Design and Evaluation of Gastroretentive Multiple Units of Dipyridamole: in-vitro and in-vivo human studies
Gastroretentive Multiple Units of Dipyridamole
Abstract
Objective: The pH dependent solubility of Dipyridamole was made to select as a model drug for the formulation of gastroretentive drug delivery system. Dipyridamole is highly soluble in acidic pH and as the pH increases the solubility of the drug decreases. The study was planned to formulate, characterize with in-vitro and in-vivo evaluation in human volunteers.
Method: In this study floating mini matrix tablets of Dipyridamole was formulated using HPMC grade polymers by wet granulation method and prepared multiple units equivalent to one dose were filled in one 000 size empty gelatin capsule. The prepared multiple units were subjected to physical evaluation, in-vitro drug release, and stability studies as per ICH guidelines. The in-vivo radiographic studies were conducted for determining the residence time of dosage form in human subjects.
Results: All the prepared batches showed good physical properties and in-vitro buoyancy. The optimized FD7 formulation remained buoyant for more than 12 h with drug release of more than 90% in 12 h. The drug release kinetics for optimized formulation FD7 followed a first order kinetics with non fickian mechanism. Formulation FD7 was selected as the best formulation based on the in-vitro characteristics and subjected for stability and in-vivo radiographic studies. These studies revealed that the multiple units were stable during the stability period and remained in the stomach for upto 6 h in human subjects.
Conclusion: Based on in-vitro characteristics and in-vivo radiographic studies, formulation FD7 was concluded as the best formulation among others. Due to increase in gastric retention time, by choosing floating mini matrix tablets we can improve patient compliance and ensure better disease management.
Keywords: Dipyridamole, Mini matrix tablets, In-vitro buoyancy, Stability studies Radiographic Studies
Keywords:
Dipyridamole, Mini matrix tablets, In-vitro buoyancy, Stability studies, Radiographic StudiesDOI
https://doi.org/10.22270/jddt.v12i2.5393References
Streubel A, Siepmann J, Bodmeier R. Gastroretentive drug delivery systems. Expert opinion on drug delivery. 2006 Mar 1; 3(2):217-33. https://doi.org/10.1517/17425247.3.2.217
Badoni A, Ojha A, Gnanarajan G, Kothiyal P. Review on gastro retentive drug delivery system. The pharma innovation. 2012 Oct 1; 1(8, Part A):32.
Sanjay S, Vaibhav J, Kumar BP. Gastro retentive drug delivery systems. InNational Institute of Pharmaceutical Education and Research (NIPER), Pharmatech 2003.
Nayak AK, Malakar J, Sen KK. Gastroretentive drug delivery technologies: Current approaches and future potential. Journal of Pharmaceutical Education and Research. 2010 Dec 1; 1(2):1.
Harker LA, Kadatz RA. Mechanism of action of dipyridamole. Thrombosis research. 1983 Jan 1; 29:39-46. https://doi.org/10.1016/0049-3848(83)90356-0
Kim HH, Liao JK. Translational therapeutics of dipyridamole. Arteriosclerosis, thrombosis, and vascular biology. 2008 Mar 1; 28(3):s39-42. https://doi.org/10.1161/ATVBAHA.107.160226
Kumar K, Gurunath S, Srikanth P, Ajitha M, Rao YM, Development and Clinical Evaluation of Mucoadhesive Gastroretentive Tablets of Dipyridamole. International Journal of Pharmaceutical Sciences and Nanotechnology. 2017; 10(3):3736-3744. https://doi.org/10.37285/ijpsn.2017.10.3.6
Katakam VK, Reddy S, Somagoni JM, Panakanti PK, Rallabandi RC, Rao YM. Preparation and evaluation of a gas formation-based multiple-unit gastro-retentive floating delivery system of dipyridamole. Int J Pharm Sci Nanotechnol. 2012; 5:1607. https://doi.org/10.37285/ijpsn.2012.5.1.3
Zhu CY, Wang JY, Huang J, Han GH, Ji YY, Zhang XR, Liang D. Preparation and evaluation of gastro-floating hollow adhesive microspheres of carbomer/ethyl cellulose encapsulating dipyridamole. New Journal of Chemistry. 2019; 43(15):5897-903. https://doi.org/10.1039/C8NJ06398B
Kumar K, Srikanth P, Ajitha M, Rao YM, formulation and evaluation of floating matrix tablets of Dipyridamole; Am. J. PharmTech Res. 2015; 5(4):131- 144.
