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/ 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

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spelling	iium-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.
repository_type	Digital Repository
institution_category	Local University
institution	International Islamic University Malaysia
building	IIUM Repository
collection	Online Access
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/ 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
first_indexed	2023-09-18T21:37:01Z
last_indexed	2023-09-18T21:37:01Z
_version_	1777412888117379072

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

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