Preliminary evaluation of the in vitro release and in vivo absorption in rabbits of the modified-release dosage forms
Samo za registrovane korisnike
2013
Autori
Petrović, AleksandraPetricević, Sasa M.
Ristić, Slavica M.
Ibrić, Svetlana
Simić, Slobodanka
Đurić, Zorica
Popović, Radmila
Članak u časopisu (Objavljena verzija)
Metapodaci
Prikaz svih podataka o dokumentuApstrakt
Objective: The suitability of the rabbit as an animal model for the primary screening and selection of the pilot scale batches during the early stages of the formulation development was studied. Materials and methods: Three modified-release formulations of aminophylline consisted of Carbopol (R) 971P/HPMC K4M (F-I), and HPMC K100M (F-II) or HPMC K4M (F-III) were used. Commercial products were Aminofilin retard 350 mg tablets, Srbolek, Serbia (R-I) and Phyllocontin (R) 350, tablets Purdue Frederic, Canada (R-II). Results: Calculated release rate constants and the f2 values between R-I/F-I (84.1) and R-II/F-III (83.4) indicated similar in vitro release while the coefficient n showed presence of different mechanisms of release from Anomalous transport, Fickian diffusion to Case-II transport. Higher T-max, was found in the rabbits, dosed with F-II (12.00 h), F-III (10.50 h), and R-II (15.00 h) formulation. The highest C-max (9.22 mg/L) was obtained with F-II, similar lower values was seen ...for F-I and F-III, while commercial products showed the lowest values R-I (5.58 mg/L) and R-II (4.18 mg/L). Higher AUC values were detected for all three formulations (from 115.90 to 204.06 mgh/L) in relation to commercial products (105.33 and 113.25 mgh/L). Discussion and conclusion: The results demonstrated a good correlation of Level A (r(2) = 0.97) for the two formulations (F-I, F-III) and commercial product (R-I) indicates that there is a reasonable assumption that the rabbit might be use as a model for the preliminary comparison of scale up formulations in the early stages of the product development.
Ključne reči:
Modified release tablets / aminophylline / in vitro dissolution / rabbit / absorption in vivo / in vitro-in vivo / correlationIzvor:
Drug Development and Industrial Pharmacy, 2013, 39, 6, 889-900Izdavač:
- Informa Healthcare, London
DOI: 10.3109/03639045.2012.713364
ISSN: 0363-9045
PubMed: 22905673
WoS: 000318358300009
Scopus: 2-s2.0-84877010684
Institucija/grupa
PharmacyTY - JOUR AU - Petrović, Aleksandra AU - Petricević, Sasa M. AU - Ristić, Slavica M. AU - Ibrić, Svetlana AU - Simić, Slobodanka AU - Đurić, Zorica AU - Popović, Radmila PY - 2013 UR - https://farfar.pharmacy.bg.ac.rs/handle/123456789/2002 AB - Objective: The suitability of the rabbit as an animal model for the primary screening and selection of the pilot scale batches during the early stages of the formulation development was studied. Materials and methods: Three modified-release formulations of aminophylline consisted of Carbopol (R) 971P/HPMC K4M (F-I), and HPMC K100M (F-II) or HPMC K4M (F-III) were used. Commercial products were Aminofilin retard 350 mg tablets, Srbolek, Serbia (R-I) and Phyllocontin (R) 350, tablets Purdue Frederic, Canada (R-II). Results: Calculated release rate constants and the f2 values between R-I/F-I (84.1) and R-II/F-III (83.4) indicated similar in vitro release while the coefficient n showed presence of different mechanisms of release from Anomalous transport, Fickian diffusion to Case-II transport. Higher T-max, was found in the rabbits, dosed with F-II (12.00 h), F-III (10.50 h), and R-II (15.00 h) formulation. The highest C-max (9.22 mg/L) was obtained with F-II, similar lower values was seen for F-I and F-III, while commercial products showed the lowest values R-I (5.58 mg/L) and R-II (4.18 mg/L). Higher AUC values were detected for all three formulations (from 115.90 to 204.06 mgh/L) in