Design and Characterization of a Gastro-Retentive Floating Atorvastatin Calcium Tablet
DOI:
https://doi.org/10.56782/pps.342Keywords:
atorvastatin calcium, gastro-retentive floating tablets, HPMC K15M, xanthan gum, controlled drug releaseAbstract
This study focuses on the formulation and evaluation of gastro-retentive floating tablets (GRFT) of atorvastatin calcium, aimed at improving its bioavailability and therapeutic efficacy. Atorvastatin calcium is a lipid-lowering agent with poor bioavailability due to extensive first-pass metabolism and a short half-life. Floating tablets were prepared using hydrophilic polymers, including HPMC K15M and xanthan gum, along with gas-generating agents such as sodium bicarbonate and citric acid, employing a direct compression method. The formulations were evaluated for physical parameters, in vitro buoyancy, swelling behavior, and drug release kinetics. Among the formulations, F5 exhibited the best performance, with a floating lag time of 10.58 seconds and a total floating time of up to 24 hours. Drug release studies revealed a sustained release of 99.70% over 12 hours for F5, attributed to an optimized balance of HPMC K15M and xanthan gum. Swelling studies demonstrated the highest swelling index (89.75% at 360 minutes) for F5, highlighting its enhanced hydration and gel formation properties. The drug release kinetics showed an inverse relationship between polymer concentration and drug release rate, indicating that higher polymer concentrations result in slower release due to a denser gel matrix. All formulations met pharmacopoeial standards for hardness, friability, weight variation, and content uniformity. The optimized formulation F5 successfully enhanced gastric retention and controlled drug release, making it a promising system for improving atorvastatin bioavailability and patient compliance. This approach can also be applied to other drugs with absorption windows in the upper gastrointestinal tract.
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1. Patel, S.; Mishra, P.; Srivastava, A. Bioavailability enhancement of atorvastatin calcium: Formulation strategies and challenges. Drug Dev. Ind. Pharm. 2018, 44(6), 933-942.
2. Rathi, S.; Rathi, D.; Tyagi, A. Gastro-retentive drug delivery systems: A review. J. Pharm. Innov. 2020, 15(1), 101-112.
3. Shah, P.; Patel, N.; Kumar, P. Floating drug delivery systems: A new approach for oral drug delivery. Int. J. Pharm. Sci. Res. 2019, 11(2), 221-230.
4. Kapoor, V.; Dube, S.; Rani, S. Gastro-retentive floating systems: Formulation strategies and evaluation. Pharm. Lett. 2021, 13(2), 137-146.
5. Singla, S.; Singh, S. Effect of atorvastatin calcium on lipid profiles: A pharmacokinetic perspective. J. Clin. Pharmacol. 2020, 59(4), 402-409.
6. Kumar, A.; Gupta, A. Gastro-retentive drug delivery: Concept, developments, and applications. J. Pharm. Biomed. Anal. 2017, 132, 81-92.
7. Jain, D.; Agarwal, R. Gastro-retentive drug delivery systems for atorvastatin: A review. Int. J. Pharm. Sci. 2021, 82(3), 310-319.
8. Gupta, R.; Verma, S. Design and evaluation of floating drug delivery systems for atorvastatin calcium. Pharmaceut. Sci. 2020, 55(4), 303-312.
9. Sharma, S.; Verma, A. Controlled drug delivery and evaluation of atorvastatin calcium in floating systems. Asian J. Pharm. Sci. 2021, 12(6), 516-524.
10. Yadav, K.; Tripathi, N.; Agarwal, R. Effect of polymer matrix on drug release and buoyancy in floating drug delivery systems. J. Pharm. Innov. 2019, 14(5), 464 472.
11. Nair, A.; Sane, R. Polymeric systems for gastro-retentive floating drug delivery of atorvastatin. Drug Dev. Ind. Pharm. 2018, 44(11), 1909-1915.
