Mucoadhesive buccal tablets with propranolol hydrochloride: Formulation development and in vivo performances in experimental essential hypertension
Samo za registrovane korisnike
2021
Autori
Kurćubić, IvanaVajić, Una-Jovana
Cvijić, Sandra
Crevar-Sakač, Milkica
Bogavac-Stanojević, Nataša
Miloradović, Zoran
Mihajlović-Stanojević, Nevena
Ivanov, Milan
Karanović, Danijela
Jovović, Đurđica
Đuriš, Jelena
Članak u časopisu (Objavljena verzija)
Metapodaci
Prikaz svih podataka o dokumentuApstrakt
The objective of this study was to formulate extended-release mucoadhesive buccal tablets of propranolol hydrochloride in order to provide a prolonged absorption of propranolol hydrochloride from the buccal mucosa and to reduce presystemic metabolism and thus provide a better therapeutic effect. Besides, the aim was to perform comparative in vivo pharmacokinetic and hemodynamic studies of the developed extended-release (ER) propranolol hydrochloride 10 mg mucoadhesive buccal tablets and commercial immediate-release (IR) propranolol hydrochloride 10 mg tablets in spontaneously hypertensive rats. Formulation with 15% polyethylene oxide showed the highest degree of propranolol hydrochloride permeation, satisfactory mucoadhesiveness, and extended-release of propranolol hydrochloride, thus it was selected for further in vivo study. The pharmacokinetic study in rats showed the superiority of ER mucoadhesive buccal tablets over IR tablets in terms of propranolol hydrochloride absorption exten...t (AUC values: 70.32 ± 19.56 versus 31.69 ± 6.97 μg⋅h/mL), although lower maximum plasma propranolol hydrochloride concentration (Cmax) was achieved. However, no statistically significant difference was observed in Cmax between these treatments. The hemodynamic study showed that ER mucoadhesive buccal tablets provide a more pronounced decrease primarily in heart rate, but also in systolic and diastolic arterial pressure, as well as a longer heart rate reduction compared to IR tablets.
Ključne reči:
Spontaneously hypertensive rats / Essential hypertension / Extended-release / Mucoadhesive buccal tablets / Pharmacokinetics / Propranolol hydrochlorideIzvor:
International Journal of Pharmaceutics, 2021, 610Izdavač:
- Elsevier B.V.
Finansiranje / projekti:
- Ministarstvo nauke, tehnološkog razvoja i inovacija Republike Srbije, institucionalno finansiranje - 200161 (Univerzitet u Beogradu, Farmaceutski fakultet) (RS-MESTD-inst-2020-200161)
- Ministarstvo nauke, tehnološkog razvoja i inovacija Republike Srbije, institucionalno finansiranje - 200015 (Univerzitet u Beogradu, Institut za medicinska istraživanja) (RS-MESTD-inst-2020-200015)
DOI: 10.1016/j.ijpharm.2021.121266
ISSN: 0378-5173
WoS: 000718955600008
Scopus: 2-s2.0-85118892119
Institucija/grupa
PharmacyTY - JOUR AU - Kurćubić, Ivana AU - Vajić, Una-Jovana AU - Cvijić, Sandra AU - Crevar-Sakač, Milkica AU - Bogavac-Stanojević, Nataša AU - Miloradović, Zoran AU - Mihajlović-Stanojević, Nevena AU - Ivanov, Milan AU - Karanović, Danijela AU - Jovović, Đurđica AU - Đuriš, Jelena PY - 2021 PY - 2021 UR - https://farfar.pharmacy.bg.ac.rs/handle/123456789/3990 AB - The objective of this study was to formulate extended-release mucoadhesive buccal tablets of propranolol hydrochloride in order to provide a prolonged absorption of propranolol hydrochloride from the buccal mucosa and to reduce presystemic metabolism and thus provide a better therapeutic effect. Besides, the aim was to perform comparative in vivo pharmacokinetic and hemodynamic studies of the developed extended-release (ER) propranolol hydrochloride 10 mg mucoadhesive buccal tablets and commercial immediate-release (IR) propranolol hydrochloride 10 mg tablets in spontaneously hypertensive rats. Formulation with 15% polyethylene oxide showed the highest degree of propranolol hydrochloride permeation, satisfactory mucoadhesiveness, and extended-release of propranolol hydrochloride, thus it was selected for further in vivo study. The pharmacokinetic study in rats showed the superiority of ER mucoadhesive buccal tablets over IR tablets in terms of propranolol hydrochloride absorption extent (AUC values: 