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Improved solubility of telmisartan by using freeze-dried solid dispersion method

Introduction: Drugs with poor water solubility often result in low dissolution and consequently reduced bioavailability. Telmisartan is an angiotensin II receptor antagonist, which is used in the prevention and treatment of hypertension. One of the major problems with this drug is it has poor water...

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Main Authors: Aljapairai, Khater Ahmed Saeed, Chatterjee, Bappaditya
Format: Conference or Workshop Item
Language:English
English
Published: 2017
Subjects:
RS192 Materia Medica-Pharmaceutical Technology
Online Access:http://irep.iium.edu.my/68354/7/354%20Pahang%20RnD%20Prog%20book.pdf
http://irep.iium.edu.my/68354/19/Improved%20solubility%20of%20telmisartan%20by%20freeze-dried%20solid%20dispersion_Khater.pdf
http://irep.iium.edu.my/68354/
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spelling my.iium.irep.683542018-12-27T07:34:59Z http://irep.iium.edu.my/68354/ Improved solubility of telmisartan by using freeze-dried solid dispersion method Aljapairai, Khater Ahmed Saeed Chatterjee, Bappaditya RS192 Materia Medica-Pharmaceutical Technology Introduction: Drugs with poor water solubility often result in low dissolution and consequently reduced bioavailability. Telmisartan is an angiotensin II receptor antagonist, which is used in the prevention and treatment of hypertension. One of the major problems with this drug is it has poor water solubility that lead to its low bioavailability. Objective: The aim of this study is to improve solubility of telmisartan by using freeze-dried solid dispersion (SD) method. Methods: PVP K30 was selected as carrier and sodium carbonate (Na2CO3) as pH modifier for the formulation. After checking the compatibility between all ingredients by differential scanning calorimetry (DSC) and attenuated total reflectance spectroscopy (ATR-FTIR), the SD was prepared by using freeze-dried method (Martyn Christ, Germany). The selected drug: carrier ratios were 1:3, 1:5, and 1:10 (w/w). The SD powders were evaluated for aqueous solubility. Telmisartan concentration was measured by a high performance liquid chromatographic system (HPLC) with UV detector at 231 nm wavelength. Results: The SD containing telmisartan: PVP K30 (1:5) showed the highest solubility (151.46 µg/ml), followed by 1:10 (121.37 µg/ml) and 1:3 (114.48µg/ml). Na2CO3 played important role to enhance telmisartan solubility by alkalinizing the formulation which is proved by comparing SD prepared with and without Na2CO3. The conversion of crystalline telmisartan to amorphous by freeze drying might be the factor behind improved solubility. This is established by DSC and X-ray diffraction (XRD) studies. Conclusion: We suggest the prepared telmisartan solid dispersion by using freeze -dried method shall improve solubility of the drug and can be formulated as final dosage form such as tablet or capsule after relevant pre-formulation studies. 2017-08 Conference or Workshop Item NonPeerReviewed application/pdf en http://irep.iium.edu.my/68354/7/354%20Pahang%20RnD%20Prog%20book.pdf application/pdf en http://irep.iium.edu.my/68354/19/Improved%20solubility%20of%20telmisartan%20by%20freeze-dried%20solid%20dispersion_Khater.pdf Aljapairai, Khater Ahmed Saeed and Chatterjee, Bappaditya (2017) Improved solubility of telmisartan by using freeze-dried solid dispersion method. In: 4th Pahang State Pharmacy Research & Development (R&D) Convention, 19th-20th August 2017, IIUM, Kuantan.
institution Universiti Islam Antarabangsa Malaysia
building IIUM Library
collection Institutional Repository
continent Asia
country Malaysia
content_provider International Islamic University Malaysia
content_source IIUM Repository (IREP)
url_provider http://irep.iium.edu.my/
language English
English
topic RS192 Materia Medica-Pharmaceutical Technology
spellingShingle RS192 Materia Medica-Pharmaceutical Technology
Aljapairai, Khater Ahmed Saeed
Chatterjee, Bappaditya
Improved solubility of telmisartan by using freeze-dried solid dispersion method
description Introduction: Drugs with poor water solubility often result in low dissolution and consequently reduced bioavailability. Telmisartan is an angiotensin II receptor antagonist, which is used in the prevention and treatment of hypertension. One of the major problems with this drug is it has poor water solubility that lead to its low bioavailability. Objective: The aim of this study is to improve solubility of telmisartan by using freeze-dried solid dispersion (SD) method. Methods: PVP K30 was selected as carrier and sodium carbonate (Na2CO3) as pH modifier for the formulation. After checking the compatibility between all ingredients by differential scanning calorimetry (DSC) and attenuated total reflectance spectroscopy (ATR-FTIR), the SD was prepared by using freeze-dried method (Martyn Christ, Germany). The selected drug: carrier ratios were 1:3, 1:5, and 1:10 (w/w). The SD powders were evaluated for aqueous solubility. Telmisartan concentration was measured by a high performance liquid chromatographic system (HPLC) with UV detector at 231 nm wavelength. Results: The SD containing telmisartan: PVP K30 (1:5) showed the highest solubility (151.46 µg/ml), followed by 1:10 (121.37 µg/ml) and 1:3 (114.48µg/ml). Na2CO3 played important role to enhance telmisartan solubility by alkalinizing the formulation which is proved by comparing SD prepared with and without Na2CO3. The conversion of crystalline telmisartan to amorphous by freeze drying might be the factor behind improved solubility. This is established by DSC and X-ray diffraction (XRD) studies. Conclusion: We suggest the prepared telmisartan solid dispersion by using freeze -dried method shall improve solubility of the drug and can be formulated as final dosage form such as tablet or capsule after relevant pre-formulation studies.
format Conference or Workshop Item
author Aljapairai, Khater Ahmed Saeed
Chatterjee, Bappaditya
author_facet Aljapairai, Khater Ahmed Saeed
Chatterjee, Bappaditya
author_sort Aljapairai, Khater Ahmed Saeed
title Improved solubility of telmisartan by using freeze-dried solid dispersion method
title_short Improved solubility of telmisartan by using freeze-dried solid dispersion method
title_full Improved solubility of telmisartan by using freeze-dried solid dispersion method
title_fullStr Improved solubility of telmisartan by using freeze-dried solid dispersion method
title_full_unstemmed Improved solubility of telmisartan by using freeze-dried solid dispersion method
title_sort improved solubility of telmisartan by using freeze-dried solid dispersion method
publishDate 2017
url http://irep.iium.edu.my/68354/7/354%20Pahang%20RnD%20Prog%20book.pdf
http://irep.iium.edu.my/68354/19/Improved%20solubility%20of%20telmisartan%20by%20freeze-dried%20solid%20dispersion_Khater.pdf
http://irep.iium.edu.my/68354/
_version_ 1643618587129151488
score 13.211869

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