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Yıl 2020, Cilt: 24 Sayı: 3, 410 - 415, 27.06.2025

Dwi Setyawan Abhimata Paramanandana , V. Eres Erfadrin Retno Sari , Diajeng Putri Paramita

https://doi.org/10.35333/jrp.2020.163
Cited By: 2

Öz

Kaynakça

  • [1] Vlaia L, Coneac G, Olariu I, Mut AM, Anghel DF, Maxim ME, Maxim ME, Şaramet G, Mitu M, Lupuliasa D, Vlaia V. Loratadine-loaded Microemulsions for Topical Application. Formulation, physicochemical characterization and in vitro drug release evaluation. Farmacia. 2017; 65(6): 851-861.
  • [2] Khan MZ, Rausl D, Zanoski R, Zidar S, Mikulcić JH, Krizmanić L, Eskinja M, Mildner B, Knezević Z. Classification of Loratadine Based on the Biopharmaceutics Drug Classification Concept and Possible in Vitro–in Vivo Correlation. Biol Pharm Bull. 2004; 27(10): 1630-1635. [CrossRef]
  • [3] Alshweiat A, Katona G, Csóka I, Ambrus R. Design and characterization of loratadine nanosuspension prepared by ultrasonic-assisted precipitation. Eur J Pharm Sci. 2018; 122: 94-104. [CrossRef]
  • [4] Milak S, Medlicott N, Tucker IG. Solid lipid microparticles containing loratadine prepared using a Micromixer. J Microencapsul. 2006; 23(8): 823-831. [CrossRef]
  • [5] Frizon F, Eloy JO, Donaduzzi CM, Mitsui ML, Marchetti JM. Dissolution rate enhancement of loratadine in polyvinylpyrrolidone K-30 solid dispersions by solvent methods. Powder Technol. 2013; 235: 532-539. [CrossRef]
  • [6] Omar L. El-Barghouthi MI, Masoud NA, Abdoh AA, Al Omari MM, Zughul MB, Badwan AA. Inclusion complexation of loratadine with natural and modified cyclodextrins: phase solubility and thermodynamic studies. J. Solution Chem. 2007; 36(5): 605-616. [CrossRef]
  • [7] Setyawan D, Pravianti ERD, Pratiwi KD, Isadiartuti D, Paramita DP. Cocrystallization of loratadine with succinic acid using neat grinding method (September 30, 2019). Proceedings of International Conference on Applied Pharmaceutical Sciences (ICoAPS) 2018. [CrossRef]
  • [8] Setyawan D, Permata AS, Zainul A, Lestari MLAD. Improvement in Vitro Dissolution Rate of Quercetin Using Cocrystallization of Quercetin-Malonic Acid. Indones J Chem. 2018; 18(3): 531-536. [CrossRef]
  • [9] Gadade DD, Pekamwar SS, Lahoti SR, Patni SD, Sarode MC. Cocrystallization of etodolac: prediction of cocrystallization, synthesis, solid state characterization and in vitro drug release. Marmara Pharm J. 2017; 21: 78-88.
  • [10] Paramanandana A, Setyawan D. Loratadine-Succinic Acid Cocrystals Physical Modification Made Using Slurry Method. Proceeding of the 2nd International Conference on Medicine and Health Sciences; 2018 Nov 30-Des 1; Jember, Indonesia. Universitas Jember, 2018.
  • [11] Duggirala NK, Perry ML, Almarsson Ö, Zaworotko MJ. Pharmaceutical cocrystals: along the path to improved medicines. Chem Commun (Camb). 2016; 52(4): 640-655. [CrossRef]
  • [12] Qiao N, Li M, Schlindwein W, Malek N, Davies A, Trappitt G. Pharmaceutical cocrystals: an overview. Int J Pharm. 2011; 419(1-2): 1-11. [CrossRef]
