Formulation and Evaluation of Gastroretentive Floating Tablets of Lovastatin Using Natural Polymers

Authors

  • Vinesh Kumar Department of Pharmacy, Lal Bahadur Shastri College of Pharmacy, Jaipur, India
  • Rakesh Kumar Sodavat Department of Pharmacy, Lal Bahadur Shastri College of Pharmacy, Jaipur, India
  • Garvendra Singh Rathore Department of Pharmacy, Lal Bahadur Shastri College of Pharmacy, Jaipur, India

Abstract

Background: Lovastatin, a lipid-lowering agent, suffers from low bioavailability due to extensive first-pass metabolism and limited absorption in the gastrointestinal tract. A gastroretentive drug delivery system (GRDDS) offers a promising solution to enhance its therapeutic effectiveness.

Objective: The present study aims to formulate and optimize gastroretentive floating tablets of Lovastatin using various grades of hydroxypropyl methylcellulose (HPMC) and natural polymers to achieve sustained drug release.

Methods: Floating tablets were prepared by direct compression using HPMC K4M, HPMC K15M, and guar gum in varying ratios. The tablets were evaluated for pre-compression (bulk density, tapped density, Carr’s index, Hausner ratio) and post-compression (thickness, hardness, friability, drug content, buoyancy) parameters. In vitro dissolution studies were conducted for 12 hours, and the data were fitted into kinetic models to determine the release mechanism.
Results: All formulations exhibited acceptable physicochemical characteristics. The optimized batch (F8) demonstrated more than 12 hours of buoyancy, high drug content (99.23%), and sustained release of 99.45% over 12 hours. Drug release followed first-order kinetics with Higuchi diffusion and non-Fickian transport mechanisms.

Conclusion: Floating tablets of Lovastatin prepared with HPMC K4M, K15M, and guar gum can effectively sustain drug release over 12 hours and improve gastric retention. This system holds potential for enhanced therapeutic efficiency in hyperlipidaemia treatment.

Keywords: Lovastatin, gastroretentive tablet, floating drug delivery, HPMC, sustained release, in vitro kinetics

Keywords:

Lovastatin, gastroretentive tablet, floating drug delivery, HPMC, sustained release, in vitro kinetics

DOI

https://doi.org/10.22270/jddt.v15i7.7280

Author Biographies

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

Department of Pharmacy, Lal Bahadur Shastri College of Pharmacy, Jaipur, India

Rakesh Kumar Sodavat, Department of Pharmacy, Lal Bahadur Shastri College of Pharmacy, Jaipur, India

Department of Pharmacy, Lal Bahadur Shastri College of Pharmacy, Jaipur, India

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

Department of Pharmacy, Lal Bahadur Shastri College of Pharmacy, Jaipur, India

References

1. Ansel HC, Popovich NG, Allen LV. Pharmaceutical Dosage Forms and Drug Delivery Systems. 1st ed. 1995; p. 78.

2. Jain NK, Sharma SN. A Textbook of Professional Pharmacy. 1st ed. 1995; p. 78.

3. Banker GS, Rhodes CT. Modern Pharmaceutics. 3rd ed. New York: Marcel Dekker Inc.; 1996. p. 503.

4. Hoffman A. Pharmacodynamic aspects of sustained release preparations. Adv Drug Deliv Rev. 1998;33:185-199. https://doi.org/10.1016/S0169-409X(98)00027-1 PMid:10837659

5. Gren T, Bjerre C, Camber O. In vitro drug release from porous cellulose matrices. Int J Pharm. 1996;141:53-62. https://doi.org/10.1016/0378-5173(96)04614-5

6. Munday DC, Cox PJ. Compressed xanthan and karaya gum matrices: hydration, erosion and drug release mechanisms. Int J Pharm. 2000;203:179-192. https://doi.org/10.1016/S0378-5173(00)00444-0 PMid:10967440

7. Remington JP. Remington: The Science and Practice of Pharmacy. 20th ed. Philadelphia: Lippincott Williams & Wilkins; 2000.

8. Lachman L, Lieberman HA, Kanig JL. The Theory and Practice of Industrial Pharmacy. 3rd ed. Philadelphia: Lea & Febiger; 1986. p. 303-314.

