Pharmacology Commons^™

Non-Destructive Analysis Of Glycyrrhizin In Ummaruekvati Dispensatory Thai Traditional Medicine, Thanattaporn Charoenkittrakul, Chanamate Noi-Ang, Prathan Luecha, Jomjai Peerapattana

The Thai Journal of Pharmaceutical Sciences

Ummaruekvati is an antitussive traditional medicine. It contains licorice as the main ingredient and the major chemical component is glycyrrhizin. The conventional method for quantitative analysis of glycyrrhizin content in licorice is by high-performance liquid chromatography, which is destructive of the sample, time consuming, high cost, and has many steps in the sample preparation process. In this study, a rapid and non-destructive near-infrared spectroscopy (NIR) method was applied for quantitative analysis of glycyrrhizin content in Ummaruekvati dispensatories. A partial least squares chemometric method with various data pre-treatments was performed to establish the calibration model. The best calibration model was obtained …

Monitoring Of Crystalline Transition During Wet Granulation Process Using Probe Type Low Frequency Raman Spectrometer, Kanako Fukui, Yota Suzuki, Kazuki Haneishi, Varin Titapiwatanakun, Hiroshi Hisada, Tatsuo Koide, Toshiro Fukami

The Thai Journal of Pharmaceutical Sciences

In recent years, real time analysis has been widely studied using various Process Analytical Technology tools particularly in the quality control of drug products. In this study, we investigated the improvement of sensitivity and the reduction of measurement time using a low frequency (LF) Raman spectrometer equipped with a new light source for in situ monitoring of crystalline transformation of active pharmaceutical ingredients (API) during wet granulation process. Three model drugs were chosen to assess the system sensitivity, hydrate transition, and cocrystal dissociation. LF Raman spectra showed the specific peaks for crystalline indomethacin and theophylline which were typical and well …

In-Line Prediction Of Secondary Drying Time From Measured Ice Nucleation Temperature During Lyophilization Process, Tharavich Supakatisant, Narueporn Sutanthavibul, Oran Kittithreerapronchai

The Thai Journal of Pharmaceutical Sciences

Purpose: To propose an approach to find optimal secondary drying time (tSD) specifically for each lyophilized batch by predicting residual moisture at the beginning of secondary drying (Cs0) using measured ice nucleation temperatures (TN) obtained in-line. Materials and Methods: Value of Cs0 was determined by minimizing the residual error between measured (Tp SD,mea) and calculated (Tp SD,cal) product temperatures during secondary drying. Value of TN was determined by using product temperatures during freezing (TP Fr). Then, the correlation between Cs0 and TN was conducted and resulted in the Cs0 prediction equation. This equation was used with developed mathematical simulation to …

Inhibition Of Viper Venom-Induced Toxicity By Moringa Oleifera Leaves Extracts, Asha B. Thomas, Snehal Karanjkhele, Nitin Salvi, Lata Kothapalli, Aaftab Shaikh, Seema Kamble

The Thai Journal of Pharmaceutical Sciences

Snakebite, a medical emergency, is a socially significant but neglected issue in India. Antivenom serum therapy that is currently used against venomous snakebites is expensive and showed severe side effects. Traditional claims reported the use of Moringa oleifera to treat snakebite in rural India. To scientifically validate these claims, in the present investigation, the antivenom potential of the extracts of M. oleifera was investigated. The extracts effectively neutralized Russell’s viper venom-induced lethality (LD50: 10.9 μg) at 10 μg/mice and 300 μg/mice (ED50), respectively. Both extracts neutralized venom-induced hemolysis (50–100 μg). Inhibitory concentrations against phospholipase A2 activity exhibited by aqueous and …

Probable Selective Compounds For Inhibition Of Sars-Cov-2 Infection: A Review, Nagaraju Rajendraprasad

