Formulation, design, and evaluation of valsartan sodium-sustained-release matrix tablets
Abstract
The main aim of present work was to formulate and evaluate sustain release matrix tablets of Valsartan, an angiotensin II Receptor type 1 antagonist. Sustain release formulation are those which delivers the drug locally or systemically at a predetermined rate for a fixed period of time. The matrix tablet was prepared by direct compression method using by various concentration of chitosan and sodium alginate with combination of various release retardant polymer. The powder mixtures were subjected to various pre-compression parameters such as angle of repose, bulk density, tapped density and Carr’s index shows satisfactory result and the compressed tablets are evaluated for post-compression parameters such as weight variation, thickness, hardness, friability, drug content, in-vitro dissolution and stability studies. In-vitro dissolution studies were carried out for 24 hours using 0.1N HCl for first 2 hours and pH 6.8 phosphate buffers for 24 hours and the result showed that formulations F4 and F7 showed good dissolution profile to control the drug release respectively. Formulation containing higher concentration of chitosan and sodium alginate along with polymers sustainedthedrugreleasefor theperiodof24hours.The compatibilityof thedrug, polymers and other excipients were determined by FT-IR Spectroscopy. Results showed that the drug was compatible with polymers and other excipients. The release data was fitted to various mathematical models such as Zero-order, First-order, Higuchi equation and Korsmeyer- Peppas model to evaluate the kinetics and the drug release. The drug release followed first order and the mechanism was found to be non-Fickian. The stability studies were carried out for 3 months and result indicates that the selected formulations (F4and F7) were stable.
Keywords:
Antihypertensive, Carbopol 934P, Chitosan, Sodium alginate, Sustain release matrix tablet, Valsartan
References
1. Ravi Y, Najmuddin M and Dewalkar HV. Development and Evaluation of Theophylline Microballoons Drug Delivery System. Int Res J Pharm. 2012;3(5):241-245.
2. Kumar S, Kumar A, Gupta V, Malodia K and Rakha P. Oral Extended Release Drug Delivery System: A Promising Approach. Asian J Pharm Tech. 2012;2(2):38-43.
3. Rathore AS, Jat RC, Sharma N and Tiwari R. An Overview: Matrix Tablet as Controlled Drug Delivery System. Int J Res and Development in Pharm and Life Sci. 2013;2(4):482-492.
4. Chugh I, Seth N and Rana A.C. Oral sustained release drug delivery system. Int Res JPharmacy 2012;3(5):57-62.
5. Vinay K, S K Prajapati, Girish C,S, Mahendra S and Neeraj k. Sustained release matrix type drug delivery system. IRJP 2012;1(3):934-60.
6. ParasharT, Soniya, Singh V, Singh G, Tyagi S, Patel C and Gupta A. Novel Oral Sustained Release Technology: A Concise Review. Int J Res & Development in Pharm and Life Sci. 2013;2(2):262-269.
7. Hemnani M, Patel U, Patel G, Daslaniya D, Shah A and Bhimani B. Matrix Tablets: A Tool of Controlled Drug Delivery. American J PharmTech Res. 2011;1(4):127-143.
8. Ankit B, Rathore RPS, Tanwar YS, Gupta S and Bhaduka G. Oral Sustained Release Dosage Form: An Opportunity to Prolong the Release of Drug. Int J Advanced Res Pharm & Bio Sci. 2013;3(1):7-14.
9. Chowdary KPR and Kalyani GS. Recent Research on Matrix Tablets for Controlled Release – A Review. Int Res J Pharmaceutical & Applied Sci. 2013;3(1):142-148.
10. Gennaro AR. (Ed.) Remington’s. pharmaceutical science. 20thEdn. Lippincott Williams and wilkini publishing co, Newyork. 2000;1:905-06.
11. Zalte HD, Saudagar RB. Review on Sustained Release Matrix Tablet. Int J Pharm & Bio Sci. 2013;3(4):17-29.
12. Neetu K, Ajay B, Kumar KM, Ankit G. Patented Pharmaceutical Oral Controlled Release Matrix System. J Biological & Scientific Opinion. 2013;1(3):263-270.
13. Patel H, Panchal DR, Patel U, Brahmbhatt T, Suthar M. Matrix Type Drug Delivery System: A Review. J Pharm SciBiosci Res. 2011;1(3):143–51
14. Dash TR, Varma P. Matrix Tablets: An Approach Towards Oral Extentded Release Drug Delivery. Int J Pharma Res & Review. 2013;2(2).
