The primary aim of the study is to test safety and tolerance of oral intake of GT oil in the form of a non-diary based emulsion (10g of GT per emulsion) in healthy men. This will be a single center study, and the recruitment is expected to happen over a 1-2- month's period.

开始日期2017-08-28

申办/合作机构

National University Hospital

100 项与十三酸甘油酯相关的临床结果

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100 项与十三酸甘油酯相关的转化医学

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100 项与十三酸甘油酯相关的专利（医药）

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项与十三酸甘油酯相关的文献（医药）

2023-09-06·International journal of molecular sciences

Enhancing the Hydrolytic Activity of a Lipase towards Larger Triglycerides through Lid Domain Engineering.

Article

作者: Muñoz-Tafalla, Rubén ; Roda, Sergi ; Ferrer, Manuel ; Almendral, David ; Robles-Martín, Ana ; Fernandez-Lopez, Laura ; Guallar, Víctor

Lipases have valuable potential for industrial use, particularly those mostly active against water-insoluble substrates, such as triglycerides composed of long-carbon chain fatty acids. However, in most cases, engineered variants often need to be constructed to achieve optimal performance for such substrates. Protein engineering techniques have been reported as strategies for improving lipase characteristics by introducing specific mutations in the cap domain of esterases or in the lid domain of lipases or through lid domain swapping. Here, we improved the lipase activity of a lipase (WP_075743487.1, or Lip_MRD) retrieved from the Marine Metagenomics MarRef Database and assigned to the Actinoalloteichus genus. The improvement was achieved through site-directed mutagenesis and by substituting its lid domain (FRGTEITQIKDWLTDA) with that of Rhizopus delemar lipase (previously R. oryzae; UniProt accession number, I1BGQ3) (FRGTNSFRSAITDIVF). The results demonstrated that the redesigned mutants gain activity against bulkier triglycerides, such as glyceryl tridecanoate and tridodecanoate, olive oil, coconut oil, and palm oil. Residue W89 (Lip_MRD numbering) appears to be key to the increase in lipase activity, an increase that was also achieved with lid swapping. This study reinforces the importance of the lid domains and their amino acid compositions in determining the substrate specificity of lipases, but the generalization of the lid domain swapping between lipases or the introduction of specific mutations in the lid domain to improve lipase activity may require further investigation.

2020-11-01·International Journal of Pharmaceutics2区 · 医学

Studying effect of glyceryl palmitostearate amount, manufacturing method and stability on polymorphic transformation and dissolution of rifaximin tablets

2区 · 医学

Article

作者: Barakh Ali, Sogra F ; Dharani, Sathish ; Afrooz, Hamideh ; Rahman, Ziyaur ; Khan, Mansoor A

Rifaximin (RFX) exhibit polymorphism and commercial formulation contains the α form. The polymorphic transformation of the RFX in the drug product have significant effect on the clinical outcome. The focus of present work was to understand effect of formulation component and manufacturing method, and exposure to stability condition on polymorphic stability and dissolution of RFX tablets. The RFX tablets containing 2.5, 5 and 10% glyceryl palmitostearate (GPS) were manufactured by direct-compression and wet-granulation followed by compression. Ethanol was used as a granulating solvent. The tablets were packed in pharmacy vials and exposed to 40 °C/75% RH for four weeks. The tablets were characterized for polymorphic form by X-ray powder diffraction (XRPD) and Fourier infrared spectroscopy (FTIR), assay and dissolution. Before exposure to stability condition, dissolution ranged from 78.0 ± 2.3 to 81.9 ± 3.5%, and 72.7 ± 2.0 and 75.9 ± 5.8% in directly compressed and ethanol-granulated formulations, respectively. GPS amount of 10% caused a decrease in dissolution albeit insignificant (p > 0.05). The polymorphic forms of RFX were α and γ in directly compressed and ethanol-granulated formulations, respectively. There was a decrease in dissolution rate and extent after exposure to 40 °C/75% RH in directly compressed formulations. On the other hand, only dissolution rate was affected in ethanol-granulated formulations. The dissolution ranged from 52.8 ± 2.0 to 70.0 ± 3.0% in directly compressed formulations after four weeks exposure to 40 °C/75% RH exposure. A decrease in dissolution was linked to polymorphic transformation of the drug and GPS in the formulations after exposure to stability condition. XRPD and FTIR data indicated α to β transformation in directly compressed formulations while no polymorphic change was observed in ethanol-granulated formulations. In conclusion, this study clearly showed effect of formulation and manufacturing variables, and stability exposure on the polymorphic stability and dissolution of RFX, which may have clinical ramification.

