Robustness of Palm Kernel Oil Blend in Suppository Preparation Using Acetaminophen as a Model Drug

Abstract

Background:

Theobroma oil suppository base has good characteristics for the delivery of most drugs, but its polymorphism renders it a difficult medium with which to work. Preparation of suppositories using theobroma oil must be carried out at a temperature below 36 °C to avoid formation of metastable polymorphs. Substitutes for theobroma oil are therefore desirable.

Objective:

To compare the characteristics of theobroma oil- and palm kernel oil blend (PKOB)-based suppositories, each produced by 2 different techniques of preparation.

Methods:

Theobroma oil and PKOB (consisting of hydrogenated palm kernel oil and hydrogenated palm kernel stearin in an 8:2 ratio, with 5% stearic acid and 5% glyceryl monostearate) were used as a base. Suppositories were prepared by 2 different techniques, with acetaminophen used as the model drug. The standard technique used a water bath to melt the base preparation at 36 °C before incorporation of acetaminophen, while the second technique involved melting the base in an oven at 60 °C. The 2 types of suppositories produced by these techniques were then tested physically for appearance, hardness, liquefaction time, and melting characteristics using differential scanning calorimetry.

Results:

Satisfactory theobroma oil–based suppositories were produced by the water bath technique at 36 °C, but the oven technique at 60 °C failed to produce a good product. On the other hand, both techniques produced satisfactory PKOB-based suppositories that were similar in both physical and thermal characteristics.

Conclusions:

PKOB constituted with the above-mentioned ingredients can be exposed to a wider range of temperatures without risk of polymorphism.

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References

The pharmaceutical codex. Rectal and vaginal products. In: Walter L. Principles and practice of pharmaceutics. 12th ed. London: The Pharmaceutical Press, 1994: 170–6.

Gold

. Suppository development and production. In: Lieberman

Rieger

Banker

. Pharmaceutical dosage forms. Dispersed system. Vol. 1. New York: Marcel Dekker, Inc., 1988: 533–65.

Simon

Suverkrup

. Comparison of recent techniques to characterize the crystallization behaviour of fatty suppository bases. Thermochim Acta 1995; 248: 271–87.

de Blaey

Tukker

. Suppositories and pessaries. In: Aulton

, ed. Pharmaceutics: the science of dosage form design. International student ed. London: Churchill Livingstone, 1996: 412–20.

Loisel

Keller

Lecq

Bourgaux

Ollivon

. Phase transitions and polymorphism of cocoa butter. J Am Oil Chem Soc 1998; 75: 425–39.

Collet

. Suppositories and pessaries. In: Aulton

. Pharmaceutical practice. International student ed. London: Churchill Livingstone: 1996: 135–41.

Tan

Man

Che YB

. Differential scanning calorimetric analysis of edible oils: Comparison of thermal properties and chemical composition. J Am Oil Chem Soc 2000; 77: 143–55.

British Pharmacopoeia Commission. British Pharmacopoeia. Vol. 2. London: HMSO, 2000:A198–A200.

Noordin

Chung

. A rapid micro quantification method of paracetamol in suppositories using differential scanning calorimetry. Drug Dev Ind Pharm 2004; 30: 925–30.

10.

Barker

Yuen

Craig

DQM

. An investigation into the low temperature thermal behaviour of vitamin E preparation USP using differential scanning calorimetry and low frequency dielectric analysis. J Pharm Pharmacol 2000; 52: 941–7.