Lyophilized amorphous dispersion of telmisartan in a combined carrier–alkalizer system: formulation development and in vivo study
Telmisartan suffers from low oral bioavailability due to its poor water solubility. The research work presents a formulation of solid dispersed (SD) telmisartan formulation as a ternary mixture of a drug, a polymeric carrier (poly(vinylpyrrolidone) (PVP) K30), and an alkalizer (Na2CO3). The preparat...
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American Chemical Society
2020
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my.iium.irep.882392021-02-04T07:17:36Z http://irep.iium.edu.my/88239/ Lyophilized amorphous dispersion of telmisartan in a combined carrier–alkalizer system: formulation development and in vivo study Aljapairai, Khater Ahmed Saeed Alkhalidi, Hala M. Mahmood, Syed Almurisi, Samah Hamed Doolaanea, Abd Almonem Al-Sindi, Taha A. Chatterjee, Bappaditya RS Pharmacy and materia medica Telmisartan suffers from low oral bioavailability due to its poor water solubility. The research work presents a formulation of solid dispersed (SD) telmisartan formulation as a ternary mixture of a drug, a polymeric carrier (poly(vinylpyrrolidone) (PVP) K30), and an alkalizer (Na2CO3). The preparation method, which was lyophilization of an aqueous solution containing the ingredients, was free from any organic solvent. The developed SD formulations resulted in a significant improvement in in vitro dissolution (>90% drug dissolution in 15 min) compared to pure telmisartan. Solid-state characterization by scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and X-ray diffraction (XRD) studies indicated the conversion of crystalline telmisartan into an amorphous form. Fourier transform infrared (FTIR) spectroscopy revealed the drug–polymer interaction that was responsible for reducing the chances of recrystallization. A short-term stability study showed that selected SD formulations were stable in terms of in vitro dissolution and retained their amorphous structure in ambient and accelerated conditions over 2 months. Selected formulations (drug/PVP K30/Na2CO3 as 1:1:2 or 1:2:2 weight ratio) resulted in >2.48 times relative oral bioavailability compared to marketed formulations. It was considered that the incorporation of an alkalizer and a hydrophilic polymer, and amorphization of telmisartan by lyophilization, could enhance in vitro dissolution and improve oral bioavailability. American Chemical Society 2020-12-22 Article PeerReviewed application/pdf en http://irep.iium.edu.my/88239/7/88239_Lyophilized%20amorphous%20dispersion.pdf application/pdf en http://irep.iium.edu.my/88239/8/88239_Lyophilized%20amorphous%20dispersion%20of%20telmisartan%20in%20a%20combined%20_Scopus.pdf Aljapairai, Khater Ahmed Saeed and Alkhalidi, Hala M. and Mahmood, Syed and Almurisi, Samah Hamed and Doolaanea, Abd Almonem and Al-Sindi, Taha A. and Chatterjee, Bappaditya (2020) Lyophilized amorphous dispersion of telmisartan in a combined carrier–alkalizer system: formulation development and in vivo study. ACS Omega, 5 (50). pp. 32466-32480. ISSN 2470-1343 https://pubs.acs.org/doi/10.1021/acsomega.0c04588 10.1021/acsomega.0c04588 |
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RS Pharmacy and materia medica Aljapairai, Khater Ahmed Saeed Alkhalidi, Hala M. Mahmood, Syed Almurisi, Samah Hamed Doolaanea, Abd Almonem Al-Sindi, Taha A. Chatterjee, Bappaditya Lyophilized amorphous dispersion of telmisartan in a combined carrier–alkalizer system: formulation development and in vivo study |
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Telmisartan suffers from low oral bioavailability due to its poor water solubility. The research work presents a formulation of solid dispersed (SD) telmisartan formulation as a ternary mixture of a drug, a polymeric carrier (poly(vinylpyrrolidone) (PVP) K30), and an alkalizer (Na2CO3). The preparation method, which was lyophilization of an aqueous solution containing the ingredients, was free from any organic solvent. The developed SD formulations resulted in a significant improvement in in vitro dissolution (>90% drug dissolution in 15 min) compared to pure telmisartan. Solid-state characterization by scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and X-ray diffraction (XRD) studies indicated the conversion of crystalline telmisartan into an amorphous form. Fourier transform infrared (FTIR) spectroscopy revealed the drug–polymer interaction that was responsible for reducing the chances of recrystallization. A short-term stability study showed that selected SD formulations were stable in terms of in vitro dissolution and retained their amorphous structure in ambient and accelerated conditions over 2 months. Selected formulations (drug/PVP K30/Na2CO3 as 1:1:2 or 1:2:2 weight ratio) resulted in >2.48 times relative oral bioavailability compared to marketed formulations. It was considered that the incorporation of an alkalizer and a hydrophilic polymer, and amorphization of telmisartan by lyophilization, could enhance in vitro dissolution and improve oral bioavailability. |
format |
Article |
author |
Aljapairai, Khater Ahmed Saeed Alkhalidi, Hala M. Mahmood, Syed Almurisi, Samah Hamed Doolaanea, Abd Almonem Al-Sindi, Taha A. Chatterjee, Bappaditya |
author_facet |
Aljapairai, Khater Ahmed Saeed Alkhalidi, Hala M. Mahmood, Syed Almurisi, Samah Hamed Doolaanea, Abd Almonem Al-Sindi, Taha A. Chatterjee, Bappaditya |
author_sort |
Aljapairai, Khater Ahmed Saeed |
title |
Lyophilized amorphous dispersion of telmisartan in a combined carrier–alkalizer system: formulation development and in vivo study |
title_short |
Lyophilized amorphous dispersion of telmisartan in a combined carrier–alkalizer system: formulation development and in vivo study |
title_full |
Lyophilized amorphous dispersion of telmisartan in a combined carrier–alkalizer system: formulation development and in vivo study |
title_fullStr |
Lyophilized amorphous dispersion of telmisartan in a combined carrier–alkalizer system: formulation development and in vivo study |
title_full_unstemmed |
Lyophilized amorphous dispersion of telmisartan in a combined carrier–alkalizer system: formulation development and in vivo study |
title_sort |
lyophilized amorphous dispersion of telmisartan in a combined carrier–alkalizer system: formulation development and in vivo study |
publisher |
American Chemical Society |
publishDate |
2020 |
url |
http://irep.iium.edu.my/88239/7/88239_Lyophilized%20amorphous%20dispersion.pdf http://irep.iium.edu.my/88239/8/88239_Lyophilized%20amorphous%20dispersion%20of%20telmisartan%20in%20a%20combined%20_Scopus.pdf http://irep.iium.edu.my/88239/ https://pubs.acs.org/doi/10.1021/acsomega.0c04588 |
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1691732930199552000 |
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13.18916 |