Novel mono, di and tri-fatty acid esters bearing secondary amino acid ester head groups as transdermal permeation enhancers

2018 ◽  
Vol 42 (3) ◽  
pp. 2232-2242
Author(s):  
S. Rambharose ◽  
R. S. Kalhapure ◽  
M. Jadhav ◽  
T. Govender

Mono-oleate derivative (MOAPE) enhancing in vitro transdermal permeation of tenofovir.

2012 ◽  
Vol 79 ◽  
pp. 61-65 ◽  
Author(s):  
Mohd Basyaruddin Abdul Rahman ◽  
Khairulazhar Jumbri ◽  
Nurul Ain Mohd Ali Hanafiah ◽  
Emilia Abdulmalek ◽  
Bimo Ario Tejo ◽  
...  

1987 ◽  
Vol 58 (3) ◽  
pp. 493-502 ◽  
Author(s):  
M. Wakita ◽  
S. Hoshino

1.The effect of sugar fatty acid esters (SFEs; currently used as food additives for human consumption) on rumen volatile fatty acids (VFA) and gas production was studied with sheep rumen contents in vitro.2. Some SFEs having monoester contents of more than 70 % increased the molar proportion of propionate in conjunction with reduction in the acetate: propionate ratio when the individual SFE was added to rumen contents in a final concentration of 4 g/l. Laurate sugar ester was the most potent propionate enhancer and rumen gas depressor, the effective dose being as low as 1 g/l in a final concentration. Fatty acid esters other than SFEs had little, if any, effect on rumen VFA production and their molar proportions.3. Approximately 50% of laurate sugar ester was hydrolysed by in vitro incubation with rumen fluid for 2 h. The addition of fatty acids and sucrose was also effective in the alterations of rumen VFA and gas production. However, the effect of SFEs on in vitro rumen fermentation was significantly greater than that of their constituent fatty acids or sucrose, or both. Accordingly, the effect appeared to be ascribed to the complex action of SFE itself and to its constituents, free fatty acids and sucrose.4. SFEs, at the level of 4 g/l, reduced substantially the froth formation (ingesta volume increase) and seemed to be effective for the prevention of bloat.


1992 ◽  
Vol 3 (3) ◽  
pp. 157-164 ◽  
Author(s):  
L. M. Beauchamp ◽  
G. F. Orr ◽  
P. de Miranda ◽  
T. Bumette ◽  
T. A. Krenitsky

Eighteen amino acid esters of the antiherpetic drug, acyclovir, were synthesized as potential prodrugs for oral administration. The esters were examined for in vitro antiviral activity against herpes simplex virus Type 1 (HSV-1). They were found to have less potency than the parent compound. Their efficiencies as prodrugs were evaluated in rats by measuring the urinary recovery of acyclovir. Ten prodrugs produced greater amounts of the parent drug in the urine. The L-amino acid esters were better prodrugs than the corresponding D- or D, L-isomers, suggesting the involvement of a stereoselective transporter. The L-valyl ester, 256U87, was the best prodrug. Sixty three per cent of its administered dose was excreted as acyclovir in the urine, a considerable improvement over acyclovir itself, for which this value was 19%. Since 256U87 was stable in aqueous solutions, its conversion to acyclovir in vivo was probably enzyme catalyzed. This L-valyl ester prodrug of acyclovir is now undergoing clinical evaluation.


2019 ◽  
Vol 56 (6) ◽  
pp. 526-533
Author(s):  
Qiaoyun Zhang ◽  
Wenwei Jiang

Steroids ◽  
2017 ◽  
Vol 125 ◽  
pp. 81-92 ◽  
Author(s):  
Birgit Scholz ◽  
Renate Weiherer ◽  
Karl-Heinz Engel

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