤维素钠粉体学性质存在明显差异,可压性差异不大。结论：建立的羧甲基纤维素钠物理参数表征方法,可以用于评价不同来源粉体的质量一致性,为药用辅料质量评价和口服固体制剂处方开发及工艺控制提供新的思路。     

羧甲基纤维素钠敷料在急性伤口中的应用

“湿性愈合理论”认为,将创面置于一个封闭、湿润的环境中,有利于创面的加速愈合。封闭敷料（occlusive dressings）是在“湿性愈合理论”指导下研发的新型伤口敷料。其中应用最多的水胶体敷料其基本成分是羧甲基纤维素钠（sodium carboxymethyl cellulose,CMC）,具有吸收创面渗液形成凝胶的特性,可以起到保持创面适宜的温湿度、支撑创面的作用。本文对羧甲基纤维素钠在急性伤口中的应用进行简述。     

羧甲基纤维素钠胶浆配制工艺的改进

羧甲基纤维素钠有强烈亲水性而极易溶于水，其水溶液具有粘性且较少受溶液pH及无机盐的影响，常用作固体制剂的粘合剂和液体制剂的增粘、增稠及助悬剂。但由于本品在水中溶解容易形成高粘度的凝胶层而阻止水份的进一步渗入，其溶胀性能不甚理想。     

正交试验考察羧甲基纤维素钠胶浆的制备工艺

目的:考察羧甲基纤维素钠(CMC-Na)胶浆的制备工艺。方法:以溶媒种类、CMC-Na处方含量及CMC-Na加入方式3因素3水平设计正交试验,考察CMC-Nz胶浆相对最佳的配制方法和处方。结果:以热纯化水为溶媒、CMC-Na处方含量2.5%、搅拌下将CMC-Na撒入溶媒中的工艺为最佳工艺。结论:用正交试验优选出的CMC-Na胶浆的配方、制备方法与《中国医院制剂规范》中收载的一致。     

羧甲基纤维素钠质量一致性评价及性能参数智能可视化研究

本文通过物理指纹图谱、多元分析方法评价不同来源羧甲基纤维素钠质量一致性,用R语言可视化功能探索了其性能参数之间的内在联系,并绘制自变量与粉体流动性的等高线图,求得设计空间。通过物理指纹图谱及多元分析方法,发现不同来源的羧甲基纤维素钠粉体学性质存在差异,其含水量、松密度及振实密度对流动性影响较大。运用R智能可视化分析得出样品流动性与填充性呈正相关,与可压性呈负相关,且具有统计学意义(P <0.01)。在休止角为30°～40°时,确定了合适的设计空间,即5.092 2%<含水量<7.006 7%、0.560 2 g·cm^-3<松密度<0.579 9 g·cm^-3、0.646 3 g·cm^-3<振实密度<0.816 5 g·cm^-3。结果表明,运用物理指纹图谱、多元分析及可视化方法对药用辅料质量一致性进行评价是科学可行的,为辅料生产、质量评价及仿制药处方开发提供了新的思路。     

以牡蛎壳粉-CMC为载体制备阿司匹林胃漂浮片的研究

目的:研制具有多微孔吸附特性的牡蛎壳粉和羧甲基纤维素钠(CMC)为复合药物载体的阿司匹林(ASP)胃漂浮片,并考察其体外释药特性和体外漂浮性能.方法:采用紫外分光光度法进行释放度试验.根据累积释药曲线对各组阿司匹林(ASP)胃漂浮片的释药过程分别进行数学模型拟合,从而研究片剂中的牡蛎壳粉与CMC的用量对释药过程的影响.结果:处方Ⅱ具有良好的漂浮性能,释药过程最理想,其释药过程符合体外释药特征零级动力学过程,其模拟方程为Q=0.080 4T 0.146 2,相关系数r=0.998 7.结论:阿司匹林胃漂浮片达到设计要求.     

