Mefenamic acid (MA) is a popular nonsteroidal anti-inflammatory drug classified into BCS class II which has a low solubility and dissolution rate in an aqueous medium. The present study aimed to improve the dissolution rate of MA by preparing multicomponent crystals with tromethamine (TM) through the solvent evaporation technique. The resulting powder was characterized for its solid-state properties and evaluated for the dissolution rate. The results showed that the powder X-ray diffraction pattern of the MA-TM binary system was different from its starting materials, indicating the formation of a new crystalline phase. The differential scanning calorimetry analysis of the MA-TM binary system showed a single and sharp endothermic peak at 110 °C, which was attributed to the melting point of MA-TM multicomponent crystals. The Fourier transform infrared spectroscopy analysis showed the occurrence of solid-state interaction involving proton transfer between MA and TM. The dissolution efficiency of MA-TM multicomponent crystal was 2.5-fold higher than the intact MA. The study concludes that the MA-TM binary system forms a salt-type multicomponent crystal. The multicomponent crystals can significantly increase its dissolution rate and is an alternative technique for modifying the physicochemical properties of active pharmaceutical ingredients.
This study aims to improve the dissolution rate of ketoprofen by preparing multicomponent crystals with tromethamine. The multicomponent crystals (equimolar ratio) of ketoprofen and tromethamine were prepared by the solvent co-evaporation method. The solid-state properties of the resulting powder were characterized by powder X-ray diffraction, DSC thermal analysis, FT–IR spectroscopy, solubility, and in vitro dissolution rate. The crystal structure of the multicomponent crystal was determined by single-crystal X-ray diffraction analysis. The results showed that the powder X-ray diffraction pattern of the ketoprofen–tromethamine binary system was different from that of the starting materials. This difference indicates the formation of a new crystalline phase between ketoprofen and tromethamine (equimolar ratio). The DSC thermogram of the ketoprofen–tromethamine binary system exhibited a single and sharp endothermic peak at 128.67 °C, attributed to the melting point of a multicomponent crystal of ketoprofen–tromethamine. A single-crystal X-ray analysis revealed that ketoprofen–tromethamine formed a layered structure, salt-type multicomponent crystal. The solubility and dissolution rate of the multicomponent crystal were notably enhanced compared to the intact ketoprofen. The ketoprofen–tromethamine binary system forms salt-type multicomponent crystals, which can significantly increase the solubility and dissolution rate.
Nimodipin merupakan salah satu senyawa yang tidak larut dalam air dan termasuk ke dalam Biopharmaceutical Classification System (BCS) kelas II. Sistem dispersi padat adalah campuran yang homogen dari satu atau lebih bahan aktif dalam matriks yang inert dengan tujuan meningkatkan bioavaibilitas dari bahan obat yang sukar larut. Penelitian ini bertujuan untuk melihat pengaruh penambahan poloxamer 188 terhadap sifat fisikokimia dan profil disolusi dari nimodipin yang dibuat dengan metode penggilingan bersama. Perbandingan nimodipin dengan poloxamer 188 untuk F1, F2, F3 berturut – turut adalah 1:9, 2:8, dan 3:7 (b/b). Karakterisasi campuran fisik dan dispersi padat meliputi distribusi ukuran partikel, XRD, FT-IR, DSC, penetapan kadar dan laju disolusi. Hasil penelitian menunjukan bahwa sifat fisikokimia dari setiap formula sudah berbentuk amorf dan nimodipin terdispersi ke dalam matriks polimer. Laju disolusi dari formula meningkat dibandingkan zat murni dan campuran fisik. Laju disolusi paling tinggi ditunjukkan pada F1, dimana pada waktu 60 menit persentase terdisolusinya sebesar 90,5920 %. Analisa statistik efisiensi disolusi menunjukkan perbedaan yang bermakna (sig<0,005) antara semua formula.
Solubility is an important parameter for the bioavailability of drugs that are difficult to dissolve. Natural compounds that are included in class II in the Biopharmaceutics Classification System (BCS) are Apigenin, Quercetin, Genistein, Curcumin, and Piperin. These drugs have low solubility in water and high permeability so that they affect the dissolution rate and as well as their bioavailability, to increase the solubility they are made with multicomponent crystals. This review aims to provide information on the method of making crystal multicomponent to increase the solubility and dissolution rate of BCS II drugs. Several methods that can be used in multicomponent are solvent drop grinding, solvent evaporation, assisted grinding, and slurry. The results showed that multicomponent crystals using several methods could increase the solubility and dissolution rates.
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