The effect of cocrystallization method and citric acid as coformer on water solubility of ethyl p-metoxycinnamate particle

Rachmaniar, Revika; Riasari, Hesti; Fauziah, Lisarah; Kenti,; Ferdiansyah, Rival

doi:10.1063/5.0003178

Cited by 3 publications

(5 citation statements)

References 22 publications

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“…Additionally, norfloxacin-citric acid cocrystals showed improved solubility compared to norfloxacin alone [191]. Another report by Revika et al [192] described that ethyl p-methoxycinnamate used as anti-inflammatory agent showed a 44.19% increase in solubility in its cocrystal form compared to ethyl pmethoxycinnamate alone. Fahad et al [193] reported that cocrystals of simvastatin in which citric acid was used as a coformer showed greater solubility, dissolution rate, and bioavailability.…”

Section: Citric Acid As a Coformermentioning

confidence: 97%

Cocrystals by Design: A Rational Coformer Selection Approach for Tackling the API Problems

et al. 2023

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Active pharmaceutical ingredients (API) with unfavorable physicochemical properties and stability present a significant challenge during their processing into final dosage forms. Cocrystallization of such APIs with suitable coformers is an efficient approach to mitigate the solubility and stability concerns. A considerable number of cocrystal-based products are currently being marketed and show an upward trend. However, to improve the API properties by cocrystallization, coformer selection plays a paramount role. Selection of suitable coformers not only improves the drug’s physicochemical properties but also improves the therapeutic effectiveness and reduces side effects. Numerous coformers have been used till date to prepare pharmaceutically acceptable cocrystals. The carboxylic acid-based coformers, such as fumaric acid, oxalic acid, succinic acid, and citric acid, are the most commonly used coformers in the currently marketed cocrystal-based products. Carboxylic acid-based coformers are capable of forming the hydrogen bond and contain smaller carbon chain with the APIs. This review summarizes the role of coformers in improving the physicochemical and pharmaceutical properties of APIs, and deeply explains the utility of afore-mentioned coformers in API cocrystal formation. The review concludes with a brief discussion on the patentability and regulatory issues related to pharmaceutical cocrystals.

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Section: Citric Acid As a Coformermentioning

confidence: 97%

Cocrystals by Design: A Rational Coformer Selection Approach for Tackling the API Problems

et al. 2023

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“…The solvent evaporation technique has been successfully used to form multicomponent crystals and has succeeded in increasing the solubility of pharmaceutically active substances [15][16][17][18][19][20][21][22][23][24]28].…”

Section: Solvent Evaporationmentioning

confidence: 99%

A Review of Coformer Utilization in Multicomponent Crystal Formation

et al. 2022

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Most recently discovered active pharmaceutical molecules and market-approved medicines are poorly soluble in water, resulting in limited drug bioavailability and therapeutic effectiveness. The application of coformers in a multicomponent crystal method is one possible strategy to modulate a drug’s solubility. A multicomponent crystal is a solid phase formed when several molecules of different substances crystallize in a crystal lattice with a certain stoichiometric ratio. The goal of this review paper is to comprehensively describe the application of coformers in the formation of multicomponent crystals as solutions for pharmaceutically active ingredients with limited solubility. Owing to their benefits including improved physicochemical profile of pharmaceutically active ingredients, multicomponent crystal methods are predicted to become increasingly prevalent in the development of active drug ingredients in the future

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“…EPMS termasuk ke dalam senyawa ester yang mengandung cincin benzen dan gugus metoksi yang bersifat non polar, dan juga gugus karbonil yang mengikat etil yang bersifat sedikit polar sehingga cenderung tidak larut dalam air (Barus, 2009). EPMS memiliki kelarutan dalam air sebesar 0,0301 mg/mL atau praktis tidak larut (Rachmaniar, et al, 2020a). Kelarutan obat memainkan peranan penting dalam penentuan khasiat dan aktivitas obat (Bavishi and Borkhataria, 2016;Riasari, et al, 2016).…”

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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).…”

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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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The effect of cocrystallization method and citric acid as coformer on water solubility of ethyl p-metoxycinnamate particle

Cited by 3 publications

References 22 publications

Cocrystals by Design: A Rational Coformer Selection Approach for Tackling the API Problems

Cocrystals by Design: A Rational Coformer Selection Approach for Tackling the API Problems

A Review of Coformer Utilization in Multicomponent Crystal Formation

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

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