15. Rieder A. Awareness and control of hypertension in Austria. J Human Hypertension. 2004:535-537.
16. Ramu Samineni, K Sumalatha, G Dharani, J Rachana, P Anitha, K Manasa. Formulation and Evaluation of Oral Disintegrating Tablets of Montelukast Sodium and Desloratidine. Research Journal of Pharmaceutical Dosage Forms and Technology. 2019; 11(3): 152-158.
17. Tanira MOM, Balushi KA. Genetic Variations Related To Hypertension: A Review. J Human Hypertension. 2005:7-19.
18. Remington’s The Science and Practice of Pharmacy, 20thEdn., Lippincott Williams andWilkins,ThomasWai-Yip Lee and Joseph R. Robinson,In; Maryland. 2000: 1069-1070.
19. Ramu Samineni, Jithendra Chimakurthy, Sathish Kumar Konidala, Udayaratna K, Devatulasi K, Ager Dengoc. Effect of Hydroxy propyl methyl cellulose and microcrystalline cellulose in design and optimization of Nebivolol Hydrochloride immediate release tablets by response surface methodology. International Journal of Research in Pharmaceutical Science. 2021; 12(3): 1990-1998
20. Harsh Mohan. The kidney and lower urinary tract. In chapter 19, Texbook of pathology: 4th edition. New Delhi:Jayppe Brothers Medical Pubhlishers; 2000:670-672.
21. NealL,BenowitzMD.Anti-hypertensiveAgents.Inchapter11,Basicandclinical pharmacology, 6th edition, editorBertram G.KatzungAppleton and Lange: 1995; 147:165-166.
22. Appel LJ. ASH Position Paper: Dietary Approaches to Lower Blood Pressure. J Clinical Hypertension. 2009;11(9):358-368.
23. Tripathi KD. Anti- hypertensive drugs. Essentials of medical pharmacology. 5th edition, Jayppe brothers medical publishers; New Delhi;
24. Smith DHG. Comparison of Angiotensin II Type 1 Receptor Antagonists in the Treatment of Essential Hypertension. Drugs. 2008;68(9):1207-1225.
25. Babu GD, Sagar KC and Bhoot MR. Design and Evaluation of Valsartan Transdermal Patches. Int J Res Ayurveda & Pharmacy. 2012;3(3):461-464.
26. SH Lakade and MR Bhalekar. Formulation and Evaluation of Sustained Release Matrix Tablet of Anti-Anginal Drug Influence of Combination of Hydrophobic and Hydrophlic Matrix Former. Research J. Pharm.2008;1(4):410-13.
27. Ramu Samineni, G Ramakrishna, M Balaji, K Kondala Rao. Formulation and evaluation of sumatriptan succinate mouth disintegrating tablets. American J Advanced Drug Delivery. 2013; 1(5): 759-769.
28. Shanmugam S, Ramya C, Sundaramoorthy K, Ayyappan T, Vetrichelvan T. Formulation and evaluation of sustained release matrix tablets of Losartan potassium. IJPRIF 2011;3(1):526-34.
29. Krishnaiah YSR, Karthikeyan RS, Satyanarayana V. A three-layer guar gum matrix tablet for oral controlled delivery of highly soluble metoprolol tartrate. IntJ Pharm 2002; (241): 353-66.
30. Akhlaq M, Majid GK, Abdul W, Abid H, Arshad K, Asif N, Kifayat US. Formulation and in-vitro evaluation of Flurbiprofen controlled release matrix tablets using cellulose derivative polymers. Pak. J. Pharm 2007-2010;20- 23(1&2):23-29.
31. S Ramu, Y Ashok Kumar, D Srinivasa Rao, G Ramakrishna. Formulation and evaluation of Valsartan oral dispersible tablets by direct compression method. American Journal of Advanced Drug Delivery. 2014; 2(6): 719-733.
32. Tabandeh H, Mortazavi SA, Guilani TB. Preparation of sustained-release matrix tablet of asprin with ethyl cellulose, eudragit RS100 and studying the release profilesandtheirsensitivitytotablethardness.IranianJPharmRes2003;2: 201-06.
33. Phani Kumar GK, Gangarao B, LovaRaju NSK. Preparation and evaluation of sustained release matrix tablets of Lornoxicam using tamarind seed polysaccharide. IJPRD 2011;2(12):89-98.
