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Drug Research

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https://www.readbyqxmd.com/read/29791923/inhaled-treprostinil-prodrug-lipid-nanoparticle-formulations-provide-long-acting-pulmonary-vasodilation
#1
Franziska G Leifer, Donna M Konicek, Kuan-Ju Chen, Adam J Plaunt, Dany Salvail, Charles E Laurent, Michel R Corboz, Zhili Li, Richard W Chapman, Walter R Perkins, Vladimir S Malinin
Treprostinil (TRE), a prostanoid analogue approved in the USA for the treatment of pulmonary arterial hypertension, requires continuous infusion or multiple dosing sessions per day for inhaled and oral routes of administration due to its short half-life. The inhaled drug is known to induce adverse systemic and local effects including headache, nausea, cough, and throat irritation which may be due at least in part to transiently high drug concentrations in the lungs and plasma immediately following administration [1]...
May 23, 2018: Drug Research
https://www.readbyqxmd.com/read/29791922/p2y12-polymorphisms-and-the-risk-of-adverse-clinical-events-in-patients-treated-with-clopidogrel-a-meta-analysis
#2
Kun Zhao, Ming Yang, Yanxia Lu, Shusen Sun, Wei Li, Xingang Li, Zhigang Zhao
BACKGROUND AND STUDY AIM: Some studies have reported an association between P2Y12 gene polymorphisms and clopidogrel adverse outcomes with inconsistent results. We aimed to explore the relationship between P2Y12 polymorphisms and the risk of adverse clinical events in patients treated with clopidogrel through a meta-analysis. METHODS: A systematic search of PubMed, Web of Science and the Cochrane Library was conducted. Retrieved articles were comprehensively reviewed and eligible studies were included, and the relevant data was extracted for this meta-analysis...
May 23, 2018: Drug Research
https://www.readbyqxmd.com/read/29791921/does-gastroplus-support-similarity-and-dissimilarity-factors-of-in-vitro-in-vivo-prediction-in-biowaiver-studies-a-lower-strength-amlodipine-as-a-model-drug
#3
Abdel Naser Zaid, Naser Shraim, Asmaa Radwan, Nidal Jaradat, Samah Hirzallah, Ibrahim Issa, Aya Khraim
BACKGROUND: Many generic pharmaceutical products are currently available on the market place worldwide. Recently, there is a growing concern on the quality and efficacy of generic products. However, health care professionals such as physicians and pharmacists are in difficult situations to choose among alternatives. PURPOSE: The aim of this study is to assess the effectiveness of the in silico technique (Gastro Plus® ) in the biowaiver study and whether similarity and dissimilarity factors ( f 2 and f 1 respectively) are effective in this regard...
May 23, 2018: Drug Research
https://www.readbyqxmd.com/read/29758567/synthesis-and-in-vitro-evaluation-of-2-heteroarylidene-1-tetralone-derivatives-as-monoamine-oxidase-inhibitors
#4
Klaudia T Amakali, Lesetja J Legoabe, Anél Petzer, Jacobus P Petzer
The present study investigates the human monoamine oxidase (MAO) inhibition properties of a series of twelve 2-heteroarylidene-1-tetralone derivatives. Also included are related cyclohexylmethylidene, cyclopentylmethylidene and benzylidene substituted 1-tetralones. These compounds are related to the 2-benzylidene-1-indanone class of compounds which has previously been shown to inhibit the MAOs, with specificity for the MAO-B isoform. The target compounds were synthesised by the Claisen-Schmidt condensation between 7-methoxy-1-tetralone or 1-tetralone, and various aldehydes, under acid (hydrochloric acid) or base (potassium hydroxide) catalysis...
May 14, 2018: Drug Research
https://www.readbyqxmd.com/read/29734452/hepatoprotective-potential-of-elsholtzia-densa-against-acute-and-chronic-models-of-liver-damage-in-wistar-rats
#5
Ovais Ahmad Zargar, Rohina Bashir, Showkat Ahmad Ganie, Akbar Masood, Mohammad Afzal Zargar, Rabia Hamid
The aim of the present study was to evaluate the hepatoprotective activity of methanolic extract of Elsholtzia densa against experimentally induced acute (CCl4 ) and chronic (paracetamol) liver injury in albino wistar rats. Activity was measured by monitoring the serum levels of ALT, ALP AST and LDH, total protein levels, bilirubin and albumin. The results of the CCl4 and paracetamol-induced liver toxicity experiments showed that the rats treated with the methanolic extract of Elsholtzia densa exhibited a significant decrease in biochemical parameters as well as the proteins, which were all elevated in the CCl4 and paracetamol group...
