Structural description of the marketed form of valsartan: A crystalline mesophase characterized by nanocrystals and conformational disorder
Publication date: 30 June 2017 Source:International Journal of Pharmaceutics, Volume 526, Issues 1–2 Author(s): Yannick Guinet, Laurent Paccou, Florence Danède, Patrick Derollez, Alain Hédoux Valsartan is an antihypertensive drug, recognized to be marketed in an amorphous state, different from that obtained by quenching the liquid state below T g. This is an unusual and very original situation, given that the amorphous state is unstable. Low-wavenumber Raman spectroscopy and X-ray diffraction investigations were carried out on the various solid-state forms of valsartan. It was found that the marketed form is not amorphous and can be described in terms of mesophase in which the long-range order of the stable crystal is limited on the lengthscale of tens nanometers, inducing a melting temperature lower than that of the stable crystalline state, inherent to the crystallite size. This unusual physical state of a marketed drug was correlated to the relative population of cis–trans conformers, preventing the development of the hydrogen-bond network distinctive of the long-range order in the crystalline state. Graphical abstract
Authors: Egeland K, Hugo TG, Løvold M, Nystuen G Abstract The Treaty on the Prohibition of Nuclear Weapons (TPNW), adopted by the United Nations General Assembly in July 2017, has been met with mixed reactions. While supporters have described the Treaty as a watershed in the struggle for disarmament, others have expressed fervent opposition. One of the most serious charges levelled at the TPNW is that it will undermine the long-standing nuclear Non-Proliferation Treaty (NPT), by many regarded as a cornerstone of the international security architecture. Critics have contended that the new agreement risks erod...
PMID: 29911911 [PubMed - in process]
Authors: Qiu S, Pellino G, Warren OJ, Mills S, Goldin R, Kontovounisios C, Tekkis PP Abstract Mixed adenoneuroendocrine carcinoma (MANEC) are rare cancers of the gastrointestinal (GI) and pancreatobiliary tract. They are characterized by the presence of a combination of epithelial and neuroendocrine elements, where each component represents at least 30% of the tumour. Review of literature and consolidation of clinicopathological data. Sixty-one cases of colorectal MANEC have been reported in literature and one seen in this centre. The median age of the patients affected was 61.9 ± 12.4 years (2...
CONCLUSIONS: We show in this feasibility study for the first time an increase of copeptin in combination with glucocorticoids as stress biomarkers by open surgery compared to minimally invasive procedures in patients undergoing colorectal surgery. Exceeding an individual threshold of 'stress burden' may have unfavorable effects on the long-time clinical outcome. PMID: 29911494 [PubMed - as supplied by publisher]
CONCLUSIONS: β-Eudesmol may serve as a potential anti-CCA candidate particularly when used in combination with conventional chemotherapeutics. The mechanisms involved may be mediated via NQO1 suppression-related apoptosis pathway. PMID: 29914576 [PubMed - in process]
CONCLUSIONS: This current analysis showed no significant difference in stent thrombosis with the addition of cilostazol to the standard dual antiplatelet therapy during any follow-up time period after PCI. PMID: 29914573 [PubMed - in process]
CONCLUSIONS: Given that over-use of opioids is a major public health problem and that long-term use has substantial side effects including dependence, it is important to understand spatial patterns of opioid prescribing to enable targeted interventions. Nationwide implementation of real-time drug-monitoring programs and access to monitoring databases from both doctor and pharmacy point-of-care sources may potentially reduce excessive and undue use of opioid. PMID: 29914572 [PubMed - in process]
In conclusion, we suggest that, castrate-resistant prostate cancers progression might be retarded with the combination of MYC and chemical JNK inhibitors, involving AR-dependent mechanism.
Conclusion: Factors including a larger tumor size (diameter> 5cm), lymphovascular invasion, lymph node metastasis, synchronous metastasis and positive margin may increase the risk of recurrences of resected pancreatic SPTs. All SPTs should be excised and patients with high-risk features should undergo a long-term follow-up.
Oral cavity cancer is a type of head and neck squamous cell carcinoma (HNSCC) and contributes to significant morbidity and mortality each year. An epigenetic pathway of transcriptional inactivation for many genes has been described in various cancers, including HNSCC. For our study, we selected genes for which silencing caused by hypermethylation can promote cancer development. In 75 primary HNSCC tumours and paired surgical margins, we investigated the methylation status of the p16, APC, MGMT, TIMP3 and CDH1 gene promoters by methylation-specific PCR after bisulphite treatment. The promoter methylation rates of p16, APC, ...