Author(s):
Alaa Abdulrazzaq AL- Nuaimi, Asmaa Abdelaziz Mohamed, Jinan M. Al-Mousawy
Email(s):
asmaa.abdelaziz@alzahraa.edu.iq
DOI:
10.52711/0974-360X.2025.00681
Address:
Alaa Abdulrazzaq AL- Nuaimi1, Asmaa Abdelaziz Mohamed1*, Jinan M. Al-Mousawy2
1College of Pharmacy, Al-Zahraa University for Women, Karbala, Iraq.
2Department of pharmaceutics, College of Pharmacy, University of Karbala, Karbala, Iraq.
*Corresponding Author
Published In:
Volume - 18,
Issue - 10,
Year - 2025
ABSTRACT:
Our research was to manufacture of rapid-release tablets containing valsartan (VA). Despite, VA has a high degree of water insolubility, which hinders its oral bioavailability. The tablets were formulated using different methods and excipients like Ac-Di-sol, starch, Avicel PH 101, and Povidone K30 (P.V.P K30). Assessments were conducted to measure weight variation, hardness, content, friability, disintegration, and in vitro dissolution. Some tablet formulations exhibited satisfactory characteristics and adhered to compendial standards. The dissolution studies demonstrated that Ac-Di-Sol, in conjunction with the binding of starch paste, resulted in a dissolution rate of valsartan from formula F8 that exceeded 91% after 10 minutes. The manufactured tablets were compared with commercially available Diovan® 160 mg tablets, Novartis Pharma and the improved formulation was subjected to a stability study. Kneading with starch paste may improve VA flowability and Ac-Di-sol increases the release of VA from the tablets.
Cite this article:
Alaa Abdulrazzaq AL- Nuaimi, Asmaa Abdelaziz Mohamed, Jinan M. Al-Mousawy. Formulation and In vitro Assessment of Valsartan Immediate Release Tablets. Research Journal of Pharmacy and Technology. 2025;18(10):4736-2. doi: 10.52711/0974-360X.2025.00681
Cite(Electronic):
Alaa Abdulrazzaq AL- Nuaimi, Asmaa Abdelaziz Mohamed, Jinan M. Al-Mousawy. Formulation and In vitro Assessment of Valsartan Immediate Release Tablets. Research Journal of Pharmacy and Technology. 2025;18(10):4736-2. doi: 10.52711/0974-360X.2025.00681 Available on: https://www.rjptonline.org/AbstractView.aspx?PID=2025-18-10-20
REFERENCES:
1. Jozo M, Simon N, Yi L, Moczo J, Pukanszky B. Improved Release of a Drug with Poor Water Solubility by Using Electrospun Water-Soluble Polymers as Carriers. Pharmaceutics. 2022; 14, 34. https://doi.org/10.3390/pharmaceutics14010034
2. Yeom DW, Chae BR, Son HY, Kim JH, Chae JS, Song SH, Oh D, Choi YW. Enhanced oral bioavailability of valsartan using a polymer-based supersaturable self-microemulsifying drug delivery system. Int J Nanomedicine. 2017; 12: 3533-3545. https://doi.org/10.2147/IJN.S136599
3. Sapkal, S, Shinde, S, Darakhe, R., Shrikhande, V. Solid Dispersion of Valsartan for Solubility Improvement. World Journal of Pharmaceutical Sciences. 2018; 7: 1863-1883. https://doi.org/10.20959/wjpps20185-12288.
4. Biswas N. Modified mesoporous silica nanoparticles for enhancing oral bioavailability and antihypertensive activity of poorly water-soluble valsartan. Eur J Pharm Sci. 2017; 99: 152-160. https://doi.org/10.1016/j.ejps.2016.12.015.
5. Jensen CE, dos Santos RA, Denadai AM, Santos CF, Braga AN, Sinisterra RD. Pharmaceutical composition of valsartan: beta-cyclodextrin: physico-chemical characterization and anti-hypertensive evaluation. Molecules. 2010; 15(6): 4067-84. https://doi.org/10.3390/molecules15064067.
