药物掩味技术的研究进展

药物研发过程中会有不良臭味而应用受到限制。本文从添加矫味剂、装胶囊,对药片或药物颗粒包衣,用离子交换树脂吸附,将药物制成包合物、毫微囊或无味前体药物等方面综述了改善药物不良臭味的方法。     

克拉霉素掩味颗粒的制备及评价

制备克拉霉素掩味颗粒并对其进行评价。通过流化床包衣和造粒工艺制备克拉霉素掩味颗粒。对样品在不同pH溶出介质的溶出度进行分析,通过傅里叶红外光谱、热分析、扫描电镜及X-射线粉末衍射对样品和物理混合物(克拉霉素+卡波姆+邻苯二甲酸羟丙甲基纤维素酯)进行分析,比较两者差异,通过志愿者对掩味效果进行评价。通过该工艺制备的克拉霉素颗粒体外释放度良好,掩味效果优异。制备的克拉霉素掩味颗粒的耐酸性较好,与美国市售制剂相比溶出度相似性较高,并且该工艺能应用于工业化生产。     

中药口服制剂质量评价研究进展

中药复方制剂质量评价的现代化是实现中药现代化的关键领域之一。综述了近年来中药口服制剂质量评价的研究进展,介绍了中药口服制剂质量评价方面的一些新成果及有价值的经验。提出目前中药质量评价的主流仍然是以化学成分为中心,如指标性成分含量测定和指纹图谱,但是由于中药成分的复杂性,以化学成分为中心的评价方法显示出其局限性,多种对剂型、药效、代谢的评价方法应运而生,并均表现出一定的优势,如体外评价(溶出度检测、生物活性测定)及体内评价(血清药物化学法、代谢组学法);指纹图谱技术、药效学、血清化学等多学科交叉融合,将有助于进一步阐释中药复方的内在质量及其作用机理,逐步向药效物质基础控制的模式转变。     

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。     

浅谈口服固体制剂设备的确认

结合生产实际说明设备确认的意义和重要性,并区分新近设备或厂房与设备持续性确认工作。依据两种验证的区别,提出在持续性验证过程中的几点建议。     

口服固体制剂辅料跃上新台阶

我国固体口服制剂药用辅料在过去很长一段时间里一直是淀粉、糊精与糖粉这“老三样”当家，但近年来发生了较大的变化。一些新颖药用辅料如微晶纤维素、聚乙烯毗洛烷酮（PVP）、纤维素醚衍生物和新型变性淀粉等，在我国制剂行业得到大量应用，即使价格昂贵的直接压片用辅料—乳糖，现已成为国内药用辅料中的大宗产品之一。     

口服固体制剂辅料的扩张机会

全球专业药用辅料市场在地区分布上呈现出两个不同的层面——欧美成熟市场和中国等新兴市场。在美国和西欧这些早已成熟的市场，增长前景趋于平淡；其辅料生产商已经走向生产专业化、品种系列化和应用科学化的发展趋势，这也是在制药公司提出辅料具有更高功效和更多功能要求的推动下形成的。在中国等新兴市场，     

一种多剂型普药固体口服制剂车间设计方案

方案是关于12种剂型口服制剂的车间设计。根据要求设计并确定工艺流程,根据实际生产药品计算得到的物料衡算、热量衡算和主要设备选型结果,对固体口服制剂车间进行设计和布局。车间整体设计为"L"型,厂房设计为单层厂房,设计符合GMP等标准要求。用于原辅料粉碎、制粒、干燥、塑形、检验和内包等区域严格按照D级洁净区的标准进行设计。洁净生产区与辅助区用过道隔开,洁净生产区布置满足"一头三尾"的生产理论。     

没有苦味的橙油和凉味剂

橙油都是带有苦辣味的 ,但做成香精无论是油质、水质或粉末香精 ,因其在各种食品中所使用的剂量较小 ,其香精中的苦味并不影响食品发生苦味。所以食品调香师都是使用带有苦味的各种品种的橙油及橘油来进行橙油香精的调配。近年来在湖南流行嚼槟榔的习惯 ,每年消耗槟榔量很大 ,香精的需要量也不小。在制作过程中其香精的用量约在百分之三左右 ,有的甚至用量超过百分之十以上。用有苦味的橙油或橘油所配的橙子香精或橘子香精 ,其中的苦味会影响槟榔也带有苦味。因此 ,生产槟榔的厂家要求不带苦味的橘子及橙子香精。这种苦味主要来于橙油及橘油…     

LM-1耐溶剂型美纹纸保护压敏胶带的研制和开发

天然橡胶在开炼过程中由于热氧作用,分子链上会产生羟基。在配好的胶粘剂溶液中,加入RC,通过多异氰酸酯和天然橡胶的羟基以及增粘树脂的羧基进行交联,使胶粘剂的内聚能提高,耐溶剂性增强。交联过程能在胶粘剂的烘干过程中完成,因此烘干工艺和普通美纹胶粘带相同。LM-1胶带能用于分色要求较高的场合,分型清晰,对被粘物无残胶,同时胶粘带的耐温性也有所提高。     

Taste 2 Receptor Is Involved in Differentiation of 3T3-L1 Preadipocytes

Expression of taste 2 receptor (T2R) genes, also known as bitter taste receptor genes, has been reported in a variety of tissues. The white adipose tissue of mice has been shown to express Tas2r108, Tas2r126, Tas2r135, Tas2r137, and Tas2r143, but the function of T2Rs in adipocytes remains unclear. Here, we show that fasting and stimulation by bitter compounds both increased Tas2r expression in mouse white adipose tissue, and serum starvation and stimulation by bitter compounds both increased the expression of Tas2r genes in 3T3-L1 adipocytes, suggesting that T2Rs have functional roles in adipocytes. RNA sequencing analysis of 3T3-L1 adipocytes stimulated by epicatechin, the ligand of Tas2r126, suggested that this receptor may play a role in the differentiation of adipocytes. Overexpression of Tas2r126 in 3T3-L1 preadipocytes decreases fat accumulation after induction of differentiation and reduces the expression of adipogenic genes. Together, these results indicate that Tas2r126 may be involved in adipocyte differentiation.     

