Thangakamatchi, G (2019) Formulation Development and In Vitro Characterization of Gastroretentive Floating Microballoons of Labetalol Hydrochloride. Masters thesis, College of Pharmacy, Madras Medical College, Chennai.
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Abstract
The purpose of this research was to formulate Microballoons of Labetalol Hydrochloride for controlled release of drug and to improve bioavailability. Labetalol Hydrochloride is a sparingly water-soluble drug with absolute bioavailability of 25%, thus selected as a drug for GRDDS to overcome the problem and to release the drug in a controlled manner. Labetalol Hydrochloride is formulated as Microballoons by Emulsion Solvent Diffusion method using Eudragit RS 100 and Ethyl Cellulose as polymers, Polyvinyl alcohol as stabilizing agent and finally filled in hard gelatin capsules. Physical compatibility study showed that the drug and excipients were physically compatible with each other. Chemical compatibility study of Labetalol Hydrochloride with polymers were analysed by using FTIR Spectrometer. The results of the FTIR study proved that there is no interaction between the drug and polymers. Standard graph was drawn for Labetalol Hydrochloride and it was found that the solutions show linearity (0.999) and obeyed Beer’s and Lambert’s law. The formulations F1, F2, F3 were prepared using Ethyl Cellulose (EC) as polymer in the ratio of (Drug: EC- 1:1, 1:2, 1:3) and Polyvinyl Alcohol as a surfactant at 0.5 % w/v concentration. The formulations F4, F5, F6 were prepared using Eudragit RS 100 (EUD) as polymer in the ratio of (Drug: EUD- 1:1, 1:2, 1:3) and Polyvinyl Alcohol as a surfactant at 0.5 % w/v concentration. The formulations F7, F8, F9 were prepared using Ethyl Cellulose and Eudragit RS 100 as polymers in the ratio of (Drug: EC: EUD - 1:1:1, 1:2:1, 1:1:2) and Polyvinyl Alcohol as a surfactant at 0.5 % w/v concentration. The particle size of microballoons of all 9 formulations were found to be in the range of 55.4μm - 219.33μm. All 9 formulations characterized for percentage yield were found to be within the range of 48.33-86.25 %. The drug entrapment efficiency of all formulations was found to be in the range between 80.5 to 97.2%. With the increase in polymer concentration, increased entrapment efficiency was seen. The entrapment efficiency was found to be higher in F3-93.4% and F8-97.2% comparatively with other formulations. The buoyancy of all the formulations were found to be in the range of 76 - 94%. Formulation F4 showed least percentage buoyancy of 76.0%, while F8 showed highest buoyancy of 94.0%. In the test of floating time, microballoons remained floating for more than 12 hours. The in vitro release study was carried out for all 9 formulations. The percentage of drug release in formulation F3 was found to be 99.04% and F8 was 100.2 % at the end of 12 h and the release profile was in controlled manner comparatively with other formulations. Based on the higher entrapment efficiency and prolonged in vitro drug release F3 and F8 was selected as optimized formulations. The optimized formulation F3 and F8 are characterized for surface morphology. The shape and surface morphology of optimized formulations were observed in SEM. The image showed that nanoparticles were in spherical and circular shape with smooth surface. Flow property measurements (Bulk density, tapped density, angle of repose, Carr’s index and Hausner’s ratio) were carried out for optimized Labetalol Hydrochloride Microballoons. It revealed that the flow property of Labetalol Hydrochloride Microballoons have good flow. The optimized microballoons were filled into “0” size hard gelatin capsules without adding glidant because of its good flow property. Post formulation parameters (uniformity of weight, disintegration test, drug content, and in vitro drug release) for microballoon capsules were evaluated. The results were found to comply with official specifications. The drug release data of the optimized formulations were fitted to various kinetic models and the formulations F3 and F8 were best fitted to Zero order kinetics. The slope of the Korsmeyer Peppas plot indicating the diffusion was Super Case II Transport for F3 and anomalous diffusion (Non Fickian diffusion) for F8. The optimized formulations F3 and F8 were subjected to accelerated stability study (temperature 40°C±2°C and RH 75±5%). No significant change was found in appearance, entrapment efficiency, In vitro buoyancy and disintegration time at the end of 30 days. The foregoing results attempt to suggest that Labetalol Hydrochloride Microballoons capsules can be considered as an alternative to conventional drug delivery for better management of Hypertension.
| Item Type: | Thesis (Masters) |
|---|---|
| Additional Information: | 261711259 |
| Uncontrolled Keywords: | Formulation Development, In Vitro Characterization, Gastroretentive Floating Microballoons, Labetalol Hydrochloride |
| Subjects: | PHARMACY > Pharmaceutics |
| Depositing User: | Ramakrishnan J |
| Date Deposited: | 17 May 2022 07:23 |
| Last Modified: | 17 May 2022 07:23 |
| URI: | http://repository-tnmgrmu.ac.in/id/eprint/20078 |
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