relation to commercial products (105.33 and 113.25 mgh/L). Discussion and conclusion: The results demonstrated a good correlation of Level A (r(2) = 0.97) for the two formulations (F-I, F-III) and commercial product (R-I) indicates that there is a reasonable assumption that the rabbit might be use as a model for the preliminary comparison of scale up formulations in the early stages of the product development. PB - Informa Healthcare, London T2 - Drug Development and Industrial Pharmacy T1 - Preliminary evaluation of the in vitro release and in vivo absorption in rabbits of the modified-release dosage forms VL - 39 IS - 6 SP - 889 EP - 900 DO - 10.3109/03639045.2012.713364 ER -
@article{ author = "Petrović, Aleksandra and Petricević, Sasa M. and Ristić, Slavica M. and Ibrić, Svetlana and Simić, Slobodanka and Đurić, Zorica and Popović, Radmila", year = "2013", abstract = "Objective: The suitability of the rabbit as an animal model for the primary screening and selection of the pilot scale batches during the early stages of the formulation development was studied. Materials and methods: Three modified-release formulations of aminophylline consisted of Carbopol (R) 971P/HPMC K4M (F-I), and HPMC K100M (F-II) or HPMC K4M (F-III) were used. Commercial products were Aminofilin retard 350 mg tablets, Srbolek, Serbia (R-I) and Phyllocontin (R) 350, tablets Purdue Frederic, Canada (R-II). Results: Calculated release rate constants and the f2 values between R-I/F-I (84.1) and R-II/F-III (83.4) indicated similar in vitro release while the coefficient n showed presence of different mechanisms of release from Anomalous transport, Fickian diffusion to Case-II transport. Higher T-max, was found in the rabbits, dosed with F-II (12.00 h), F-III (10.50 h), and R-II (15.00 h) formulation. The highest C-max (9.22 mg/L) was obtained with F-II, similar lower values was seen for F-I and F-III, while commercial products showed the lowest values R-I (5.58 mg/L) and R-II (4.18 mg/L). Higher AUC values were detected for all three formulations (from 115.90 to 204.06 mgh/L) in relation to commercial products (105.33 and 113.25 mgh/L). Discussion and conclusion: The results demonstrated a good correlation of Level A (r(2) = 0.97) for the two formulations (F-I, F-III) and commercial product (R-I) indicates that there is a reasonable assumption that the rabbit might be use as a model for the preliminary comparison of scale up formulations in the early stages of the product development.", publisher = "Informa Healthcare, London", journal = "Drug Development and Industrial Pharmacy", title = "Preliminary evaluation of the in vitro release and in vivo absorption in rabbits of the modified-release dosage forms", volume = "39", number = "6", pages = "889-900", doi = "10.3109/03639045.2012.713364" }
Petrović, A., Petricević, S. M., Ristić, S. M., Ibrić, S., Simić, S., Đurić, Z.,& Popović, R.. (2013). Preliminary evaluation of the in vitro release and in vivo absorption in rabbits of the modified-release dosage forms. in Drug Development and Industrial Pharmacy Informa Healthcare, London., 39(6), 889-900. https://doi.org/10.3109/03639045.2012.713364
Petrović A, Petricević SM, Ristić SM, Ibrić S, Simić S, Đurić Z, Popović R. Preliminary evaluation of the in vitro release and in vivo absorption in rabbits of the modified-release dosage forms. in Drug Development and Industrial Pharmacy. 2013;39(6):889-900. doi:10.3109/03639045.2012.713364 .
Petrović, Aleksandra, Petricević, Sasa M., Ristić, Slavica M., Ibrić, Svetlana, Simić, Slobodanka, Đurić, Zorica, Popović, Radmila, "Preliminary evaluation of the in vitro release and in vivo absorption in rabbits of the modified-release dosage forms" in Drug Development and Industrial Pharmacy, 39, no. 6 (2013):889-900, https://doi.org/10.3109/03639045.2012.713364 . .