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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| Format: | Article |
| Language: | English |
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American Chemical Society
2020
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| Online Access: | http://umpir.ump.edu.my/id/eprint/31657/ http://umpir.ump.edu.my/id/eprint/31657/1/Lyophilized%20Amorphous%20Dispersion%20of%20Telmisartan%20in%20a%20Combined.pdf |
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| author | AL-japairai, Khater Ahmed Saeed Alkhalidi, Hala M. Mahmood, Syed Almurisi, Samah Hamed Doolaanea, Abd Almonem Al-Sindi, Taha A. Chatterjee, Bappaditya |
| author_facet | AL-japairai, Khater Ahmed Saeed Alkhalidi, Hala M. Mahmood, Syed Almurisi, Samah Hamed Doolaanea, Abd Almonem Al-Sindi, Taha A. Chatterjee, Bappaditya |
| author_sort | AL-japairai, Khater Ahmed Saeed |
| building | UMP Institutional Repository |
| collection | Online Access |
| description | 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 |
| first_indexed | 2025-11-15T03:03:15Z |
| format | Article |
| id | ump-31657 |
| institution | Universiti Malaysia Pahang |
| institution_category | Local University |
| language | English |
| last_indexed | 2025-11-15T03:03:15Z |
| publishDate | 2020 |
| publisher | American Chemical Society |
| recordtype | eprints |
| repository_type | Digital Repository |
| spelling | ump-316572021-07-15T09:16:46Z http://umpir.ump.edu.my/id/eprint/31657/ Lyophilized amorphous dispersion of telmisartan in a combined carrier−alkalizer system: formulation development and in vivo study AL-japairai, Khater Ahmed Saeed Alkhalidi, Hala M. Mahmood, Syed Almurisi, Samah Hamed Doolaanea, Abd Almonem Al-Sindi, Taha A. Chatterjee, Bappaditya Q Science (General) 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 2020-12-10 Article PeerReviewed pdf en http://umpir.ump.edu.my/id/eprint/31657/1/Lyophilized%20Amorphous%20Dispersion%20of%20Telmisartan%20in%20a%20Combined.pdf AL-japairai, 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. (Published) https://doi.org/10.1021/acsomega.0c04588 |
| spellingShingle | Q Science (General) AL-japairai, 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 |
| title | 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_short | 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 |
| topic | Q Science (General) |
| url | http://umpir.ump.edu.my/id/eprint/31657/ http://umpir.ump.edu.my/id/eprint/31657/ http://umpir.ump.edu.my/id/eprint/31657/1/Lyophilized%20Amorphous%20Dispersion%20of%20Telmisartan%20in%20a%20Combined.pdf |