Formulation and Evaluation of Mouth Dissolving Tablets of Metoprolol Tartrate

Suganya, M (2019) Formulation and Evaluation of Mouth Dissolving Tablets of Metoprolol Tartrate. Masters thesis, Jaya College of Paramedical Sciences College of Pharmacy, Thiruninravur, Chennai.

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Abstract

The most popular solid dosage forms are being tablets and capsules;one important drawback of these dosage form for some patients, is the difficulty to swallow. Drinking water plays an important role in swallowing of oral dosage forms. For these reasons tablets that can rapidly dissolve or disintegrate in the oral cavity have attracted a great deal of attention. Orodispersible tablets are not only indicated for people who have swallowing difficulties, but also are ideal for active people. Orodispersible tablets are those when put on tongue, disintegrates instantaneously releasing the drug, which dissolves or disperse in saliva. The concept of formulating mouth dissolving tablets containing Metoprolol Tartrate offer a suitable and practical approach in serving the desired objective of faster disintegration and dissolution characteristic with increase bioavailability. Metoprolol Tartrate is a selective beta1-adrenoreceptor blocking agent, by blocking catecholamine-induced increases in heart rate, in velocity and extent of myocardial contraction, and in blood pressure, Metoprolol reduces the oxygen requirements of the heart at any given level of effort, thus making it useful in the management of angina pectoris and in acute myocardial infarction. However, in patients with heart failure, beta-adrenergic blockade may increase oxygen requirements by increasing left ventricular fiber length and end-diastolic pressure. Mouth dissolving tablets of Metoprolol Tartrate were prepared using various superdisintegrants such as indion 414, croscarmellose sodium, sodium starch glycolate, crospovidone, Microcrystalline cellulose and camphor (as subliming agent)in different ratio. Prepared tablets were subjected to different evaluation parameters such as hardness, friability, weight variation, drug content uniformity, wetting time, water absorption ratio, in-vitro disintegration time, in-vitro dissolution studies. Results revealed that the tablet of all formulations have acceptable physical parameters .The tablet prepared by direct compression method passes weight variation was found in the range 196 to 205 mg which is below ±7.5%, hardness 2 to 3 Kg / cm2, percentage friability of 0.54 to 0.81 %, in vitro disintegration time of 21 to 59 sec, drug content uniformity was in between 99.08 to 100.76%, water absorption ratio were found between 46.77 to 85.64% and wetting time between 37 to 50 seconds. Shows maximum drug release within 5 min. The tablet prepared by sublimation method passes weight variation was found in the range 197 to 204 mg which is below ±7.5%, hardness 2.1 to 2.9kg/cm², percentage friability of 0.53 to 0.85, in vitro disintegration time of 18 to 48 sec, drug content uniformity was in between 98.56 to 100.65%, water absorption ration were found between 51.15 to 85.15% and wetting time between 37 to 50 sec. Shows maximum drug release within 5 min. The FTIR spectra and DSC studies of formulation shows that no interaction between drug and excipient. Conclusion: In the present work mouth dissolving tablets of Metoprolol Tartrate were prepared by direct compression and sublimation methods using superdisintegrants such as indion 414, sodium starch glycolate, croscarmellose sodium and crospovidone. In sublimation method, camphor is used as sub limingagent. All the tablets of Metoprolol Tartrate were subjected to weight variation, hardness, friability, in vitro dispersion, drug polymer interaction, drug content uniformity, water absorption ratio, wetting time, and in vitro drug release. Based on the above studies following conclusions can be drawn:s • Tablet prepared by direct compression and sublimation methods were found to be good and were free from chipping and capping. • The low values of the standard deviation of average weight of the prepared tablets indicate weight uniformity within the batches prepared. • The hardness of the prepared tablets was found to be in the range of 2 to 3 Kg/cm². • The friability values of the prepared tablet were found to be less than1%. • IR spectroscopic and DSC studies indicated that the drug is compatible with all the excipients. • The in vitro disintegration time of Metoprolol Tartrate prepared by direct compression and sublimation method were found to be in the range of 18 to 59 sec fulfilling the official requirements. • Based on the in vitro disintegration time, formulation DCI3 (9% Indion 414) and SBI1 (3% Indion 414) were found to be promising and showed a disintegration time of 21 and 18 sec, wetting time of 48 and 37 sec respectively, which facilitate the faster disintegration in the mouth. • TheformulationDCI3andSBI1havedisplayedgoodwaterabsorptionratioof 85.77 and 85.15%, which indicate better and faster swelling ability of the disintegrants in presence of little amount of water. • The drug content of tablets was uniform in all the batches and was between 98.12 to 100.76%. • The drug release from mouth dissolving tablets of Metoprolol Tartrate prepared by direct compression and sublimation methods were found to be in the range of 96.05 to 99.56% and the result of DCI3 and SBI1 showed 97.83% and 99.01% drug release within 5minutes. • Among the two methods used namely direct compression and sublimation, the sublimation method was found to be superior to direct compression method. • Compressed tablets containing mannitol and camphor have been prepared by sublimation technique. Removal of volatile material by sublimation generated a porous structure. The tablets dissolve within 10-20 seconds and exhibit enough mechanical strength for practical use, which is effective than the direct compression method.

Item Type: Thesis (Masters)
Uncontrolled Keywords: Formulation, Evaluation, Mouth Dissolving Tablets, Metoprolol Tartrate
Subjects: PHARMACY > Pharmaceutics
Depositing User: Ramakrishnan J
Date Deposited: 04 Dec 2021 06:07
Last Modified: 23 Mar 2022 06:48
URI: http://repository-tnmgrmu.ac.in/id/eprint/18816

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