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Effect of Selected Surfactants on Kinetics of Meloxicam Release from Rectal Suppositories

By: Szulc-Musiol, B.
Contributor(s): Bulas, L.
Publisher: Mumbai Indian Journal of Pharmaceutical Science 2019Edition: Vol.81(6), Nov-Dec.Description: 1115-1121p.Subject(s): PHARMACEUTICSOnline resources: Click here In: Indian journal of pharmaceutical sciencesSummary: The use of surfactants in suppository formulations has been suggested to improve the bioavailability of poorly soluble drugs. In the present study, different kinds of surfactants were investigated to understand their influence on meloxicam release from suppositories formulated with a lipophilic base. Tween 80, Span 80, soy lecithin and sodium lauryl sulphate were the surfactants used in this study. The suppositories were prepared in a recipe mixer using Witepsol H15 and cacao oleum as a base. The suppositories with and without the addition of surfactants were examined using physicochemical tests according to the Polish Pharmacopeia, the uniformity of mass of single-dose preparation test, the content uniformity test, the softening time determination of lipophilic suppositories test, the disintegration test of suppositories, and the dissolution test. All the prepared formulations complied with the pharmacopeia requirements. The prepared suppositories were evaluated for in vitro drug release immediately after preparation and after storage. The results revealed that the bioavailability of meloxicam was to 36 % from suppositories formulated with Witepsol H15 and 23.4 % those formulated with cacao oleum. Addition of surfactants to the suppository base significantly influenced both the amount and rate of meloxicam released into the phosphate buffer. The highest release rate of meloxicam was observed with the formulation prepared on a Witepsol H15 base with Tween 80. Present results have confirmed the possibility of using surfactants in suppository formulations, in order to improve the dissolution rate of meloxicam in vitro. As a consequence, a faster onset of pharmacodynamic action and better therapeutic effects of the medication can be obtained.
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The use of surfactants in suppository formulations has been suggested to improve the bioavailability of poorly soluble drugs. In the present study, different kinds of surfactants were investigated to understand their influence on meloxicam release from suppositories formulated with a lipophilic base. Tween 80, Span 80, soy lecithin and sodium lauryl sulphate were the surfactants used in this study. The suppositories were prepared in a recipe mixer using Witepsol H15 and cacao oleum as a base. The suppositories with and without the addition of surfactants were examined using physicochemical tests according to the Polish Pharmacopeia, the uniformity of mass of single-dose preparation test, the content uniformity test, the softening time determination of lipophilic suppositories test, the disintegration test of suppositories, and the dissolution test. All the prepared formulations complied with the pharmacopeia requirements. The prepared suppositories were evaluated for in vitro drug release immediately after preparation and after storage. The results revealed that the bioavailability of meloxicam was to 36 % from suppositories formulated with Witepsol H15 and 23.4 % those formulated with cacao oleum. Addition of surfactants to the suppository base significantly influenced both the amount and rate of meloxicam released into the phosphate buffer. The highest release rate of meloxicam was observed with the formulation prepared on a Witepsol H15 base with Tween 80. Present results have confirmed the possibility of using surfactants in suppository formulations, in order to improve the dissolution rate of meloxicam in vitro. As a consequence, a faster onset of pharmacodynamic action and better therapeutic effects of the medication can be obtained.

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