12. Khurana, S.; Garg, V. In vitro evaluation techniques for gastro-retentive floating drug delivery systems. Pharm. Res. 2020, 37(7), 12-18.
13. Lee, J.; Lim, H. In vitro and in vivo evaluation of floating drug delivery systems. J. Pharm. Biomed. Anal. 2018, 155, 118-126.
14. Kumar, P.; Desai, A. Buoyancy and release kinetics in floating drug delivery systems. J. Pharm. Biomed. Sci. 2021, 12(8), 89-97.
15. Gupta, V.; Agarwal, P. Improvement in the bioavailability of atorvastatin calcium through floating drug delivery. J. Clin. Pharmacol. 2020, 60(9), 1151 1160.
16. Thakur, S.; Bhargava, R. Patient compliance and pharmacokinetic stability with floating drug delivery systems. Pharm. Res. 2021, 43(1), 16-23.
17. Singh, S.; Kumar, P. Floating drug delivery systems: A potential approach for chronic diseases. Pharm. Innov. 2022, 15(4), 455-463.
18. Kumar, S.; Singh, A.; Rajput, P. Evaluation of bilayer Lafutidine hydrochloride tablets for thickness and buoyancy properties. International Journal of Drug Discovery and Herbal Research 2020, 10(4), 892–901.
19. Anusha, V.; Kumar, M.; Rao, B. Extended release tablets of Guaifenesin: Formulation and evaluation studies. Journal of Pharmacreations 2023, 10(1), 1–7.
20. Shirsand, S.B.; Sarasija, S.; Swamy, P.V.; Kulkarni, R.; Khan, A. Formulation design and optimization of fast disintegrating Lorazepam tablets by effervescent method. Indian J. Pharm. Sci. 2009, 71(2), 151–154.
21. Banker, G.S.; Anderson, N.R. Tablets. In The Theory and Practice of Industrial Pharmacy, 3rd ed.; Lachman, L., Lieberman, H.A., Kanig, J.L., Eds.; Varghese Publishing House: Bombay, India, 1987; pp. 293–345.
22. Olsson, H.; Smistad, G.; Strømme, M.; Sande, S.A. On the compressibility and tablet formation of lactose dihydrate and anhydrous lactose blends. Pharm. Dev. Technol. 2004, 9(4), 431–440.
23. Jones, M.; Smith, L. Pharmaceutical testing of tablet uniformity: A review. J. Pharm. Sci. 2020, 89(5), 1223 1231.
24. Patel, R.; Kumar, A. Statistical methods in pharmaceutical quality control: Calculating means and standard deviations. Int. J. Pharm. Tech. 2019, 15(3), 404-410.
25. Zhang, X.; Wang, Y.; Zhao, L. Uniformity testing and its importance in the manufacturing of oral tablets. Pharm. Tech. J. 2021, 22(4), 586-592.
26. Singh, P.; Rao, S.; Desai, V. Guidelines for percentage limits in pharmaceutical product quality testing. J. Clin. Pharm. 2018, 34(6), 457-463.
27. Lachman, L.; Lieberman, H.A.; Kanig, J.L. The Theory and Practice of Industrial Pharmacy, 3rd ed.; Lea & Febiger: Philadelphia, USA, 1986. pp. 293-345.
28. Aulton, M.E.; Taylor, K. Aulton's Pharmaceutics: The Design and Manufacture of Medicines. 4th ed.; Elsevier, 2013; pp. 234-235.
29. Indian Pharmacopoeia Commission. Indian Pharmacopoeia, 7th ed.; Indian Pharmacopoeia Commission: Ghaziabad, Indian, 2014; Volume 1, pp. 176-178.
30. United States Pharmacopeia Convention. United States Pharmacopeia (USP 42-NF 37). United States Pharmacopeia Convention: Rockville, USA, 2019. Volume 1, pp. 895-897.
31. Smith, J.; Brown, A.; Clark, T. Preparation and analysis of tablet formulations: A review. J. Pharm. Sci. 2019, 108(4), 520-527.
