คุณลักษระของพอลิเมอร์ผสมเพื่อใช้เป็นสารเกาะติดเยื่อเมือกสำหรับระบบนำส่งยาคงค้างในกระเพาะอาหาร

Thesis (Ph.D., Pharmaceutical Sciences)--Prince of Songkla University, 201

Report Synthesis and characterization of biopolymers for local application against helicobacter pylori

Thailand Research Fun

Masculinizing Effects of Chrysin-Loaded Poloxamer Micelles on Siamese Fighting Fish

Siamese fighting fish (Betta splendens) are freshwater fish that are commonly found in Thailand and other Southeast Asian countries. In the present study, chrysin-loaded polymeric micelles (CPs) were developed and investigated for the masculinizing effects, survival rate, growth indices, and toxicity on Siamese fighting fish. CPs were prepared using a poloxamer. The micelle system of CPs that were formed at a chrysin-to-polymer ratio of 1:2 was found to be the most suitable monodispersed system and exhibited a nanosized diameter (74.2 ± 1.6 nm) with a narrow size distribution (0.288 ± 0.012). In vivo studies were performed using Siamese fighting fish larvae as animal models. In the in vivo toxicity study, the fish larvae were immersed in aqueous systems containing CPs that had five different chrysin concentrations of 1, 10, 100, 1000, and 10,000 ng/mL for 24, 48, and 72 h. Blank polymeric micelles and water were used as controls. The in vivo masculinization effect of CPs with different chrysin concentrations on the fish larvae was evaluated after 5 weeks of exposure. The results demonstrated that CPs with a chrysin concentration of 1000 ng/mL showed a masculinization effect of 94.59 ± 2.76% with a high fish larvae survival rate of 72.45 ± 5.09% and low toxicity. It was concluded that the developed CPs had a significant effect on the sex reversal of Siamese fighting fish larvae with a high survival rate

The Binding of Alpinia galanga Oil and Its Nanoemulsion to Mammal GABA(A) Receptors Using Rat Cortical Membranes and an In Silico Modeling Platform

The anesthetic effect of Alpinia galanga oil (AGO) has been reported. However, knowledge of its pathway in mammals is limited. In the present study, the binding of AGO and its key compounds, methyl eugenol, 1,8-cineole, and 4-allylphenyl acetate, to gamma-aminobutyric acid type A (GABA(A)) receptors in rat cortical membranes, was investigated using a [(3)H]muscimol binding assay and an in silico modeling platform. The results showed that only AGO and methyl eugenol displayed a positive modulation at the highest concentrations, whereas 1,8-cineole and 4-allylphenyl acetate were inactive. The result of AGO correlated well to the amount of methyl eugenol in AGO. Computational docking and dynamics simulations into the GABA(A) receptor complex model (PDB: 6X3T) showed the stable structure of the GABA(A) receptor–methyl eugenol complex with the lowest binding energy of −22.16 kcal/mol. This result shows that the anesthetic activity of AGO and methyl eugenol in mammals is associated with GABA(A) receptor modulation. An oil-in-water nanoemulsion containing 20% w/w AGO (NE-AGO) was formulated. NE-AGO showed a significant increase in specific [(3)H]muscimol binding, to 179% of the control, with an EC(50) of 391 µg/mL. Intracellular studies show that normal human cells are highly tolerant to AGO and the nanoemulsion, indicating that NE-AGO may be useful for human anesthesia

sj-doc-1-hpx-10.1177_00185787241229141 – Supplemental material for Development and Evaluation of a Prototype Mobile Application for Intravenous Drug Dose Calculation in Overweight and Obese Thai Children: Precision Dosing in Practice

Supplemental material, sj-doc-1-hpx-10.1177_00185787241229141 for Development and Evaluation of a Prototype Mobile Application for Intravenous Drug Dose Calculation in Overweight and Obese Thai Children: Precision Dosing in Practice by Nuntapong Boonrit, Nansinee Klaidokchan, Apisit Niyomdecha, Janyaporn Noppamas, Krit Suknuntha, Pharsai Prasertsan, Supatcha Thaworncheep and Warit Ruanglertboon in Hospital Pharmacy</p

Characterization of Cimetidine–Piroxicam Coprecipitate Interaction Using Experimental Studies and Molecular Dynamic Simulations

The crystalline states of cimetidine and piroxicam, when coprecipitated from solvents containing 1:1 mole ratio, were transformed to amorphous states as observed using powder X-ray diffraction (PXRD). Amorphous forms of drugs generally exhibit higher water solubility than crystalline forms. It is therefore interesting to investigate the interactions that cause the transformation of both the crystalline drugs. Intermolecular interactions between the drugs were determined using Fourier-transform infrared spectroscopy (FTIR) and solid-state 13C CP/MAS NMR. Molecular dynamic (MD) simulation was performed for the first time for this type of study to indicate the specific groups involved in the interactions based on radial distribution function (RDF) analyses. RDF is a useful tool to describe the average density of atoms at a distance from a specified atom. FTIR spectra revealed a shift of the C≡N stretching band of cimetidine. The 13C CP/MAS NMR spectra indicated downfield shifts of C11, C15 and C7 of piroxicam. RDF analyses indicated that intermolecular interactions occurred between the amide oxygen atom as well as the pyridyl nitrogen of piroxicam and H-N3 of cimetidine. The hydrogen atom (O–H) at C7 interacts with the N1 of cimetidine. Since the MD simulation results are consistent with, and complementary to the experimental analyses, such simulations could provide a novel strategy for investigating specific interacting groups of drugs in coprecipitates, or in amorphous mixtures

Crystal Structure Transformations and Dissolution Studies of Cimetidine–Piroxicam Coprecipitates and Physical Mixtures

We have recently demonstrated that coprecipitation of cimetidine (C) and piroxicam (P) at a mole ratio of 1:1 results in the transformation of the crystalline forms of both drugs to an amorphous state. In this study, coprecipitates and physical mixtures of cimetidine and piroxicam were further investigated at C/P mole ratios of 1:10, 1:5, 1:4, 1:2, 10:1, 20:1, 30:1, 40:1, and 52.5:1, the latter being the composition of a clinically used dosage. The physicochemical properties of these samples were examined using X-ray diffraction and Fourier transform infrared spectroscopy. Additionally, dissolution of piroxicam in the samples at C/P mole ratios of 10:1, 20:1, 30:1, 40:1, and 52.5:1 was investigated at pH 1.2 and pH 4. In coprecipitates with C/P mole ratios of 10:1, 20:1, 30:1, and 40:1, crystalline forms of both drugs were transformed to amorphous states. A mixture of an amorphous state and cimetidine crystalline form A was observed for the coprecipitate with a C/P mole ratio of 52.5:1. For the coprecipitates with C/P mole ratios of 1:2, 1:4, 1:5, and 1:10, cimetidine form A was transformed to form C, whereas piroxicam form II was modified to form I. It is interesting that small molecules, instead of polymers or solvents, can cause such crystal structure transformations. The dissolution of piroxicam at pH 4 is lower than that at pH 1.2. Additionally, the coprecipitates and physical mixtures with C/P mole ratios of 10:1, 20:1, 30:1, 40:1, and 52.5:1 demonstrate substantially higher dissolution of piroxicam compared to that of drug alone