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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| Format: | Proceeding Paper |
| Language: | English English |
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2017
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| 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 |
| _version_ | 1848786926390214656 |
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| author | Aljapairai, Khater Ahmed Saeed Chatterjee, Bappaditya |
| author_facet | Aljapairai, Khater Ahmed Saeed Chatterjee, Bappaditya |
| author_sort | Aljapairai, Khater Ahmed Saeed |
| building | IIUM Repository |
| collection | Online Access |
| 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. |
| first_indexed | 2025-11-14T17:16:48Z |
| format | Proceeding Paper |
| id | iium-68354 |
| institution | International Islamic University Malaysia |
| institution_category | Local University |
| language | English English |
| last_indexed | 2025-11-14T17:16:48Z |
| publishDate | 2017 |
| recordtype | eprints |
| repository_type | Digital Repository |
| 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 Proceeding Paper 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. |
| spellingShingle | RS192 Materia Medica-Pharmaceutical Technology Aljapairai, Khater Ahmed Saeed Chatterjee, Bappaditya Improved solubility of telmisartan by using freeze-dried solid dispersion method |
| title | 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_short | Improved solubility of telmisartan by using freeze-dried solid dispersion method |
| title_sort | improved solubility of telmisartan by using freeze-dried solid dispersion method |
| topic | RS192 Materia Medica-Pharmaceutical Technology |
| 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 |