May 7, 2018: Drug Research
https://www.readbyqxmd.com/read/29719880/ethanol-extract-of-crataegus-oxyacantha-l-ameliorate-dietary-non-alcoholic-fatty-liver-disease-in-rat
#6
Golbahar Saeedi, Fereshteh Jeivad, Mohammadhadi Goharbari, Gholamreza Hassanzadeh Gheshlaghi, Omid Sabzevari
BACKGROUND: Non-alcoholic fatty liver (NAFLD) is one the most prevalent disease worldwide which characterized by fat accumulation in liver with no established efficient therapy. We designed this study to investigate protective and therapeutic effect of Crataegus oxyacantha L. (C. oxyacantha) on NAFLD induced by high fat diet in rat models. METHODS: NAFLD was induced by High Fat Diet+fructose (HFD), 45 Wistar rats were divided to 8 groups including control, HFD, HFD+diet change, HFD+diet change+C...
May 2, 2018: Drug Research
https://www.readbyqxmd.com/read/29684922/saliva-versus-plasma-therapeutic-drug-monitoring-of-pregabalin-in-jordanian-patients
#7
Nasir Idkaidek, Salim Hamadi, Manal El-Assi, Ahmad Al-Shalalfeh, Ahmad Al-Ghazawi
The objective is using saliva instead of plasma for pregabalin therapeutic drug monitoring (TDM) since saliva reflects the free non-protein bound drug concentration, simple and noninvasive sampling, cheaper and does not require the expertise of drawing blood. Forty four patients participated in this study, two samples of saliva and another two of blood were taken from each patient; first sample of both saliva and blood is the trough sample and was taken just before the first dose of the day and second sample is the peak sample and was taken 1 h after taking the first dose of the day...
April 23, 2018: Drug Research
https://www.readbyqxmd.com/read/29669380/quantification-and-brain-targeting-of-eugenol-loaded-surface-modified-nanoparticles-through-intranasal-route-in-the-treatment-of-cerebral-ischemia
#8
Niyaz Ahmad, Rizwan Ahmad, Md Aftab Alam, Farhan Jalees Ahmad
OBJECTIVE: To enhance brain bioavailability for intranasally administered Eugenol-encapsulated-chitosan-coated-PCL-Nanoparticles (CS-EUG-PCL-NPs). METHODS: Chitosan-coated-PCL-Nanoparticles (CS-PCL-NPs) were developed through double emulsification-solvent evaporation technique and further characterized for particle size, zeta potential, size distribution, encapsulation efficiency as well as in vitro drug release. UPLC-PDA method was developed to evaluate brain-drug uptake for optimized CS-EUG-PCL-NPs and to determine it's pharmacokinetic in rat's brain as well as plasma...
April 18, 2018: Drug Research
https://www.readbyqxmd.com/read/29665591/development-of-ph-dependent-nanospheres-for-nebulisation-in-vitro-diffusion-aerodynamic-and-cytotoxicity-studies
#9
Pradum P Ige, Sagar R Pardeshi, Raju O Sonawane
The aim of this work was to evaluate the in vitro performance of nebulized nanosuspension formulation when nebulized using ultrasonic nebulizer. The present investigation deals with successful formulation of Beclomethasone dipropionate loaded HPMCP nanospheres prepared by solvent evaporation technique using PEG 400 as a stabilizer. Beclomethasone dipropionate is a water insoluble drug molecule was encapsulated in HPMCP nanospheres to have pH dependent solubility at basic pH for targeted drug delivery in lung and studied for in vitro cytotoxicity and immediate release capability...
April 17, 2018: Drug Research
https://www.readbyqxmd.com/read/29660749/antimicrobial-peptidomimetics-for-recurrent-septicemia-infections-in-vitro-study-for-immuno-compromised-disease-target
#10
Priyanka Sharma, Kandasamy Nagarajan, Bihu Prasad Panda
The frequency of Bacillus subtilis infection such as pneumonia pan-opthalmitis, visceral abscess or musculoskeletal infection etc. complications following bacteremia, meningitis in children & the infection associated with majority of motor vehicle accidents associated with trauma & gun shoot injury. Antibiotics which appear especially useful in the treatment of Bacillus. infection are clindamycin and vancomycin to which vast majority of strains are susceptible in vitro. Our objective is to test the synthesized peptidomimetics with the efforts mainly directed towards the identification of antibacterial compounds against recurrent septicemia infection...
