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Journal : Borneo Journal of Pharmacy

Identification of Candesartan Cilexetil-L-Arginine Co-amorphous Formation and Its Solubility Test Fikri Alatas; Erina Sifa Mutmainah; Hestiary Ratih; Titta Hartyana Sutarna; Sundani Nurono Soewandhi
Borneo Journal of Pharmacy Vol. 5 No. 1 (2022): Borneo Journal of Pharmacy
Publisher : Institute for Research and Community Services Universitas Muhammadiyah Palangkaraya

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.33084/bjop.v5i1.2942

Abstract

The formation of co-amorphous is one alternative that can be attempted to enhance the solubility of drugs. The study aimed to identify the co-amorphous formation between candesartan cilexetil (CAN) and l-arginine (ARG) and to know its effect on the solubility and dissolution rate of candesartan cilexetil. Initial prediction of co-crystal formation was undertaken by observing differences in crystal morphology between the candesartan cilexetil-l-arginine (CAN-ARG) mixture and each of its initial components due to crystallization in ethanol. The CAN-ARG co-amorphous was produced by the liquid-assisted grinding (LAG) method with the same molar ratio of the CAN and ARG mixture using ethanol as solvent. The co-amorphous formation of CAN-ARG was identified by powder X-ray diffraction (PXRD) and differential scanning calorimetry (DSC) methods. The solubility and dissolution test was performed to know the impact of the co-amorphous CAN-ARG formation. The PXRD pattern of CAN-ARG of LAG result showed a very low peak intensity compared to pure CAN and ARG. The DSC thermogram of the CAN-ARG LAG result does not show any sharp endothermic peaks. The PXRD and DSC results reveal that CAN and ARG can form co-amorphous. The solubility and dissolution rate of candesartan cilexetil in co-amorphous CAN-ARG was better than that of pure CAN. It can be concluded, liquid-assisted grinding of CAN-ARG mixture is identified to form co-amorphous which has an impact on increasing the solubility and dissolution rate of candesartan cilexetil.
Solubility and Scale-Up Potency of Norfloxacin-Urea Co-Crystal Prepared by Ultrasound-Assisted Slurry Co-Crystallization Method Fikri Alatas; Dery Stiawan; Nur Achsan Al-Hakim
Borneo Journal of Pharmacy Vol. 6 No. 2 (2023): Borneo Journal of Pharmacy
Publisher : Institute for Research and Community Services Universitas Muhammadiyah Palangkaraya

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.33084/bjop.v6i2.4173

Abstract

Norfloxacin is an antimicrobial in treating urinary tract infections with low water solubility. This study aims to know the effect of norfloxacin-urea co-crystal formation on the solubility of norfloxacin and the potential for scale-up when prepared by ultrasound-assisted slurry co-crystallization method. Identification of the screening result of the norfloxacin-urea (1 : 1) co-crystal formation by a wet grinding method using an ethanol-acetone (1 : 1) solvent mixture was performed by powder X-ray diffractometer (PXRD). The ultrasound-assisted slurry co-crystallization method was used for co-crystal formation with five-fold the weight of norfloxacin and urea than the wet grinding method. The co-crystal product prepared by the ultrasound-assisted slurry co-crystallization method was observed for its crystal morphology and characterized by PXRD and differential scanning calorimeter (DSC). Solubility and dissolution tests in water and acetate buffer solution pH 4.0 were used to evaluate the physicochemical properties. Identification of co-crystal screening by PXRD revealed the formation of norfloxacin-urea co-crystal. The PXRD pattern of the norfloxacin-urea co-crystal product prepared by the ultrasound-assisted slurry co-crystallization method was similar to the wet grinding method. Norfloxacin-urea co-crystal has a different melting point and crystal morphology from pure norfloxacin and urea. The solubility and dissolution rate of norfloxacin-urea co-crystal was higher in water and not significantly different in acetate buffer solution pH 4.0 compared to pure norfloxacin. This study showed that the norfloxacin-urea co-crystal formation could enhance the solubility of norfloxacin in water and had the potential for scale-up when prepared using the ultrasound-assisted slurry co-crystallization method.
Co-Authors Abdul Azizsidiq, Fahmi Afifah Bambang Sutjiatmo, Afifah Bambang Alisha Ramadhanty Ludin Alya Nur Asilla Anggraeni Wulan Angraeni, Wulan Asih Rahaju Aulia Rachmadian Bella Dewinta Saraswati Bintary, Dyan Dery Stiawan Dessy Adriani Putri Diamona Ayu Lestari Dina Apriani Dini Tereslina Dolih Gozali Dzaza Syahidatul Alamiah Elivas Simatupang Endah Wahyuni Erina Sifa Mutmainah Euis Reni Yuslianti, Euis Fahrauk Faramayuda, Fahrauk Faizal Hermanto Fani Wahyuni Fani Wahyuni, Fani Febrianti, Mia Fitria Hanako Gladdis Kamilah Pratiwi Haq, Fahmy Ahsanul Hartyana Sutarna, Titta Hernandi Sujono Hesti Kurnia Hestiary Ratih Iis Inayati Rakhmat Ine Rosmala Dewi Ismunandar Ismunandar Jessie Sofia Pamudji Karin, Amada Kintan Putri Nur Shafarkiani Lucky Rachmawan Lucy D. N. Sasongko Lucy Sasongko Mia Agustin Moch. Reza Pratama Muliana, Muliana Nadira Cantika Putri Ananda Nira Purnamasari, Nira Nur Achsan Al-Hakim Nurono Soewandhi, Sundani Pratama, Moch. Reza Pratiwi, Gladdis Kamilah Prianto, Ulla L. F. Purnamasari Nira Purwoko, Agus Qotrunnada, Daffa Rachmah, Mutia Alifah Rahayu, Novitri Sri Raisa Fakhrona Salman Rani Sugandi Rani Sugandi, Rani Ratih Hestiary Ratih, Hestyari Regita Ayu Lestari Resina Hajar Ririn Puspadewi, Ririn Risanteni Riskasari Riskia Putri Peratiwi Riskia Putri Peratiwi, Riskia Putri Setia Permana Sintia Resni Pratiwi Suci Nar Vikasari, Suci Nar Sukmadjaja Asyarie Sundani N. Soewandhi Sundani Nurono S. Sundani Nurono Soewandhi Sundani Nurono Soewandhi Sundani Nurono Soewandhi Sundani Nurono Soewandhi Sundani Nurono Soewandhi Syahidatul Alamiah, Dzaza Titta H. Sutarna Tresa Tri Rayani Tresa Tri Rayani, Tresa Tri Tresna Lestari, Tresna Woro Artati Sucipto Wulan Anggraeni Yesi Desmiaty, Yesi Yoga Windhu Wardhana Yoga Windu Wardhana Zwista Yulia Dewi