Physicochemical characterization of tacrolimus-loaded solid dispersion with sodium carboxylmethyl cellulose and sodium lauryl sulfate

To develop a novel tacrolimus-loaded solid dispersion with improved solubility, various solid dispersions were prepared with various ratios of water, sodium lauryl sulfate, citric acid and carboxylmethylcellulose-Na using spray drying technique. The physicochemical properties of solid dispersions were investigated using scanning electron microscopy, differential scanning calorimetery and powder X-ray diffraction. Furthermore, their solubility and dissolution were evaluated compared to drug powder. The solid dispersion at the tacrolimus/CMC-Na/sodium lauryl sulfate/citric acid ratio of 3/24/3/0.2 significantly improved the drug solubility and dissolution compared to powder. The scanning electron microscopy result suggested that carriers might be attached to the surface of drug in this solid dispersion. Unlike traditional solid dispersion systems, the crystal form of drug in this solid dispersion could not be converted to amorphous form, which was confirmed by the analysis of DSC and powder X-ray diffraction. Thus, the solid dispersion system with water, sodium lauryl sulfate, citric acid and CMC-Na should be a potential candidate for delivering a poorly water-soluble tacrolimus with enhanced solubility and no convertible crystalline.     

Preparation and characterization of mucinated cellulose microparticles for therapeutic and drug delivery purposes

Mucinated cellulose microparticles were generated by mixing equal concentrations of colloidal dispersions of porcine mucin (Mc) and microcrystalline cellulose (MCC). The hybrid polymer was recovered by precipitating at controlled temperature and pH conditions using acetone. Some physicochemical, functional and thermal properties of the hybrid polymer were determined and compared with those of Mc and MCC. The new polymer Mc-MCC had swelling and moisture sorption profiles that were different from those of Mc and MCC in buffer solutions with different pH values and relative humidity, respectively. The mucoadhesive property of the new polymer was similar to that of Mc. The scanning electron micrographs (SEMs) showed that the microparticles generated from the hybridization were similar to those of MCC, but with larger and denser particles. The Fourier Transform Infrared (FT-IR) spectrum and Differential Scanning Calorimeter (DSC) thermogram of the hybrid polymer were characteristically different from those of Mc and MCC. The presence of new peaks in the FT-IR spectrum and distinct cold crystallization exotherm, which were absent in both Mc and MCC, confirms the formation of a new polymer type with synergistic physicochemical and functional properties.     

Thixotropy of different concentrations of microcrystalline cellulose:sodium carboxymethyl cellulose gels

An extensive study is made of the rheologic behavior of microcrystalline cellulose:sodium carboxymethyl cellulose gels at six different concentrations (between 1 and 2.5% by weight). The thixotropy of these gels was analyzed in terms of agitation time, the duration of storage, concentration, and temperature; a semiempirical function was thus obtained providing thixotropic area as a function of these variables. The instantaneous variation rate in thixotropic area was defined, providing a better understanding of the rate of structural breakdown. Also, it is shown that after 5 min of agitation, the variation rate becomes negligible (approximately 0.7% of the initial value); this result is practically independent of the remaining variables.     

Novel probiotic dissolvable carboxymethyl cellulose films as oral health biotherapeutics: in vitro preparation and characterization

Objectives: Oral health is influenced by the mouth's resident microorganisms. Dental caries and periodontitis are oral disorders caused by imbalances in the oral microbiota. Probiotics have potential for the prevention and treatment of oral disorders. Current formulations, including supplements and foods, have limitations for oral delivery including short storage time, low residence time in the mouth, effects on food consistency, and low patient compliance. Oral thin films (OTFs) may be efficient in delivering probiotics to the mouth. This research aims to develop a novel carboxymethyl cellulose (CMC)-probiotic-OTF to deliver probiotics for the treatment/prevention of oral disorders.

Methods: CMC-OTFs were developed with varying CMC concentration (1.25 – 10 mg/mL), weight (5 – 40 g), thickness (16 – 262 μm), hygroscopicity (30.8 – 78.9 mg/cm² film), and dissolving time (135 – 600 s). The 10 g 5 mg/mL CMC-OTF was selected and used to incorporate Lactobacillus fermentum NCIMB 5221 (6.75 × 10⁸ cells/film), a probiotic with anti-inflammatory potential for periodontitis treatment and capable of inhibiting microorganisms responsible for dental caries and oral candidiasis.

