Lazić, Irina

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  • Lazić, Irina (1)
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Formulation of ibuprofen-modified release hydrophilic and lipid matrix tablets using co-processed excipients

Lazić, Irina; Kučević, Sabina; Ćirin-Varađan, Slobodanka; Aleksić, Ivana; Đuriš, Jelena

(Savez farmaceutskih udruženja Srbije (SFUS), 2022)

TY  - CONF
AU  - Lazić, Irina
AU  - Kučević, Sabina
AU  - Ćirin-Varađan, Slobodanka
AU  - Aleksić, Ivana
AU  - Đuriš, Jelena
PY  - 2022
UR  - https://farfar.pharmacy.bg.ac.rs/handle/123456789/4569
AB  - Formulation of modified-release ibuprofen tablets presents a challenge due to its high
dose, limited compressibility and compactibility. The potential for preparing ibuprofen
modified release matrix tablets, by direct compression procedure using co-processed
excipients (1, 2), was evaluated. Co-processed excipients of hydrophilic and lipid properties
were used. Commercially available co-processed excipient based on
hydroxypropylmethylcellulose and lactose (RetaLac ®), as well as co-processed excipient
made in-house, using lipid matrix forming agent based on glyceryl palmitostearate
(Precirol® ) and lactose were used. The influence of co-processed excipient type, ibuprofen
ammount in tablets (25% and 50%) and the compression load (100 and 500 kg) on the
mechanical properties of the hydrophilic or lipid matrix tablets was evaluated. Also,
ibuprofen release rate was investigated in a rotating paddle apparatus with medium change
(0.1M HCl and phosphate buffer pH 6.8). The tensile strength of formulations was in the
range of 0.5-2 MPa. The compression load and the co-processed excipient type showed a
significant effect on tensile strength. Ibuprofen was released in a sustained manner from all
formulations, with the amount released after 8 hours varying from 35 to 80%, depending on
the matrix forming material type. The release of ibuprofen from lipid matrix tablets was
slower compared to hydrophilic tablets, with neither the compression load nor the ibuprofen
content showing a significant effect. Zero-order kinetics was achieved from both types of
matrix tablets. Based on the obtained results, it can be concluded that co-processed
excipients enable direct compression of ibuprofen modified release hydrophilic and lipid
matrix tablets.
AB  - Formulacija tableta sa modifikovanim oslobađanjem ibuprofena predstavlja izazov
zbog visoke doze lekovite supstance ograničene kompresibilnosti i kompaktibilnosti. U ovom
radu procenjena je mogućnost izrade matriks tableta sa modifikovanim oslobađanjem
ibuprofena postupkom direktne kompresije uz primenu koprocesovanih ekscipijenasa (1, 2).
Upotrebljeni su koprocesovani ekscipijensi hidrofilnih i lipidnih karakteristika. Korišćeni su
komercijalno dostupan koprocesovani ekscipijens na bazi hidroksipropilmetilceluloze i
laktoze (RetaLac® ), kao i koprocesovani ekscipijens izrađen u laboratorijskim uslovima, kao
lipidno matriks formirajuće sredstvo na bazi glicerilpalmitostearata (Precirol ®) i laktoze.
Praćen je uticaj vrste koprocesovanog ekscipijensa, udela ibuprofena u tabletama (25%,
odnosno 50%) i opterećenja pri kompresiji (100, odnosno 500 kg) na mehaničke
karakteristike izrađenih hidrofilnih, odnosno lipidnih matriks tableta. Takođe, ispitivana je
brzina oslobađanja ibuprofena iz pripremljenih matriks tableta u aparaturi sa rotirajućim
lopaticama uz izmenu medijuma (0,1M HCl i fosfatni pufer pH 6,8). Zatezna čvrstoća
ispitivanih formulacija je bila u opsegu ~ 0.5-2 MPa. Opterećenje pri kompresiji i tip
koprocesovanog ekscipijensa su pokazali značajan uticaj na zateznu čvrstoću. Ibuprofen se iz
svih formulacija oslobađao usporeno, pri čemu je količina oslobođena nakon 8 sati
ispitivanja varirala od 35 do 80%, u zavisnosti od prirode matriks formirajućeg materijala.
Oslobađanje ibuprofena iz lipidnih matriks tableta je bilo sporije u poređenju sa hidrofilnim
tabletama, pri čemu ni opterećenje pri kompresiji ni udeo ibuprofena nisu pokazali značajan
uticaj. Iz oba tipa matriks tableta postignuto je oslobađanje ibuprofena kinetikom nultog
reda. Na osnovu dobijenih rezultata može se zaključiti da koprocesovani ekscipijensi
omogućavaju izradu hidrofilnih i lipidnih matriks tableta sa modifikovanim oslobađanjem
ibuprofena postupkom direktne kompresije.
PB  - Savez farmaceutskih udruženja Srbije (SFUS)
C3  - Arhiv za farmaciju
T1  - Formulation of ibuprofen-modified release hydrophilic and lipid matrix tablets using co-processed excipients
T1  - Formulacija hidrofilnih i lipidnih matriks tableta sa modifikovanim oslobađanjem ibuprofena primenom koprocesovanih ekscipijenasa
VL  - 72
IS  - 4 suplement
SP  - S3400
EP  - S401
UR  - https://hdl.handle.net/21.15107/rcub_farfar_4569
ER  - 
@conference{
author = "Lazić, Irina and Kučević, Sabina and Ćirin-Varađan, Slobodanka and Aleksić, Ivana and Đuriš, Jelena",
year = "2022",
abstract = "Formulation of modified-release ibuprofen tablets presents a challenge due to its high
