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Original scientific paper
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

Fulltext: english, pdf (270 KB) pages 99-109 downloads: 745* cite
APA 6th Edition
RASHEED, A. & 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 and C. K. ASHOK KUMAR. "Design, synthesis, hydrolysis kinetics and phamacodynamic profiles of histidine and alanine conjugates of aceclofenac." Acta Pharmaceutica, vol. 60, no. 1, 2010, pp. 99-109. https://doi.org/10.2478/v10007-010-0003-1. Accessed 24 Nov. 2020.
Chicago 17th Edition
RASHEED, ARUN and C. K. ASHOK KUMAR. "Design, synthesis, hydrolysis kinetics and phamacodynamic profiles of histidine and alanine conjugates of aceclofenac." Acta Pharmaceutica 60, no. 1 (2010): 99-109. https://doi.org/10.2478/v10007-010-0003-1
Harvard
RASHEED, A., and KUMAR, C.K.A. (2010). 'Design, synthesis, hydrolysis kinetics and phamacodynamic profiles of histidine and alanine conjugates of aceclofenac', Acta Pharmaceutica, 60(1), pp. 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 [cited 2020 November 24];60(1):99-109. https://doi.org/10.2478/v10007-010-0003-1
IEEE
A. RASHEED and C.K.A. KUMAR, "Design, synthesis, hydrolysis kinetics and phamacodynamic profiles of histidine and alanine conjugates of aceclofenac", Acta Pharmaceutica, vol.60, no. 1, pp. 99-109, 2010. [Online]. https://doi.org/10.2478/v10007-010-0003-1

Abstracts
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.

Keywords
aceklofenak; aminokiselinski konjugat; prolijekovi; farmakokinetika; ulcerogenost

Hrčak ID: 48277

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

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