Azharuddin, K S (2014) Formulation and Evaluation of Felodipine Solid Dispertions. Masters thesis, Annai Veilankanni’s Pharmacy College, Chennai.
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Abstract
OBJECTIVES: Felodipine is used as an antihypertensive and antianginal drug, widely used orally in the treatment of hypertension. The model drug belongs to BCS class II and undergoes extensive first-pass metabolism with a bioavailability of only about 15%. Hence this work was planned to improve the oral bioavailability of felodipine by increasing its solubility and dissolution characteristics through the solid dispersion technique using polyethylene glycol (PEG 4000) and hydroxypropyl cellulose (HPC) as carriers. METHODS: Solid binary systems of felodipine were prepared with PEG 4000 by solvent deposition (SD) and kneading method (KM) at different drug:carrier ratios of 1:1, 1:3 and 1:5. Then ternary systems were prepared with the addition of different concentrations of HPC to felodipine-PEG 4000 binary systems to investigate the effect of hydrophilic polymer on the solubility and dissolution rate of the felodipine. Solid binary and ternary systems were characterized by drug content, FT-IR, XRD and in vitro dissolution test using USP dissolution test apparatus Type II (paddle method) in dissolution medium of 0.1N HCl. The in vitro dissolution results of all preparations were computed by using dissolution software PCP DISSO V3. RESULTS: All prepared solid binary and ternary systems were found to be fine and free flowing. Low standard deviation (SD) values (i.e., < 1) indicated uniform drug distribution in all prepared batches. FT-IR studies indicated the possibility of intermolecular hydrogen bonding between amide group of the felodipine and hydroxyl group of the PEG 4000. The XRD results indicated the significant reduction in felodipine crystallinity in the solid binary and ternary systems. The DE30 and DE60 values of the solid binary systems prepared by the kneading and solvent deposition methods were relatively high (P < 0.01) compared to the values rom the physical mixtures (PMs) and felodipine alone. The overall the rank order of improvement in dissolution properties of felodipine with different methods in all ratios was KM > SD > PMs > felodipine. All ternary systems exhibited a significant increase in dissolution rate with respect to the PMs and the reference drug. The value of T50 and MDT of all solid binary and ternary systems were lower than felodipine alone. It was noted that the dissolution was progressively increased with increasing concentration of carriers in both binary and ternary systems. The release pattern in felodipine, PMs and all solid binary and ternary systems showed best fit into first-order with highest ‘r’ (correlation coefficient) values. CONCLUSIONS: Solid binary and ternary systems of felodipine prepared with PEG 4000 and HPC were found to be effective in improving the solubility and dissolution rate of the model drug. Enhanced dissolution of felodipine from solid binary and ternary systems could be mainly attributed to the particle size reduction as well as decreased drug crystallinity (demonstrated by XRD). The study revealed that optimum ratios of hydrophilic carriers ensure a prompt and complete dissolution of felodipine from solid binary and ternary systems that are used in oral pharmaceutical formulations.
| Item Type: | Thesis (Masters) |
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| Additional Information: | Reg.No.261211052 |
| Uncontrolled Keywords: | Felodipine ; polyethylene glycol (PEG 4000) ; hydroxypropyl cellulose (HPC) ; solid binary and ternary systems. |
| Subjects: | PHARMACY > Pharmaceutics |
| Depositing User: | Subramani R |
| Date Deposited: | 27 Jun 2019 01:57 |
| Last Modified: | 27 Jun 2019 04:22 |
| URI: | http://repository-tnmgrmu.ac.in/id/eprint/10620 |
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