Amorphous solid dispersions of a poorly water-soluble drug genistein in PVP K-30 were prepared by solvent co-evaporation technique using organic solvent methanol. Solid dispersions system was prepared with several variations of the drug to polymer 2:1, 1:1 dan 1:2 w/w. Solid state properties of solid dispersion system were evaluated by powder X-ray diffraction, Fourier transform infrared spectroscopy, and differential scanning calorimetry, and microscopic SEM. Dissolution rate profile was conducted in distilled water medium by using dissolution tester apparatus type II USP. Base on X-ray diffractometry analysis, differential scanning calorimetry and microscopic SEM, crystalline phase of genistein decreased in crystallinity index and formation of the amorphous state. Dissolution rate profile showed that genistein in amorphous solid dispersion had a faster dissolution rate in comparison to intact genistein. This study suggests that preparation of the solid dispersion of genistein in PVP K-30 is an effective approach to improve the dissolution rate of genistein. ABSTRAK:Sistem dispersi padat amorf senyawa obat yang sukar larut air genistein dalam PVP K-30 dibuat dengan metode penguapan pelarut menggunakan pelarut metanol. Sistem dispersi padat dibuat dengan variasi perbandingan obat : polimer 2:1, 1:1 dan 1:2 b/b. Sifat padatan serbuk sistem dispersi padat dievaluasi dengan metode analisa difraksi sinar-X, termal DSC, spektrokopik FT-IR dan mikroskopik SEM. Profil disolusi dilakukan dalam medium air suling dengan alat uji disolusi tipe II USP. Hasil analisa difraksi sinar-X, termal DSC dan mikroskopik SEM, fase kristalin genistein mengalami penurunan derajat kristalinitas dan pembentukan fase amorf. Profil laju disolusi menunjukkan bahwa sistem dispersi padat genistein memiliki laju disolusi yang lebih tinggi dibandingkan genistein murni. Studi ini membuktikan bahwa pembentukan sistem dispersi padat genistein dengan polimer PVP K-30 efektif memperbaiki laju disolusi genistein. Keywords 67 PENDAHULUANKelarutan dan laju disolusi senyawa obat yang rendah dalam air merupakan salah satu permasalahan besar dalam pengembangan dan manufaktur sediaan padat (tablet, kapsul) di industri farmasi. Lebih dari 80 % sediaan obat dipasaran adalah dalam bentuk tablet, dan 40 % dari senyawa obat tersebut memiliki kelarutan yang rendah dalam air, serta hampir 80 -90 % senyawa kandidat obat yang dalam tahap penelitian juga memiliki permasalahan kelarutan dan laju disolusi [1,2].Berdasarkan Biopharmaceutical classification system (BCS) senyawa obat diklasifikasi kedalam empat kategori, kelas I (kelarutan tinggi, permeabilitas tinggi), II (kelarutan rendah, permeabilitas tinggi), III (kelarutan tinggi, permeabilitas rendah dan kelas IV (kelarutan rendah, permeabilitas rendah) Senyawa obat yang masuk dalam kategori kelas II dan IV seringkali mengalami absorpsi yang rendah dalam cairan saluran pencernaan [3]. Berbagai strategi telah dilaporkan untuk memperbaiki laju disolusi senyawa obat kelas II dan IV ini, antara lain pembuata...

Introduction:The aim of this study was to investigate the influence of the milling process on the solubility of efavirenz.Materials and Methods:Milling process was done using Nanomilling for 30, 60, and 180 min. Intact and milled efavirenz were characterized by powder X-ray diffraction, scanning electron microscopy (SEM), spectroscopy infrared (IR), differential scanning calorimetry (DSC), and solubility test.Results:The X-ray diffractogram showed a decline on peak intensity of milled efavirenz compared to intact efavirenz. The SEM graph depicted the change from crystalline to amorphous habit after milling process. The IR spectrum showed there was no difference between intact and milled efavirenz. Thermal analysis which performed by DSC showed a reduction on endothermic peak after milling process which related to decreasing of crystallinity. Solubility test of intact and milled efavirenz was conducted in distilled water free CO2 with 0.25% sodium lauryl sulfate media and measured using high-performance liquid chromatography method with acetonitrile: distilled water (80:20) as mobile phases. The solubility was significantly increased (P < 0.05) after milling processes, which the intact efavirenz was 27.12 ± 2.05, while the milled efavirenz for 30, 60, and 180 min were 75.53 ± 1.59, 82.34 ± 1.23, and 104.75 ± 0.96 μg/mL, respectively.Conclusions:Based on the results, the solubility of efavirenz improved after milling process.

