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Oral suspensions

Fugen Gu, Weina Ma, Gendalai Meng, Chunzhi Wu, Yi Wang
The aim of this study was to prepare a nasal gel of risperidone and to investigate the pharmacokinetics and relative bioavailability of the drug in rats. Compared with oral dosing, the risperidone nasal gel exhibited very fast absorption and high bioavailability. Maximal plasma concentration (cmax) and the time to reach cmax (tmax) were 15.2 μg mL-1 and 5 min for the nasal gel, 3.6 μg mL-1 and 30 min for the oral drug suspension, respectively. Pharmacokinetic parameters such as tmax', cmax and AUC of oral and nasal routes were significantly different (p < 0...
December 1, 2016: Acta Pharmaceutica
Kuo Zhang, Jingyu Yang, Fang Wang, Xing Pan, Jian Liu, Lijuan Wang, Guanyue Su, Jie Ma, Yinxu Dong, Zhili Xiong, Chufu Wu
ETHNOPHARMACOLOGICAL RELEVANCE: Hyperactivity of hypothalamic-pituitary-adrenal (HPA) axis is often observed in the pathophysiology of depression. Antidepressant therapy can restore hippocampal neurogenesis to rescue the HPA axis regulation defects. Xiaochaihutang (XCHT), a famous Chinese herbal formula, has been used clinically in depressive disorders in China. Our previous studies have demonstrated XCHT improved depressive-like behaviors in chronic unpredictable mild stress rat, but the underlying mechanisms of XCHT on hippocampal neurogenesis and the HPA axis were still unclear...
October 13, 2016: Journal of Ethnopharmacology
Vivian B Neis, Luis E B Bettio, Morgana Moretti, Priscila B Rosa, Camille M Ribeiro, Andiara E Freitas, Filipe M Gonçalves, Rodrigo B Leal, Ana Lúcia S Rodrigues
Agmatine is an endogenous neuromodulator that has been shown to have antidepressant-like properties. We have previously demonstrated that it can induce a rapid increase in BDNF levels after acute administration, suggesting that agmatine may be a fast-acting antidepressant. To investigate this hypothesis, the present study evaluated the effects of a single administration of agmatine in mice subjected to chronic unpredictable stress (CUS), a model of depression responsive only to chronic treatment with conventional antidepressants...
October 12, 2016: Pharmacology, Biochemistry, and Behavior
Maria Eliza Freitas, Marta Ruiz-Lopez, Susan H Fox
Levodopa remains the most effective treatment for Parkinson's disease and is considered the gold standard therapy. However, disease progression and changes in the gastrointestinal tract result in a declining window of treatment response in a majority of patients. Efforts have been made recently to improve levodopa bioavailability either by developing more effective oral formulations or by innovating routes of administration (intestinal infusion, transcutaneous or inhaled levodopa). IPX066 is a novel levodopa-carbidopa (LD/CD) oral formulation combining immediate-release (IR) and extended-release (ER) LD/CD recently approved in the USA and the EU...
October 14, 2016: CNS Drugs
Tongkai Chen, Chuwen Li, Ye Li, Yi Xiang, Simon Ming Yuen Lee, Ying Zheng
Schisantherin A (SA) is a promising anti-Parkinsonism Chinese herbal medicine but with poor water solubility and challenges to be delivered to the brain. We formulated SA as nanocrystals (SA-NC), aiming to improve its solubility, pharmacokinetic profile and thus provide a potential therapeutic agent for the treatment of Parkinson's disease (PD). The rod-shaped SA-NC had a particle size of ~160 nm with 33.3% drug loading, and the nanocrystals exhibited a fast dissolution rate in vitro. The intact drug nanocrystals could be internalized into Madin-Darby canine kidney (MDCK) cells, which were followed by rapid intracellular release, and most of the drug was transported to the basolateral side in its soluble form...
October 14, 2016: Molecular Pharmaceutics
Alexandros Kourentas, Maria Vertzoni, Mira Symillides, Bart Hens, Joachim Brouwers, Patrick Augustijns, Christos Reppas
Biorelevant Gastrointestinal Transfer system (BioGIT) has been shown to be useful in reproducing concentrations of drugs in the fasted upper small intestine after their administration in the stomach. In the present investigation, we evaluated the impact of gastrointestinal transfer on luminal performance of commercially available products of two highly lipophilic weak bases, posaconazole (Noxafil(®) suspension) and itraconazole (Sporanox(®) hard gelatin capsules and Sporanox(®) oral solution) by comparing % solid fraction, concentrations and supersaturation in the duodenal compartment of BioGIT with recently reported data in the upper small intestine of healthy adults...