Katakam VK, Reddy S, Somagoni JM, Panakanti PK, Rallabandi RC, Rao YM. Preparation and evaluation of a gas formation-based multiple-unit gastro-retentive floating delivery system of dipyridamole. Int J Pharm Sci Nanotechnol 2012; 5:1607-16. https://doi.org/10.37285/ijpsn.2012.5.1.3
Momin S, Khan S, Ghadage DM, Yadav AV, Wagh A, Formulation and evaluation of bilayer tablets of propranolol hydrochloride. Journal of Drug Delivery and Therapeutics 2017; 7(2):50-57 https://doi.org/10.22270/jddt.v7i2.1399
Kumar K, Srikanth P, Ajitha M, Rao YM, formulation and evaluation of floating mini matrix tablets of Thiamine mononitrate; WJPR; 2015; 4(5):2718-2736.
Baumgartner S., Kristl J., Vrecer F., Vodopivec P., Zorko B. Optimization of floating matrix tablets and evaluation of their gastric residence time. Int. J. Pharm. 2000; 195:125-135. https://doi.org/10.1016/S0378-5173(99)00378-6
Dhumal R.S., Rajmane S.T., Dhumal S.T., Pawar A.P. Design and evaluation of bi-layered floating tablets of cefuroxime axetil for bimodal release. J. Sci. Ind. Res. 2006; 65:812-816
Machida Y., Inouy K., Tokumura T., Iwata M., Nagai T. Preparation and evaluation of intragastric buoyant preparations. Drug Des. Deliv. 1989; 4:155-161.
Kumar K, Srikanth P, Ajitha M, Rao YM, Design and Clinical Evaluation of Floating Mini Matrix Tablets of Pyridoxine HCl. Asian Journal of Pharmaceutics. Apr-Jun 2017; 11(2):159-167.
Swarnalatha N, Kumar K, Vidhyawathi M, International Journal of Pharmaceutical Research, Formulation, Invitro And Invivo Evaluation Of Taste Masked Oral Disintegrating Tablets Of Famotidine. International Journal of Pharmaceutical Research. 2019; 11(2):370-382. https://doi.org/10.31838/ijpr/2019.11.02.047
Xi Z, Sharma N, Paprikar A, Lin S. Development and evaluation of dipyridamole sustained release tablets containing micro-environmental pH modifiers. Journal of Drug Delivery Science and Technology. 2019 Dec 1; 54:101231. https://doi.org/10.1016/j.jddst.2019.101231
Mohammed F.A., Khedr H. Preparation and in vitro/in vivo evaluation of the buccal bioadhesive properties of slow-release tablets containing miconazole nitrate. Drug Dev. Ind. Pharm. 2003; 29(3):321-337. https://doi.org/10.1081/DDC-120018206
Kumar K, Srikanth P, Ajitha M, Rao YM, formulation and evaluation of floating matrix tablets of Dipyridamole; Am. J. PharmTech Res. 2015; 5(4):131- 144.
Rosa M., Zia H., Rhodes T. Design and testing in vitro of a bioadhesive and floating drug delivery system for oral application. Int. J. Pharm. 1994; 105:65-70. https://doi.org/10.1016/0378-5173(94)90236-4
Mathews BR. Regulatory aspects of stability testing in Europe. Drug Dev. Ind. Pharm 1999; 25:831-856. https://doi.org/10.1081/DDC-100102245
Moore J. W., Flanner H. H.. Mathematical comparison of curves with an emphasis on in-vitro dissolution profiles. Pharm. Technol. 1996; 20:64-74.
Kumar K, Gurunath S, Ajitha M, Rao YM, Design and Evaluation of Mucoadhesive Gastroretentive dosage form of Atenolol - in-vitro and in-vivo human studies. Iranian Journal of Pharmaceutical Sciences. 2021; 16(4):53-70
Lingam M, Bhasker K, Mohan CK, Venkateswarlu V, Rao YM. Preparation of a matrix type multiple unit gastro retentive floating drug delivery system for captopril based on gas formation technique: in vitro evaluation. AAPS Pharm Sci Tech, 2008; 9(2):612-619. https://doi.org/10.1208/s12249-008-9090-4
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