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/30970/ http://umpir.ump.edu.my/id/eprint/30970/1/Lyophilized%20amorphous%20dispersion%20of%20telmisartan%20in%20a%20combined%20carrier.pdf |
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| author | Al-Japairai, Khater A. S. Alkhalidi, Hala M. Mahmood, Syed Almurisi, Samah H. Doolaanea, Abd Almonem Al-Sindi, Taha A. Chatterjee, Bappaditya |
| author_facet | Al-Japairai, Khater A. S. Alkhalidi, Hala M. Mahmood, Syed Almurisi, Samah H. Doolaanea, Abd Almonem Al-Sindi, Taha A. Chatterjee, Bappaditya |
| author_sort | Al-Japairai, Khater A. S. |
| 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 | 2025-11-15T03:00:30Z |
| format | Article |
| id | ump-30970 |
| institution | Universiti Malaysia Pahang |
| institution_category | Local University |
| language | English |
| last_indexed | 2025-11-15T03:00:30Z |
| publishDate | 2020 |
| publisher | American Chemical Society |
| recordtype | eprints |
| repository_type | Digital Repository |
| spelling | ump-309702021-05-17T01:39:43Z http://umpir.ump.edu.my/id/eprint/30970/ Lyophilized amorphous dispersion of telmisartan in a combined carrier–alkalizer system: formulation development and in vivo study Al-Japairai, Khater A. S. Alkhalidi, Hala M. Mahmood, Syed Almurisi, Samah H. Doolaanea, Abd Almonem Al-Sindi, Taha A. Chatterjee, Bappaditya TP Chemical technology 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 pdf en cc_by_nc_nd_4 http://umpir.ump.edu.my/id/eprint/30970/1/Lyophilized%20amorphous%20dispersion%20of%20telmisartan%20in%20a%20combined%20carrier.pdf Al-Japairai, Khater A. S. and Alkhalidi, Hala M. and Mahmood, Syed and Almurisi, Samah H. 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 https://doi.org/10.1021/acsomega.0c04588 |
| spellingShingle | TP Chemical technology Al-Japairai, Khater A. S. Alkhalidi, Hala M. Mahmood, Syed Almurisi, Samah H. 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 | TP Chemical technology |
| url | http://umpir.ump.edu.my/id/eprint/30970/ http://umpir.ump.edu.my/id/eprint/30970/ http://umpir.ump.edu.my/id/eprint/30970/ http://umpir.ump.edu.my/id/eprint/30970/1/Lyophilized%20amorphous%20dispersion%20of%20telmisartan%20in%20a%20combined%20carrier.pdf |