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Synthesis of transdermal permeation enhancers based on piperidine carboxylic acids
Fratričová, Veronika ; Vávrová, Kateřina (advisor) ; Hrabálek, Alexandr (referee)
Transdermal permeation enhancers are chemical compounds, which promote drug absorption through the skin via the barrier resistance decrease. The model structure was molecule of transkarbam 12. I have synthesized these compounds: 2-(decyloxycarbonyl)piperidinium bromide 2-(dodecyloxycarbonyl)piperidinium bromide 1-acetylpiperidine-2-carboxylic acid decyl ester 1-acetylpiperidine-2-carboxylic acid dodecyl ester (R)-N -acetylpiperidin-2-carboxylic acid decyl ester (R)-N -acetylpiperidin-2-carboxylic acid dodecyl ester (R)-N -acetylpiperidin-3-carboxylic acid decyl ester (R)-N -acetylpiperidin-3-carboxylic acid dodecyl ester 2-(decyloxycarbonyl)piperidinium 2-(decyloxycarbonyl)piperidine-1-carbamate 2-(dodecyloxycarbonyl)piperidinium 2-(dodecyloxycarbonyl)piperidine-1-carbamate Transdermal permeation-enhancing activity of the prepared compounds was evaluated on the porcine skin in the Franz diffusion cells using theophylline as the model drug. The enhancement ratio values were compared with the results of structurally related compounds synthesized in the previous diploma theses. The results showed that the least active substances were the hydrobromides, N-acetylderivatives were more active, comparable with model enhancer transkarbam 12. No significant difference between racemates and (R)-izomers of N-...
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Synthesis of transdermal permeation enhancers on basis of piperidine carboxylic acids derivatives I
Fratričová, Veronika ; Hrabálek, Alexandr (advisor) ; Vávrová, Kateřina (referee)
4 SYNTHESIS OF TRANSDERMAL PERMEATION ACCELERANTS ON THE BASIS OF PIPERIDIN-3-KARBOXYLIC ACID Veronika Fratričová Supervisor: Doc. PharmDr. Alexandr Hrabálek, Csc. Transdermal permation enhancers are chemical compounds which facilitate the drug delivery through the skin. They influence the stratum corneum, as the outer layer of the epidermis. Basic requirements for the enhancer are safety, drug compatibility, biodegradability, and that they must be non-toxic and non-irritating. The model structure was effective trancarbame 12, according to which have been synthetized its cyclic analogues: Hydrobromide of piperidine-3-carboxylic acid decylester Hydrobromide of piperidine-3-carboxylic acid dodecylester N-acetylderivative of piperidine-3-carboxylic acid decylester N-acetylderivative of piperidine-3-carboxylic acid dodecylester 3-(decyloxycarbonyl)piperidinium-3-(decyloxycarbonyl)piperidine-1-carbamate 3-(dodecylexycarbonyl)piperidinium-3-(dodecyloxycarbonyl)piperidine-1-carbamate Those compounds have been characterized by common spectral methods. The transdermal permation activity has been consequently evaluated on the porcine skin in the Franz cells, using theophylline as the model penetrating drug. The activity has been evaluated using the HPLC method and determined by the Microsoft Excel. The results...
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Synthesis of transdermal permeation enhancers based on piperidine carboxylic acids
Fratričová, Veronika ; Vávrová, Kateřina (advisor) ; Hrabálek, Alexandr (referee)
Transdermal permeation enhancers are chemical compounds, which promote drug absorption through the skin via the barrier resistance decrease. The model structure was molecule of transkarbam 12. I have synthesized these compounds: 2-(decyloxycarbonyl)piperidinium bromide 2-(dodecyloxycarbonyl)piperidinium bromide 1-acetylpiperidine-2-carboxylic acid decyl ester 1-acetylpiperidine-2-carboxylic acid dodecyl ester (R)-N -acetylpiperidin-2-carboxylic acid decyl ester (R)-N -acetylpiperidin-2-carboxylic acid dodecyl ester (R)-N -acetylpiperidin-3-carboxylic acid decyl ester (R)-N -acetylpiperidin-3-carboxylic acid dodecyl ester 2-(decyloxycarbonyl)piperidinium 2-(decyloxycarbonyl)piperidine-1-carbamate 2-(dodecyloxycarbonyl)piperidinium 2-(dodecyloxycarbonyl)piperidine-1-carbamate Transdermal permeation-enhancing activity of the prepared compounds was evaluated on the porcine skin in the Franz diffusion cells using theophylline as the model drug. The enhancement ratio values were compared with the results of structurally related compounds synthesized in the previous diploma theses. The results showed that the least active substances were the hydrobromides, N-acetylderivatives were more active, comparable with model enhancer transkarbam 12. No significant difference between racemates and (R)-izomers of N-...
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