  • [13] Hosaka S, Sadoshima T, Sato M, Hamada C, Takahashi Y, Kitamori N. Effects of compression on the interaction between 1,4-dihydropyridine compounds and lactose monohydrate (II): differences in powder properties of 1,4- dihydropyridine compounds. Chem Pharm Bull. 2007; 55(5): 793-795. [CrossRef]
  • [14] Hayashi Y, Oishi T, Shirotori K, Marumo Y, Kosugi A, Kumada S, Hirai D, Takayama K, Onuki Y. Modeling of quantitative relationships between physicochemical properties of active pharmaceutical ingredients and tensile strength of tablets using a boosted tree. Drug Dev Ind Pharm. 2018; 44(7): 1090-1098. [CrossRef]
  • [15] Ainurofiq A, Mauludin R, Mudhakir D, Umeda D, Soewandhi SN, Putra OD. Improving mechanical properties of desloratadine via multicomponent crystal formation. Eur J Pharm Sci. 2018; 111: 65-72. [CrossRef]
  • [16] Perumalla SR, Sun CC. Enabling tablet product development of 5‐ fluorocytosine through integrated crystal and particle engineering. J Pharm Sci. 2014; 103(4): 1126-1132. [CrossRef]
  • [17] Ramos LA, Cavalheiro ÉTG. Thermal behavior of loratadine. J Therm Anal Calorim. 2007; 87: 831–834. [CrossRef]
  • [18] Caires FJ, Lima LS, Carvalho CT, Ionashiro M. Thermal behaviour of succinic acid, sodium succinate and its compounds with some bivalent transition metal ions. Thermochim Acta. 2010; 500(1-2): 6-12. [CrossRef]
  • [19] Ober CA, Gupta RB. Formation of itraconazole–succinic acid cocrystals by gas antisolvent cocrystallization. AAPS PharmSciTech. 2012; 13(4): 1396-1406. [CrossRef]
  • [20] Sinka IC, Cunningham JC, Zavaliangos A. Analysis of tablet compaction. II. Finite element analysis of density distributions in convex tablets. J Pharm Sci. 2004; 93(8): 2040-2053. [CrossRef]
  • [21] Athiyah U, Kusuma PA, Tutik T, Lestari MLAD, Isadiartuti D, Paramita DP, Setyawan D. Crystal engineering of quercetin by liquid assisted grinding method. J Teknol. 2019; 81(1): 1-7. [CrossRef]
  • [22] Rahman Z, Agarabi C, Zidan AR, Khan SR, Khan MA. Physico-mechanical and Stability Evaluation of Carbamazepine Cocrystal with Nicotinamide. AAPS PharmSciTech. 2011; 12(2): 693-704. [CrossRef]
  • [23] Rao MRP, Ranpise AA, Thanki KC, Borate SG, Parikh GN. Effect of Processing and Sintering on Controlled Release Wax Matrix Tablets of Ketorolac Tromethamine. Indian J Pharm Sci. 2009; 71(5): 538-544. [CrossRef]
  • [24] Setyawan D, Isadiartuti D, Betari SD, Paramita DP. Physical Characterization of Ibuprofen-Stearic Acid Binary Mixture Due to Compression Force. Indones J Pharm. 2016; 27(1): 28-34. [CrossRef]
  • [25] Setyawan D, Sumirtapura YC, Soewandhi SN, Hadi Tj D. Characterization of Physical Properties and Dissolution Rate of Binary Systems Erythromycin Stearate-Microcrystalline Cellulose and Spray Dried Lactose Due to Compression Forces. Int J Pharm Pharm Sci. 2012; 4(1): 652-657.
  • [26] Singh R, Poddar SS, Chivate A. Sintering of Wax for Controlling Release from Pellets. AAPS PharmSciTech. 2007; 8(3): E1-E9. [CrossRef]

