(Craib) A. Schmitz Extracts Moderate the Expression of Drug-Metabolizing Enzymes: In Vivo Study to Clinical Propose.

(Craib) A. Schmitz (LS) has been traditionally used as a medicinal herb by folk healers in Thailand with rare evidence-based support. Hepatic cytochrome P450s (CYPs450) are well known as the drug-metabolizing enzymes that catalyze all drugs and toxicants.

Design, Synthesis, and Neuroprotective Activity of Phenoxyindole Derivatives on Antiamyloid Beta (Aβ) Aggregation, Antiacetylcholinesterase, and Antioxidant Activities.

In this investigation, a number of phenoxyindole derivatives were designed, synthesized, and tested for their neuroprotective ability on SK-N-SH cells against Aβ-induced cell death and biologically specific activities involved in anti-Aβ aggregation, anti-AChE, and antioxidant effects. The proposed compounds, except compounds and , could protect SK-N-SH cells at the IC of anti-Aβ aggregation with cell viability values ranging from 63.05% ± 2.

Evaluation of the Intestinal Permeability of Rosmarinic Acid from Leaf Water Extract in a Caco-2 Cell Model.

(TL) has been traditionally used as an antidote and an antipyretic drug by folk healers for centuries in Thailand. Rosmarinic acid (RA) is major compound in TL extract and has attracted great interest due to its potential broad pharmacological effects. Herein, the permeability of RA was investigated in TL extract and as a pure compound in a Caco-2 cell model by using high-performance liquid chromatography with a photodiode array detector (HPLC-PDA).

The in vitro and in vivo study of novel formulation of andrographolide PLGA nanoparticle embedded into gelatin-based hydrogel to prolong delivery and extend residence time in joint.

Andrographolide (AG), a well-known traditional medicinal plant in Southeast Asia, is widely used for treatment of many chronic diseases. Interestingly, AG has been reported to have inhibitory effects on osteoclast function and anti-inflammatory properties. Because of these therapeutic properties, this study aimed to develop and optimize the formulation of AG using PLGA nanocarriers and gelatin-based hydrogel to prolong the retention time in the joint.

The Effects of Andrographolide on the Enhancement of Chondrogenesis and Osteogenesis in Human Suprapatellar Fat Pad Derived Mesenchymal Stem Cells.

Andrographolide is a labdane diterpenoid herb, which is isolated from the leaves of and widely used for its potential medical properties. However, there are no reports on the effects of andrographolide on the human suprapatellar fat pad of osteoarthritis patients. In the present study, our goal was to evaluate the innovative effects of andrographolide on viability and Tri-lineage differentiation of human mesenchymal stem cells from suprapatellar fat pad tissues.

The Intestinal Efflux Transporter Inhibition Activity of Xanthones from Mangosteen Pericarp: An In Silico, In Vitro and Ex Vivo Approach.

The capacity of α-mangostin (α-MG) and β-mangostin (β-MG) from mangosteen pericarp on P-glycoprotein (Pgp) in silico, in vitro, and ex vivo was investigated in this study. Screening with the ADMET Predictor™ program predicted the two compounds to be both a Pgp inhibitor and Pgp substrate. The compounds tended to interact with Pgp and inhibit Pgp ATPase activity.

Modified tetra-oxygenated xanthones analogues as anti-MRSA and P. aeruginosa agent and their synergism with vancomycin.

Five isolated xanthones from the C. cochinchinense and G. mangostana were evaluated and tested for antibacterial activities.

Pharmacokinetic/Pharmacodynamic (PK/PD) Simulation for Dosage Optimization of Colistin Against Carbapenem-Resistant and Carbapenem-Resistant .

The purpose was to explore the optimal dosage regimen of colistin using Monte Carlo simulations, for the treatment of carbapenem-resistant and carbapenem-resistant based on PK/PD targets in critically ill patients. A total of 116 carbapenem-resistant and were obtained from various clinical specimens at Siriraj Hospital in Bangkok, Thailand. Minimum inhibitory concentrations (MICs) of colistin were determined by broth microdilution method.

Chitosan-based nanoparticles with damnacanthal suppress CRM1 expression.

Cancer is one of the leading causes of mortality worldwide. Phytochemicals may be promising anticancer agents given their various chemical structures and diverse biological activities. Damnacanthal (DAM) is a major bioactive component of Noni, which has been investigated previously as a cancer-preventive or chemotherapeutic agent.

Comparative Fasting Bioavailability of 2 Cilostazol Formulations in Healthy Thai Volunteers: An Open-Label, Single-Dose, Randomized, 2-Way Crossover Study.

Objective: To evaluate the bioequivalence of50 mg cilostazol tablets manufactured locally (Citazol®) and originally (Pletaal®) in healthy Thai volunteers.

Material And Method: An open-label, single dose, randomized, two-period, two-sequence, crossover study in 30 healthy volunteers. Each volunteer received a 50 mg cilostazol tablet of bothformulations with a washoutperiodofat least 14 days.

Pharmacokinetics of mitragynine in man.

Background: Kratom, known botanically as Mitragyna speciosa (Korth.), is an indigenous tree in Southeast Asia. Kratom is currently easily available worldwide via special shops and the Internet to use as a drug of abuse, opioid alternative, or pain killer.

Development of phyllanthin-loaded self-microemulsifying drug delivery system for oral bioavailability enhancement.