70.32 ± 19.56 versus 31.69 ± 6.97 μg⋅h/mL), although lower maximum plasma propranolol hydrochloride concentration (Cmax) was achieved. However, no statistically significant difference was observed in Cmax between these treatments. The hemodynamic study showed that ER mucoadhesive buccal tablets provide a more pronounced decrease primarily in heart rate, but also in systolic and diastolic arterial pressure, as well as a longer heart rate reduction compared to IR tablets. PB - Elsevier B.V. T2 - International Journal of Pharmaceutics T1 - Mucoadhesive buccal tablets with propranolol hydrochloride: Formulation development and in vivo performances in experimental essential hypertension VL - 610 DO - 10.1016/j.ijpharm.2021.121266 ER -
@article{ author = "Kurćubić, Ivana and Vajić, Una-Jovana and Cvijić, Sandra and Crevar-Sakač, Milkica and Bogavac-Stanojević, Nataša and Miloradović, Zoran and Mihajlović-Stanojević, Nevena and Ivanov, Milan and Karanović, Danijela and Jovović, Đurđica and Đuriš, Jelena", year = "2021, 2021", abstract = "The objective of this study was to formulate extended-release mucoadhesive buccal tablets of propranolol hydrochloride in order to provide a prolonged absorption of propranolol hydrochloride from the buccal mucosa and to reduce presystemic metabolism and thus provide a better therapeutic effect. Besides, the aim was to perform comparative in vivo pharmacokinetic and hemodynamic studies of the developed extended-release (ER) propranolol hydrochloride 10 mg mucoadhesive buccal tablets and commercial immediate-release (IR) propranolol hydrochloride 10 mg tablets in spontaneously hypertensive rats. Formulation with 15% polyethylene oxide showed the highest degree of propranolol hydrochloride permeation, satisfactory mucoadhesiveness, and extended-release of propranolol hydrochloride, thus it was selected for further in vivo study. The pharmacokinetic study in rats showed the superiority of ER mucoadhesive buccal tablets over IR tablets in terms of propranolol hydrochloride absorption extent (AUC values: 70.32 ± 19.56 versus 31.69 ± 6.97 μg⋅h/mL), although lower maximum plasma propranolol hydrochloride concentration (Cmax) was achieved. However, no statistically significant difference was observed in Cmax between these treatments. The hemodynamic study showed that ER mucoadhesive buccal tablets provide a more pronounced decrease primarily in heart rate, but also in systolic and diastolic arterial pressure, as well as a longer heart rate reduction compared to IR tablets.", publisher = "Elsevier B.V.", journal = "International Journal of Pharmaceutics", title = "Mucoadhesive buccal tablets with propranolol hydrochloride: Formulation development and in vivo performances in experimental essential hypertension", volume = "610", doi = "10.1016/j.ijpharm.2021.121266" }
Kurćubić, I., Vajić, U., Cvijić, S., Crevar-Sakač, M., Bogavac-Stanojević, N., Miloradović, Z., Mihajlović-Stanojević, N., Ivanov, M., Karanović, D., Jovović, Đ.,& Đuriš, J.. (2021). Mucoadhesive buccal tablets with propranolol hydrochloride: Formulation development and in vivo performances in experimental essential hypertension. in International Journal of Pharmaceutics Elsevier B.V.., 610. https://doi.org/10.1016/j.ijpharm.2021.121266
Kurćubić I, Vajić U, Cvijić S, Crevar-Sakač M, Bogavac-Stanojević N, Miloradović Z, Mihajlović-Stanojević N, Ivanov M, Karanović D, Jovović Đ, Đuriš J. Mucoadhesive buccal tablets with propranolol hydrochloride: Formulation development and in vivo performances in experimental essential hypertension. in International Journal of Pharmaceutics. 2021;610. doi:10.1016/j.ijpharm.2021.121266 .
Kurćubić, Ivana, Vajić, Una-Jovana, Cvijić, Sandra, Crevar-Sakač, Milkica, Bogavac-Stanojević, Nataša, Miloradović, Zoran, Mihajlović-Stanojević, Nevena, Ivanov, Milan, Karanović, Danijela, Jovović, Đurđica, Đuriš, Jelena, "Mucoadhesive buccal tablets with propranolol hydrochloride: Formulation development and in vivo performances in experimental essential hypertension" in International Journal of Pharmaceutics, 610 (2021), https://doi.org/10.1016/j.ijpharm.2021.121266 . .