Compression force effect on characteristics of loratadinesuccinic acid cocrystal prepared by slurry method

Yıl 2020, Cilt: 24 Sayı: 3, 410 - 415, 27.06.2025

Dwi Setyawan Abhimata Paramanandana , V. Eres Erfadrin Retno Sari , Diajeng Putri Paramita

https://doi.org/10.35333/jrp.2020.163
Cited By: 2

Öz

Loratadine belongs to second generation antihistamine (H1) drug and is known to form cocrystal with succinic acid in stoichiometry of 1:1 using slurry method. This study was conducted to further investigate cocrystal phase behavior upon compression. Sample of cocrystal phase was compressed with various compression forces into tablet form on 10 mm diameter punch. Then, the tablet was characterized for the mechanical properties and physical characterization was conducted using Differential Thermal Analysis (DTA), X-ray Powder Diffraction (XRPD), and Scanning Electron Microscope (SEM). According to tensile strength profile, cocrystal phase showed better mechanical property as it possessed higher tensile strength value compared to loratadine alone. DTA thermograms exhibited succinic acid characteristic peak alongside with endothermic peak of cocrystal phase which were compressed on higher force. It suggests that cocrystal undergoes partial dissociation to the starting components under compression. Powder diffractograms showed reduced intensity of tableted cocrystal compared to powder one for all compression force. SEM photomicrograph observed a loss of particle boundaries of cocrystal upon compression, as sintering phenomena occurred. It is predicted that compression force can influence physical characteristics of cocrystal of loratadine-succinic acid by driving dissociation and sintering phenomena.

