罗红霉素在两种介质中的溶出度考察

目的 比较7厂家罗红霉素在两种介质中的体外溶出度。方法 采用紫外分光光度法测定含量和在两种不同介质中的溶出度。结果 7厂家罗红霉素在人工胃液中溶出度不符合要求，有2家在人工肠液中不符合要求。结论 罗红霉素在两种介质中溶出度有很大差异，各厂家之间的产品溶出度也存在差异。     

吉他霉素片溶出度测定的探讨

目的 比较两种方法配制自身对照溶液对测定吉他霉素片溶出度结果的影响.方法 在测定吉他霉素片溶出度的过程中,采用自身对照法(两种对照溶液配制方法)测定其溶出度.结果 用两种不同的方法配制对照溶液,对测定吉他霉素片溶出度的结果影响很小.结论 两种对照溶液配制方法,均能满足吉他霉素片溶出度测定的要求.     

包装对81-1型饮水消毒片稳定性的影响

通过两种包装的81－1型饮水消毒片定量考察，证明用玻璃安瓿包装比塑料管包装更稳定。     

阿奇霉素片溶出度方法的改进

目的对阿奇霉素片溶出度检查方法进行改进，使溶出度检查的方法与结果更为合理。方法分别以0．1mol／1盐酸溶液与pH6．0的磷酸盐缓冲液为溶出介质，对同批样品的溶出度检查结果进行比较。结果以两种溶液为溶出介质的溶出度检查结果无明显差异。结论实验表明该法可行，并能够符合片剂在胃中的溶出情况。     

速溶对乙酰氨基酚片的溶出度测定方法比较

应用中国药典与美国药典规定的方法测定速溶对乙酰胺基酚片的溶出度，实验结果表明，两种溶出度测定方法的结果是一致的。     

医院药品制剂需要搞好"文字包装"

提到医院药品制剂包装问题，常常仅注意到玻璃瓶、塑料瓶、纸盒纸袋等包装材料，我们把这些叫作药品的“硬包装”；药品制剂还有另一种包装，那就是药品的标签、说明书、宣传手册等，我们把这些叫做药品的“文字包装”或称“理论包装”。１加强医院药品制剂文字包装的必要...     

国产和进口盐酸二甲双胍片的体外指标比较

目的考察市售进口和国产两种盐酸二甲双胍的溶出度及其他体外指标。方法采用转篮法对两种盐酸二甲双胍进行溶出度测定并用片剂四用仪测定其他指标,并进行溶出参数的方差分析。结果两种盐酸二甲双胍的体外溶出度均符合中国药典2000年版二部的规定,但溶出参数各不相同。结论国产和进口两种盐酸二甲双胍片其溶出参数存在显著性差异。     

酶法测定盐酸氟桂利嗪胶囊溶出度的考察

目的建立有效的体外溶出度测定方法。方法采用在溶出介质中加酶与不加酶两种方法分别测定不同厂家的盐酸氟桂利嗪胶囊的溶出度，并将两法测定结果进行比较。结果与结论对用药典法测定的溶出度不合格的盐酸氟桂利嗪胶囊，两法的测定结果有显著性差异。     

甲硝唑微栓溶出度及稳定性的研究

本文用进口Ｄｕ－６５型溶出度自动测定仪，按中国药典１９９０年版规定的转兰法，测定三批自制甲硝唑微栓主药的溶出度，在２５分钟内均溶出８０％以上。而静止状态下２４小时内溶出８０％以上。三批自制甲硝唑微栓，在铝塑袋包装条件下，低温加速试验三个月，结果各项指标均合符质量标准。     

两种包装对医院乳膏制剂长期稳定性影响的研究

目的:探讨两种不同包装对乳膏制剂长期稳定性的影响.方法:采用长期稳定性实验方法测定使用两种包装的3种乳膏制剂的装量及有效成分含量.结果:3种乳膏制荆使用新包装的与使用旧包装的样品,两种装量变化差异有统计学意义(P<0.05),且旧包装的装量及有效成份含量变化明显,制剂质量不稳定,敌不宜使用.结论:包装方法对医院乳膏制剂长期稳定性影响大,我院改进包装后,新包装有助于确保乳膏制荆质量稳定.     