6. de Castro LML, de Souza J, Caldeira TG, de Carvalho Mapa B, Soares AFM, Pegorelli BG, Della Croce CC, Barcellos NMS. The Evaluation of Valsartan Biopharmaceutics Properties. Curr Drug Res Rev. 2020; 12(1): 52-62. https://doi.org/10.2174/2589977511666191210151120.
7. Park, Y.J., Lee, HK., Im, Y.B. et al. Improved pH-independent dissolution and oral absorption of valsartan via the preparation of solid dispersion. Arch. Pharm. Res.2010; 33:1235–1240. https://doi.org/10.1007/s12272-010-0814-0
8. Saydam M, Takka S. Scientific review: bioavailability file: valsartan. (2007). FABAD J. Pharm. Sci. 2007; 32: 185-196.
9. Hajba-Horváth E, Fodor-Kardos A, Shah N, Wacker MG, Feczkó T. Sustainable Stabilizer-Free Nanoparticle Formulations of Valsartan Using Eudragit® RLPO. Int J Mol Sci. 2021; 22:13069. https://doi.org/10.3390/ijms222313069.
10. Sattar M, Alshawi MA., & Mosa, M.N. Formulation and in Vitro Evaluation of Valsartan Flash Tablet. Systematic Reviews in Pharmacy. 2020; 11:213-219.
11. Tirumalesh N, Chowdary KPR. Formulation Optimization and In Vitro and In Vivo Preclinical Evaluation of Valsartan IR Tablets, International Research Journal of Pharmacy and Medical Sciences. 2019; 2(2): 66-70.
12. Abdalla, A., Hagop, A., Boya, D. Impact of Solubility Enhancement Methods on the Dissolution Rate of Valsartan Sachet. Polytechnic Journal. 2021; 11: 63-69. https://doi.org/10.25156/ptj.v11n1y2021.
13. Kumari P, Kumar K, Joshi A, Chauhan V, Rajput V. Development and Evaluation of Microemulsion Formulations of Valsartan for Solubility Enhancement. Journal of Drug Delivery and Therapeutics. 2023; 13:117-120. https://doi.org/10.22270/jddt.v13i10.5990.
14. Prusty A. Solubility Enhancement of Valsartan Tablets Using Mixture of Alkalizer And Solubilizing Agent, J. Bio. Innov. 2022; 11(3): 851-863. https://doi.org/10.46344/JBINO.2022.v11i03.28
15. Haque M, Amrohi S, Mohanty D, Diwan P. Stability indicating RP-HPLC method for the estimation of Valsartan in pharmaceutical dosage form. IOSR Journal of Pharmacy. 2018; 2 (4): 12-18
16. The Pharmacopoeia of United States of America", 43th Ed., National Formulary 38, Mack publishing Co. Easton, vol. 2, Electronic version, 2020.
17. ICH (2005) Validation of Analytical Procedures: Text and Methodology. International Conference on Harmonization (ICH), Q2(R1), Geneva, 17 pp.
18. Al Jamal M, Al Bathish M, Gazy A. Validated ion exchange HPLC method for the quantification of levothyroxine – a narrow therapeutic index drug – used for the treatment of hypothyroidism. Pharmacia 2023; 70(2): 299-305. https://doi.org/10.3897/pharmacia.70.e103242
19. Suneetha A, Mounika V, Sajid SM. Development and Validation of Stability indicating RP-HPLC Method for the simultaneous Estimation of Sitagliptin and Ertugliflozin in bulk and Tablet Dosage Forms. Asian J. Pharm. Ana. 2020; 10(2): 81-85. https://doi.org/ 10.5958/2231-5675.2020.00014.9
20. Priyanka. R. Varade, Mahavir G. Narwade, Varsha N. Tambe. Method Development and Validation of Irbesartan by RP-HPLC Method. Research J. Science and Tech. 2020; 12(2): 131-135. https://doi.org/10.5958/2349-2988.2020.00016.9
21. Kudupudi Chandrasekhar, A. Manikandan. A New RP-HPLC Method Development and Validation of Paracetamol and Aceclofenac in Tablets by separating Diclofenac. Research J. Pharm. and Tech 2020; 13(9):4334-4338. https://doi.org/10.5958/0974-360X.2020.00766.0