The Thai Journal of Pharmaceutical Sciences

The world is severely facing the pandemic COVID-19 Corona viral disease. Many people died and more than five millions are fighting for their life in the world. The viral candidate has become to play villain role for the real life due to non-availability of medication. In this background attempt is made to present a review report on the probable and effective compounds to inhibit the viral activity of SARS-CoV-2. The works on the use of plant-based and synthetic compounds to suppress the viral functioning is summarized. Wherever possible, the mechanism of action with the results and effect of dose are …

Development And Validation Of High- Performance Liquid Chromatography Method For Estimation Of Seratrodast In Spiked Human Plasma, Sandeep S. Sonawane, Priyanka T. Shinde, Gayatri S. Joshi, Sanjay J. Kshirsagar

The Thai Journal of Pharmaceutical Sciences

In the work presented, an high-performance liquid chromatography method was developed and validated for the estimation of seratrodast (SER) in spiked human plasma, using flurbiprofen as an internal standard (IS). The drug and IS were extracted from pooled human plasma sample using 5 mL of tert-butyl methyl ether with 200 μL of 1% v/v formic acid. Both SER and IS were well separated and resolved from each other and plasma interferents using 20 mM phosphate buffer (pH 3.0) with acetonitrile in the proportion of 30: 70% v/v, in an isocratic mode at 1 mL/min on a C18 column and detection …

Moss Bryum Weigelii Spreng Improves Survival In Septic Rats Induced By Cecal Ligation And Puncture, Ho Viet Hieu, Surendra Babu Lagu, Vinay Bharadwaj Tatipamula

The Thai Journal of Pharmaceutical Sciences

The present study investigated the phytochemical, high-performance thin-layer chromatography (HPTLC) profiling, total phenolic content, antibacterial activity, acute toxicity studies, hemodynamic parameters, myeloperoxidase (MPO) activity and serum procalcitonin (PCT) levels of hydroalcoholic extract of Bryum weigelii (HE-Bw), and its effects on cecal ligation and puncture (CLP) induced sepsis in mice. The preliminary phytochemical screening showed that HE-Bw contains alkaloids, terpenoids, flavonoids, phenolics, and tannins. The HPTLC analysis of HE-Bw identified three unknown components with different Rf values and area percentage. The total phenolic amount for HE-Bw was equivalent to 211.6 ± 0.8 mg of gallic acid per 100 g of dried …

Treatment Outcomes And Their Predictive Factors In Patients Withenterobacter Spp., Serratia Spp.,Citrobacter Spp., Providencia Spp., I-Indole-Positive Proteus Spp., Andmorganella Spp, Bloodstream Infection, Wichai Santimaleeworagun, Dhitiwat Changpradub, Sudaluck Thunyaharn, Piraporn Juntanawiwat, Patsachon Kungsahadhum6, Phornusa Leartamornsakulchai, Waramporn Seubsai, Pratewee Satavetin

The Thai Journal of Pharmaceutical Sciences

The present study examined the treatment outcomes and factors related to mortality in patients with Enterobacter spp., Serratia spp., Citrobacter spp., Providencia spp., I-indole-positive Proteus spp., and Morganella spp. (ESCPIM) bloodstream infections and determined the susceptibility of ESCPIM pathogens to antimicrobial compounds. This retrospective study was performed at a university hospital in Thailand, using records from March 2017 to December 2018. Fifty-six patients with ESCPIM bacteremia were included. Approximately, half the patient cohort (55.4%) was infected with Enterobacter spp. The in-hospital mortality rate was 23.2%. Of the 56 patients studied, 20 patients (35.7%) had received a carbapenem treatment regimen, whereas …

In Vitro And In Vivo Effects Of Zanthoxylum Limonella (Dennst.) Alston. Crude Extracts And Volatile Oil On Blood Glucose Reduction, Attarat Pattanawongsa, Chaweewan Klongsiriwet, Peerarat Thaina, Aunchalee Prammano, Nattaphop Maneechai, Phitchapha Saengphrom, Gorawit Yusakul, Maleeruk Utsintong