Results: The CMC-OTF maintained probiotic viability and antioxidant activity following 150 days of storage with a production of 549.52 ± 26.08 μM Trolox equivalents.

Conclusion: This research shows the successful development and characterization of a novel probiotic-CMC-OTF with potential as an oral health biotherapeutic.     

盐霉素钠纳米脂质体的制备及表征

目的制备并表征盐霉素钠纳米脂质体(SLN)。方法采用薄膜分散法制备盐霉素钠纳米脂质体,通过调节脂质体中胆固醇比例,以盐霉素钠包封率为评价指标,筛选盐霉素钠纳米脂质体的优化处方。结果透射电镜显示盐霉素钠纳米脂质体形态圆整,分散性良好,激光粒度仪显示盐霉素钠纳米脂质体平均粒径为99.0nm,Zeta电位为-33.5mV,包封率为85.7%,载药量为6.7%。通过脂质体包裹,盐霉素钠在水中的最高浓度可提高15倍,并证明其具有一定缓释效果。结论笔者得到了粒径大小在100nm左右,形态均一,包封率和载药量较高的盐霉素钠纳米脂质体,为进一步测定其杀伤肿瘤活性奠定了坚实的制剂学基础。     

肺靶向地塞米松微球的制备及体外释药

目的:研究水溶性药物地塞米松磷酸钠肺靶向微球制备工艺的优化。方法:以油/水型乳化-溶剂挥发法制备微球,考察微球的性质及肺靶向性。维持其他条件不变,内相中加入甲醇和改变外相中氯化钠的加入量后,考察微球的载药量变化。结果:所制的微球的平均粒径为(8.37±4.0)μm。突释性好,最初0.5h释药量达48.28%。各器官石蜡切片中,肺组织中有较多微球嵌顿。随着内相中加入甲醇和外相中加入氯化钠,微球载药量提高。结论:地塞米松微球有良好的肺靶向性。采用油/水型乳化-溶剂挥发法制备水溶性地塞米松微球时,内相中加入甲醇和外相中加入氯化钠有助于提高微球的载药量。     

Preparation,characterization and dissolution studies of fast release diclofenac sodium tablets from PVP solid dispersions

Diclofenac sodium is a non-steroidal anti-inflammatory drug widely used in the treatment of ankylosing spondylitis, rheumatoid arthritis and osteoarthritis. In this context, a rapid onset of action is required. Thus, the aim of this study was to formulate diclofenac sodium-PVP K-30 fast release tablets from solid dispersions. The physical state and drug:carrier interactions were analyzed by X-ray diffraction and scanning electron microscopy and stability upon storage was also studied. Dissolution rate of diclofenac sodium from solid dispersions was markedly enhanced by increasing the polymer concentration.     

Preparation and in vitro evaluation of sustained release tablet formulations of diclofenac sodium

The effects of formulation variables on the release profile of diclofenac sodium (DS) from hydroxypropylmethyl cellulose (HPMC) and chitosan matrix tablets were studied. DS tablets were prepared by wet granulation and direct compression methods and different ratios of HPMC and chitosan were used. Physical properties of the prepared tablets and targeted commercial sustained release (SR) tablet and the drug release were studied in tablets that were placed in 0.1 M HCl for 1 h and phosphate buffer solution was added to reach pH value of 7.5. In vitro studies showed that 20% HPMC contained SR formulation with direct (dry) compression method is the optimum formulation due to its better targeting profile in terms of release. This formulation also exhibited the best-fitted formulation into the zero order kinetics. The precision and accuracy of the analytical method were also checked. The repeatability and reproducibility of the method were also determined.     

阿洛西林钠的制备

目的　制备阿洛西林钠。方法　以氨苄西林三水酸为原料,经与侧链1-氯甲酰基- 2 -咪唑烷酮缩合得阿洛西林酸,成钠盐后,真空冷冻干燥制得阿洛西林钠。结果与结论　本制备工艺操作简便,收率高,成本低,易于工业化生产。