Development and Evaluation of a Chronomodulated Delivery System of Metoclopramide Hydrochloride
By: Shenoy, Sandhya
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Contributor(s): Jain, P | Kulkarni, Madhur.
Publisher: Mumbai Indian Journal of Pharmaceutical Science 2018Edition: Vol. 80(05), September-October.Description: 883-891.Subject(s): PHARMACEUTICS | Optimization | Glyceryl dibehenate | Hydrogenated castor oilOnline resources: Click here
In:
Indian journal of pharmaceutical sciencesSummary: Chronomodulated delivery system of metoclopramide hydrochloride was developed for the treatment of morning sickness and diabetic gastroparesis. Drug-excipient compatibility studies revealed no significant degradation of metoclopramide hydrochloride in presence of selected tabletting and compression coating excipients. Immediate release core tablets of metoclopramide hydrochloride were prepared using direct compression technique and various physico-chemical parameters were evaluated. The core tablets were subjected to compression coating with a mixture of glyceryl dibehenate, hydrogenated castor oil and dicalcium phosphate; the levels of which were optimized statistically using face-centred cube design to achieve desired in vitro drug release profile of not more than 10% at 4 h, not less than 50% at 4.5 h and not less than 85 % at 5 h interval. Increase in the concentration of glyceryl dibehenate and hydrogenated castor oil in the formulation significantly decreased drug release at 4.5 and 5 h time intervals in distilled water as dissolution medium whereas quantity of dicalcium phosphate was found to have no influence on drug release characteristics. A quadratic model was suggested for the release profile at 4 h whereas linear model signified the release at 4.5 and 5 h. Formulation containing 100, 92 and 150 mg of glyceryl dibehenate, hydrogenated castor oil and dicalcium phosphate respectively per tablet was considered optimum since it showed the desired release profile. As the formulation showed the desired lag time during in vitro drug release, night time administration of the formulation could be expected to prevent the symptoms of morning sickness among pregnant women and hypoglycaemia upon administration of antidiabetic medication in gastroparetic patients.
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School of Pharmacy Archieval Section | Not for loan | 2018334 |
Chronomodulated delivery system of metoclopramide hydrochloride was developed for the treatment of morning sickness and diabetic gastroparesis. Drug-excipient compatibility studies revealed no significant degradation of metoclopramide hydrochloride in presence of selected tabletting and compression coating excipients. Immediate release core tablets of metoclopramide hydrochloride were prepared using direct compression technique and various physico-chemical parameters were evaluated. The core tablets were subjected to compression coating with a mixture of glyceryl dibehenate, hydrogenated castor oil and dicalcium phosphate; the levels of which were optimized statistically using face-centred cube design to achieve desired in vitro drug release profile of not more than 10% at 4 h, not less than 50% at 4.5 h and not less than 85 % at 5 h interval. Increase in the concentration of glyceryl dibehenate and hydrogenated castor oil in the formulation significantly decreased drug release at 4.5 and 5 h time intervals in distilled water as dissolution medium whereas quantity of dicalcium phosphate was found to have no influence on drug release characteristics. A quadratic model was suggested for the release profile at 4 h whereas linear model signified the release at 4.5 and 5 h. Formulation containing 100, 92 and 150 mg of glyceryl dibehenate, hydrogenated castor oil and dicalcium phosphate respectively per tablet was considered optimum since it showed the desired release profile. As the formulation showed the desired lag time during in vitro drug release, night time administration of the formulation could be expected to prevent the symptoms of morning sickness among pregnant women and hypoglycaemia upon administration of antidiabetic medication in gastroparetic patients.
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