Formulation of Diazepam suppositories with hydrophilic and lipophilic bases

Miceva, Dijana and Angelovska, Bistra (2022) Formulation of Diazepam suppositories with hydrophilic and lipophilic bases. Knowledge – International Journal.

Text FORMULATION OF DIAZEPAM SUPPOSITORIES WITH HYDROPHILIC AND (1).pdf - Accepted Version Download (514kB)

Abstract

Diazepam belongs to a class of a long-acting benzodiazepine with anticonvulsant, sedative, and anxiolytic properties. Because of its rapid absorption it is a commonly used drug for the treatment of acute recurrent epileptic seizures that occur at children. It is also used for the treatment of acute febrile convulsions and as the drug of choice diazepam is given intravenously to produce the effect more quickly. But the intravenous method of application requires professional competence from medical personnel. Due to the difficult swallowing during a seizures, the oral and sublingual administration of diazepam in that case is impossible. Rectal formulations with diazepam stand out as a type of drug administration that achieves rapid application and timely action. Diazepam rectal solutions are not widely used because of the possibility of incorrect dosing and rectal leakage. Suppositories as a pharmaceutical dosage form are the drug of choice for administering diazepam. Absorption of the active component after rectal administration depends on: the melting or dissolution of the suppository and the diffusion of the active substance and the penetration of the dissolved molecules through the epithelial cells of the mucous membrane of the rectum. In the formulation of suppositories, the solubility of the active component in the base plays a major role. The bases used in manufacturing the suppositories can be hydrophilic or lipophilic. The aim of this study is to define a base of choice for the manufacture of diazepam suppositories, following the pharmaceutical-technological manufacturing process and the physico-chemical properties of the obtained suppositories. Suppositories were made with two types of bases, hydrophilic and lipophilic. Macrogol (Polyethylene glycol-PEG) with a different molecular weight is used as a hydrophilic base. During the technological development, three different formulations of suppositories were made with diazepam and a hydrophilic base Macrogol (PEG) with different molecular mass in different ratio. The first formulation consists of diazepam and Macrogol 6000, the second diazepam and Macrogol 6000- 40% and PEG 1500- 60% and the third of diazepam and Macrogol 6000 - 40%, Macrogol 1500 - 40% and Macrogol 400 - 20%. Lipophilic base Withepsol H15 was used in the other formulations, and one formulation was made with diazepam and Withepsol H15, and one formulation with diazepam and Withepsol H15 + Tween 80. Based on the obtained results, it is estimated that the third developed formulation, which in its composition has diazepam and a hydrophilic base in the following ratio Macrogol 6000 - 40%, Macrogol 1500 - 40% and Macrogol 400 - 20%, shows the best physico-chemical characteristics in relation to the rest. Keywords: diazepam, suppositories, formulations

Item Type:	Article
Subjects:	Natural sciences > Other natural sciences
Divisions:	Faculty of Medical Science
Depositing User:	Dijana Miceva
Date Deposited:	21 Feb 2023 12:08
Last Modified:	21 Feb 2023 12:08
URI:	https://eprints.ugd.edu.mk/id/eprint/31469

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