Anahtar Kelimeler

Cocrystal compression force loratadine physical characterization succinic acid

Kaynakça

  • [1] Vlaia L, Coneac G, Olariu I, Mut AM, Anghel DF, Maxim ME, Maxim ME, Şaramet G, Mitu M, Lupuliasa D, Vlaia V. Loratadine-loaded Microemulsions for Topical Application. Formulation, physicochemical characterization and in vitro drug release evaluation. Farmacia. 2017; 65(6): 851-861.
  • [2] Khan MZ, Rausl D, Zanoski R, Zidar S, Mikulcić JH, Krizmanić L, Eskinja M, Mildner B, Knezević Z. Classification of Loratadine Based on the Biopharmaceutics Drug Classification Concept and Possible in Vitro–in Vivo Correlation. Biol Pharm Bull. 2004; 27(10): 1630-1635. [CrossRef]
  • [3] Alshweiat A, Katona G, Csóka I, Ambrus R. Design and characterization of loratadine nanosuspension prepared by ultrasonic-assisted precipitation. Eur J Pharm Sci. 2018; 122: 94-104. [CrossRef]
  • [4] Milak S, Medlicott N, Tucker IG. Solid lipid microparticles containing loratadine prepared using a Micromixer. J Microencapsul. 2006; 23(8): 823-831. [CrossRef]
  • [5] Frizon F, Eloy JO, Donaduzzi CM, Mitsui ML, Marchetti JM. Dissolution rate enhancement of loratadine in polyvinylpyrrolidone K-30 solid dispersions by solvent methods. Powder Technol. 2013; 235: 532-539. [CrossRef]
  • [6] Omar L. El-Barghouthi MI, Masoud NA, Abdoh AA, Al Omari MM, Zughul MB, Badwan AA. Inclusion complexation of loratadine with natural and modified cyclodextrins: phase solubility and thermodynamic studies. J. Solution Chem. 2007; 36(5): 605-616. [CrossRef]
  • [7] Setyawan D, Pravianti ERD, Pratiwi KD, Isadiartuti D, Paramita DP. Cocrystallization of loratadine with succinic acid using neat grinding method (September 30, 2019). Proceedings of International Conference on Applied Pharmaceutical Sciences (ICoAPS) 2018. [CrossRef]
  • [8] Setyawan D, Permata AS, Zainul A, Lestari MLAD. Improvement in Vitro Dissolution Rate of Quercetin Using Cocrystallization of Quercetin-Malonic Acid. Indones J Chem. 2018; 18(3): 531-536. [CrossRef]
  • [9] Gadade DD, Pekamwar SS, Lahoti SR, Patni SD, Sarode MC. Cocrystallization of etodolac: prediction of cocrystallization, synthesis, solid state characterization and in vitro drug release. Marmara Pharm J. 2017; 21: 78-88.
  • [10] Paramanandana A, Setyawan D. Loratadine-Succinic Acid Cocrystals Physical Modification Made Using Slurry Method. Proceeding of the 2nd International Conference on Medicine and Health Sciences; 2018 Nov 30-Des 1; Jember, Indonesia. Universitas Jember, 2018.
  • [11] Duggirala NK, Perry ML, Almarsson Ö, Zaworotko MJ. Pharmaceutical cocrystals: along the path to improved medicines. Chem Commun (Camb). 2016; 52(4): 640-655. [CrossRef]
  • [12] Qiao N, Li M, Schlindwein W, Malek N, Davies A, Trappitt G. Pharmaceutical cocrystals: an overview. Int J Pharm. 2011; 419(1-2): 1-11. [CrossRef]
  • [13] Hosaka S, Sadoshima T, Sato M, Hamada C, Takahashi Y, Kitamori N. Effects of compression on the interaction between 1,4-dihydropyridine compounds and lactose monohydrate (II): differences in powder properties of 1,4- dihydropyridine compounds. Chem Pharm Bull. 2007; 55(5): 793-795. [CrossRef]
  • [14] Hayashi Y, Oishi T, Shirotori K, Marumo Y, Kosugi A, Kumada S, Hirai D, Takayama K, Onuki Y. Modeling of quantitative relationships between physicochemical properties of active pharmaceutical ingredients and tensile strength of tablets using a boosted tree. Drug Dev Ind Pharm. 2018; 44(7): 1090-1098. [CrossRef]
  • [15] Ainurofiq A, Mauludin R, Mudhakir D, Umeda D, Soewandhi SN, Putra OD. Improving mechanical properties of desloratadine via multicomponent crystal formation. Eur J Pharm Sci. 2018; 111: 65-72. [CrossRef]
  • [16] Perumalla SR, Sun CC. Enabling tablet product development of 5‐ fluorocytosine through integrated crystal and particle engineering. J Pharm Sci. 2014; 103(4): 1126-1132. [CrossRef]
  • [17] Ramos LA, Cavalheiro ÉTG. Thermal behavior of loratadine. J Therm Anal Calorim. 2007; 87: 831–834. [CrossRef]
  • [18] Caires FJ, Lima LS, Carvalho CT, Ionashiro M. Thermal behaviour of succinic acid, sodium succinate and its compounds with some bivalent transition metal ions. Thermochim Acta. 2010; 500(1-2): 6-12. [CrossRef]
  • [19] Ober CA, Gupta RB. Formation of itraconazole–succinic acid cocrystals by gas antisolvent cocrystallization. AAPS PharmSciTech. 2012; 13(4): 1396-1406. [CrossRef]
  • [20] Sinka IC, Cunningham JC, Zavaliangos A. Analysis of tablet compaction. II. Finite element analysis of density distributions in convex tablets. J Pharm Sci. 2004; 93(8): 2040-2053. [CrossRef]
  • [21] Athiyah U, Kusuma PA, Tutik T, Lestari MLAD, Isadiartuti D, Paramita DP, Setyawan D. Crystal engineering of quercetin by liquid assisted grinding method. J Teknol. 2019; 81(1): 1-7. [CrossRef]
  • [22] Rahman Z, Agarabi C, Zidan AR, Khan SR, Khan MA. Physico-mechanical and Stability Evaluation of Carbamazepine Cocrystal with Nicotinamide. AAPS PharmSciTech. 2011; 12(2): 693-704. [CrossRef]
  • [23] Rao MRP, Ranpise AA, Thanki KC, Borate SG, Parikh GN. Effect of Processing and Sintering on Controlled Release Wax Matrix Tablets of Ketorolac Tromethamine. Indian J Pharm Sci. 2009; 71(5): 538-544. [CrossRef]
  • [24] Setyawan D, Isadiartuti D, Betari SD, Paramita DP. Physical Characterization of Ibuprofen-Stearic Acid Binary Mixture Due to Compression Force. Indones J Pharm. 2016; 27(1): 28-34. [CrossRef]
  • [25] Setyawan D, Sumirtapura YC, Soewandhi SN, Hadi Tj D. Characterization of Physical Properties and Dissolution Rate of Binary Systems Erythromycin Stearate-Microcrystalline Cellulose and Spray Dried Lactose Due to Compression Forces. Int J Pharm Pharm Sci. 2012; 4(1): 652-657.
  • [26] Singh R, Poddar SS, Chivate A. Sintering of Wax for Controlling Release from Pellets. AAPS PharmSciTech. 2007; 8(3): E1-E9. [CrossRef]
Toplam 26 adet kaynakça vardır.