Phyllanthin, a poorly water-soluble herbal active component from Phyllanthus amarus, exhibited a low oral bioavailability. This study aims at formulating self-microemulsifying drug delivery systems (SMEDDS) containing phyllanthin and evaluating their in-vitro and in-vivo performances. Excipient screening was carried out to select oil, surfactant and co-surfactant.

In vitro-in vivo correlation study for the dermatopharmacokinetics of terbinafine hydrochloride topical cream.

Background: To investigate the relationship between dermatopharmacokinetic (DPK) tape stripping from in vitro and in vivo using 1% terbinafine hydrochloride topical cream as the model formulation.

Methodology: In vitro and in vivo tape strippings were conducted on separated pig ear skin used as a biological membrane for franz diffusion cell testing and the non-hairy skin area at the ventral forearms of healthy volunteers, respectively. Terbinafine (1%) topical cream was applied to the skin for 0.

Dermal pharmacokinetics of Terpinen-4-ol following topical administration of Zingiber cassumunar (plai) oil.

The purpose of this study was to investigate dermal pharmacokinetics of terpinen-4-ol in rats following topical administration of plai oil derived from the rhizomes of Zingiber cassumunar Roxb. Unbound terpinen-4-ol concentrations in dermal tissue were measured by microdialysis. The dermal pharmacokinetic study of terpinen-4-ol was performed under non-occlusive conditions.

Bioequivalence study of 10 mg ramipril tablets in healthy Thai volunteers.

Objective: To determine the bioequivalence of 10 mg dose of ramipril tablets between the test product (Ramtace 10 mg, Unison Laboratories, Thailand) and the reference product (Tritace 10 mg, Aventis Pharma SPA, Italy).

Material And Method: The present study was carried out with a single dose, 2-treatment, 2-period, 2-sequence randomized crossover design under fasting condition with a minimum of 14 days washout period in 24 healthy Thai male and female volunteers. Plasma samples for determination of ramipril and ramiprilat were obtained pre-dose and at frequent intervals for up to 72 h post dose.

Bioequivalence study of 500 mg glucosamine sulfate in Thai healthy volunteers.

Background And Objective: Glucosamine sulfate is widely used to relieve symptoms from osteoarthritis. The present study was conducted in order to determine pharmacokinetic and assess the in-vivo bioequivalence of two different hard capsule formulations of glucosamine sulfate when administered as equal dose of 500 mg. The two formulations contained different salt form where reference product is NaCl and test product is KCl.

Bioequivalence study of 50 mg sertraline tablets in healthy Thai volunteers.

Objective: To determine the bioavailability of 50 mg sertraline tablets between the test product (Zotaline, M&H Manufacturing Co., Ltd, Thailand) and the reference product (Zoloft, Pfizer Australia Pty Ltd, Australia).

Material And Method: An open-labeled, single dose, 2-treatment, 2-period, 2-sequence, randomized crossover study under fasting conditions with 14 days washout period was conducted in 24 healthy Thai volunteers.

Elucidation of the natural artemisinin decomposition route upon iron interaction: a fine electronic redistribution promotes reactivity.

The conformational analysis of artemisinin by molecular dynamics and quantum chemistry calculations revealed the existence of seven energy minima with specific interconversion pathways. Among the seven conformers, only , and were able to undergo bond rearrangements upon Fe(2+) interaction. These rearrangements were due to a peculiar puckering of the trioxane ring that brings its three oxygen atoms in an ideal geometrical position for interacting with Fe(2+) ions, promoting an electronic redistribution in the molecule.

Evaluation of the safety and relative bioavailability of a new dihydroartemisinin tablet formulation in healthy Thai volunteers.

A new dihydroartemisinin (DHA) tablet formulation has been developed by the Thai Government Pharmaceutical Organization (GPO). In this report, its in vitro dissolution and in vivo pharmacokinetics as well as its safety in healthy volunteers were evaluated, using the DHA tablet made by Dafra Pharma NV as a reference. A two-period crossover clinical study design was utilised.

Bioequivalence study of 30 mg pioglitazone tablets in Thai healthy volunteers.

Objective: To compare the bioequivalent parameters of 30 mg pioglitazone tablets manufactured locally (Glista) and originally (Actos).

Material And Method: A randomized, single dose, two-treatment, two-period, two-sequence crossover study was conducted Twenty-four healthy volunteers were recruited at Siriraj Clinical Research Unit. Each subject received a 30 mg pioglitazone tablet of both formulations with at least a week washout period Blood samples were collected over 48 h after the oral administration.

Olanzapine pharmacokinetics are similar in Chinese and Caucasian subjects.

Aim: To compare the pharmacokinetic profiles and dose proportionality of olanzapine in Chinese and Caucasian subjects.

Methods: Randomized, three-period study with 12 Chinese and 12 Caucasian, healthy, male subjects administered 2.5, 5 and 10 mg olanzapine.

Duloxetine is both an inhibitor and a substrate of cytochrome P4502D6 in healthy volunteers.

Background And Objectives: Duloxetine, a potent dual reuptake inhibitor of serotonin and norepinephrine currently undergoing clinical investigation for treatment of depression and stress urinary incontinence, has the potential to act as both a substrate and an inhibitor of cytochrome P4502D6 (CYP2D6). Our objectives were to determine the effect of duloxetine on the pharmacokinetics of desipramine, a tricyclic antidepressant metabolized by CYP2D6 (study 1), and the effect of paroxetine, a potent CYP2D6 inhibitor, on duloxetine pharmacokinetics (study 2).

Methods: Subjects were healthy men and women between 21 and 63 years old.