October 9, 2016: International Journal of Pharmaceutics
Mihaela Friciu, Sarra Zaraa, V Gaëlle Roullin, Grégoire Leclair
The objective of this study was to evaluate the stability of diazoxide in extemporaneously compounded oral suspensions. Oral suspensions of diazoxide 10 mg/mL were prepared from either bulk drug or capsules dispersed in either Oral Mix or Oral Mix Sugar Free. These suspensions were stored at 5°C and 25°C/60%RH in bottles and oral syringes for a total of 90 days. At predetermined time intervals, suspensions were inspected for homogeneity, color or odor change; the pH was measured and the concentration of diazoxide was evaluated by ultraviolet detection using a stability-indicating high pressure liquid chromatography method...
2016: PloS One
Wei Li, Wenxi He, Ping Gao, Chengliang Zhang, Hongjiao Cai, Ying Chen, Dong Liu
The aim of this study was to develop and to investigate a film of compound Calculus Bovis Sativus (CBS) and ornidazole film. A uniform mucoadhesive film was herein successfully obtained by a film-forming solusion containing insoluable drug. This film, as a valid adjunct for the treatment of oral mucosal ulcer, consisted of two main drugs (CBS, ornidazole) and three polymers (hydroxypropyl methyl cellulose, chitosan, poly(vinyl alcohol) (PVA)). The film was prepared with the film-forming suspension, using casting-solvent evaporation technique...
2016: Biological & Pharmaceutical Bulletin
Germain Sotoing Taiwe, Thierry Bang Tchoya, Joseph Renaud Menanga, Bernard Dabole, Michel De Waard
ETHNOPHARMACOLOGICAL RELEVANCE: The leaf extract of Crinum jagus L. (Amaryllidaceae) is widely used in traditional Cameroonian medicine as antiepileptic remedy and for the treatment of convulsion, depression and mood disorders associated with epilepsy. AIM OF THE STUDY: Hence, this study was conducted to evaluate the effects of an active fraction extracted from the leaves of Crinum jagus against seizures, depression-like behaviour and oxidative stress in pentylenetetrazole (PTZ)-induced kindling in mice...
October 7, 2016: Journal of Ethnopharmacology
Gayaprasad Upadhyay, Sarvesh Khoshla, Ramoji Kosuru, Sanjay Singh
OBJECTIVE: The current study was designed to explore anxiolytic, antidepressant, and antistress actions of Cinnamomum tamala (CT) leaves (aqueous extract) in rats. MATERIALS AND METHODS: Behavioral procedures of anxiety, depression, and stress were assessed in rats. CT (100, 200, and 400 mg/kg) was given once a daily for 7 days via oral route and the efficacy was matched by those elicited by lorazepam (1 mg/kg, p.o.), imipramine (10 mg/kg, p.o.), and Withania somnifera (100 mg/kg, p...
September 2016: Indian Journal of Pharmacology
Acheenta Gohain Barua, Himangshu Raj, Pranab Konch, P Hussain, Chandana C Barua
OBJECTIVES: The present study was carried out to investigate the in vivo antimycobacterial activity of methanol extract of Alstonia scholaris and Mucuna imbricata in murine model. MATERIALS AND METHODS: Female BALB/c mice were infected with the Mycobacterium tuberculosis H37Rv suspension. Extracts were administered orally for 2 weeks from 7(th) day postinfection at a dose of 200 mg/kg and rifampicin at 20 mg/kg as standard. The synergistic groups were 10 and 100 mg/kg for rifampicin and extract, respectively...
September 2016: Indian Journal of Pharmacology
Ankit Dhaundiyal, Sunil K Jena, Sanjaya K Samal, Bhavin Sonvane, Mahesh Chand, Abhay T Sangamwar
OBJECTIVES: This study was designed to demonstrate the potential of novel α-lipoic acid-stearylamine (ALA-SA) conjugate-based solid lipid nanoparticles in modulating the pharmacokinetics and hepatotoxicity of tamoxifen (TMX). METHODS: α-lipoic acid-stearylamine bioconjugate was synthesized via carbodiimide chemistry and used as a lipid moiety for the generation of TMX-loaded solid lipid nanoparticles (TMX-SLNs). TMX-SLNs were prepared by solvent emulsification-diffusion method and optimized for maximum drug loading using rotatable central composite design...
October 5, 2016: Journal of Pharmacy and Pharmacology
Shafeeque Ahmad, Khursheed Alam, M Mobarak Hossain, Mahino Fatima, Fakiha Firdaus, Mohammad Faraz Zafeer, Zarina Arif, Murad Ahmed, K A Nafees
Atherosclerosis has been linked to chronic inflammatory processes. Changes in the levels of lipoproteins, especially low-density lipoprotein or its variants, as well as inflammatory markers are risk factors for the atherosclerosis. In the present study, an experimental model of rheumatoid arthritis was developed by administrating collagen suspension intradermally in the tail region of Wistar albino rats. At the same time, a suspension of hesperidin (50 mg/kg body weight) and daidzein (20 mg/kg body weight) was orally administrated...