Ayrıntılar

Birincil Dil İngilizce
Konular Eczacılık ve İlaç Bilimleri (Diğer)
Bölüm Articles
Yazarlar

Dwi Setyawan

Abhimata Paramanandana

V. Eres Erfadrin

Retno Sari

Diajeng Putri Paramita

Yayımlanma Tarihi 27 Haziran 2025
Yayımlandığı Sayı Yıl 2020 Cilt: 24 Sayı: 3

Kaynak Göster

APA Setyawan, D., Paramanandana, A., Erfadrin, V. E., Sari, R., vd. (2025). Compression force effect on characteristics of loratadinesuccinic acid cocrystal prepared by slurry method. Journal of Research in Pharmacy, 24(3), 410-415. https://doi.org/10.35333/jrp.2020.163
AMA Setyawan D, Paramanandana A, Erfadrin VE, Sari R, Paramita DP. Compression force effect on characteristics of loratadinesuccinic acid cocrystal prepared by slurry method. J. Res. Pharm. Haziran 2025;24(3):410-415. doi:10.35333/jrp.2020.163
Chicago Setyawan, Dwi, Abhimata Paramanandana, V. Eres Erfadrin, Retno Sari, ve Diajeng Putri Paramita. “Compression Force Effect on Characteristics of Loratadinesuccinic Acid Cocrystal Prepared by Slurry Method”. Journal of Research in Pharmacy 24, sy. 3 (Haziran 2025): 410-15. https://doi.org/10.35333/jrp.2020.163.
EndNote Setyawan D, Paramanandana A, Erfadrin VE, Sari R, Paramita DP (01 Haziran 2025) Compression force effect on characteristics of loratadinesuccinic acid cocrystal prepared by slurry method. Journal of Research in Pharmacy 24 3 410–415.
IEEE D. Setyawan, A. Paramanandana, V. E. Erfadrin, R. Sari, ve D. P. Paramita, “Compression force effect on characteristics of loratadinesuccinic acid cocrystal prepared by slurry method”, J. Res. Pharm., c. 24, sy. 3, ss. 410–415, 2025, doi: 10.35333/jrp.2020.163.
ISNAD Setyawan, Dwi vd. “Compression Force Effect on Characteristics of Loratadinesuccinic Acid Cocrystal Prepared by Slurry Method”. Journal of Research in Pharmacy 24/3 (Haziran 2025), 410-415. https://doi.org/10.35333/jrp.2020.163.
JAMA Setyawan D, Paramanandana A, Erfadrin VE, Sari R, Paramita DP. Compression force effect on characteristics of loratadinesuccinic acid cocrystal prepared by slurry method. J. Res. Pharm. 2025;24:410–415.
MLA Setyawan, Dwi vd. “Compression Force Effect on Characteristics of Loratadinesuccinic Acid Cocrystal Prepared by Slurry Method”. Journal of Research in Pharmacy, c. 24, sy. 3, 2025, ss. 410-5, doi:10.35333/jrp.2020.163.
Vancouver Setyawan D, Paramanandana A, Erfadrin VE, Sari R, Paramita DP. Compression force effect on characteristics of loratadinesuccinic acid cocrystal prepared by slurry method. J. Res. Pharm. 2025;24(3):410-5.

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Cocrystal formation of loratadine-succinic acid and its improved solubility
Journal of Basic and Clinical Physiology and Pharmacology
https://doi.org/10.1515/jbcpp-2020-0456