Solubility of drugs in aqueous solutions. Part 5. Thermodynamic consistency test for the solubility data

This paper is devoted to the verification of the quality of experimental data regarding the solubility of sparingly soluble solids, such as drugs, environmentally important substances, etc. in mixed solvents. A thermodynamic consistency test based on the Gibbs-Duhem equation for ternary mixtures is suggested. This test has the form of an equation, which connects the solubilities of the solid, and the activity coefficients of the constituents of the solute-free mixed solvent in two mixed solvents of close compositions. The experimental data regarding the solubility of sparingly soluble substances can be verified with the suggested test if accurate data for the activity coefficients of the constituents of the solute-free mixed solvent are available. The test was applied to a number of systems representing the solubilities of sparingly soluble substances in mixed solvents. First, the test was scrutinized for four nonaqueous systems for which accurate solubility data were available. Second, the suggested test was applied to a number of systems representing experimental data regarding the solubility of sparingly soluble substances in aqueous mixed solvents.     

Statistical analysis of the extended Hansen method using the bootstrap technique.

In this study, simple bootstrap techniques are combined with the extended Hansen solubility approach to calculate biases, standard errors, and confidence limits of the partial solubility parameters and to obtain bias-corrected values for these solubility parameters. The bootstrap method is rather new in its application to problems in the pharmaceutical sciences and, therefore, is described here in some detail. This method provides measures of the statistical variation of ratios of regression coefficients without making unwarranted assumptions about data variability. The bootstrap can be used in many statistical packages such as MINITAB, SPSS, SAS, BMDP, or GLIM, all of which are widely available, and could be useful in other areas of the pharmaceutical sciences where regression analysis is employed.     

Prediction and improvement of protected peptide solubility in organic solvents*

A predictive method of solubility for protected peptide fragments of globular proteins was described. The solubility prediction was performed on the basis of both the randomness of peptide structures in a solid state and the existence of tertiary peptide bonds such as X-Pro and X-(Z)Y bonds, in which X and Y are arbitrary amino acid residues and Z is a suitable protecting group for the X-Y peptide bond. In order to predict the randomness, the coil conformational parameter, P_e, was utilized. Solubility prediction by this method was success fully applied to the two classes of protected peptides composed solely of hydrophobic and of various amino acid residues. The solubility test results also indicate that the protection of peptide bonds at suitable intervals is effective in achieving a remarkable improvement in the solubility of extraordinarily insoluble peptides. Lastly, the strategy for the selection of the coupling routes in the protein syntheses was proposed.     

Griseofulvin absorption from different sites in the human small intestine

The site-dependent small-intestinal absorption pattern of griseofulvin was investigated in man. Griseofulvin was chosen as a model substance having extremely low water solubility and moderate lipid solubility. A conventional steady-state perfusion technique (triple-lumen tubing system with a 20 cm test segment) was applied. Dissolved griseofulvin (10.0 mg L^?1) was perfused (10 mL min^?1) during 160 min into different parts of the small intestine with the middle of the test segment between 85 cm and 270 cm beyond the teeth. Each of the ten healthy volunteers was examined twice with the test segment localized in different regions to allow for intraindividual comparisons. Mean drug absorption rates calculated from intestinal aspirate concentrations were similar in the two intestinal parts (proximal, 15.0 ± 5.9 μg (20cm min)^?1; distal, 16.2 ± 4.3 μg (20 cm min)^?1; mean ± SD). Absorption rate was strongly correlated to the amount of griseofulvin offered to the test segment per unit time. Extrapolating these findings it follows that an amount of griseofulvin, once dissolved, would be absorbed completely (>99%) along 100 cm of the small intestine. A significant, positive correlation between the rate of transmucosal fluid transport and the absorption rate of griseofulvin was observed in the distal parts investigated.     

盐酸克林霉素胶囊的体外溶出度考察与结果分析

目的通过对4个不同厂家的盐酸克林霉素胶囊体外溶出度的考察与比较,为临床合理用药提供参考。方法参考相关文献,采用《中国药典》2010年版(二部)附录溶出度第一法装置,以高效液相色谱法测定各样品不同时间的溶出量,并以Weibull方程拟合溶出参数,并对检测结果进行分析。结果根据T50,T d等溶出参数显示,不同厂家盐酸克林霉素胶囊在不同溶出介质中溶出行为有一定差异。结论该药的溶出速率与所处pH环境有关,在临床用药过程中应予以注意。     

A novel method for determination of drug solubility in polymeric matrices

Crystallization of drugs in metastable, supersaturated adhesive polymeric matrices in transdermal drug delivery devices can be avoided by determination of the solubility of the drug in the adhesive polymer. A novel method is described to determine the solubility of the drug in polymeric matrices. Unlike existing methods, this method does not require a long and uncertain experimental time, and is accurate. In this study, an easy and accurate method is presented for the determination of solubility of drugs in polymers based on the relationship between thermodynamic activity of drugs and steady-state flux. In particular, the steady-state flux from a reference saturated solution across a test membrane was compared to an experimentally determined relationship between the polymeric loading concentration and the observed steady-state fluxes. The validity of this method was demonstrated by comparing the results to microscopic observation of crystallization and the study of aged drug-loaded adhesives for lidocaine as a model drug and an acrylate pressure-sensitive adhesive as a model polymer. The solubility of lidocaine was 20.8 +/- 0.5% (w/w) in the acrylate polymer.     