9. Qiu Y, Zhang G, Wise DL. Handbook of Pharmaceutical Controlled Release Technology. New York: Marcel Dekker; 2000. p. 465-503.

10. Kamboj S, Gupta GD. Matrix Tablets: An Important Tool for Oral Controlled-Release Dosage Forms. Pharmainfo.net. 2009;7(6).

11. Gambhire MN, Ambade KW, Kurmi SD. Development and in vitro evaluation of an oral floating matrix tablet formulation of diltiazem HCl. AAPS PharmSciTech. 2007;8(3):E1-E9. https://doi.org/10.1208/pt0803073 PMid:17915823 PMCid:PMC2750569

12. Talukdar MM, Vercammen JP. Evaluation of xanthan gum as a hydrophilic matrix for controlled-release dosage form preparations. Drug Dev Ind Pharm. 1993;19(9):1037-1046. https://doi.org/10.3109/03639049309062999

13. Prakash SS, Niranjan PC, Kumar PH, et al. Design and evaluation of verapamil hydrochloride controlled release tablets using hydrogel polymers. J Pharm Res. 2007;6(2):122-125.

14. Reynolds TD, Tajeer J. Polymer erosion and drug release characterization of HPMC matrices. Pharm Res. 1991;11:1115-1119.

15. Robinson JR, Lee VH. Controlled Drug Delivery: Fundamentals and Applications. 2nd ed. New York: Marcel Dekker; 1987. p. 3-61. https://doi.org/10.1201/b14193

16. Popli H, Sharma SN. Trends in oral sustained release formulation-I. The Eastern Pharmacist. 1989;32:99-103.

17. Modi SA, Gaikwad PD, Bankar VH, Pawar SP. Sustained release drug delivery system: a review. Int J Pharm Res Dev. 2011;2(12):147-160.

18. Shabaraya AR, Narayanacharyulu R. Design and evaluation of chitosan matrix of metoprolol tartrate for sustained release. J Pharm Pharmaceut Sci. 2000;8(1):231-236.

19. Roldy RK, Midovert S, Redlen S. Once daily matrix tablet of azithromycin: in-vitro and in-vivo evaluation. Pharm Sci Tech. 2003;4(4):55-59.

20. Rouge N, Allemann E, Gex-Fabry M, et al. Comparative pharmacokinetic study of a floating multiple-unit capsule, a high-density capsule, and an immediate-release tablet containing 25 mg atenolol. Pharm Acta Helv. 1998;73:81-87. https://doi.org/10.1016/S0031-6865(97)00050-2 PMid:9700936

21. Streubel A, Siepmann J, Bodmeier R. Multiple unit gastroretentive drug delivery: a new preparation method for low-density microparticles. J Microencapsul. 2003;20:329-347. https://doi.org/10.3109/02652040309178073 PMid:12881114

22. Goole J, Vanderbist F, Amighi K. Gastroretentive dosage forms: a review. Drug Dev Ind Pharm. 2007;33(11):1281-1296.

23. Shrma S, Pawar A. Low density multiparticulate system for pulsatile release of meloxicam. Int J Pharm 2006; 313: 150-58. https://doi.org/10.1016/j.ijpharm.2006.02.001 PMid:16540268

24. Santus G, Lazzarini G, Bottoni G, Sandefer EP, Page RC, Doll WJ, Ryo UY, Digenis GA. An in vitro- in vivo investigation of oral bioadhesive controlled release furosemide formulations. Eur J Pharm Biopharm 1997;44: 39-52. https://doi.org/10.1016/S0939-6411(97)00100-8

25. Klausner EA, Lavy E, Friedman M, Hoffman A. Expandable gastroretentive dosage forms. J Control Release 2003; 90: 143-62. https://doi.org/10.1016/S0168-3659(03)00203-7 PMid:12810298

26. Deshpande AA, Shah N, Rhodes CT, Malik W. Development of a novel controlled-release system for gastric retention. Pharm Res 1997; 14:815-19. https://doi.org/10.1023/A:1012171010492 PMid:9210203

27. Park K. Enzyme-digestible swelling as platforms for long-term oral drug delivery: synthesis and characterization. Biomaterials 1988; 9: 435. https://doi.org/10.1016/0142-9612(88)90009-9 PMid:3146993

28. Fujimori J, Machida Y, Nagai T. Preparation of a magnetically-responsive tablet and configuration of its gastric residence in beagle dogs. STP Pharma Sci 1994; 4: 425-30.

