Pharmaceutical Cocrystal of Ethyl p-Methoxycinnamate: Formulation and Characterization

Rachmaniar, Revika; Warya, Sohadi; Ferdiansyah, Rival; Riasari, Hesti; Gumelar, Aswin; Kenti,

doi:10.2991/ahsr.k.200523.024

Cited by 3 publications

(3 citation statements)

References 4 publications

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“…Oleh sebab itu, EPMS dapat larut pada beberapa pelarut polar dan nonpolar (Kurniawati, 2016). Pelarut polar yang dapat melarutkan EPMS diantaranya yaitu metanol, etanol, dan air (0,0301 mg/mL) (Rachmaniar, 2020) (Kurniawati, 2016).…”

Section: Pendahuluanunclassified

VALIDASI METODE ANALISIS SENYAWA ETIL p-METOKSISINAMAT DALAM PLASMA DARAH TIKUS PUTIH JANTAN GALUR WISTAR MENGGUNAKAN KROMATOGRAFI CAIR KINERJA TINGGI

Rachmaniar¹,

Suryanata²,

Simanjuntak³

2022

Pharma Xplore

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Ethyl p-methoxycinnamate (EPMC) isolated from the rhizome of kencur (Kaempferia galanga L) is being developed at STFI. Validation of EPMC analysis in blood plasma using High-Performance Liquid Chromatography (HPLC) needs to be conducted to perform in vivo EPMC analysis. This study aims to validate the EPMC analysis method in blood plasma using HPLC. The HPLC column used is column C18, with methanol : phosphoric acid 70:30 and 80:20 mobile phases, a flow rate of 1.0 mL/min, and a maximum wavelength of 310 nm. The blood plasma used was the blood plasma of white male rats of the Wistar strain. EPMC was added to blood plasma and analyzed using HPLC. Parameter validation used is system suitability test, linearity, accuracy, precision, limit of detection (LOD), and limit of quantification (LOQ). The results showed that the optimum mobile phase for analyzing EPMS in plasma was methanol : phosphoric acid with a ratio of 70:30. Based on the validation, the linear regression was 0.998. In the accuracy test, the average value range for the percent recovery is 98% - 102%. In the precision test, the average value of the RSD percentage was 4.10% - 68.83%. The LOD value is 2.747 g/mL, and the LOQ value is 9.158 g/mL. Based on this research, it can be concluded that EPMC in blood plasma can be analyzed using KKKT with column C18 and mobile phase methanol : phosphoric acid 70:30.

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Section: Pendahuluanunclassified

VALIDASI METODE ANALISIS SENYAWA ETIL p-METOKSISINAMAT DALAM PLASMA DARAH TIKUS PUTIH JANTAN GALUR WISTAR MENGGUNAKAN KROMATOGRAFI CAIR KINERJA TINGGI

Rachmaniar¹,

Suryanata²,

Simanjuntak³

2022

Pharma Xplore

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“…Sebelumnya EPMS berhasil ditingkatkan kelarutannya menggunakan teknik kokristalisasi menggunakan metode liquid assisted grinding dengan koformer asam sitrat (Rachmaniar, et al, 2020a) dan asam tartrat (Rachmaniar, et al, 2020b). Akan tetapi, peningkatan kelarutan kokristal EPMS-asam sitrat dan kokristal EPMS-asam tartrat dalam air tidak signifikan.…”

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“…Kokristal terdiri dari dua senyawa yakni zat aktif farmasi dan koformer (pembentuk kokristal) yang pada umumnya berada pada posisi netral (Qiao, et al, 2011). (Rachmaniar, et al, 2020a;Rachmaniar, et al, 2020b). Ikatan hidrogen ini akan membentuk formasi supermolekular sinton yang terdiri dari dua jenis formasi, yaitu homosinton dan heterosinton yang dapat membentuk kokristal dengan kuat (Qiao, et al, 2011).…”

unclassified

PENINGKATAN KELARUTAN ETIL p-METOKSISINAMAT DENGAN PEMBENTUKAN KOKRISTAL MENGGUNAKAN METODE SOLVENT EVAPORATION DAN KOFORMER UREA