2017-12-01·Lipids in Health and Disease3区 · 医学

Lipids bearing extruded-spheronized pellets for extended release of poorly soluble antiemetic agent—Meclizine HCl

3区 · 医学

ArticleOA

作者: Shoaib, Muhammad Harris ; Yousuf, Rabia Ismail ; Ahmad, Mansoor ; Qazi, Faaiza ; Ahmed, Kamran ; Nasiri, Muhammad Iqbal

BACKGROUNDAntiemetic agent Meclizine HCl, widely prescribed in vertigo, is available only in immediate release dosage forms. The approved therapeutic dose and shorter elimination half-life make Meclizine HCl a potential candidate to be formulated in extended release dosage form. This study was aimed to develop extended release Meclizine HCl pellets by extrusion spheronization using natural and synthetic lipids. Influence of lipid type, drug/lipid ratio and combinations of different lipids on drug release and sphericity of pellets were evaluated.METHODSThirty two formulations were prepared with four different lipids, Glyceryl monostearate (Geleol^®), Glyceryl palmitostearate (Precirol^®), Glyceryl behenate (Compritol^®) and Carnauba wax, utilized either alone or in combinations of drug/lipid ratio of 1:0.5-1:3. Dissolution studies were performed at variable pH and release kinetics were analyzed. Fourier transform infrared spectroscopy was conducted and no drug lipid interaction was found.RESULTSSphericity indicated by shape factor (e_R) varied with type and concentration of lipids: Geleol^® (e_R = 0.891-0.997), Precirol^® (e_R = 0.611-0.743), Compritol^® (e_R = 0.665-0.729) and Carnauba wax (e_R = 0.499-0.551). Highly spherical pellets were obtained with Geleol^® (Aspect ratio = 1.005-1.052) whereas irregularly shaped pellets were formed using Carnauba wax (Aspect ratio = 1.153-1.309). Drug release was effectively controlled by three different combinations of lipids: (i) Geleol^® and Compritol^®, (ii) Geleol^® and Carnauba wax and (iii) Geleol^®, Compritol^® and Carnauba wax. Scanning electron microscopy of Compritol^® pellets showed smooth surface with pores, whereas, irregular rough surface with hollow depressions was observed in Carnauba wax pellets. Energy dispersive spectroscopy indicated elemental composition of lipid matrix pellets. Kinetics of (i) Geleol^® and Compritol^® pellets, explained by Korsmeyer-Peppas (R² = 0.978-0.993) indicated non-Fickian diffusion (n = 0.519-0.597). Combinations of (ii) Geleol^® and Carnauba wax and (iii) Geleol^®, Compritol^® and Carnauba wax pellets followed Zero-order (R² = 0.991-0.995). Similarity test was performed using combination of Geleol^® and Compritol^® (i) as a reference.CONCLUSIONSMatrices for the extended release of Meclizine HCl from extruded-spheronized pellets were successfully formed by using three lipids (Geleol^®, Compritol^® and Carnauba wax) in different combinations. The encapsulated pellets of Meclizine HCl can be effectively used for treatment of motion sickness, nausea and vertigo for extended period of time.

100 项与十三酸甘油酯相关的药物交易

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适应症	最高研发状态	国家/地区	公司	日期
心血管疾病	临床1期	新加坡	National University Hospital	2017-08-28
2型糖尿病	临床1期	新加坡	National University Hospital	2017-08-28
肠阻塞	临床1期	新加坡	National University Hospital	2017-08-28
不孕	临床1期	新加坡	National University Hospital	2017-08-28
恶性类癌综合征	临床1期	新加坡	National University Hospital	2017-08-28
代谢综合征	临床1期	新加坡	National University Hospital	2017-08-28
恶心	临床1期	新加坡	National University Hospital	2017-08-28
多囊卵巢综合征	临床1期	新加坡	National University Hospital	2017-08-28
呕吐	临床1期	新加坡	National University Hospital	2017-08-28