The Thai Journal of Pharmaceutical Sciences

Introduction: Complimentary medicines have been long investigated as new and alternative therapeutic options for treating type 2 diabetes mellitus because the current drugs are associated with adverse drug reactions. The antidiabetic potential of the Zanthoxylum genus has been demonstrated previously. However, Zanthoxylum limonella (Dennst.) (ZL) has not been evaluated in any clinical trials. Objectives: This study aimed to examine the inhibition of α-glucosidases in vitro and in vivo using ZL fruit extracts, thereby determining the reduction in blood glucose levels using oral glucose and sucrose tolerance tests. Results and Discussion: The water extract of ZL fruits showed the greatest inhibition …

Simultaneous Estimation Of Ivacaftor And Tezacaftor In Rat Plasma By Liquid Chromatography Coupled With Tandem-Mass-Spectrometry: Application To Pharmacokinetic Studies, M. Satya Venkata, A. Lakshmana Rao, M. William Carey

The Thai Journal of Pharmaceutical Sciences

Background: Ivacaftor and Tezacaftor belong to the CFTR potentiator class, in combination approved to manage cystic fibrosis. Objective: To establish a sensitive LC-MS/MS approach for the synchronized analysis of Ivacaftor and Tezacaftor and its appliance to rat pharmacokinetic investigation. Methodology: Method is developed with protein precipitation by acetonitrile and Ivacaftor-d4, Tezacaftor-d4 are used as internal standards. Separation is done on an Eclipse plus C18 analysis column (100 mm × 4.6 mm 1.8 μm) with a mobile phase consisting of 0.1% trifluoroacetic acid: acetonitrile (ratio 60:40, v/v, and pH 2.5) and flow stream of 1.0 mL/min at ambient temperature. Results: The …

Gas Chromatography-Flame Ionization Detector Analysis Of Amb-Fubinaca From Criminal Evidences In Vietnam, Anh Tuan Nguyen, Dang Tien Nguyen, Duy Toan Pham

The Thai Journal of Pharmaceutical Sciences

Synthetic cannabinoids are currently the largest group of new psychoactive substances. Among them, one of the most recent compounds in Vietnam is AMB-Fubinaca. No quantitative method has been officially implied for AMB-Fubinaca in criminal evidences, thus, making the police investigations burdensome. This study, for the 1st time, aimed to develop and validate the gas chromatography with flame ionization detector (GC-FID) method to determine and quantify AMB-Fubinaca in criminal evidences found in the South of Vietnam from 2016 to 2018. Chromatography separation was achieved on diphenyl dimethyl polysiloxane GC column (30 m × 0.32 mm × 0.25 μm) with a total …

Effect Of The Hydrophilic-Lipophilic Balance Values Of Non-Ionic Surfactants On Size And Size Distribution And Stability Of Oil/Water Soybean Oil Nanoemulsions, Kamonwan Singpanna, Dusadee Charnvanich

The Thai Journal of Pharmaceutical Sciences

Objective: This study aims at investigating the effect of the hydrophilic-lipophilic balance (HLB) of non-ionic surfactants on physical property and stability of nanoemulsions. Materials and Methods: The nanoemulsions were prepared using the Microfluidizer. The oil phase consisted of 10% w/w soybean oil and 5% w/w surfactant(s). Types of nanoemulsions were confirmed by dilution test. The average droplet size and size distribution (polydispersity index [PDI]) were measured by dynamic light scattering Zetasizer Nano ZS™. The screening physical stability was done by centrifugation. Only the formulations with no phase separation were further evaluated for physical stability. Results: All nanoemulsions were single phase …

Systematic Development By The Design-Of-Experiment Approach And Physicochemical Evaluations Of The Optimized Self-Microemulsifying Astaxanthin Delivery System, Mo Mo Ko Zin, Veerakiet Boonkanokwong