Rachmaniar¹,

Tristiyanti²,

Triyadi³

2021

JSTFI

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Etil p-metoksisinamat (EPMS) merupakan isolat dengan persentase terbesar pada kencur (Kampferia galanga), tetapi sifatnya yang sukar larut air menyebabkan keterbatasan pada disolusi dan bioavailabilitas. Bioavailabilitas yang terbatas mengakibatkan aktivitas farmakologi yang rendah. Untuk mengatasi permasalahan tersebut, kelarutan EPMS dalam air perlu ditingkatkan. Penelitian ini bertujuan untuk meningkatkan kelarutan EPMS melalui pembentukan kokristal menggunakan metode solvent evaporation dan koformer urea. EPMS dan urea dengan perbandingan 1:1, 1:2, 1:3, dan 2:1 dilarutkan dalam etanol kemudian diuapkan. Kokristal EPMS-urea yang diperoleh dikarakterisasi menggunakan mikroskop digital, High Performance Liquid Chromatography (HPLC), spektrofotometer Fourier Transform Infrared (FT-IR), Powder X-Ray diffraction (PXRD), dan uji kelarutan di dalam air. Hasil penelitian menunjukkan kokristal EPMS-urea terbentuk akibat terjadinya ikatan hidrogen dan mengalami penurunan ukuran partikel, penurunan kristalinitas, dan peningkatan kelarutan. Kadar EPMS dalam sistem kokristal sebesar 91 -106%.

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Preparation and Solid-State Characterization of Ketoprofen-Succinic Acid-Saccharin Co-Crystal With Improved Solubility

IMANTO,

WIKANTYASNING,

NURWAINI

et al. 2024

Int J App Pharm

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Objective: This study aimed to improve the solubility of Ketoprofen, a non-steroidal anti-inflammatory drug (NSAID) that belongs to the Biopharmaceutical Classification System (BCS) Class II, through co-crystallization using succinic acid and saccharin coformers in a 1:1:1 and 2:1:1 molar ratio. Methods: The slurry method was utilized to prepare the ketoprofen co-crystals, which were then subjected to various physical-chemical characterization techniques such as melting point determination, dissolution studies, differential scanning calorimetry (DSC), X-ray diffraction (XRD), and Fourier transform infrared (FTIR) spectroscopy. Results: The results showed that the 1:1:1 molar ratio of ketoprofen-succinic acid-saccharin co-crystal (Formula 1) exhibited higher solubility than the solubility standard of Ketoprofen and the 2:1:1 molar ratio of the co-crystal (Formula 2). The dissolution profile (Q30) of Formula 1, Formula 2, and standard Ketoprofen were 96.73±1.77, 93.09±1.16, and 70.22±4.72, respectively. These findings suggest that co-crystallization with succinic acid and saccharin conformers using the slurry method can significantly enhance the solubility of Ketoprofen. Conclusion: The 1:1:1 molar ratio of ketoprofen-succinic acid-saccharin co-crystal (Formula 1) was the most effective formulation among the tested samples, demonstrating the highest solubility. This research may provide valuable insights for developing novel drug formulations with improved bioavailability and therapeutic efficacy.

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Pharmaceutical Cocrystal of Ethyl p-Methoxycinnamate: Formulation and Characterization

Cited by 3 publications

References 4 publications

VALIDASI METODE ANALISIS SENYAWA ETIL p-METOKSISINAMAT DALAM PLASMA DARAH TIKUS PUTIH JANTAN GALUR WISTAR MENGGUNAKAN KROMATOGRAFI CAIR KINERJA TINGGI

VALIDASI METODE ANALISIS SENYAWA ETIL p-METOKSISINAMAT DALAM PLASMA DARAH TIKUS PUTIH JANTAN GALUR WISTAR MENGGUNAKAN KROMATOGRAFI CAIR KINERJA TINGGI

PENINGKATAN KELARUTAN ETIL p-METOKSISINAMAT DENGAN PEMBENTUKAN KOKRISTAL MENGGUNAKAN METODE SOLVENT EVAPORATION DAN KOFORMER UREA

Preparation and Solid-State Characterization of Ketoprofen-Succinic Acid-Saccharin Co-Crystal With Improved Solubility

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