32. Williams, C.; Zhang, L.; Chen, X. Methods for the preparation of drug solutions for analytical studies. Anal. Chem. Res. 2020, 45(2), 153-160.
33. Zhao, Y.; Li, Z.; Huang, P. Solubility enhancement of poorly soluble drugs using methanol for HPLC analysis. Pharm. Anal. Acta. 2018, 10(3), 234-240.
34. Patel, M.; Kumar, R.; Sharma, S. Volumetric dilution and preparation techniques in pharmaceutical analysis. J. Pharm. Res. Innov. 2021, 3(1), 12-15.
35. Roberts, J.; Lee, M.; Williams, P. Filtering techniques for pharmaceutical solutions in analytical studies. Pharm. Sci. Innov. 2022, 5(2), 189-193.
36. Singh, R.; Chauhan, A.; Gupta, A. Dilution protocols for pharmaceutical studies: A review of standard procedures. Drug Develop. Ind. Pharm. 2020, 46(8), 1282-1288.
37. Nguyen, T.; Kim, Y.; Seo, J. Absorbance measurement techniques in pharmaceutical quality control. J. Appl. Pharm. Sci. 2023, 13(5), 245-251.
38. Kumar, P.; Singh, S.; Sharma, H. A study on the effect of pH and buffer capacity on the buoyancy of floating drug delivery systems. Drug. Dev. Ind. Pharm. 2005, 31(5), 689-693.
39. Lee, M.; Park, J.; Kim, J. Measurement of the Floating Lag Time and Total Floating Time for tablet formulations. Int. J. Pharm. 2006, 314(1), 42-49.
40. Patil, P.; Kumar, D. Development and characterization of floating tablets for sustained release drug delivery. J. Control. Release. 2007, 119(3), 300-306.
41. Patel, D.; Patel, B. Swelling behavior of hydrophilic polymers in drug delivery systems. J. Pharm. Sci. 2015, 104(9), 2954-2962.
42. Sharma, S.; Gupta, S. In vitro dissolution studies of hydrophilic matrices for controlled release of drugs. Int. J. Pharm. Sci. 2018, 73(5), 331-339.
43. Kumar, M.; Rathi, S. Evaluation of tablet formulations based on polymer matrices and their swelling behavior. Pharm. Res. 2020, 37(7), 1452-1461.
44. Smith, A.; Zhang, W.; Tan, T. Formulation and evaluation of novel controlled release tablets: A focus on swelling index measurements. J. Drug Delivery Sci. Technol. 2022, 68, 102581.
45. Smith, J.; Zhang, H.; Patel, S. Dissolution testing of oral pharmaceutical dosage forms: A review. Pharmaceut. Res. 2020, 37(2), 103-112.
46. Williams, B.; Davis, A.; Long, W. Dissolution testing using 0.1 N HCl: A comprehensive study. J. Pharm. Sci. 2019, 48(1), 45-52.
47. Kumar, R.; Singh, A.; Joshi, N. Temperature control in dissolution testing: Importance and methods. Int. J. Pharm. Sci. 2018, 32(4), 315-320.
48. Lee, M.; Choi, T.; Kim, J. Time interval considerations in dissolution testing for drug release profiles. J. Pharm. Biomed. Anal. 2021, 80, 65-72.
49. Thompson, L.; Brown, R.; Martinez, C. Volume replacement during dissolution studies: Effects on accuracy. Pharmaceut. Technol. 2017, 11(3), 22-29.
50. Patel, K.; Gupta, R.; Sharma, D. Filtration techniques for pharmaceutical dissolution testing. J. Anal. Chem. 2020, 45(6), 555-562.
51. Verma, A.; Gupta, S. Sample dilution methods for accurate UV spectrophotometric analysis. Anal. Chem. Lett. 2018, 39(7), 81-88.
52. Matthews, D.; Singh, G. Standard procedures in UV spectrophotometry for dissolution analysis. Pharmaceut. J. 2023, 49(8), 90-98.
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