This work reports a new biocompatible surfactant structure, of which the hydrophilic head group is composed of a folded, stable self-inclusion complex of a ferrocenyl substituted beta-cyclodextrin (betaCD). While multiple intra- or intermolecular complexes can exist for this amphiphile, the molecule folds into a unique intramolecular complex with well-defined conformation, in which part of the aliphatic chain and the ferrocene group are both included in the annular cavity of betaCD. Study of different isosteric covalent linkages indicates that this folded structure is stable against displacement by the presence of other small guest molecules. Furthermore, in contrast to ferrocene-CD conjugates that are without the aliphatic chain, the presence of small guest molecules in solution does not influence at all the induced circular dichroism signal of this amphiphile, indicating a sterically congested, but stable, folded conformation of the inclusion complex. This new amphiphile is surface active and, more importantly, does not denature the membrane protein bacteriorhodopsin. Finally, because this surfactant forms self-assembled aggregates, this work introduces a folded structure into soft matters formed by amphiphiles in water.

No abstract

Background and objective:Colonoscopy is the most important method for the diagnosis and treatment of intestinal diseases, and there are many factors affecting the quality of examination. Although the assistant is one of the factors influencing the quality of colonoscopy, there are few studies on the effect of different assistants with different experiences on the quality of colonoscopy. Therefore, the study was aimed to research the correlation between different assistants with different experiences and the quality of water-injection colonoscopy.Method:In this study, a single-center randomized controlled trial was conducted to analyze the key quality indicators (the rate to arrive cecum, time to arrive cecum, total operation time, detection rate of polyps, detection rate of adenoma, pain score, operation satisfaction, and the pressure on abdomen) of patients who underwent water-injection colonoscopy under non-sedation from January 2018 to June 2018 in the center. Patients were randomly assigned to different assistant groups based on the actual working period of 6 months (0∼6 months inexperienced assistant group and assistant group with more than 6 months of experience). Through fitting the bivariate and multivariate logistic regression models, the differences between the two groups and the effects on the key quality indicators of colon examination were analyzed.Results:A total of 331 patients who were eligible for non-sedation colonoscopy were randomly assigned to the experienced assistant group (n = 179) and the inexperienced assistant group (n = 152). Among them, 103 cases of polyp and 70 cases of adenoma were detected. The rate to arrive cecum, polyp detection rate and adenoma detection rate were compared between the two groups during operation (P > 0.05). However, there were significant differences in the time to arrive cecum, patients’ satisfaction with operation, pain score and abdominal pressure (P < .05). In the inexperienced assistant group, 20% of the operation time was one standard deviation higher than the mean value, while the experienced assistant group was 12% (339 s vs 405s, OR 0.541, 95% 0.295–0.990). Compared with the inexperienced assistant group, patients in the experienced assistant group had higher operational satisfaction (98.32% vs 92.11%, OR 0.199, 95% 0.055–0.718) and lower pain score (0.3 vs 0.49, OR 1.993, 95% 1.52–3.775). All relations remained unchanged after adjusting for potential confounders.Conclusion:The assistant is a key factor in the quality of colonoscopy, especially in the case of non-sedating colonoscopy. The experience of the assistant is related to the time to arrive cecum, the degree of pain and the overall satisfaction of patient with the operation. The assistant should be subject to the quality supervision of the endoscopic inspector. Proof of human Clinical Trial Registration: The institutional review board of Fifth Affiliated Hospital of Wenzhou Medical College, Zhejiang Province, China approved the study. The study is registered on. Chinese Clinical Trial Re...

To date, few examples of dissolution models for real-time release testing (RTRT) have been approved for commercial drug products or published in literature. Thus, a structured approach has not been established by which a novice to the field could design, develop, validate, and implement an RTRT dissolution model. Moreover, with scant examples available, there has not been a body of work by which to learn of general regulatory expectations for such models.To address these gaps and to encourage conversation between regulatory and industrial experts on these topics, a virtual (web-based) workshop entitled "Predictive Dissolution Models for Real-Time Release Testing: Development and Implementation" was held November 11-12, 2021. This article summarizes key points from the podium presentations, panel discussions, and breakout sessions focusing on (1) the current best practices to establish predictive model specifications; (2) designing models to predict the "safe space" of a release test and creating models utilizing process analytical technology (PAT); and (3) exploring the strategy of compliant regulatory submissions, including model validation and post-approval lifecycle management. Industrial case studies were presented showcasing attempted approaches to and successful implementations of RTRT of dissolution for drug product manufacturing.

Aim. Fuyang Jiedu Huayu (FYJDHY) granules are a combination of five traditional Chinese medicines with known therapeutic effects against chronic liver failure (CLF). The aim of the present study was to investigate the efficacy of FYJDHY to ameliorate the effects of carbon tetrachloride- (CCl4-) induced CLF in rats and to explore the possible molecular mechanisms underlying its therapeutic efficacy. Methods. A model of chronic liver failure was established by intraperitoneal injection of 50% carbon tetrachloride into SD rats for 8 weeks. After establishing the model, rats were treated with either low-dose (4.725 kg/d), medium-dose (9.45 kg/d), or high-dose (18.9 g/kg/d) FYJDHY for 2 weeks. After treatment, samples of liver tissue and blood were harvested from rats in each group. Serum ALT, AST, and TBIL levels and prothrombin time were measured using a biochemical analyzer. The expression of Gab1 (Grb2-associated binder 1), TPO (thrombopoietin), and its receptor c-Mpl were measured using quantitative real-time PCR (RT-PCR) and Western blot analysis, and assessment of histological improvement in liver tissue was by H&E-stained tissue sections. Results. Compared with the model group, serum ALT, AST, and TBIL levels and PT of rats in the intervention group were significantly reduced ( P < 0.05 ). In addition, FYJDHY alleviated pathological damage to liver tissue and increased the expression of Gab1, TPO, and its receptor c-Mpl in liver tissue, to levels statistically significant compared with the model group ( P < 0.05 ). Conclusions. The therapeutic effect of FYJDHY on CLF may be related to the promotion of angiogenesis and improvement in hemopoietic function in individuals suffering from CLF.