Preparation and Evaluation of Oil Entrapped Gastro-Retentive Floating Gel Beads of Metoprolol Succinate as Antihypertensive

Authors

  • Mohit Vijay Lal Bahadur Shastri College of Pharmacy, Jaipur, India
  • Garvendra Singh Rathore Lal Bahadur Shastri College of Pharmacy, Jaipur, India
  • Vinesh Kumar Lal Bahadur Shastri College of Pharmacy, Jaipur, India

Abstract

The objective of this study was to manufacture gastrointestinal-retentive floating liquid beads made of Metoprolol Succinate (MS). MS is a beta blocker antihypertensive medicine that is metabolized in the liver by first-pass action, which greatly decreases its availability throughout the body. This formulation was made to make the medicine more bioavailable by making it stay in the stomach for up to 12 hours longer. There were 24 different formulas made. These were split into four groups based on the type and amount of polymers utilized, with each group having six formulations. The emulsion gelation technique was employed to create these oil-encapsulated floating medication beads. We looked at a lot of things for each of the formulations we made, such as morphology, floating behavior, drug content, and in vitro % cumulative drug release (%CDR). The physicochemical characteristics of the generated microgel beads were deemed excellent. In vitro testing also showed that each of the prepared batches had good buoyancy. The benchmark was AstraZeneca's Toprol XL 25mg. We used different model-dependent release kinetics, like zero and first order, Higuchi, and Pappas models, to compare the chosen optimal formulation (SF4) with the ordinary marketed formulation. The results showed that the equation of Korsemeyer-Peppa fit the data best for the formulation SF4 (with R2 = 0.9952). This meant that the drug release followed a non-Fickian diffusion process.

Keywords: Metoprolol succinate, gastro retentive, FDDS, Sodium alginate, model dependent release kinetics

Keywords:

Metoprolol succinate, gastro retentive, FDDS, Sodium alginate, model dependent release kinetics

DOI

https://doi.org/10.22270/jddt.v16i3.7626

Author Biographies

Mohit Vijay, Lal Bahadur Shastri College of Pharmacy, Jaipur, India

Lal Bahadur Shastri College of Pharmacy, Jaipur, India

Garvendra Singh Rathore , Lal Bahadur Shastri College of Pharmacy, Jaipur, India

Lal Bahadur Shastri College of Pharmacy, Jaipur, India

Vinesh Kumar, Lal Bahadur Shastri College of Pharmacy, Jaipur, India

Lal Bahadur Shastri College of Pharmacy, Jaipur, India

References

1. Dehghan M, Kha F. Gastroretentive drug delivery systems: A patent perspective. Int J Heal Res. 2009;2(1):23-44. https://doi.org/10.4314/ijhr.v2i1.55385

2. Narendra C, Srinath MS, Babu G. Optimization of bilayer floating tablet containing metoprolol tartrate as a model drug for gastric retention. AAPS Pharm Sci Tech. 2006;7(2):E23-9. https://doi.org/10.1208/pt070234 PMid:16796352

3. Pawar HA, Gharat PR, Dhavale RV, Joshi PR, Rakshit PP. Development and Evaluation of Gastroretentive Floating Tablets of an Antihypertensive Drug Using Hydrogenated Cottonseed Oil. ISRN Pharm. 2013;2013:1-9. https://doi.org/10.1155/2013/137238 PMid:24455312 PMCid:PMC3880749

4. Rocca JG, Omidian H, Shah K. Progress in gastroretentive drug delivery systems: Business briefing. Pharma Tech. 2003;5:152-6.

5. Hardman JG, Limbird LE, Gilman AG. Goodman and Gilman's: The PharmacologicalBasis of Therapeutics. In New York: McGraw-Hill Publishers ; 2001. p. 255-6.

6. Kendall MJ, Maxwell SRJ, Sandberg A, Westergren G. Controlled release metoprolol. Clinical pharmacokinetic and therapeutic implications. Clin Pharmacokinet. 1991;21(5):319-30. https://doi.org/10.2165/00003088-199121050-00001 PMid:1773547

7. Jobin G, Cortot A, Godbillon J, Duval M, Schoeller J, Hirtz J, et al. Investigation of drug absorption from the gastrointestinal tract of man. I. Metoprolol in the stomach, duodenum and jejunum. Br J Clin Pharmacol. 1985;19 Suppl 2(Suppl 2):97S-105S. https://doi.org/10.1111/j.1365-2125.1985.tb02749.x

8. Ravishankar H, Patil P, Samel A, Petereit HU, Lizio R, Iyer-Chavan J. Modulated release metoprolol succinate formulation based on ionic interactions: In vivo proof of concept. J Control Release. 2006;111(1-2):65-72. https://doi.org/10.1016/j.jconrel.2005.12.007 PMid:16446006

9. Mathur P, Saroha K, Syan N, Verma S, Kumar V. Floating drug delivery systems: An innovative acceptable approach in gastroretentive drug delivery. Arch Apll Sci Res . 2010;2:257-70.