34. Ramu Samineni, P. Aravanan, Jithendra Chimakurthy, Y. Ratna Sindhu, B. Jeevan Kumar, M.S. Srikanth. Factorial Design and Optimization of Antiepileptic Drug: Lamotrigine Cocrystals Immediate Release Tablets. Journal of Positive School Psychology. 2022; 6(9): 4070-4077.
35. Yassin EI- Said Hamza, Mona Hassan Aburahma. Design and invitroevalution of novel sustained- release Double- layer tablets of Lorinoxicam: Utility of cyclodextrin and xantan gum combination.AAPS pharm sciTech.2009;10(4):1357-67.
36. Ravi KN, Narayanaswamy VB, Senthil A, Mehul D, Tejas L, Mahalaxmi R. Formulation and evaluation of sustained release matrix tablets of Lornoxicam. Indo-Global Research Journal of Pharmaceutical Sciences 2011;1(3):92-99.
37. Uddin M. Development of sustained release tablet of Valsartan. World J Pharm Pharma Sci. 2015;3(5):1196-05.
38. Sharma V, Sharma S, Khokra SL, Sahu RKR, Jangde R, Singh J. Formulation, development and evaluation of Pregabalin Sustained release matrix tablets. Der Pharmacia Lettre. 2011; 3(5):326-31.
39. Madhavi N, Sudhakar B, Ravikanth PV, Mohon K, Kolapalli RM. Formulation and Evaluation of Phenytoin Sodium Sustained Release Matrix Tablet. Bioequivalence and Bioavailability. J BioequivAvailab. 2012; 4 (7):128-133.
40. KatareVB,Bhutkar MA,KumbharAP,PolSK,KatarePB.Formulationand Evaluation of Sustained Release Matrix Tablets of Pregabalin. Research Journalof Pharmacy and Technology. 2013; 6: 1190-94.
41. Ali MS, Singh S, kumar A, singh S, Ansari MT,pattnaik G. Preparation and in- vitro evaluation of sustained release matrix tablets of phenytoin sodium using natural polymers. InternationalJournal ofPharmacyand Pharmaceutical Sciences. 2010; 2(3):174-179.
42. Subramaniam K, Rangasamy M, Kugalur G, Parthiban KN, Senthil NK. Formulation and evaluation of sustained release tablets of Aceclofenac using hydrophilic matrix system. IJPRIF 2010;2(3):1775-78.
43. Ramu Samineni, Dr. Ram Kumar Choudhary*, D.P. Sujala, Anwar Khan, Dr. Sampath A Gouru, Molakpogu Ravindra Babu, Palakurthi Yanadaiah . A Prospective Review on Novel Strategies for Preparation and Evaluation of Nanosponge Tablets. European Chemical Bulletin. 2023; 12(5): 2482-2496.
2. Kumar S, Kumar A, Gupta V, Malodia K and Rakha P. Oral Extended Release Drug Delivery System: A Promising Approach. Asian J Pharm Tech. 2012;2(2):38-43.
3. Rathore AS, Jat RC, Sharma N and Tiwari R. An Overview: Matrix Tablet as Controlled Drug Delivery System. Int J Res and Development in Pharm and Life Sci. 2013;2(4):482-492.
4. Chugh I, Seth N and Rana A.C. Oral sustained release drug delivery system. Int Res JPharmacy 2012;3(5):57-62.
5. Vinay K, S K Prajapati, Girish C,S, Mahendra S and Neeraj k. Sustained release matrix type drug delivery system. IRJP 2012;1(3):934-60.
6. ParasharT, Soniya, Singh V, Singh G, Tyagi S, Patel C and Gupta A. Novel Oral Sustained Release Technology: A Concise Review. Int J Res & Development in Pharm and Life Sci. 2013;2(2):262-269.
7. Hemnani M, Patel U, Patel G, Daslaniya D, Shah A and Bhimani B. Matrix Tablets: A Tool of Controlled Drug Delivery. American J PharmTech Res. 2011;1(4):127-143.
8. Ankit B, Rathore RPS, Tanwar YS, Gupta S and Bhaduka G. Oral Sustained Release Dosage Form: An Opportunity to Prolong the Release of Drug. Int J Advanced Res Pharm & Bio Sci. 2013;3(1):7-14.
