Formulation and evaluation of tramadol hydrochloride rectal suppositories

Abstract

Rectal suppositories of tramadol hydrochloride were prepared using different bases and polymers like PEG, cocoa butter, agar and the effect of different additives on in vitro release of tramadol hydrochloride was studied. The agar-based suppositories were non-disintegrating/non-dissolving, whereas PEGs were disintegrating/dissolving and cocoa butter were melting suppositories. All the prepared suppositories were evaluated for various physical parameters like weight variation, drug content and hardness. The PEG and cocoa butter suppositories were evaluated for macromelting range, disintegration and liquefaction time. In vitro release study was performed by USP type I apparatus. The prepared suppositories were within the permissible range of all physical parameters. In vitro drug release was in the order of PEG>Agar>cocoa butter. Addition of PVP, HPMC in agar suppositories retards the release. The mechanism of drug release was diffusion controlled and follows first order kinetics. The results suggested that blends of PEG of low molecular weight (1000) with high molecular weight (4000 and 6000) in different percentage and agar in 10% w/w as base used to formulate rapid release suppositories. The sustained release suppositories can be prepared by addition of PVP, HPMC in agar-based suppositories and by use of cocoa butter as base.

Pharmaceutical development and optimization of azithromycin suppository for paediatric use

“…As PEGs might be slightly irritant in children (EMA, 2006), no other surfactants were added to avoid problems with local tolerability or early expulsion of the form. A mixture of two PEGs, one of low and the other of high molecular weight, is commonly used for conventional rapid-release suppositories (Saleem et al, 2008). Different ratios of PEG 1500/4000 were tested; 80% PEG 1500 plus 20% PEG 4000 (melting point >50 °C as per the TPP) was selected (Fig.…”

Pharmaceutical assessment of polyvinylpyrrolidone (PVP): As excipient from conventional to controlled delivery systems with a spotlight on COVID-19 inhibition

“…Liquid suppositories are also reported by PVP applications [ 112 ]. Saleem et al reported the use of PVP along with agar for developing sustained release rectal suppositories of tramadol hydrochloride [ 119 ].…”

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“…Hardness test was carried out to determine the tensile strength and ability of the suppositories to withstand the hazards of packing and transportation using Monsanto hardness tester (Veego Scientific, Model HT-1). [21] Liquefaction time Liquefaction time was measured using a pipette having a broad opening on one side and a narrow opening on the other. Suppository was pushed inside in such a way that the broad end side of suppository to reach to the narrow end of pipette.…”