手性药物的研究进展

讨论了手性药物的不对称合成及拆分的发展状况,介绍了不对称合成及拆分的几种具体方法,其中包括:环氧化反应;还原反应;不对称相转移催化反应;杂原子化合物的不对称开环反应等。     

无菌药品生产车间灭菌系统设计探讨

灭菌是无菌药品生产的关键环节,根据《药品生产质量管理规范》(2010年修订)的要求,结合本人的设计实例,对无菌药品生产车间灭菌系统的设计做简单的探讨和归纳。阐述了干热灭菌、湿热灭菌、过滤除菌三种方法的工作原理及影响灭菌效果的主要因素,并对灭菌设备的选用情况作简要说明。     

WTO环境下的中国制药业

中国加入WTO后，制药业将面临前所未有的机遇与挑战，如何加强企业市场控制力，适应WTO游戏规则，提高技术开发实力，是我国制药企业所面临的一个重要课题。     

Recent Advances in Lipase-Mediated Preparation of Pharmaceuticals and Their Intermediates

Biocatalysis offers an alternative approach to conventional chemical processes for the production of single-isomer chiral drugs. Lipases are one of the most used enzymes in the synthesis of enantiomerically pure intermediates. The use of this type of enzyme is mainly due to the characteristics of their regio-, chemo- and enantioselectivity in the resolution process of racemates, without the use of cofactors. Moreover, this class of enzymes has generally excellent stability in the presence of organic solvents, facilitating the solubility of the organic substrate to be modified. Further improvements and new applications have been achieved in the syntheses of biologically active compounds catalyzed by lipases. This review critically reports and discusses examples from recent literature (2007 to mid-2015), concerning the synthesis of enantiomerically pure active pharmaceutical ingredients (APIs) and their intermediates in which the key step involves the action of a lipase.     

我国原料药企业发展策略探讨

我国原料药企业在国际上已经具有一定优势和市场占有率 ,但还必须直面技术、贸易壁垒带来的阻力 ,通过积极技术创新、规范认证、管理科学来增强自身在规范性市场的竞争优势 ,实现可持续发展。     

Association between Downstream Taste Signaling Genes,Oral Microbiome,and Severe Early Childhood Caries

Polymorphisms in taste receptor genes have been shown to play a role in early childhood caries (ECC), a multifactorial, biofilm-mediated disease. This study aimed to evaluate associations between severe-ECC (S-ECC), the oral microbiome, and variants in genes that encode components of the G protein-coupled receptor (GPCR) signaling cascade involved in taste sensation. A total of 176 children (88 caries-free; 88 with S-ECC) were recruited. Analyses of 16S and ITS1 rRNA microbial genes and seven (GNAQ, GNAS, GNAT3, GNAI2, RAC1, RALB, and PLCB2) human genes were pursued using next-generation sequencing. Regression analyses were performed to evaluate associations between genetic variants, S-ECC, and the supragingival plaque microbiome. Results suggest that PLCB2 rs2305645 (T), rs1869901 (G), and rs2305649 (G) alleles had a protective effect on S-ECC (rs2305645, odds ratio (OR) = 0.27 (95% confidence interval (CI): 0.14–0.51); rs1869901, OR = 0.34 (95% CI: 0.20–0.58); and rs2305649, OR = 0.43 (95% CI: 0.26–0.71)). Variants in GNAQ, GNAS, GNAT3, PLCB2, RALB, and RAC1 were associated with oral fungal and bacterial community composition. This study revealed that three loci at PLCB2 are significantly associated with S-ECC. Variants in multiple genes were associated with the composition of dental biofilm. These findings contribute to the current knowledge about the role of genetics in S-ECC.     

TAS2R38 Bitter Taste Receptor Expression in Chronic Rhinosinusitis with Nasal Polyps: New Data on Polypoid Tissue

Studies have shown differences in TAS2R38 receptor expression in patients with chronic rhinosinusitis (CRS) compared to healthy controls. Known agonists of TAS2R38 stimulate epithelial cells, leading to robust intracellular nitric oxide (NO) production, which damages bacterial membranes, enzymes, and DNA, but also increases ciliary beat frequency. In this study we examined, using qRT-PCR, the expression of TAS2R38 receptor in nasal polyps (NP) of patients with CRS (N = 107) and in inferior turbinate mucosa (ITM) of patients with CRS and controls (N = 39), and confronted it with clinical features and the severity of the disease. The expression was shown in 43 (50.00%) samples of ITM in the study group (N = 107), in 28 (71.79%) in the control group (N = 39) (p = 0.037), and in 43 (46.24%) of NP. There were no differences in levels of the expression in all analyzed tissues. Patients who rated their symptoms at 0–3 showed higher TAS2R38 expression in ITM in comparison to the patients with 8–10 points on the VAS scale (p = 0.020). A noticeable, however not significant, correlation between the TAS2R38 expression in ITM and the Lund–Mackay CT score was shown (p = 0.068; R = −0.28). Patients with coexisting asthma had significantly higher receptor expression in the NP (p = 0.012). Our study is the first to confirm the presence of the TAS2R38 receptor in NP. Expression of the TAS2R38 receptor is reduced in the sinonasal mucosa in patients with more advanced CRS with NP.