Investigation of the solubility relationships of polar,semi-polar and non-polar drugs in mixed co-solvent systems

The solubility relationships of a non-polar (tioconazole), polar (oxfenieine) and semi-polar (caffeine) drug have been investigated in aqueous ethanol, propylene glycol and polyethylene glycol 400 (PEG 400) binary co-solvent systems. A semi-empirical equation was deduced to describe the relationship between the amount of drug dissolved and the volume fraction of co-solvent employed. The data for tioconazole and oxfenicine followed the expected semi-logarithmic relationship between solubility and fraction co-solvent. However, the semi-polar drug, caffeine followed this relationship only with PEG 400; the other two co-solvents yielded parabolic relationships.Using the binary solubility data, multiple linear regression was used to deduce an equation for the solubility of tioconazole in ternary ethanol, propylene glycol and PEG 400 co-solvent systems. The derived relationship gave excellent prediction of the drug solubility throughout the complete volume fraction range. This allowed a graphical representation of the drug solubility-co-solvent fraction relationship to be established. This visualization of are drug solubility relationship was then used to demonstrate its utility to optimize drug solubility within the competing constraints of the pharmaceutical system.     

Variation in commercial smoking mixtures containing third‐generation synthetic cannabinoids

Variation in ingredients (qualitative variation) and in quantity of active compounds (quantitative variation) in herbal smoking mixtures containing synthetic cannabinoids has been shown for older products. This can be dangerous to the user, as accurate and reproducible dosing is impossible. In this study, 69 packages containing third‐generation cannabinoids of seven brands on the UK market in 2014 were analyzed both qualitatively and quantitatively for variation. When comparing the labels to actual active ingredients identified in the sample, only one brand was shown to be correctly labelled. The other six brands contained less, more, or ingredients other than those listed on the label. Only two brands were inconsistent, containing different active ingredients in different samples. Quantitative variation was assessed both within one package and between several packages. Within‐package variation was within a 10% range for five of the seven brands, but two brands showed larger variation, up to 25% (Relative Standard Deviation). Variation between packages was significantly higher, with variation up to 38% and maximum concentration up to 2.7 times higher than the minimum concentration. Both qualitative and quantitative variation are common in smoking mixtures and endanger the user, as it is impossible to estimate the dose or to know the compound consumed when smoking commercial mixtures. Copyright © 2016 John Wiley & Sons, Ltd.     

Inverse gas chromatographic determination of solubility parameters of excipients

The principle aim of this work was an application of inverse gas chromatography (IGC) for the estimation of solubility parameter for pharmaceutical excipients. The retention data of number of test solutes were used to calculate Flory-Huggins interaction parameter (chi1,2infinity) and than solubility parameter (delta2), corrected solubility parameter (deltaT) and its components (deltad, deltap, deltah) by using different procedures. The influence of different values of test solutes solubility parameter (delta1) over calculated values was estimated. The solubility parameter values obtained for all excipients from the slope, from Guillet and co-workers' procedure are higher than that obtained from components according Voelkel and Janas procedure. It was found that solubility parameter's value of the test solutes influences, but not significantly, values of solubility parameter of excipients.     

圣肤霜中地塞米松稳定性的影响因素及处方工艺优化

目的：考察圣肤霜中地塞米松的稳定性,剔除影响因素,优化处方工艺.方法：采用分散均匀性和高温破坏实验方法,定量筛查影响地塞米松稳定性的因素,调整处方、改进工艺.结果：基质中pH 〉 7.3时地塞米松含量不稳定,呈明显的下降趋势;地塞米松在极性较强的溶液中溶解性降低,是导致药物分散不均匀的主要因素.以适量氮酮溶解地塞米松,依照工艺制备成乳膏可达到均匀分散的效果.调整处方pH在5.5 ～6.5 之间,地塞米松含量稳定.结论：以加速破坏实验和溶解度考察法综合分析影响药物稳定性的因素,该方法科学合理,适用于处方工艺的快速筛查及优化.