ABSTRAK:Telah dilakukan penelitian tentang pengaruh kombinasi magnesium stearat dan talkum sebagai lubrikan terhadap profil disolusi tablet Ibuprofen. Dari ketiga formula dibuat tablet Ibuprofen dengan metoda granulasi basah. Evaluasi tablet meliputi keseragaman ukuran, keseragaman bobot, kekerasan tablet, waktu hancur, kerapuhan tablet, penetapan kadar dan disolusi. Hasil persen terdisolusi menit ke 60 menunjukkan bahwa disolusi rata-rata berturut-turut adalah 95,7209%, 97,6474% dan 99,9373%. Dan untuk hasil efisiensi disolusi pada menit ke 60 masing-masing formula adalah 82,1089%, 87,5888% dan 90,7635%. Dari data disolusi, formula III yang mempunyai hasil disolusi yang tinggi dibandingkan formula I dan formula II yang disebabkan oleh perbandingan kombinasi magnesium stearat dan talkum sebagai lubrikan lebih kecil kadar magnesium stearatnya.

Aim: To improve the solubility and antibacterial activity of trimethoprim (TMP) by preparing its multicomponent crystals with malic acid (MA). Methods: Multicomponent crystals of TMP-MA were prepared by solvent co-evaporation. The solid-state properties were characterised by powder X-ray diffraction (PXRD), differential thermal analysis (DTA), Fourier transform infrared (FT-IR) spectroscopy, and scanning electron microscopy (SEM) analyses. The solubility was investigated in an aqueous medium, while the antibacterial activity against Escherichia coli was investigated using the agar disk diffusion method. Results: The PXRD pattern of the TMP-MA binary system differed from the starting materials, supporting the formation of a new crystalline phase (equimolar ratio). The DTA thermogram showed a single, sharp, endothermic peak at 212.5 °C attributable to the TMP-MA multicomponent crystal's melting point. FT-IR spectroscopy showed a solid-state interaction involving proton transfer between TMP and MA. The multicomponent crystal displayed a 2.5-fold higher solubility and had increased antibacterial activity compared to TMP alone. Conclusions: The TMP-MA binary system forms salt-type multicomponent crystals that significantly increase solubility and antibacterial activity. Multicomponent crystal formation is a viable technique for modifying the physicochemical properties of active pharmaceutical ingredients.

The objective of the present study was to prepare amorphous solid dispersion system simvastatin-hydroxypropylmethylcellulose (HPMC) to enhance the dissolution rate. Amorphous solid dispersion of simvastatin was prepared by solvent technique using HPMC as carrier with ratio of 1:1, 1:3 and 1:5 (w/w). Physicochemical properties of solid dispersions were investigated by X-ray powder diffraction, thermal analysis of differential scanning calorimetry (DSC) and scanning electron microscopy. The dissolution rate profile was performed at 37 ± 0.5 °C and 50 rpm in phosphate buffer solution (pH 7) containing 0,5% sodium laurylsulphate. Powder X-ray diffraction of solid dispersion system exhibited decrease in peak diffraction intensity of simvastatin when increasing the HPMC ratio in solid dispersion system. DSC thermogram of solid dispersion system showed the absence of endothermic peak of simvastatin. All the solid dispersion demonstrated faster dissolution rate in comparison with intact simvastatin and its physical mixture. The dissolution rate of simvastatin from solid dispersion increased with an increased ratio of HPMC polymer. The solid dispersion system of simvastatin with HPMC provide a promising way to improve its dissolution rate.