9. Chowdary KPR and Kalyani GS. Recent Research on Matrix Tablets for Controlled Release – A Review. Int Res J Pharmaceutical & Applied Sci. 2013;3(1):142-148.
10. Gennaro AR. (Ed.) Remington’s. pharmaceutical science. 20thEdn. Lippincott Williams and wilkini publishing co, Newyork. 2000;1:905-06.
11. Zalte HD, Saudagar RB. Review on Sustained Release Matrix Tablet. Int J Pharm & Bio Sci. 2013;3(4):17-29.
12. Neetu K, Ajay B, Kumar KM, Ankit G. Patented Pharmaceutical Oral Controlled Release Matrix System. J Biological & Scientific Opinion. 2013;1(3):263-270.
13. Patel H, Panchal DR, Patel U, Brahmbhatt T, Suthar M. Matrix Type Drug Delivery System: A Review. J Pharm SciBiosci Res. 2011;1(3):143–51
14. Dash TR, Varma P. Matrix Tablets: An Approach Towards Oral Extentded Release Drug Delivery. Int J Pharma Res & Review. 2013;2(2).
15. Rieder A. Awareness and control of hypertension in Austria. J Human Hypertension. 2004:535-537.
16. Ramu Samineni, K Sumalatha, G Dharani, J Rachana, P Anitha, K Manasa. Formulation and Evaluation of Oral Disintegrating Tablets of Montelukast Sodium and Desloratidine. Research Journal of Pharmaceutical Dosage Forms and Technology. 2019; 11(3): 152-158.
17. Tanira MOM, Balushi KA. Genetic Variations Related To Hypertension: A Review. J Human Hypertension. 2005:7-19.
18. Remington’s The Science and Practice of Pharmacy, 20thEdn., Lippincott Williams andWilkins,ThomasWai-Yip Lee and Joseph R. Robinson,In; Maryland. 2000: 1069-1070.
19. Ramu Samineni, Jithendra Chimakurthy, Sathish Kumar Konidala, Udayaratna K, Devatulasi K, Ager Dengoc. Effect of Hydroxy propyl methyl cellulose and microcrystalline cellulose in design and optimization of Nebivolol Hydrochloride immediate release tablets by response surface methodology. International Journal of Research in Pharmaceutical Science. 2021; 12(3): 1990-1998
20. Harsh Mohan. The kidney and lower urinary tract. In chapter 19, Texbook of pathology: 4th edition. New Delhi:Jayppe Brothers Medical Pubhlishers; 2000:670-672.
21. NealL,BenowitzMD.Anti-hypertensiveAgents.Inchapter11,Basicandclinical pharmacology, 6th edition, editorBertram G.KatzungAppleton and Lange: 1995; 147:165-166.
22. Appel LJ. ASH Position Paper: Dietary Approaches to Lower Blood Pressure. J Clinical Hypertension. 2009;11(9):358-368.
23. Tripathi KD. Anti- hypertensive drugs. Essentials of medical pharmacology. 5th edition, Jayppe brothers medical publishers; New Delhi;
24. Smith DHG. Comparison of Angiotensin II Type 1 Receptor Antagonists in the Treatment of Essential Hypertension. Drugs. 2008;68(9):1207-1225.
25. Babu GD, Sagar KC and Bhoot MR. Design and Evaluation of Valsartan Transdermal Patches. Int J Res Ayurveda & Pharmacy. 2012;3(3):461-464.
26. SH Lakade and MR Bhalekar. Formulation and Evaluation of Sustained Release Matrix Tablet of Anti-Anginal Drug Influence of Combination of Hydrophobic and Hydrophlic Matrix Former. Research J. Pharm.2008;1(4):410-13.
27. Ramu Samineni, G Ramakrishna, M Balaji, K Kondala Rao. Formulation and evaluation of sumatriptan succinate mouth disintegrating tablets. American J Advanced Drug Delivery. 2013; 1(5): 759-769.
28. Shanmugam S, Ramya C, Sundaramoorthy K, Ayyappan T, Vetrichelvan T. Formulation and evaluation of sustained release matrix tablets of Losartan potassium. IJPRIF 2011;3(1):526-34.
29. Krishnaiah YSR, Karthikeyan RS, Satyanarayana V. A three-layer guar gum matrix tablet for oral controlled delivery of highly soluble metoprolol tartrate. IntJ Pharm 2002; (241): 353-66.