April 16, 2018: Drug Research
https://www.readbyqxmd.com/read/29660748/monodisperse-rattle-structured-gold-nanorod-mesoporous-silica-nanoparticles-core-shell-as-sulforaphane-carrier-and-its-sustained-release-property
#11
Hamidreza Kheiri Manjili, Leila Ma'mani, Hossein Naderi-Manesh
Sulforaphane (SF) was loaded into the multi-functioned rattle-structured gold nanorod mesoporous silica nanoparticles core-shell to improve its stability and efficacy through its efficient delivery to tumors. The rattle-structured gold nanorod mesoporous silica nanoparticles (rattle-structured AuNR@mSiO2 core-shell NPs) were obtained by covering the surface of Au NPs with Ag and mSiO2 shell and subsequently selective Ag shell etching strategy. Then the surface of rattle-structured AuNR@mSiO2 NPs was decorated with thiolated polyethylene glycol-FITC and thiolated polyethylene glycol-folic acid to the designed form...
April 16, 2018: Drug Research
https://www.readbyqxmd.com/read/29635674/anti-obesity-effect-of-arq-zeera-and-its-main-components-thymol-and-cuminaldehyde-in-high-fat-diet-induced-obese-rats
#12
Mohammad Rafiul Haque, H Shahid Ansari
Arq zeera is a distillate product that prepared from four different herbs namely Trachyspermum ammi L., apiaceae, Zingiber officinale Roxb., zingiberaceae, Carum carvi L.,apiaceae and Cuminum cyminum L., apiaceae. The present study aims to determine the antiobesity effect of arq zeera and its main components thymol and cuminaldehyde in high fat diet induced obese rats and to explore its mechanism of action. In current study, orlistat was used as positive controls. Male Wistar rats were fed with HFD for 42 days to induce obesity...
April 10, 2018: Drug Research
https://www.readbyqxmd.com/read/29635673/hplc-esi-ms-characterization-of-certain-polyphenolic-compounds-of-carica-papaya-l-fruit-extracts-and-evaluation-of-their-potential-against-murine-schistosomiasis-mansoni
#13
Ezzat El-Sayed Abdel-Lateef, Ibrahim Aly Rabia, Mortada Mohamed El-Sayed, El-Sayed Saleh Abdel-Hameed
The in vivo antischistosomal activities of Carica papaya L. extracts were evaluated and the characterization of the active secondary metabolites of the defatted methanolic extract was performed using HPLC-ESI-MS. The plant fruit powders were extracted with 85% methanol and fractionated using organic solvents. The in vivo antischistosomal effects of the methanolic extracts and its fractions, as well as the assessment of the relationship between the antischistosomal activity of these plant extracts and oxidative stress, was determined...
April 10, 2018: Drug Research
https://www.readbyqxmd.com/read/29631297/preparation-and-evaluation-of-midazolam-rectal-gel-in-vitro-and-in-vivo
#14
Xiaojia Chen, Wanqin Li, Ying Li, Fei Guo, Hui Zhang, Jing Gao, Jianxu Sun, Aiping Zheng
Midazolam has been successfully used for sedation, which the tablets, injections and oral solutions were available in market. However, the oral bioavailability of midazolam is less due to the first effect, while injection formulation has a low patient compliance. The purpose of this study was to obtain midazolam rectal gel to meet the production and market requirements. We evaluated the in vitro release behavior of midazolam powder, a physical mixture of midazolam and HPMC, and midazolam gel. The results showed that the midazolam gel has superior release degree compared to the other...
April 9, 2018: Drug Research
https://www.readbyqxmd.com/read/29631296/nanocrystalization-of-pioglitazone-by-precipitation-method
#15
Jaleh Varshosaz, Saeedeh Ahmadipour, Majid Tabbakhian, Shokoufeh Ahmadipour
BACKGROUND: Poor solubility in aqueous medium limits the use of many drugs. Different methods have been adopted to promote the rate of dissolution of slightly water soluble drugs. Crystallization improves solubility, and bioavailability by increasing the surface area of slightly water soluble drugs. Pioglitazone (PGZ), which is a class II Biopharmaceutical Classification System drug has a slight solubility in water and a slow rate of dissolution, which may have a negative effect on its metabolism leading to a therapeutic failure...
