Research Journal of Pharmaceutical Dosage Form and Technology

Open Access Open Access  Restricted Access Subscription Access
Open Access Open Access Open Access  Restricted Access Restricted Access Subscription Access

Formulation and Evaluation of Floating Microspheres for an Antihypertensive drug Telmisartan


Affiliations
1 Centre of Pharmaceutics, Amity Institute of Pharmacy, Amity University, Noida, Uttar Pradesh,, India
     

   Subscribe/Renew Journal


Telmisartan is one of the best options either in combination or alone, to treat hypertension. telmisartan belongs to class II antagonist angiotensin converting enzyme inhibitor. One of the main causes of hypertension is vasoconstriction of blood vessels hence increasing blood pressure which can be controlled by drugs that have vasoconstriction property and telmisartan is one of them, and it also relaxes the blood vessels. The dosage form opted here is floating microspheres as it can provide sustain release of drug over long period of time. Floatingmicrospheres have a tendency to float over gastric fluid hence increasing gastric retention time. These are preferred over conventional form as they provide advantage of reducing gastric irritation, lesser dosing frequency will be required as it provide slow continuous release for prolong period of time. The present research aims to formulate telmisartan floating microspheres and its evaluation. The technique used is solvent evaporation method by using magnetic stirrer. Already formulated telmisartan microspheres have lower bioavailability, drugentrapment and lower release kinetics so our main aim is to formulate such a preparation which have greater bioavailability, drug entrapment and greater kinetic release, and to formulate such a formulation we have opted using variant ratios of polymer Eudragit RS 100, Ethyl Cellulose with constant dose of drug. After formulation, various characterization is done that include micromeritics properties, floating efficiency, solubility, drug entrapment efficiency along with yield and release kinetics. The study revealed that, using a more than one polymer in a different ratio have an impact on every parameter of microspheres.

Keywords

Telmisartan, Floating Microspheres, Solvent evaporation technique, Eudragit RS 100, Ethyl Cellulose.
Subscription Login to verify subscription
User
Notifications
Font Size


  • Jagtap, Yogesh and Bhujbal, Rohan and Ranpise, Nisharani. (2012). Floating microspheres: A review. Brazilian Journal of Pharmaceutical Sciences. 48. 17-30. 10.1590/S1984- 82502012000100003.

  • Varma Kumar Ajit, Gupta Kumar Arun, Khare Piush, Patel Rakesh. Formulation and Development of Floating Microspheres containing Levodopa and Carbidopa. Asian J. Pharm. Tech. 2018; 8 (4):200-202

  • Rohilla S, Bhatt DC, Ahalwat S. Fabrication of potential gastroretentive microspheres of itraconazole for stomachspecific delivery: Statistical optimization and in vitro evaluation. J Appl Pharm Sci, 2020; 10(03):119–127

  • Kendre, Prakash and Chaudhari, Pravin. (2012). Formulation and Evaluation of Telmisartan Microspheres by Solvent Evaporation Technique.

  • Rahul Rawat, Yogesh Josh. Effect of Antihypertensive Drugs on Homocysteine level among Hypertensive Patients. Asian J. Res. Pharm. Sci. 2018; 8(4): 219-222

  • Sonali S. Jaiswal, Shashikant D. Barhate. Formulation Optimization and Evaluation of Immediate Release Tablet of Telmisartan. Asian J. Res. Pharm. Sci. 2019; 9(3):167-173.

  • Praveen Kumar Gaur, Shikha Mishra, Meenakshi Bajpai, Formulation and evaluation of controlled-release of telmisartan microspheres: In vitro/in vivo study, Journal of Food and Drug Analysis, Volume 22, Issue 4,2014, Pages 542-548, ISSN 1021- 9498, https://doi.org/10.1016/j.jfda.2014.05.001.