The Thai Journal of Pharmaceutical Sciences

A self-microemulsifying delivery system (SMEDS) containing astaxanthin (AST) was developed and optimized using a mixture design and its desirability function. Independent factors studied in the experimental design were the amounts of castor oil, Cremophor® RH 40, and Tween® 80 in a formula. The measured response variables included droplet size, polydispersity index (PDI), zeta potential, active ingredient content, and transmittance of microemulsions obtained from the AST SMEDS formulations. The desirability function was then adjusted to optimize the formulation. The optimized AST SMEDS was composted of 19.59% castor oil, 62.34% Cremophor® RH 40, and 18.03% Tween® 80, and the resulting self microemulsions …

Antiplasmodial Activity Of Hyptis Pectinata Extract And Its Analog Against 3d7 Plasmodium Falciparum Through Caseinolytic Protease Proteolytic (Clpp) Inhibition, Meiny Suzery, Bambang Cahyono, Nur Dina Amalina, Cahyo Budiman, Ibnu Bayu, Mukhammad Asy’Ari, Widayat

The Thai Journal of Pharmaceutical Sciences

Hyptolide and epoxy hyptolide were successfully isolated and synthesized from Hyptis pectinata extract that potential to cure malaria diseases. The previous studies showed that these compounds contained lactone groups associated with antibacterial and anticancer activities. However, the antimalarial activity remained unclear. This study aimed to investigate the antiplasmodial activity of H. pectinata extract, hyptolide, and epoxy hyptolide. These compounds were tested in vitro for antiplasmodial activity against chloroquinesensitive 3D7 strain of Plasmodium falciparum. Thin blood smears were used to assess the levels of parasitemia and growth inhibition of the isolates and the ClpP inhibition was analyzed under well diffusion assay. …

Comparative Studies On Biochemical And Pharmacological Profiles Of Unfractionated Heparins & Their Depolymerized Derivatives From Bovine, Ovine And Porcine Origins, Ahmed Kouta

Dissertations

Heparin and heparin related drugs have remained the anticoagulant of choice for medical and surgical indications. These drugs are comprised of poly-component sulfated chains of varying length and biophysical structure with direct and indirect pharmacological effects. Heparins produce their therapeutic effects by multiple mechanisms involving both the cellular and humoral targets. These drugs represent natural products which are isolated from mammalian tissue rich in mast cells. Currently used heparin and LMWHs are obtained from porcine mucosal tissue. Other animal sources including bovine and ovine tissues also provide additional sources for the manufacturing of heparins. While there may be microchemical and …

Retrospective Review Of Pharmacogenetic Testing At An Academic Children's Hospital., Timothy A. Roberts, Jennifer A. Wagner, Tracy L. Sandritter, Benjamin T. Black, Andrea Gaedigk, Stephani L. Stancil

Manuscripts, Articles, Book Chapters and Other Papers

There is limited evidence to support pharmacogenetic (PGx) testing in children. We conducted a retrospective review of PGx testing among 452 patients at an academic children's hospital to determine the potential utility of PGx in diseases of childhood and to identify targets for future pediatric pharmacogenetic research. An actionable gene-drug pair associated with the 28 genes tested (Clinical Pharmacogenetics Implementation Consortium (CPIC) level A or B, Pharmacogenomics Knowledge Base (PharmGKB) level 1A or B, or US Food and Drug Administration (FDA) recommendation and a PharmGKB level) was present in 98.7% of patients. We identified 203 actionable gene-drug-diagnosis groups based on …

Investigating Cannabinoid Type-1 Receptor (Cb1r) Positive Allosteric Modulators (Pams) In Mouse Models Of Overt Cannabimimetic Activity, Subjective Drug Effects, And Neuropathic Pain, Jayden Elmer

