Author(s):
Amaresh Prusty, Bijon K Gupta, Amiyakanta Mishra
Email(s):
amareshprusty@gmail.com
DOI:
10.52711/0974-360X.2022.00827
Address:
Amaresh Prusty1*, Bijon K Gupta2, Amiyakanta Mishra3.
1Department of Pharmaceutics, College of Pharmaceutical Sciences, Puri. Odisha. 752002. India.
2Jadavpur University of Technology, West Bengal.
3College of Pharmaceutical Sciences, Puri. Odisha. 752002. India.
*Corresponding Author
Published In:
Volume - 15,
Issue - 11,
Year - 2022
ABSTRACT:
In this experimental work an extended release matrix tablet of Benidipine Hydrochloride (BH) has been prepared to extend drug release for more than 18 hr which has advantage of continuous 24 hr control of blood pressure (BP) in hypertension patient, showing long-lasting pharmacological activity and increases the patient compliance. Benidipine is a calcium channel blocker that is used for the treatment of mild to moderate hypertension and angina pectoris and BH extended release tablets reduce the side effects associated with multiple dosing used during conventional tablets. Tablets are prepared tablets containing different polymers concentration through direct compression method. The in vitro percentage drug release and drug release mechanism were studied. From the drug release mechanism, the tablets showed the Higuchi square root model and R2 values for batch F2 (R2 =0.998) indicates that the drug released by diffusion mechanism and from Peppas equation n value 0.720 (range 0.89-1) indicates that diffusion–erosion mechanisms resulting from swelling and hydration behavior of Chitosan and along with HPMC K 100 M and Eudragit R S 100 extending drug release. Different pharmacokinetics parameters has been studied from results of in vivo study by using PK solver software which shows that marketed conventional BH tablet reached peak plasma concentration of 830.986 µg/ml after 2 hr of administration, where as selected optimized prepared tablets reached the maximum concentration of 708.83 µg/ml after 1 hr of administration, but it continues to release drug for more than 36 hr when in vivo was carried out in carried out on white New Zealand rabbits. These results proved that drug is released slowly for prolonged period of time and achieving better BP control. So based on this research outcome and results, we may conclude our objective is achieve by extending drug release pattern of BH.
Cite this article:
Amaresh Prusty, Bijon K Gupta, Amiyakanta Mishra. Formulation and In Vivo Evaluation of Pharmacokinetics Parameters of Extended Release Matrix Tablet Containing Drug Benidipine Hydrochloride by Using PK Solver Software. Research Journal of Pharmacy and Technology. 2022; 15(11):4924-0. doi: 10.52711/0974-360X.2022.00827
Cite(Electronic):
Amaresh Prusty, Bijon K Gupta, Amiyakanta Mishra. Formulation and In Vivo Evaluation of Pharmacokinetics Parameters of Extended Release Matrix Tablet Containing Drug Benidipine Hydrochloride by Using PK Solver Software. Research Journal of Pharmacy and Technology. 2022; 15(11):4924-0. doi: 10.52711/0974-360X.2022.00827 Available on: https://www.rjptonline.org/AbstractView.aspx?PID=2022-15-11-12
REFERENCES:
1. Lazdunski M, Frelin C and Vibne P. The sodium/hydrogen exchange system in cardiac cells: Its biochemical and pharmacological properties and its role in regulating internal concentrations of sodium and internal pH. J Mol Cell Cardiol. 1985; 17:1029-1042. doi: 10.1016/s0022-2828(85)80130-9
2. Mahnensmith RL and Aronson PS. The plasma membrane sodium hydrogen exchanger and its role in physiological and pathophysiological processes. Circ Res. 1985; 57: 773-788. https://doi.org/10.1161/01.RES.56.6.773
3. Seki S, Taniguchi M, Takeda H, Nagai M, Taniguchi I and Mochizuki S. Inhibition by KB-R7943 of the reverse mode of the Na+/Ca2+ exchanger reduces Ca2+ overload in ischemic-reperfused rat hearts. Circ J. 2002; 66: 390-396. https://doi.org/10.1253/circj.66.390
4. Tani M, Asakura Y, Hasegawa H, Shinmura K, Ebihara Y and Nakamura Y. Effect of preconditioning on ryanodine-sensitive Ca2+ release from sarcoplasmic reticulum of rat heart. Am J Physiol. 1996; 271: H876-H881.