22. Nachiket S. Dighe, Ganesh S. Shinde, Jyoti. J. Vikhe. Simultaneous Estimation, Validation and Force Degradation Study of Metformin Hydrochloride and Empagliflozin by RP-HPLC Method. Research J. Science and Tech. 2019; 11(2):135-147. doi: 10.5958/2349-2988.2019.00021.4
23. Ganesh S Shinde, Godge Rahul K , Ravindra Jadhav. Quantitative Estimation and Validation of Metformin Hydrochloride and Gliclazide in their Tablet Dosage Form by RP-HPLC. Research J. Science and Tech. 2019; 11(3):201-207. https://doi.org/10.5958/2349-2988.2019.00030.5
24. Khairi M. S. Fahelelbom, Moawia M. M. Al-Tabakha, Nermin A. M. Eissa, Dana Emad Eddin Obaid, Sadik Sayed. Development and Validation of an RP-HPLC Analytical Method for Determination of Lisinopril in Full and Split Tablets. Research J. Pharm. and Tech. 2020; 13(6): 2647-2652. https://doi.org/10.5958/0974-360X.2020.00470.9
25. Ahmad S, Khairnar M, Bakhshi A, Tare M, Baheti D, Tare H. QBD approach to develop stability indicating RP-HPLC method development for Levosulpiride and Ilaprazole. International Journal of Health Sciences. 2022; 7413-7429. https://doi.org/10.53730/ijhs.v6nS5.11625.
26. Rahi F, Sheet M, Fayyadh, M. Linagliptin and gliclazide di-loaded extended-release nanoparticles: formulation and evaluation. Wiadomości Lekarskie. 2021; 74: 2315-2322. https://doi.org/10.36740/wlek202109212
27. Chandrasekhar K, Manikandan A. A New RP-HPLC Method Development and Validation of Paracetamol and Aceclofenac in Tablets by separating Diclofenac. Research J. Pharm. and Tech. 2020; 13(9): 4334-4338. https://doi.org/10.5958/0974-360X.2020.00766.0
28. Mandhare S, Godge R, Vikhe A, Talole S. Development and validation of a QbD-based RP-HPLC method for vericiguat quantification. Journal of Applied Pharmaceutical Research. 2024; 12. 57-67. https://doi.org/10.18231/j.joapr.2024.12.2.57.67.
29. Patel D, Patel U, Shukla M, Bhimani B, Patel G. Formulation and Evaluation of Immediate Release Tablet of Simvastatin. Research J. Pharm. and Tech. 2020; 13(1): 421-224. https://doi.org/10.5958/0974-360X.2020.00082.7
30. Sawafta O, Alhadid S, Abu Awwad IA, Migdadi E, Aljaberi A. Impact of the manufacturing technique on the dissolution-enhancement functionality of PEG4000 in Cilostazol tablets. Pharmacia. 2021; 68(1): 243-250. https://doi.org/10.3897/pharmacia.68.e62465
31. Singh P, Kumar P, Prasad N. Formulation and Evaluation of Aspirin Tablets by Using Different Lubricants in Combination for better Kinetic Drug Release Study by PCP. Research J. Pharm. and Tech. 2017; 10(9): 2934-2938. https://doi.org/10.5958/0974-360X.2017.00519.4
32. Darusman F, Rusdiana T, Sopyan I, Aryani R, Cahya Eka Darma G. The in vitro equivalence study of polymorph-modified glimepiride tablets compared to Amaryl®. Pharmacia. 2023; 70(4): 1027-1037. https://doi.org/10.3897/pharmacia.70.e110374.
33. Aulton ME, Taylor KMG in Aultonʼs Pharmaceutics E-Book: The Design and Manufacture of Medicines, Elsevier Health Sciences, London, UK, 2017.
34. Kumar D, Singh J, Antil M, Kumar. V. Quality control of tablets: a review,” International Journal of Universal Pharmacy and Bio Sciences. 2016; 5(4): 54–56.
35. The British Pharmacopoeia", The Stationery Office, London: Electronic version (2022).
36. Berardi A., Bisharat L., Quodbach J., Abdel Rahim S., Perinelli D.R, Cespi, M. Advancing the understanding of the tablet disintegration phenomenon – An update on recent studies. International Journal of Pharmaceutics. 2021; 598:. 120390. https://doi.org/10.1016/j.ijpharm.2021.120390.
