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Charge-assisted bond N+H mediates the gelation of amorphous lurasidone hydrochloride during dissolution

Publication date: 25 February 2017 Source:International Journal of Pharmaceutics, Volume 518, Issues 1–2 Author(s): Shuai Qian, Shanshan Wang, Zhen Li, Xiaojie Wang, Di Ma, Shujun Liang, Yuan Gao, Jianjun Zhang, Yuanfeng Wei Lurasidone hydrochloride (LH), the hydrochloride form of lurasidone with a charge-assisted bond N+ H, is an atypical antipsychotropic agent for the treatment of schizophrenia. As a BCS class II drug, LH has a low oral bioavailability mainly due to its poor water solubility and low dissolution. In order to improve its solubility, amorphization of LH was performed and characterized. Unexpectedly, the dissolution rate of amorphous LH was much lower than that of crystalline LH. In addition, the amorphous LH powders quickly aggregated when contacting the dissolution media (water, 37°C), and formed a sticky gel adhering on the paddle. The follow-up polarized light microscope, XRPD, DSC, and FTIR analysis found that amorphous LH transformed to crystalline LH during dissolution. On the other hand, no such gelation phenomenon of amorphous lurasidone was observed under the same dissolution condition. However, the gel would reform when dropping concentrated hydrochloric acid slowly into the bottom of the medium during the dissolution of amorphous lurasidone, and XRPD/DSC/FTIR results indicated that the regenerated gel was consisted of crystalline LH, suggesting that the charge-assisted bond N+ H in the structure of LH mediated the gel formation of amorpho...
Source: International Journal of Pharmaceutics - Category: Drugs & Pharmacology Source Type: research

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Publication date: 5 December 2017 Source:Cell Reports, Volume 21, Issue 10 Author(s): Aditi Deshpande, Smita Yadav, Dang Q. Dao, Zhi-Yong Wu, Kenton C. Hokanson, Michelle K. Cahill, Arun P. Wiita, Yuh-Nung Jan, Erik M. Ullian, Lauren A. Weiss A deletion or duplication in the 16p11.2 region is associated with neurodevelopmental disorders, including autism spectrum disorder and schizophrenia. In addition to clinical characteristics, carriers of the 16p11.2 copy-number variant (CNV) manifest opposing neuroanatomical phenotypes—e.g., macrocephaly in deletion carriers (16pdel) and microcephaly in duplication carrier...
Source: Cell Reports - Category: Cytology Source Type: research
Publication date: 5 December 2017 Source:Cell Reports, Volume 21, Issue 10 Author(s): Sung Jin Park, Su Been Lee, Yeongjun Suh, Su-Jeong Kim, Namgyu Lee, Ji-Ho Hong, Cana Park, Youngsik Woo, Koko Ishizuka, Joung-Hun Kim, Per-Olof Berggren, Akira Sawa, Sang Ki Park A wide range of Ca2+-mediated functions are enabled by the dynamic properties of Ca2+, all of which are dependent on the endoplasmic reticulum (ER) and mitochondria. Disrupted-in-schizophrenia 1 (DISC1) is a scaffold protein that is involved in the function of intracellular organelles and is linked to cognitive and emotional deficits. Here, we demonstrate t...
Source: Cell Reports - Category: Cytology Source Type: research
Correction to: Asif et al., Genderwise clinical response of antipsychotics among schizophrenic patients: a prospective observational study from Lahore, Pakistan. Int J Psychiatry Clin Pract. 2017 Dec 13;:1 Authors: PMID: 29237345 [PubMed - as supplied by publisher]
Source: International Journal of Psychiatry in Clinical Practice - Category: Psychiatry Tags: Int J Psychiatry Clin Pract Source Type: research
Abstract Genes involved in synaptic plasticity, particularly genes encoding postsynaptic density proteins, have been recurrently linked to psychiatric disorders including schizophrenia and autism. Postsynaptic density Homer1 proteins contribute to synaptic plasticity through the competing actions of short and long isoforms. The activity-induced expression of short Homer1 isoforms, Homer1a and Ania-3, is thought to be related to processes of learning and memory. However, the precise regulation of Homer1a and Ania-3 with different components of learning has not been investigated. Here, we used in situ hybridization ...
Source: Neural Plasticity - Category: Neurology Authors: Tags: Neural Plast Source Type: research
Authors: Macagnino S, Steinert T, Uhlmann C Abstract Objective Examination of in-hospital suicide risk levels concerning their validity and their reliability. Method The internal suicide risk levels were evaluated in a cross sectional study of in 163 inpatients. A reliability check was performed via determining interrater-reliability of senior physician, therapist and the responsible nurse. Within the scope of the validity check, we conducted analyses of criterion validity and construct validity. Results For the total sample an "acceptable" to "good" interrater-reliability (Kendalls W = .77)...
Source: Psychiatrische Praxis - Category: Psychiatry Tags: Psychiatr Prax Source Type: research
On November 12, 2017, NIMH hosted a mini-symposium to introduce new and burgeoning field of computational psychiatry. Computational psychiatry applies cutting-edge quantitative methods and theoretical models to investigate neural or cognitive phenomena relevant to psychiatric diseases. Presentations covered practical examples of theory- and data-driven computational models of cognitive deficits associated with schizophrenia, emotion regulation, anxiety, and drug addiction.
Source: National Institute of Mental Health - Category: Psychiatry Authors: Source Type: news
CONCLUSION: The N1 dynamic range may be a marker of altered E/I balance. Reduced N1 dynamic range in individuals with schizophrenia may indicate that the auditory cortex is in an excitation-deficient or inhibition-dominant state. This may be the result of an incomplete compensation for a primary deficit in excitatory drive. PMID: 29236648 [PubMed - as supplied by publisher]
Source: Journal of Psychiatry and Neuroscience - Category: Psychiatry Tags: J Psychiatry Neurosci Source Type: research
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Source: European Journal of Neuroscience - Category: Neuroscience Authors: Tags: Special Issue Review Source Type: research
Studies on the nature and extent of prospective memory impairment in patients with obsessive-compulsive disorder are relatively scarce. The present study examined prospective memory in patients with obsessive-compulsive disorder in comparison to patients with schizophrenia and healthy controls. Prospective memory was assessed using Memory for Intentions Screening Test (MIST). Further, the participants were administered Delis-Kaplan Executive Function System Tower Test, Wisconsin Card Sorting Test, and Stroop Test for assessing their planning ability, mental flexibility and cognitive inhibition, respectively.
Source: Psychiatry Research - Category: Psychiatry Authors: Source Type: research
Publication date: 1 April 2018 Source:NeuroImage, Volume 169 Author(s): Caroline Lustenberger, Yogi A. Patel, Sankaraleengam Alagapan, Jessica M. Page, Betsy Price, Michael R. Boyle, Flavio Fröhlich Auditory rhythmic sensory stimulation modulates brain oscillations by increasing phase-locking to the temporal structure of the stimuli and by increasing the power of specific frequency bands, resulting in Auditory Steady State Responses (ASSR). The ASSR is altered in different diseases of the central nervous system such as schizophrenia. However, in order to use the ASSR as biological markers for disease states, it needs...
Source: NeuroImage - Category: Neuroscience Source Type: research
More News: Drugs & Pharmacology | Schizophrenia