dose, limited compressibility and compactibility. The potential for preparing ibuprofen
modified release matrix tablets, by direct compression procedure using co-processed
excipients (1, 2), was evaluated. Co-processed excipients of hydrophilic and lipid properties
were used. Commercially available co-processed excipient based on
hydroxypropylmethylcellulose and lactose (RetaLac ®), as well as co-processed excipient
made in-house, using lipid matrix forming agent based on glyceryl palmitostearate
(Precirol® ) and lactose were used. The influence of co-processed excipient type, ibuprofen
ammount in tablets (25% and 50%) and the compression load (100 and 500 kg) on the
mechanical properties of the hydrophilic or lipid matrix tablets was evaluated. Also,
ibuprofen release rate was investigated in a rotating paddle apparatus with medium change
(0.1M HCl and phosphate buffer pH 6.8). The tensile strength of formulations was in the
range of 0.5-2 MPa. The compression load and the co-processed excipient type showed a
significant effect on tensile strength. Ibuprofen was released in a sustained manner from all
formulations, with the amount released after 8 hours varying from 35 to 80%, depending on
the matrix forming material type. The release of ibuprofen from lipid matrix tablets was
slower compared to hydrophilic tablets, with neither the compression load nor the ibuprofen
content showing a significant effect. Zero-order kinetics was achieved from both types of
matrix tablets. Based on the obtained results, it can be concluded that co-processed
excipients enable direct compression of ibuprofen modified release hydrophilic and lipid
matrix tablets., Formulacija tableta sa modifikovanim oslobađanjem ibuprofena predstavlja izazov
zbog visoke doze lekovite supstance ograničene kompresibilnosti i kompaktibilnosti. U ovom
radu procenjena je mogućnost izrade matriks tableta sa modifikovanim oslobađanjem
ibuprofena postupkom direktne kompresije uz primenu koprocesovanih ekscipijenasa (1, 2).
Upotrebljeni su koprocesovani ekscipijensi hidrofilnih i lipidnih karakteristika. Korišćeni su
komercijalno dostupan koprocesovani ekscipijens na bazi hidroksipropilmetilceluloze i
laktoze (RetaLac® ), kao i koprocesovani ekscipijens izrađen u laboratorijskim uslovima, kao
lipidno matriks formirajuće sredstvo na bazi glicerilpalmitostearata (Precirol ®) i laktoze.
Praćen je uticaj vrste koprocesovanog ekscipijensa, udela ibuprofena u tabletama (25%,
odnosno 50%) i opterećenja pri kompresiji (100, odnosno 500 kg) na mehaničke
karakteristike izrađenih hidrofilnih, odnosno lipidnih matriks tableta. Takođe, ispitivana je
brzina oslobađanja ibuprofena iz pripremljenih matriks tableta u aparaturi sa rotirajućim
lopaticama uz izmenu medijuma (0,1M HCl i fosfatni pufer pH 6,8). Zatezna čvrstoća
ispitivanih formulacija je bila u opsegu ~ 0.5-2 MPa. Opterećenje pri kompresiji i tip
koprocesovanog ekscipijensa su pokazali značajan uticaj na zateznu čvrstoću. Ibuprofen se iz
svih formulacija oslobađao usporeno, pri čemu je količina oslobođena nakon 8 sati
ispitivanja varirala od 35 do 80%, u zavisnosti od prirode matriks formirajućeg materijala.
Oslobađanje ibuprofena iz lipidnih matriks tableta je bilo sporije u poređenju sa hidrofilnim
tabletama, pri čemu ni opterećenje pri kompresiji ni udeo ibuprofena nisu pokazali značajan
uticaj. Iz oba tipa matriks tableta postignuto je oslobađanje ibuprofena kinetikom nultog
reda. Na osnovu dobijenih rezultata može se zaključiti da koprocesovani ekscipijensi
omogućavaju izradu hidrofilnih i lipidnih matriks tableta sa modifikovanim oslobađanjem
ibuprofena postupkom direktne kompresije.",
publisher = "Savez farmaceutskih udruženja Srbije (SFUS)",
journal = "Arhiv za farmaciju",
title = "Formulation of ibuprofen-modified release hydrophilic and lipid matrix tablets using co-processed excipients, Formulacija hidrofilnih i lipidnih matriks tableta sa modifikovanim oslobađanjem ibuprofena primenom koprocesovanih ekscipijenasa",
volume = "72",
number = "4 suplement",
pages = "S3400-S401",
url = "https://hdl.handle.net/21.15107/rcub_farfar_4569"
}
Lazić, I., Kučević, S., Ćirin-Varađan, S., Aleksić, I.,& Đuriš, J.. (2022). Formulation of ibuprofen-modified release hydrophilic and lipid matrix tablets using co-processed excipients. in Arhiv za farmaciju
Savez farmaceutskih udruženja Srbije (SFUS)., 72(4 suplement), S3400-S401.
https://hdl.handle.net/21.15107/rcub_farfar_4569
Lazić I, Kučević S, Ćirin-Varađan S, Aleksić I, Đuriš J. Formulation of ibuprofen-modified release hydrophilic and lipid matrix tablets using co-processed excipients. in Arhiv za farmaciju. 2022;72(4 suplement):S3400-S401.
https://hdl.handle.net/21.15107/rcub_farfar_4569 .
Lazić, Irina, Kučević, Sabina, Ćirin-Varađan, Slobodanka, Aleksić, Ivana, Đuriš, Jelena, "Formulation of ibuprofen-modified release hydrophilic and lipid matrix tablets using co-processed excipients" in Arhiv za farmaciju, 72, no. 4 suplement (2022):S3400-S401,
https://hdl.handle.net/21.15107/rcub_farfar_4569 .