37. Rangu N, Chaitanya Kumari B, Akula G, Jaswanth A. Formulation and Evaluation of Metoprolol Orodispersible Tablets by Super Disintegration Method. Asian J. Pharm. Res. 2018; 8(3): 119-124. https://doi.org/10.5958/2231-5691.2018.00021.7
38. Abdelkader A., Moos C., Pelloux A., Pfeiffer M., Alter C., Kolling S, Keck CM. Tablets Made from Paper—An Industrially Feasible Approach. Pharmaceuticals. 2022; 15(10): 1188. https://doi.org/10.3390/ph15101188.
39. Madhavi Latha S, Ramesh Babu J. Comparative study of mode of addition of super Disintegrants on Methocarbamol tablets by Roller Compaction method. Research J. Pharm. and Tech. 2017; 10(7): 2194-2202. https://doi.org/10.5958/0974-360X.2017.00387.0
40. Dilip M. Kumbhar, Vijay D. Havaldar, Kailas K. Mali, Remeth J. Dias, Vishwajeet S. Ghorpade, Rahul B. Londhe. Formulation and Evaluation of Sustained Release Tablets of Venlafaxine Hydrochloride for the treatment of Depressive disorders. Asian J. Pharm. Res. 2017; 7(1): 8-14. https://doi.org/10.5958/2231-5691.2017.00002.8
41. Ansel HC, Popovich N G and Allen LV: Pharmaceutical dosage forms and drug delivery systems. Wolters Kluwer/Lippincott Williams and Wilkins, 9th edition, 2009, 234-237
42. Remington: The Science and Practice of Pharmacy. Mack Publishing Company, 21st Edition 2005, 916-918.
43. Anand, O., Yu, L.X., Conner, D.P. and Davit, B.M. Dissolution Testing for Generic Drugs: An FDA Perspective. The AAPS Journal. 2011; 13(3). https://doi.org/10.1208/s12248-011-9272-y.
44. Hamed, R., Kamal, A. Strength-Dependent and Strength-Independent Dissolution Patterns of Poorly-Soluble Drugs. Case Example: Valsartan. Pharm Chem J. 2021; 54: 1227–1234. https://doi.org/10.1007/s11094-021-02347-7.
45. Ghourichay MP, Kiaie SH, Nokhodchi A, Javadzadeh Y. Formulation and Quality Control of Orally Disintegrating Tablets (ODTs): Recent Advances and Perspectives. Biomed Res Int. 2021 Dec 24; 2021: 6618934. doi: 10.1155/2021/6618934.
46. Singh D. K., Singh S., Bajaj S. Methods for Stability Testing of Pharmaceuticals . Springer; 2018. Regulatory Guidelines on Stability Testing and Trending of Requirements; pp. 1–30.
47. Rao K, Jena N, Rao M. Development and Validation of a Specific Stability Indicating High Performance Liquid Chromatographic Method for Valsartan. Journal of Young Pharmacists: 2010; JYP. 2. 183-9. https://doi.org/10.4103/0975-1483.63166.
48. Peddapatla RVG, Sheridan G, Slevin C, Swaminathan S, Browning I, O’Reilly C, Worku ZA, Egan D, Sheehan S, Crean AM. Process Model Approach to Predict Tablet Weight Variability for Direct Compression Formulations at Pilot and Production Scale. Pharmaceutics. 2021; 13(7): 1033. https://doi.org/10.3390/pharmaceutics13071033
49. Shah S, Patel R, Soniwala M, Chavda J. Development and optimization of press coated tablets of release engineered valsartan for pulsatile delivery. Drug Development and Industrial Pharmacy. 2015; 41: 1-12. https://doi.org/10.3109/03639045.2015.1014374.
50. Shin DJ, Chae BR, Goo YT, Yoon HY, Kim CH, Sohn SI, Oh D, Lee A, Song SH, Choi YW. Improved Dissolution and Oral Bioavailability of Valsartan Using a Solidified Supersaturable Self-Microemulsifying Drug Delivery System Containing Gelucire® 44/14. Pharmaceutics. 2019; 31; 11(2): 58. https://doi.org/10.3390/pharmaceutics11020058