Gitika Kumari, (2019) Formulation and Evaluation of Ketorolac Mucoadhesive Buccal Tablets. Masters thesis, C.L.Baid Metha College of Pharmacy, Chennai..
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Abstract
In the present work, an attempt was made to design efficacious and prolonged release mucoadhesive buccal tablets of Ketorolac using various polymers to reduce dosing frequency, decrease gastric irritation and to improve patient compliance. Two polymer combinations (carbopol 943 and PVP K30 as well as carbopol and xanthan gum) were taken at varying proportions. The buccal tablets were tested for weight uniformity, thickness, friability and hardness. Tablets were then evaluated for their swelling index, in vitro drug release, mucoadhesion time (wash-off time) and ex vivo drug permeation. The kinetics and mechanism of the drug permeation through the excised buccal tissue of goat from the buccal tablets were also characterized. The data collected were then analyzed using software to determine the effects of each parameter. The effects of the various parameters involved were then interpreted. The best polymer composite was selected from the various ratios of the polymers. The best polymer ratio was found to be Carbopol 934 and PVP K30 in the ratio 1:2. The mucoadhesive strength of buccal tablets increases as the concentration of secondary polymer increases. The above polymer composite had shown satisfactory results in the parameters such as thickness, hardness, drug content, swelling index, mucoadhesive time, in-vitro dissolution and in-vitro diffusion. The satisfactory formulation shows a zero order drug release profile depending on the regression value and shown a satisfactory dissolution profile. Slow, controlled and maximum release of Ketorolac over a period of 6 h was obtained from buccal tablets F2 formulation containing Carbopol 934 and PVP K30. Further work is to be carried out in order to determine its efficacy and safety by long term pharmacokinetic and pharmacodynamic studies in human beings. CONCLUSION: The oral cavity and its highly permeable mucosal tissues have been taken advantage for decades as a site of absorption for delivery of drugs to the systemic circulation. So the formulations which target the oral cavity through buccal mucosa are of considerable interest to improve the bioavailability and reduce the frequency of administration of APIs. Drugs administered through the buccal route have a rapid onset of action and leads to improved bioavailability of drugs. The buccal route can bypass the first-pass metabolism, bypass contact of the drugs with the gastrointestinal fluids and paves way for easy access to the membrane sites so that the delivery system can be applied, localized and removed easily. Furthermore, there is good potential for prolonged delivery through the mucosal membrane within the oral mucosal cavity. Buccal adhesive systems offer innumerable advantages in terms of accessibility, administration and withdrawal, retentivity, low enzymatic activity, economy and high patient compliance. Adhesions of these drug delivery systems to mucosal membranes lead to an increased drug concentration gradient at the absorption site and therefore improve bioavailability of systemically delivered drugs. The research work highlights the development and evaluation of novel buccal drug delivery system of Ketorolac so that the non-invasive administration of injection as well as gastrointestinal side effects of the drug (when administered orally) can be avoided. At the current global scenario, scientists are finding ways to develop buccal adhesive systems through various approaches to improve the bioavailability of drugs used orally by manipulation of the formulation strategies like inclusion of pH modifiers, enzyme inhibitors as well as permeation enhances.
| Item Type: | Thesis (Masters) |
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| Additional Information: | 261710005 |
| Uncontrolled Keywords: | Formulation, Evaluation, Ketorolac Mucoadhesive Buccal Tablets. |
| Subjects: | PHARMACY > Pharmaceutics |
| Depositing User: | Ramakrishnan J |
| Date Deposited: | 04 Dec 2021 06:06 |
| Last Modified: | 22 Mar 2022 07:19 |
| URI: | http://repository-tnmgrmu.ac.in/id/eprint/18807 |
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