Formulation and Evaluation of Nebivolol Immediate Release Tablets with Improved Dissolution Using Solid Dispersion Technique

Subramani, M (2017) Formulation and Evaluation of Nebivolol Immediate Release Tablets with Improved Dissolution Using Solid Dispersion Technique. Masters thesis, J.K.K. Nattraja College of Pharmacy, Komarapalayam.


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AIM AND OBJECTIVE:The aim of the present work is to investigate the possibility of obtaining immediate release tablet of nebivolol with improved dissolution using solid dispersion technique. Basic goals in the development of immediate dissolving tablet are to increase patient compliance, ease of administration, safety and appropriate dosing. Orally disintegrating formulations also provide benefits for pharmaceutical companies like lifecycle management, line extension, market expansion, cost effective drug development programs. According to BCS classification nebivolol coming under class 2 category which has low solubility and high permeability. Nebivolol is a white powder, relatively insoluble in water. Solubility and dissolution was improved by formulating solid dispersion. Keeping in view the advantages of this delivery system, in the present study, attempts were made to formulate immediate dissolving tablet nebivolol, which is useful to reduce blood pressure level in the treatment of antihypertensive agents. The direct compression was used to compress the tablets as it is the easiest way to manufacture tablets. Conventional equipments, commonly available excipients and limited number of processing steps are involved in direct compression and so manufacturing cost is low. Tablets produced by direct compression are relatively strong in hardness and have less friability.Super disintegrants are the major components of immediate release tablets.Based on their origin they can be grouped in to two category, synthetic super disintegrants (micro crystalline cellulose, cross povidone, cros carmellose sodium, starch glycolate) and natural super disintegrants. Natural origin is preferred over semi synthetic and synthetic substances because they are comparatively cheper, abundantly, non irritating non toxic in nature. The formulation of immediate release using natural super disintegrants is an excellent example for the application of natural agents in the formulative field. And this proved that the natural agents have almost equivalent properties to synthetic agents, which can be widely used for formulation of dosage forms. Nebivolol used to improve the solubility, stability of drug and also to mask its bitter taste.SUMMARY:In the present study immediate release drug delivery system of nebivolol were successfully developed in the form of mouth dissolving tablets with improved dissolution characteristic by forming solid dispersion with PEG 6000, which offers a suitable and practical approach in serving desired objective of faster disintegration and dissolution characteristics with increase bioavailability. Immediate release tablets of nebivolol were prepared by using natural superintegrants like microcrystalline cellulose, croscarmellose sodium, crospovidone, sodium starch glycolate and their combination as superdisintegrants. Superdisintegrants work as an auxiliary or as a facilitator of the flowability and compressibility of the mixture and contribute to the fast dispersion of the tablet, due to its high solubility in water. For the nebivolol formulation, batch No. 2 was chosen as it has disintegration time around 5-35 seconds and hardness3.5 Kg/Cm2. IR spectra of drug with other excipients has not shown any interaction and also selected formulation was stable after stability studies.CONCLUSION:The solubility and dissolution rate of nebivolol can be enhanced by formulating SDs of nebivolol with PEG 6000.The solubilization effect of PEG 6000, reduction of particle aggregation of the drug, formation of microcrystalline or amorphous drug, increased wettability and dispersibility, and alteration of the surface properties of the drug particles might be responsible for the enhanced solubility and dissolution rate of nebivolol from its SD and to some extent in PMs. No endothermic peak of nebivolol was present in of SDs with PEG 6000 suggesting the absence of crystalline nebivolol. From FTIR spectroscopy, it was concluded that there was no well defined chemical interaction between nebivolol and PEG 6000 in SDs and in PMs, as no important new peaks could be observed. The identical composition of Superdisintegrants showed that a substantial shorter time require for disintegration can be obtained and immediate release tablet were prepared. The nebivolol immediate release tablet (F2) showed 68.30% drug release within first 5 min. and 99.93% drug release with in 30 min. The results showed that the formulation satisfied the objective of fast disintegration, dissolution, % friability, hardness, wetting time, water absorption ratio, ease of administration and safety. Success of the present study recommends a detailed investigation in to invivo studies for its effective use in clinical practice.

Item Type: Thesis (Masters)
Uncontrolled Keywords: Nebivolol Immediate Release Tablets ; Improved Dissolution Using Solid Dispersion Technique
Subjects: PHARMACY > Pharmaceutics
Depositing User: Ravindran C
Date Deposited: 02 Mar 2018 06:28
Last Modified: 02 Mar 2018 06:28

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