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https://doi.org/10.2478/v10007-010-0003-1

Dizajniranje, sinteza, kinetika hidrolize i farmakodinamski profili konjugata aceklofenaka s histidinom i alaninom

ARUN RASHEED ; Department of Pharmaceutical Chemistry, Sree Vidyanikethan College of Pharmacy, Sree Sainath Nagar, Tirupati, Andhra Pradesh-517102, India
C. K. ASHOK KUMAR ; Department of Pharmaceutical Chemistry, Sree Vidyanikethan College of Pharmacy, Sree Sainath Nagar, Tirupati, Andhra Pradesh-517102, India

Puni tekst: engleski, pdf (270 KB) str. 99-109 preuzimanja: 662* citiraj
APA 6th Edition
RASHEED, A. i KUMAR, C.K.A. (2010). Design, synthesis, hydrolysis kinetics and phamacodynamic profiles of histidine and alanine conjugates of aceclofenac. Acta Pharmaceutica, 60 (1), 99-109. https://doi.org/10.2478/v10007-010-0003-1
MLA 8th Edition
RASHEED, ARUN i C. K. ASHOK KUMAR. "Design, synthesis, hydrolysis kinetics and phamacodynamic profiles of histidine and alanine conjugates of aceclofenac." Acta Pharmaceutica, vol. 60, br. 1, 2010, str. 99-109. https://doi.org/10.2478/v10007-010-0003-1. Citirano 14.10.2019.
Chicago 17th Edition
RASHEED, ARUN i C. K. ASHOK KUMAR. "Design, synthesis, hydrolysis kinetics and phamacodynamic profiles of histidine and alanine conjugates of aceclofenac." Acta Pharmaceutica 60, br. 1 (2010): 99-109. https://doi.org/10.2478/v10007-010-0003-1
Harvard
RASHEED, A., i KUMAR, C.K.A. (2010). 'Design, synthesis, hydrolysis kinetics and phamacodynamic profiles of histidine and alanine conjugates of aceclofenac', Acta Pharmaceutica, 60(1), str. 99-109. https://doi.org/10.2478/v10007-010-0003-1
Vancouver
RASHEED A, KUMAR CKA. Design, synthesis, hydrolysis kinetics and phamacodynamic profiles of histidine and alanine conjugates of aceclofenac. Acta Pharm. [Internet]. 2010 [pristupljeno 14.10.2019.];60(1):99-109. https://doi.org/10.2478/v10007-010-0003-1
IEEE
A. RASHEED i C.K.A. KUMAR, "Design, synthesis, hydrolysis kinetics and phamacodynamic profiles of histidine and alanine conjugates of aceclofenac", Acta Pharmaceutica, vol.60, br. 1, str. 99-109, 2010. [Online]. https://doi.org/10.2478/v10007-010-0003-1

Sažetak
Gastrointestinalna toksičnost aceklofenaka može se umanjiti kondenzacijom karboksilne skupine aceklofenaka s metilnim esterima aminokiselina poput histidina i alanina, pri čemu se stvaraju nove amidne veze po Schotten-Baumannovoj metodi. Fizikokemijska karakterizacija konjugata provedena je različitim analitičkim i spektralnim metodama. Nadalje, praćena je hidroliza sintetiziranih konjugata in vitro u simuliranoj gastričnoj tekućini (SGF) pri pH 1,2, simuliranoj intestinalnoj tekućini (SIF) pri pH 7,4 i simuliranoj intestinalnoj tekućini s 80 % humane plazme pri pH 7,4. Oslobađanje aceklofenaka iz konjugata s histidinom, odnosno alaninom, bilo je zanemarivo u SGF-u, u odnosu na oslobađanje u SIF-u. To ukazuje da su konjugati stabilni u želucu, dok se u SIF-u iz njih oslobađa aceklofenak. Oba konjugata daju izvrstan farmakološki odgovor i zadovoljavajući stupanj hidrolize u SIF-u i smjesi SIF-a i humane plazme. Oba konjugata pokazala su značajno smanjenu ulcerogenost i pojačano analgetsko i protuupalno djelovanje u odnosu na aceklofenak. Rezultati ukazuju na prednost konjugata u odnosu na samu ljekovitu tvar.

Ključne riječi
aceklofenak; aminokiselinski konjugat; prolijekovi; farmakokinetika; ulcerogenost

Hrčak ID: 48277

URI
https://hrcak.srce.hr/48277

[engleski]

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