Determining the Best Poloxamer Carrier for Thiocolchicoside Solid Dispersions

Industrial pharmacists make many attempts to enhance the solubility of drugs economically. Among the various approaches for enhancing solubility, the solid dispersion (SD) approach is gaining in importance as it is simpler and requires less effort than the other approaches.1

Thiocolchicoside (TCS) is a colchicoside derivative from Gloriosa superba and Colchicum autumnale. TCS is a muscle relaxant used to tackle sore muscle shrinkages, acute and arthritic problems, and pains, and it lacks sedative side effects, unlike other muscle relaxants. It is also given with many nonsteroidal anti-inflammatory drugs. TCS is a yellow crystalline powder that is slightly soluble in ethyl alcohol and insoluble in chloroform.

The traditional method of preparing SDs is by fusion, in which the polymer-carriers used for SDs are not exposed to a uniform heat from the heat source. To overcome this, a novel microwave (MW) melting technique is adopted. Electromagnetic irradiation was applied in an MW oven with 0.3 to 300 GHz of infrared and radio frequencies equivalent to wavelengths of 1 mm to 1 m. This technique can be adopted for obtaining fast and continuous heating even in materials presenting low heat conductivity (e.g., polymers), because the relocation of energy does not depend on heat diffusion.Thus, this novel MW melting method was adopted in the preparation of SDs.

Much research has been performed on enhancing the solubility of drugs using poloxamers, i.e. poloxamer-108, poloxamer-188 poloxamer-237poloxamer-338 and poloxamer-407

Therefore, it is important to enhance the solubility of TCS, with faster discharge, absorption, and action to relieve acute patients. It also helps researchers to know which poloxamer carrier is best for releasing TCS among poloxamer-108, poloxamer-188, poloxamer-237, poloxamer-338, and poloxamer-407. The current investigation aimed to enhance the solubility of TCS with poloxamer carriers and find out the best among the better poloxamers.

Aim: The aim of this study of this study was to discover the best poloxamer as a solid dispersion carrier for thiocolchicoside (TCS).

Materials and Methods: The compatibility of TCS with excipients was studied by differential scanning colorimetry and fourier transform infrared spectroscopy. Different formulations of solid dispersions (SDs) were made with poloxamer carriers, i.e. poloxamer-108, poloxamer-188, poloxamer-237, poloxamer-338, and poloxamer-407 were made by taking TCS:poloxamer in ratios of 1:1, 1:2, 1:4, and 1:6. The SDs were made by a novel microwave fusion method and compressed using an 8-station tablet compression machine. The fabricated SD tablets were characterized by physicochemical constraints and drug release rates. The release of TCS from the prepared SDs was later analyzed by kinetic models.

Results: TCS was observed to be compatible with the poloxamer carriers. The SD formulations showed satisfactory physicochemical constraints and TCS release following first-order release.

Conclusion: Among the poloxamer carriers used, poloxamer-188 was the best for increasing the solubility and release rate of TCS from the SDs.

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or continue reading here: ANNEPOGU H, AHAD HA, NAYAKANTI D. Determining the Best Poloxamer Carrier for Thiocolchicoside Solid Dispersions. Turk J Pharm Sci 2020;17:372-380.