ENHANCING THE DISSOLUTION RATE OF TICAGRELOR THROUGH PREPARATION WITH CYCLODEXTRINS – TABLET FORMULATION AND EVALUATION

This research investigates the effect of solid-state modification of ticagrelor (TICA) by combination with selected cyclodextrins (CDs) on the release of the active pharmaceutical ingredient from formulated tablets.Particle size distribution, flowability tests, and volumetric studies were conducted on the powders intended for compression.Based on the obtained results, new oral dosage forms utilising TICA-CD formulations were designed and evaluated.The use of TICA-CD binary systems enabled the preparation of direct compression tablets with reduced drug dosage (45 mg).It was demonstrated that the type of betacyclodextrin used did not significantly influence the dissolution rate.The release of the active substance from the tablets exceeded 90% after 75 minutes under conditions of varying pH.Thus, the complexation of ticagrelor with cyclodextrins resulted in significantly higher rates of active substance release.The results of the current study suggested that TICA-CD inclusion complexes can be incorporated into oral dosage forms that can subsequently be used in therapeutic practice. RezumatAcest studiu cerceteaz modul n care modificarea strii solide a ticagrelorului (TICA) prin asocierea cu ciclodextrine (CDs) influeneaz eliberarea ingredientului activ farmaceutic din comprimatele formulate.Au fost realizate analize de distribuie granulometric a particulelor, teste de fluiditate i studii volumetrice asupra pulberilor destinate procesului de comprimare direct.Pe baza rezultatelor obinute, au fost realizate i evaluate noi forme de dozare, utiliznd formlrile TICA-CD.Utilizarea sistemelor TICA-CD a permis obinerea comprimatelor cu doze reduse de medicament (45 mg), prin comprimare direct.S-a demonstrat c tipul de beta-ciclodextrin nu are un impact semnificativ asupra ratei de eliberare.Cedarea substanei active din comprimate a depit 90% dup 75 de minute, n condiii variabile de pH.Astfel, complexarea ticagrelorului cu ciclodextrine a condus la o eliberare semnificativ mai rapid a substanei active.Rezultatele studiului sugereaz c pulberile ce conin complecii de incluziune TICA-CD pot fi ncorporate n forme formaceutice destinate administrrii pe cale oral, care pot fi utilizate n practica terapeutic.

Authors

Publication Details

Journal
FARMACIA
Published
2025-04-29
DOI
https://doi.org/10.31925/farmacia.2025.2.23
Primary Topic
Biosimilars and Bioanalytical Methods
Type
article
Field-Weighted Citation Impact
0.00

Funders

Controls
|||
ALL TIME
JAN
FEB
MAR
APR
MAY
JUN
JUL
AUG
SEP
OCT
article

ENHANCING THE DISSOLUTION RATE OF TICAGRELOR THROUGH PREPARATION WITH CYCLODEXTRINS – TABLET FORMULATION AND EVALUATION

Laurentiu Marin
FARMACIA
Biosimilars and Bioanalytical Methods
article

ENHANCING THE DISSOLUTION RATE OF TICAGRELOR THROUGH PREPARATION WITH CYCLODEXTRINS – TABLET FORMULATION AND EVALUATION

Laurentiu Marin
article en

Abstract

This research investigates the effect of solid-state modification of ticagrelor (TICA) by combination with selected cyclodextrins (CDs) on the release of the active pharmaceutical ingredient from formulated tablets.Particle size distribution, flowability tests, and volumetric studies were conducted on the powders intended for compression.Based on the obtained results, new oral dosage forms utilising TICA-CD formulations were designed and evaluated.The use of TICA-CD binary systems enabled the preparation of direct compression tablets with reduced drug dosage (45 mg).It was demonstrated that the type of betacyclodextrin used did not significantly influence the dissolution rate.The release of the active substance from the tablets exceeded 90% after 75 minutes under conditions of varying pH.Thus, the complexation of ticagrelor with cyclodextrins resulted in significantly higher rates of active substance release.The results of the current study suggested that TICA-CD inclusion complexes can be incorporated into oral dosage forms that can subsequently be used in therapeutic practice. RezumatAcest studiu cerceteaz modul n care modificarea strii solide a ticagrelorului (TICA) prin asocierea cu ciclodextrine (CDs) influeneaz eliberarea ingredientului activ farmaceutic din comprimatele formulate.Au fost realizate analize de distribuie granulometric a particulelor, teste de fluiditate i studii volumetrice asupra pulberilor destinate procesului de comprimare direct.Pe baza rezultatelor obinute, au fost realizate i evaluate noi forme de dozare, utiliznd formlrile TICA-CD.Utilizarea sistemelor TICA-CD a permis obinerea comprimatelor cu doze reduse de medicament (45 mg), prin comprimare direct.S-a demonstrat c tipul de beta-ciclodextrin nu are un impact semnificativ asupra ratei de eliberare.Cedarea substanei active din comprimate a depit 90% dup 75 de minute, n condiii variabile de pH.Astfel, complexarea ticagrelorului cu ciclodextrine a condus la o eliberare semnificativ mai rapid a substanei active.Rezultatele studiului sugereaz c pulberile ce conin complecii de incluziune TICA-CD pot fi ncorporate n forme formaceutice destinate administrrii pe cale oral, care pot fi utilizate n practica terapeutic.

FARMACIAVol. 73(2)
CEEPUS
Openalex Percentile: Top 80%
Biosimilars and Bioanalytical Methods
AI Navigator

Ask Laika to Summarize, Analyze, and Connect papers live on the map.

Summarize Papers & Methodologies

Extract key findings, datasets, and comparative methods across publications.

Benchmark Rankings & Visual Analytics

Rank top research institutions, authors, funders, topics, and journals by Field-Weighted Citation Impact (FWCI) and paper volume with instant charts.

Connect Distant Disciplines

Bridge topological clusters on the map to find hidden collaborative intersections.

ENHANCING THE DISSOLUTION RATE OF TICAGRELOR THROUGH PREPARATION WITH CYCLODEXTRINS – TABLET FORMULATION AND EVALUATION — Laurentiu Marin · FARMACIA (2025) | TGRS Research Map | TGRS