April 9, 2018: Drug Research
https://www.readbyqxmd.com/read/29631295/clinical-pharmacology-considerations-for-development-of-%C3%AE-lactamase-inhibitor-combination-with-antibiotics
#16
Nuggehally R Srinivas
The shrinking drug pipeline for antibacterial drugs has made it very precious to discover and develop novel drugs in this space. In this context, the recent approvals of β lactamase inhibitors with either cephalosporin or penem as combination drugs are welcome news to the community. There are number of β lactamase inhibitors with suggested partnered drugs that are currently in various stages of drug development. The focus of this manuscript is to provide some perspectives on clinical pharmacology considerations that may aid in the successful development of such combination drugs...
April 9, 2018: Drug Research
https://www.readbyqxmd.com/read/29614516/identification-of-non-zinc-binding-inhibitors-of-mmp-2-through-virtual-screening-and-subsequent-rescoring
#17
Jamal Shamsara
MMP-2 belongs to a large family of proteases called matrix metalloproteinases (MMPs) that degrades type IV collagen, the main structural component of basement membranes and gelatin. The main pathologic role of MMP-2 overexpression is to contribute to the development of cancer through the progression of metastasis and angiogenesis. A structure-based virtual screening was employed to find new inhibitors with possible selectivity for MMP-2. The inhibitory activities of 3 inhibitors (one was not a suitable drug-like hit) among 19 purchased compounds were approved by enzyme inhibition assay...
April 3, 2018: Drug Research
https://www.readbyqxmd.com/read/29589341/solidification-of-nanostructured-lipid-carriers-loaded-testosterone-undecanoate-in-vivo-and-in-vitro-study
#18
Yabing Hua, Wanqing Li, Zhou Cheng, Ziming Zhao, Xiaoxing Yin, Ying Li, Jianxu Sun, Jing Gao, Hui Zhang, Aiping Zheng
To enhance the bioavailability of testosterone undecanoate (TU) and overcome the current problem of soft capsules (Andriol Testocaps® ), Nano-structured lipid carriers (NLC) for TU was developed. First, suspension of TU-loaded NLC (TU-NLC) was prepared by high pressure homogenization; then adsorbent or a protective agent β-cyclodextrin was used to solidify the suspension through a vacuum system; finally, the solid powder of TU-loaded NLC (solid TU-NLC) was filled into hard capsules. The characteristics of solid TU-NLC, were investigated in vitro and vivo...
March 27, 2018: Drug Research
https://www.readbyqxmd.com/read/29579762/strategies-in-development-and-delivery-of-nanotechnology-based-cosmetic-products
#19
Usama Ahmad, Zeeshan Ahmad, Ahmed Abdullah Khan, Juber Akhtar, Satya Prakash Singh, Farhan Jalees Ahmad
The science of formulation involving cosmetic ingredients has always been a challenge since the release of active components greatly depends upon the carrier system involved and the selectivity of skin barrier. The principle obstacle of the skin resides in the epidermis and it's hard for many active components to cross it. The formulation related factors like size of particles, viscosity and lipophilicity of the components also play an important role in permeation of the dermal composition. Though widely used; conventional creams and gels still struggle in terms of success...
March 26, 2018: Drug Research
https://www.readbyqxmd.com/read/29558782/efficacy-and-tolerability-of-a-complex-homeopathic-drug-in-children-suffering-from-dry-cough-a-double-blind-placebo-controlled-clinical-trial
#20
Hans W Voß, Andreas Michalsen, Rainer Brünjes
BACKGROUND: A randomised, placebo-controlled clinical trial in children suffering from acute dry cough was performed to assess the efficacy and tolerability of a complex homeopathic drug (Drosera, Coccus cacti, Cuprum Sulfuricum, Ipecacuanha=Monapax syrup, short: verum). METHODS: 89 children received verum and 91 received placebo daily for 7 days (age groups 0.5-3, 4-7 and 8-12 years). The primary efficacy variable was the improvement of the Cough Assessment Score...
March 20, 2018: Drug Research
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