  • Jinukula Bhavani, Shah Saloni and Dhurke Rajeshri. 2019, Formulation and Evaluation of Floating Microspheres Using Factorial Design. Int J Recent Sci Res. 10(12), pp. 36363-36370. DOI: http://dx.doi.org/10.24327/ijrsr.2019.1012.4908

  • Celli GB, Ghanem A, Brooks MS. Development and evaluation of floating alginate microspheres for oral delivery of anthocyanins – A preliminary investigation. Food Sci Nutr. 2017; 5:713–721. https://doi.org/10.1002/ fsn3.451

  • Krutika Sawant, Mitali Patel, Jiten Patel, Piyush Mundada. Formulation, optimization, characterization and in vivo anti-ulcer activity of esomeprazole magnesium trihydrate gastroresistant microspheres. Int J Pharm Pharm Sci 2017;9(1):273-282

  • Design, Formulation and in vitro Drug Release from Transdermal Patches containing Nebivolol Hydrochloride as Model Drug. Asian J. Pharm. Res. 2(4): Oct. - Dec. 2012; Page 136-141.

  • Vanitha Kondi, Ramesh Alluri. In Vitro and In Vivo Evaluation of Floating Microspheres of Prazosin Hydrochloride. Asian J. Pharm. Tech. 2016; 6(4): 202-206.

  • J.M. Chavda, M.A. Raval, K.R. Dave. Simultaneous estimation of Telmisartan and Indapamide in Bulk Drug and in pharmaceutical dosage form using UV-Spectrophotometry. Asian J. Research Chem. 5(9): September, 2012; Page 1129-1135.

  • Shanmugam. S., Sandhiya. K. M., Ayyappan. T, Sundaramoorthy. K., Vetrichelvan. T. Design and In Vitro Studies of Ambroxol Hydrochloride Sustained Release Matrix Tablets. Research J. Pharma. Dosage Forms and Tech. 2011; 3(2): 48-52.

  • Shahana. V. P, Gayathri Ramya M, Rajesh A, Kathirvel. S. A Comprehensive Validation Method and Development of RP-HPLC for Simultaneous Estimation of Metoprolol, Telmisartan and Chlorthalidonein Bulk and its Formulation. Asian J. Research Chem. 2018; 11(6): 827-834.

  • Manish P Patel, MM Patel, KN Patel, DR Patel, UL Patel. Designing and Evaluation of Floating Microspheres of Verapamil Hydrochloride: Effect of Methocel. Research J. Pharma. Dosage Forms and Tech. 2009; 1(1): 22-28

  • Sethi RK, Sahoo SK, Das PK, Barik BB. Effect of Dispersing Agent on the Characteristics of Eudragit Microspheres. Research J. Pharma. Dosage Forms and Tech. 2010; 2(1):67-71.


Abstract Views: 321

PDF Views: 0




  • Formulation and Evaluation of Floating Microspheres for an Antihypertensive drug Telmisartan

Abstract Views: 321  |  PDF Views: 0

Authors

Shikha Baghel Chauhan
Centre of Pharmaceutics, Amity Institute of Pharmacy, Amity University, Noida, Uttar Pradesh,, India
Sakshi Nainwani
Centre of Pharmaceutics, Amity Institute of Pharmacy, Amity University, Noida, Uttar Pradesh,, India

Abstract


Telmisartan is one of the best options either in combination or alone, to treat hypertension. telmisartan belongs to class II antagonist angiotensin converting enzyme inhibitor. One of the main causes of hypertension is vasoconstriction of blood vessels hence increasing blood pressure which can be controlled by drugs that have vasoconstriction property and telmisartan is one of them, and it also relaxes the blood vessels. The dosage form opted here is floating microspheres as it can provide sustain release of drug over long period of time. Floatingmicrospheres have a tendency to float over gastric fluid hence increasing gastric retention time. These are preferred over conventional form as they provide advantage of reducing gastric irritation, lesser dosing frequency will be required as it provide slow continuous release for prolong period of time. The present research aims to formulate telmisartan floating microspheres and its evaluation. The technique used is solvent evaporation method by using magnetic stirrer. Already formulated telmisartan microspheres have lower bioavailability, drugentrapment and lower release kinetics so our main aim is to formulate such a preparation which have greater bioavailability, drug entrapment and greater kinetic release, and to formulate such a formulation we have opted using variant ratios of polymer Eudragit RS 100, Ethyl Cellulose with constant dose of drug. After formulation, various characterization is done that include micromeritics properties, floating efficiency, solubility, drug entrapment efficiency along with yield and release kinetics. The study revealed that, using a more than one polymer in a different ratio have an impact on every parameter of microspheres.

Keywords


Telmisartan, Floating Microspheres, Solvent evaporation technique, Eudragit RS 100, Ethyl Cellulose.

References