29. Amit Kumar Nayak, RumaMaji, Biswarup Das; Gastroretentive Drug Delivery Systems: A Review; Asian Journal of Pharmaceutical and Clinical Research, 2010;3(1):2-10

30. Klusner EA, Eyal S, Lavy E, Friedman M, Hoffman A; Novel Levodopa Gasrtroretentive Dosage form: In Vivo Evaluation in Dogs; J Control Release 2003; 88: 117-26. https://doi.org/10.1016/S0168-3659(02)00487-X PMid:12586509

31. Hoffman A; Pharmacodynamic aspects of sustained release preparation; A Drug Delivery; Rev 1998; 33:185-99. https://doi.org/10.1016/S0169-409X(98)00027-1 PMid:10837659

32. Devkant Sharma, Anjali Sharma; Gastroretentive Drug Delivery System - a mini review; Asian pacific Journal of Health Sciences, 2014; 1(2): 80-89. https://doi.org/10.21276/apjhs.2014.1.2.9

33. Robinson J, Lee R. Controlled Drug Delivery, 2nd edition, 1987: pg 418. https://doi.org/10.1201/b14193

34. Bardonnet PL, Faivre V, Pugh WJ, Piffaretti JC, Falson F; Gastroretentive Dosage Forms; Journal of Controlled Release, 2006; 111:1-18. https://doi.org/10.1016/j.jconrel.2005.10.031 PMid:16403588

35. Arora S, Javed A, Ahuja A, Khar RK, Baboota S; Floating Drug Delivery System : AReview; AAPS Pharm Sci Tech, 2000;6(3):372-390. https://doi.org/10.1208/pt060347 PMid:16353995 PMCid:PMC2750381

36. Patel GM, Patel HR, Patel M.; Floating drug delivery system an innovative approaches to prolong gastric retention; Pharmainfo.net 2007.

37. Vedha Hari; The Recent Developments on Gastric Floating Drug Delivery Systems: An Overview; Int Journal pharmtech Res.2010; 2(1): 524-534. https://doi.org/10.4103/0975-1483.71622 PMid:21264092 PMCid:PMC3019371

38. A. Badoni, A. Ojha, G. Gnanarajani, P. Kothiyali; Review on Gastro Retentive Drug Delivery System; The Pharma Innovation, 2012;1(8): 32-42.

39. Keerthi Priya, D.V. R. N. Bhikshapathi. Development and in vivo Evaluation Lovastatin by Self-Nanoemulsifying Drug Delivery System. International Journal of Pharmaceutical Sciences and Drug Research 2018; 10(3): 165- 172. https://doi.org/10.25004/IJPSDR.2018.100310

40. Doijad R.C,Sompur C.K, Goje A.J , Maske A.P And Tamboli F.ADevelopment And Characterization Of Lovastatin Controlled Release Buccoadhesive Dosage Form. International Journal of Pharma and Bio Sciences.2011; 2(3):133-144.

Published

2025-07-15
Statistics
Abstract Display: 1136
PDF Downloads: 988
PDF Downloads: 106

How to Cite

1.
Kumar V, Sodavat RK, Rathore GS. Formulation and Evaluation of Gastroretentive Floating Tablets of Lovastatin Using Natural Polymers. J. Drug Delivery Ther. [Internet]. 2025 Jul. 15 [cited 2026 Jan. 14];15(7):71-9. Available from: https://jddtonline.info/index.php/jddt/article/view/7280

How to Cite

1.
Kumar V, Sodavat RK, Rathore GS. Formulation and Evaluation of Gastroretentive Floating Tablets of Lovastatin Using Natural Polymers. J. Drug Delivery Ther. [Internet]. 2025 Jul. 15 [cited 2026 Jan. 14];15(7):71-9. Available from: https://jddtonline.info/index.php/jddt/article/view/7280