October 4, 2016: Molecular and Cellular Biochemistry
Michaela Döring, Karin Melanie Cabanillas Stanchi, Hartwig Klinker, Melinda Eikemeier, Judith Feucht, Franziska Blaeschke, Carl-Philipp Schwarze, Martin Ebinger, Tobias Feuchtinger, Rupert Handgretinger, Werner J Heinz
Invasive fungal infections are one of the major complications in pediatric patients during prolonged neutropenia after chemotherapy. Evaluation of the efficacy and safety of the triazole posaconazole in these patients is missing. This multicenter survey analyzed trough concentrations of 33 pediatric patients with a median age of 8 years during 108 neutropenic episodes who received prophylactic posaconazole oral suspension. A total of 172 posaconazole trough levels were determined to median 438 ng/ml (range 111-2011 ng/ml; mean 468 ± 244 ng/ml)...
October 4, 2016: Medical Mycology: Official Publication of the International Society for Human and Animal Mycology
Jagruti Desai, Hetal Thakkar
The present investigation aimed to study the effect of particle size of solid lipid nanoparticles (SLNs) on oral bioavailability of Darunavir. High pressure homogenization technique was used to prepare SLNs. Three different sized SLNs loaded with Darunavir were developed with mean particle sizes of around 100 nm, 200 nm and 500 nm respectively. The in-vivo pharmacokinetics in rats showed a significant increase in oral bioavailability of Darunavir from all the three formulations in comparison to plain drug suspension and reference tablet...
October 5, 2016: Journal of Microencapsulation
Kiran Jyoti, Richa Kaur Bhatia, Elvis A F Martis, Evans C Coutinho, Upendra Kumar Jain, Ramesh Chandra, Jitender Madan
In present investigation, initially curcumin was complexed with 2-HP-β-CD (curcumin-2-HP-β-CD-complex) in 1:1 ratio and later amalgamated with chitosan microspheres (curcumin-2-HP-β-CD-CMs) for selective delivery in colon only through oral route of administration. Various analytical, spectral and in-silico docking techniques revealed that the curcumin was deeply inserted in the 2-HP-β-CD cavity with apparent stability constant of 3.35×10(-3)M. Furthermore, the mean particle size of 6.8±2.6μm and +39...
September 28, 2016: Colloids and Surfaces. B, Biointerfaces
Aditya J Reddy, Shailendra S Handu, Ashok Kumar Dubey, Pramod Kumari Mediratta, Rimi Shukla, Qazi Mushtaq Ahmed
BACKGROUND: Musa sapientum, the banana plant, has shown to possess antioxidant activity in previous studies. Oxidative stress has been linked to the pathogenesis of major depressive disorder (MDD) with evidence of increased serum levels of oxidative stress biomarkers in MDD patients. OBJECTIVE: The present study aimed to evaluate the antidepressant activity of M. sapientum stem extract (MSSE) in experimental models in mice. MATERIALS AND METHODS: Forced swim test (FST) and tail suspension test (TST) were carried out in five different groups (n = 6/group) of mice...
October 2016: Pharmacognosy Research
Heiko Vogel, Henrike Schmidtberg, Andreas Vilcinskas
The spread of the invasive harlequin ladybird (Harmonia axyridis) in Europe is accompanied by the decline of the native and non-invasive two-spotted ladybird (Adalia bipunctata). Here we show that microsporidia carried by H. axyridis can kill A. bipunctata following the oral uptake of spores, suggesting that their horizontal transmission via intraguild predation may help the invader to outcompete its native competitor. The native seven-spotted ladybird (Coccinella septempunctata) is thought to be less susceptible both to the spread of H...
September 28, 2016: Developmental and Comparative Immunology
T Westers, A Jones-Bitton, P Menzies, J Van Leeuwen, Z Poljak, A S Peregrine
In Ontario, Canada, widespread resistance to ivermectin and fenbendazole, the only readily available ovine anthelmintics, has been documented, primarily in Haemonchus sp. In other parts of the world, closantel has been used to control such infections; however, the drug was not currently licensed for use in Canada and the USA. A randomized controlled trial was conducted on six client-owned farms in Ontario in 2013 and 2014 to determine the efficacy of closantel (Flukiver(®) 5% Oral Suspension, Elanco Animal Health, 10mg/kg bodyweight) against ivermectin- and fenbendazole-resistant Haemonchus sp...
September 15, 2016: Veterinary Parasitology
Donald Newgreen, Brigitte Bosman, Adriana Hollestein-Havelaar, Ellen Dahler, Robin Besuyen, Will Sawyer, Stéphane Bolduc, Søren Rittig
BACKGROUND: Solifenacin, an effective, well-tolerated treatment for adult overactive bladder (OAB) symptoms, has not been evaluated in placebo-controlled paediatric clinical trials. OBJECTIVES: To evaluate the efficacy and safety of once-daily oral solifenacin suspension in OAB patients aged 5-<12 yr (children) and 12-<18 yr (adolescents). DESIGN, SETTING, AND PARTICIPANTS: The study involved a 4-wk urotherapy run-in followed by 1:1 randomisation to 12-wk double-blind solifenacin or placebo treatment alongside urotherapy...
September 26, 2016: European Urology
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