5. Jahangir A, Ozcan C, Holmuhamedo EL and Terzic A. Increased calcium vulnerability of senescent cardiac mitochondria: Protective role for a mitochondrial potassium channel opener. Mech Ageing Dev. 2001; 122: 1073-1086. DOI: 10.1016/s0047-6374(01)00242-1
6. Borgers M, Thone F, Van Reempts J and Verheyen F. The role of calcium in cellular dysfunction. Am J Emerg Med. 1983;1: 154-161. DOI: 10.1016/0735-6757(83)90083-9
7. Hoshide S, Kario K, Mitsuhashi T, Ikeda U and Shimada K. Is there any difference between intermediate-acting and long-acting calcium antagonists in diurnal blood pressure and autonomic nervous activity in hypertensive coronary artery disease patients? Hypertens Res. 2000; 23:7-14.
8. Scholz H. Pharmacological aspects of calcium channel blockers. Cardiovasc Drugs Ther 1997; 10(S3):869-872.
9. Putikam JK , Rao YN , Anjaneyulu V and Undralla VK. Formulation and Evaluation of Metoprolol Succinate Extended Release Tablet. Research J. Pharm. and Tech. 2012; 5 (1): 75-78.
10. Aher SS, Songire PR, Saudagar RB. Formulation and Evaluation of Controlled Release Matrix Tablet of Albuterol Sulphate. International Journal of Current research. 2016; 8 (7): 35044-35050.
11. Prusty A, Mishra AK and Gupta BK. Development and evaluation of matrix tablet by taking new chemicals combination of chitosan and eudragit-l 100. J Young Pharm. 2016; 8(3): 168-176. doi:10.5530/jyp.2016.3.2
12. Prusty A and Gupta BK. Effect of Polymer in Release Profile of Extended Release Matrix Tablet Of Anti-Hypertensive Drug & To Study Impact Of Agglomerative Phase Of Comminution (Apoc) Method On Drug Release. IJPSR. 2018; 9(10): 1000-08.
13. Noda H, Saito Y and Fujita T. The antihypertensive effect and pharmacokinetics after single oral administration of Benidipine hydrochloride in patients with essential hypertension. Jpn Pharmacol Ther. 1990; 18: S703-S711.
14. Kobayashi H and Kobayashi S. Relationship between plasma concentration and antihypertensive effect of the dihydropyridine calcium antagonist, Benidipine, in rats. J Pharm Pharmacol. 1997;49:1200-1204. DOI: 10.1111/j.2042-7158.1997.tb06070.x
15. Dredan J, Istvan R, Istvan A, et al. Evaluation of mathematical model describing drug release from lipophilic matrices. Int J Pharm 1996; 145(1,2):61-64. https://doi.org/10.1016/S0378-5173(96)04725-4
16. Higuchi T. Mechanism of sustained-action medication. Theoretical analysis of rate of release of solid drugs dispersed in solid matrices. J Pharm Sci 1963; 52(12):1145-1149. https://doi.org/10.1002/jps.2600521210
17. Ritger PL and Peppas NA. A simple equation for description of solute release I. Fickian and non-fickian release from nonswellable devices in the form of slabs, spheres, cylinders or discs. J Control Release. 1987; 5: 23-36. https://doi.org/10.1016/0168-3659(87)90034-4
18. Baker RW, Lonsdale HK, Lacey RE, et al. Controlled release of biologically active agents plenum; 1974. pp. 15-71.
19. Mendyk A and Jachowicz R. Unified methodology of neural analysis in decision support systems built for pharmaceutical technology. Expert Systems with applications. 2007; 32: 1124–1131.
20. Zhang Y , Huo M, Zhou J and Xie S. PK Solver: An add-in program for pharmacokinetic and pharmacodynamic data analysis in Microsoft Excel. Comput Methods Programs Biomed. 2010; 99(3):306-14
21. Amsa P, Kosalge A, Tamizharasi S, Karthikeyan D, Sivakumar T and Shinde V. Formulation and Evaluation of Chitosan Nanoparticle of Acyclovir. Research J. Pharm. and Tech. 2010; 3 (1): 121-126
22. Peck GE, Baley GJ, McCurdy VE and Banker GS. Tablet formulation and design. In: Pharmaceutical Dosage Forms: Tablets. 2nd ed. New York: Marcel Dekker; 1989. p. 109-12.
23. Ray MR, Bose SK and Sengupta K. Design, Development and In Vitro Evaluation of Directly CompressedSustained Release Matrix Tablet of Famotidine. Research J. Pharm. and Tech. 2008; 1 (3): 175-178
24. Khanum A and Devi GS. Comparative Evaluation of Matrix Tablet of Diclofenac Sodium Employing Wet Granulation and Direct Compression Method Using Blend of Polymers. Research J. Pharm. and Tech. 2008; 1 (3): 265-269.
25. Lakade SH and Bhalekar MR. Formulation and Evaluation of Sustained Release Matrix Tablet of Anti-Anginal Drug, Influence of Combination of Hydrophobic and Hydrophlic Matrix Former. Research J. Pharm. and Tech. 2008; 1 (4): 410-413.