Theses and Dissertations

Chronic pain affects between 20 and 30 percent of the adult population in western countries and represents a wide array of specific etiologies (Berge, 2011). Neuropathic pain secondary to traumatic nerve injury, chemotherapeutic toxicity, or diseases (e.g., diabetes mellitus) is often refractory to conventional analgesics, with patients receiving less than 50% pain relief compared to placebo (Finnerup et al. 2010). The endocannabinoid system has shown potential as a therapeutic target for neuropathic pain wherein CB1 agonism via administration of exogenous agonists or pharmacological blockade of endocannabinoid catabolic enzymes exhibits efficacy in reversing allodynia in the chronic constriction injury (CCI) model …

Pharmacophoric Evaluation Of 5-Ht2a And 5-Ht2b Serotonin Recpeptors, Prithvi Hemanth

Theses and Dissertations

Serotonin (5-HT) receptors represent a class of receptors involved in a variety of physiological processes including regulation of mood, perception, cognition, appetite, and heart function, and thus serve as drug targets of several drugs such as antipsychotic agents, hallucinogenic drugs, and appetite suppressant drugs. Due to the structural similarity of certain 5-HT receptor subtypes, particularly 5-HT₂ receptors (5-HT_2A, 5-HT_2B receptors) determination and refinement of pharmacophore models of these receptor subtypes can greatly improve the therapeutic efficacy of drugs that target them.

The goals of this study were to define and/or refine existing pharmacophore models for 5-HT …

Interclass Gpcr Heteromerization Affects Localization And Trafficking, Rudy Toneatti

Theses and Dissertations

Class A serotonin (5-hydroxytryptamine) 2A (5-HT_2AR) and class C metabotropic glutamate 2 receptors (mGluR2) are seven transmembrane receptors (7TMRs or G protein-coupled receptors – GPCRs) involved in multiple neuropsychiatric disorders including schizophrenia. Previous findings from our laboratory reported that 5-HT_2AR and mGluR2 are dysregulated in the prefrontal cortex of patients suffering from this psychiatric condition, although 5-HT_2AR’s expression was recovered in antipsychotic-medicated patients. Genome-wide association studies on schizophrenia reported that endosomal trafficking that regulates cell surface abundance of another 7TMR implicated in this disease (dopamine D2 receptor) can be altered. Ligand-activated receptors, including the …

The Cb1 Receptor Positive Allosteric Modulator, Zcz011, Attenuates Naloxone-Precipitated Withdrawal Signs In Oxycodone-Dependent Mice And Inhibits Small Intestinal Transit In Mice, Julien Dodu

Theses and Dissertations

The endogenous cannabinoid system tightly regulates a myriad of physiological and pathophysiological functions. Effects of cannabinoids in ameliorating opioid withdrawal signs has been known for decades. Naloxone precipitates several withdrawal signs (e.g., diarrhea, weight loss, jumps, paw flutters, and head shakes) in opioid dependent rodents. ∆⁹-tetrahydrocannabinol (THC) has been shown to ameliorate opioid withdrawal in mice through the activation of cannabinoid type-1 (CB₁) receptors. Inhibition of the endocannabinoid degradative enzymes also attenuates these withdrawal signs (i.e., diarrhea, weight loss, jumps, paw flutters, and head shakes) in opioid-dependent mice. Specifically, inhibition of fatty acid amide hydrolase (FAAH), …

Influence Of 2,5-Dimethoxy-4-Iodoamphetamine (Doi) On Ethanol Preference And Consumption In C57bl/6 Male Mice, Alaina M. Jaster, Sam Gottlieb, Michael Miles, Javier González-Maeso

Graduate Research Posters

Substance use disorders (SUD) account for a large number of mental health diagnosis in the United States and around the world. Approximately 13.6 million adults 26 or older and 5.1 million young adults (ages 18-24) battled with a SUD in 2017. Alcohol Use Disorder (AUD) alone effects nearly 6% of the adult population within the United States. This creates a substantial burden on the individual, with alcohol being the third-leading cause of preventable death in the United States. Few treatments for AUD exist, with no new FDA-approved therapeutic treatments within the last 15 years. Additionally, the limited treatments we do …