30. Akhlaq M, Majid GK, Abdul W, Abid H, Arshad K, Asif N, Kifayat US. Formulation and in-vitro evaluation of Flurbiprofen controlled release matrix tablets using cellulose derivative polymers. Pak. J. Pharm 2007-2010;20- 23(1&2):23-29.
31. S Ramu, Y Ashok Kumar, D Srinivasa Rao, G Ramakrishna. Formulation and evaluation of Valsartan oral dispersible tablets by direct compression method. American Journal of Advanced Drug Delivery. 2014; 2(6): 719-733.
32. Tabandeh H, Mortazavi SA, Guilani TB. Preparation of sustained-release matrix tablet of asprin with ethyl cellulose, eudragit RS100 and studying the release profilesandtheirsensitivitytotablethardness.IranianJPharmRes2003;2: 201-06.
33. Phani Kumar GK, Gangarao B, LovaRaju NSK. Preparation and evaluation of sustained release matrix tablets of Lornoxicam using tamarind seed polysaccharide. IJPRD 2011;2(12):89-98.
34. Ramu Samineni, P. Aravanan, Jithendra Chimakurthy, Y. Ratna Sindhu, B. Jeevan Kumar, M.S. Srikanth. Factorial Design and Optimization of Antiepileptic Drug: Lamotrigine Cocrystals Immediate Release Tablets. Journal of Positive School Psychology. 2022; 6(9): 4070-4077.
35. Yassin EI- Said Hamza, Mona Hassan Aburahma. Design and invitroevalution of novel sustained- release Double- layer tablets of Lorinoxicam: Utility of cyclodextrin and xantan gum combination.AAPS pharm sciTech.2009;10(4):1357-67.
36. Ravi KN, Narayanaswamy VB, Senthil A, Mehul D, Tejas L, Mahalaxmi R. Formulation and evaluation of sustained release matrix tablets of Lornoxicam. Indo-Global Research Journal of Pharmaceutical Sciences 2011;1(3):92-99.
37. Uddin M. Development of sustained release tablet of Valsartan. World J Pharm Pharma Sci. 2015;3(5):1196-05.
38. Sharma V, Sharma S, Khokra SL, Sahu RKR, Jangde R, Singh J. Formulation, development and evaluation of Pregabalin Sustained release matrix tablets. Der Pharmacia Lettre. 2011; 3(5):326-31.
39. Madhavi N, Sudhakar B, Ravikanth PV, Mohon K, Kolapalli RM. Formulation and Evaluation of Phenytoin Sodium Sustained Release Matrix Tablet. Bioequivalence and Bioavailability. J BioequivAvailab. 2012; 4 (7):128-133.
40. KatareVB,Bhutkar MA,KumbharAP,PolSK,KatarePB.Formulationand Evaluation of Sustained Release Matrix Tablets of Pregabalin. Research Journalof Pharmacy and Technology. 2013; 6: 1190-94.
41. Ali MS, Singh S, kumar A, singh S, Ansari MT,pattnaik G. Preparation and in- vitro evaluation of sustained release matrix tablets of phenytoin sodium using natural polymers. InternationalJournal ofPharmacyand Pharmaceutical Sciences. 2010; 2(3):174-179.
42. Subramaniam K, Rangasamy M, Kugalur G, Parthiban KN, Senthil NK. Formulation and evaluation of sustained release tablets of Aceclofenac using hydrophilic matrix system. IJPRIF 2010;2(3):1775-78.
43. Ramu Samineni, Dr. Ram Kumar Choudhary*, D.P. Sujala, Anwar Khan, Dr. Sampath A Gouru, Molakpogu Ravindra Babu, Palakurthi Yanadaiah . A Prospective Review on Novel Strategies for Preparation and Evaluation of Nanosponge Tablets. European Chemical Bulletin. 2023; 12(5): 2482-2496.
Published
22/06/2024
Statistics
452 Views | 347 Downloads
Citatons
How to Cite
P, S. S., G, H. B., K, U., & M. , K. B. (2024). Formulation, design, and evaluation of valsartan sodium-sustained-release matrix tablets. The Journal of Multidisciplinary Research, 4(2), 1-13. https://doi.org/10.37022/tjmdr.v4i2.577
Issue
Section
Research Articles
This work is licensed under a Creative Commons Attribution-NonCommercial 4.0 International License.
Copyright © Author(s) retain the copyright of this article.
.