Ramu, P (2014) Formulation and Characterization of Rizatriptan Benzoate Sublingual Tablet with Various Permeation Enhancers. Masters thesis, College of Pharmacy, Madras Medical College, Chennai.
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Abstract
In this work an attempt was made to design sublingual drug delivery system containing an Antimigraine drug. The main objective of the present research work was to overcome the hepatic first pass metabolism, provide controlled release and to enhance the permeability. The conventional dosage forms available are associated with low bioavailability problems due to extensive first pass metabolism where in antimigraine agents are also characterized by highly soluble nature with low permeability, due to which frequency of dosing is increased, which results in patient incompliance. In order to overcome these drawbacks, drugs can be developed in form of sublingual drug delivery system. Sublingual drug delivery systems provide additional advantages over conventional tablets including termination of drug action in case of toxicity by removing the dosage form from the buccal cavity. The scheme of work has been divided into various parts. The collection of theoretical and technical data by extensive literature survey, review of literature and drug profile is presented in chapter 3 and 4 respectively. This was followed by procurement of materials and standardization of all materials used in the formulation of sublingual tablets. Sublingual tablets were prepared by direct compression method using Rizatriptan benzoate and different permeation enhancers like β-Cyclodextrin, Chitosan lactate and Sodium lauryl sulphate in different ratios and Crospovidone as superdisintegrant in order to release the drug in immediate manner. The tablets were evaluated for Disintegration time, Weight variation, Thickness, Hardness, Percentage friability, Wetting Time, Drug Content and In vitro dissolution studies, In vitro permeation study on egg membrane and Ex-vivo permeation study on goat sublingual mucosa. The resulting tablets were evaluated considering the disintegration time as well as permeation as the main criteria. Disintegration time of all batches was found to be between 08– 12 sec. Friability and hardness were also good in all batches. Exvivo as well as In vitro permeation study of Batch F-6 was found to be high with good disintegration time, friability and hardness. Batch F-6 showed rapid dissolution rate and complete dissolution was achieved within 60 min. Formulation F-6 was considered as the best formulation. The results obtained have been discussed in chapter 7. Results of FT-IR revealed that there was no chemical interaction between the drug and the permeation enhancers used. The prepared tablets showed good disintegration time. The release pattern of the formulations was good. Stability studies of the selected formulation was carried out to determine the effect of formulation additives on the stability of the drug and also to determine the physical stability of the formulation. The stability studies were carried out at 40 ºC/75% RH for 90 days. There was no significant change in the physical property and drug content during the study period. From the above the results, formulation F-6 was found to be the best formulation for the sublingual delivery of Rizatriptan benzoate that complied with all the parameters. However, in vivo experiments need to be carried out to know the absorption pattern and bioavailability of drug from the sublingual tablets and thus enabling us to establish in vitro – in vivo correlation. The concept of sublingual tablets containing Rizatriptan benzoate offers a suitable and practical approach in serving the desired objective of management of Migraine. Most of the excipients used in the formulation are water-soluble and hence have better patient acceptability. The present work of formulating a sublingual tablet containing Rizatriptan benzoate was successful in terms of reducing manufacturing difficulties, cost and providing better patient compliance with effective medication. It has been observed from the above study that excipients like Mannitol, Microcrystalline cellulose, Crospovidone, Aspartame, Chitosan lactate, Beta-Cyclodextrin and Sodium lauryl sulphate etc. were ideal excipients and effective for formulating sublingual tablets. Sublingual tablets provide several advantages especially when administered to children and elderly patients. Rapid absorption into the systemic circulation within short time period may be achieved.
| Item Type: | Thesis (Masters) |
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| Uncontrolled Keywords: | Characterization; Rizatriptan Benzoate Sublingual Tablet; |
| Subjects: | PHARMACY > Pharmaceutics |
| Depositing User: | Ravindran C |
| Date Deposited: | 09 Oct 2017 06:15 |
| Last Modified: | 09 Oct 2017 06:15 |
| URI: | http://repository-tnmgrmu.ac.in/id/eprint/3652 |
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