10. Shah SH, Patel JK, Patel N V. Stomach specific floating drug delivery system: A review. Int J PharmTech Res. 2009;1(3):623-33.

11. Srivastava AK, Wadhwa S, Ridhurkar D, Mishra B. Oral sustained delivery of atenolol from floating matrix tablets-formulation and in vitro evaluation. Drug Dev Ind Pharm. 2005;31(4-5):367-74. https://doi.org/10.1081/DDC-54313 PMid:16093202

12. Dave BS, Amin AF, Patel MM. Gastroretentive drug delivery system of ranitidine hydrochloride: Formulation and in vitro evaluation. AAPS PharmSciTech. 2004;5(2):77-82. https://doi.org/10.1208/pt050234 PMid:15760092 PMCid:PMC2750469

13. Chavanpatil M, Jain P, Chaudhari S, Shear R, Vavia P. Development of sustained release gastroretentive drug delivery system for ofloxacin: In vitro and in vivo evaluation. Int J Pharm. 2005;304(1-2):178-84. https://doi.org/10.1016/j.ijpharm.2005.08.009 PMid:16198522

14. Chowdary KP, Suresh B, Sangeeta B, Reddy GK. Design and evaluation of diltiazem mucoadhesive tablets for oral controlled release. Saudi Pharm J. 2003;11:201-5.

15. Varshosaz J, Tavakoli N, Roozbahani F. Formulation and in vitro characterization of ciprofloxacin floating and bioadhesive extended-release tablets. Drug Deliv. 2006;13(4):277-85. https://doi.org/10.1080/10717540500395106 PMid:16766469

16. Talukder R, Fassihi R. Gastroretentive Delivery Systems: A Mini Review. Drug Dev Ind Pharm. 2004;30(10):1019-28. https://doi.org/10.1081/DDC-200040239 PMid:15595568

17. Khan T, Vaidya A, Jain R. Meropenem loaded pectin microspheres for colon delivery. Asian J Biomat Res. 2018;4(4):8-20.

18. Ram Murthi M, Sandheep Kumar Reddy K, Ramanamma L, Asha S, Urmila R. COMPARATIVE STUDY OF MARKETED METOPROLOL SUCCINATE EXTENDED RELEASE TABLETS. World J Pharm Res. 2019;8(1):943-52.

19. Chander SB, Kiran RS, Babu BN. Preparation and evaluation of gastro retentive floating tablets of ketoconazole. Int J Pharm Res Dev . 2010;2(9):174-84.

20. Varma M, S. Vijaya. Development and evaluation of gastroretentive floatingdrug delivery system of atenolol. Int J Pharm Chem Sci. 2012;1(2):869.

21. Eswer G, Saritha M. Formulation and evaluation of atenolol floating tablets using different polymers: guargum, sodium alginate, Hpmc100cps and Carbopol940. Int J Pharm Biol Arch. 2011;2(4):1148-51.

22. Tayade RP, Thakare VM, Tekade BW, Patil VR. Formulation and evaluation of captopril floating matrix tablet. Int J Pharm Res Dev. 2012;4(6):116.

23. Ngwuluka NC, Lawal K, Olorunfemi PO, Ochekpe NA. Post-market in vitro bioequivalence study of six brands of ciprofloxacin tablets/caplets in Jos, Nigeria. Sci Res essay. 2009;4(4):298-305.

24. Singh S, Prajapati K, Pathak AK, Mishra A. Formulation and evaluation of floating tablet of captopril. Int J PharmTech Res. 2011;3(1):333-41.

Published

2026-03-15
Statistics
Abstract Display: 143
PDF Downloads: 121
PDF Downloads: 19

How to Cite

1.
Vijay M, Rathore GS, Kumar V. Preparation and Evaluation of Oil Entrapped Gastro-Retentive Floating Gel Beads of Metoprolol Succinate as Antihypertensive. J. Drug Delivery Ther. [Internet]. 2026 Mar. 15 [cited 2026 Apr. 18];16(3):36-4. Available from: https://www.jddtonline.info/index.php/jddt/article/view/7626

How to Cite

1.
Vijay M, Rathore GS, Kumar V. Preparation and Evaluation of Oil Entrapped Gastro-Retentive Floating Gel Beads of Metoprolol Succinate as Antihypertensive. J. Drug Delivery Ther. [Internet]. 2026 Mar. 15 [cited 2026 Apr. 18];16(3):36-4. Available from: https://www.jddtonline.info/index.php/jddt/article/view/7626