Dewi Rashati, Dinar Rizqika Fauza, Mikhania Christiningtyas Eryani, Asa Falahi, Anies Rohman

Formulation Study of Acetosal Suppositories Using PEG 400 and PEG 6000: Impact on Physical Properties

Introduction

Formulation study of acetosal suppositories using peg 400 and peg 6000: impact on physical properties. Discover how PEG 400 and PEG 6000 concentrations influence acetosal suppository physical properties. Learn about optimal formulations for effective rectal drug delivery.

Abstract

Acetosal suppositories are rectal dosage forms that can be used as an alternative route of administration to minimize gastrointestinal irritation associated with oral acetosal therapy. The suppository base plays an important role in determining the physical characteristics of the preparation. The objective of this study was to evaluate how varying concentrations of polyethylene glycol (PEG) 400 and PEG 6000 affect the physical properties of acetosal suppository formulations. Three formulations were prepared using PEG 400:PEG 6000 ratios of F1 (3:7), F2 (1:1), and F3 (7:3). Physical evaluations included organoleptic properties, weight uniformity, melting time, melting point, and hardness. All formulations exhibited similar organoleptic characteristics, namely solid shape, pale white color, and characteristic odor. The average weight uniformity values were 2594.3 ± 61.9 mg (F1), 2526.9 ± 83.1 mg (F2), and 2315.7 ± 45.4 mg (F3), with significant differences among formulations (p<0.05). The average melting times were 25.1 ± 0.981 min, 19.5 ± 0.574 min, and 15.9 ± 0.508 min for F1, F2, and F3, respectively (p<0.05). The average melting points were 36.3 ± 0.577°C, 35.7 ± 0.577°C, and 34.3 ± 0.577°C for F1, F2, and F3, respectively (p=0.014). Hardness values were 1.93 ± 0.115 kg (F1), 1.87 ± 0.115 kg (F2), and 1.53 ± 0.115 kg (F3), with significant differences among formulations (p<0,05). In conclusion, variations in PEG 400 and PEG 6000 concentrations significantly affected weight uniformity, melting time, melting point, and hardness, while organoleptic properties remained unchanged. Formulations F1 and F2 fulfilled all physical quality requirements and were considered optimal. Keywords: Acetosal, suppositories, PEG 400, PEG 6000

Review

This study addresses a relevant pharmaceutical challenge by exploring the formulation of acetosal suppositories as a potential alternative to oral administration, thereby mitigating gastrointestinal irritation. The authors appropriately focus on the critical role of the suppository base, specifically investigating the impact of varying ratios of polyethylene glycol (PEG) 400 and PEG 6000 on the physical characteristics of these formulations. The objective to systematically evaluate how these PEG concentrations influence key physical properties is well-defined and timely, given the continued interest in optimizing drug delivery systems. The study successfully demonstrates that the choice of PEG ratio significantly influences several critical physical attributes of the resultant suppositories. To achieve their objective, the researchers prepared three distinct formulations (F1, F2, F3) employing PEG 400:PEG 6000 ratios of 3:7, 1:1, and 7:3, respectively. A comprehensive battery of physical evaluations was conducted, encompassing organoleptic properties, weight uniformity, melting time, melting point, and hardness. While all formulations consistently exhibited similar organoleptic characteristics (solid, pale white, characteristic odor), statistically significant differences were observed across formulations for all other measured parameters. Specifically, F1 displayed the highest average weight (2594.3 mg), longest melting time (25.1 min), highest melting point (36.3°C), and greatest hardness (1.93 kg), with these values generally decreasing as the proportion of PEG 400 increased (from F1 to F3). The consistent statistical significance (p<0.05 or p=0.014) reported for these differences underscores the profound impact of the chosen PEG ratios. In conclusion, this formulation study clearly establishes that the relative concentrations of PEG 400 and PEG 6000 are critical determinants for the physical quality attributes of acetosal suppositories, affecting weight uniformity, melting time, melting point, and hardness. The identification of formulations F1 (PEG 400:PEG 6000 at 3:7) and F2 (1:1 ratio) as fulfilling all physical quality requirements and being optimal provides valuable guidance for future development. This work offers a sound foundational understanding for pharmacists and formulators developing rectal dosage forms of acetosal. While the study provides excellent insight into physical properties, future research could logically extend to evaluating *in vitro* drug release kinetics and stability profiles to further characterize the performance of these promising formulations.

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