Preparation of pazopanib-fumarate disodium glycyrrhizinate nanocrystalline micelles by liquid-assisted ball milling

Shen, Dan; Jin, Tingyu; Yin, Xuefeng; Zhu, Xingyi; Hua, Yunfen

doi:10.1016/j.ejps.2023.106530

Cited by 5 publications

(2 citation statements)

References 23 publications

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“…7,9 Peningkatan kelarutan secara mekanokimia juga menunjukkan hasil yang menjanjikan. 10,11 Ball milling merupakan salah satu metode yang paling umum digunakan. Ball milling melibatkan proses yang mencakup deformasi dan frakturasi, dari partikel yang bertabrakan selama proses penggilingan berenergi tinggi.…”

Section: Pendahuluanunclassified

Kombinasi Teknik Pembentukan Kokristal dan Ball milling untuk Peningkatan Disolusi Etoricoxib

Susanto,

Wikarsa,

Nugraha

2024

JINTO

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Etoricoxib (ETX) merupakan salah satu golongan anti inflamasi selektif COX-2 yang diklasifikasikan dalam BCS kelas II. Penelitian ini bertujuan untuk meningkatkan laju disolusi etoricoxib melalui kombinasi pembentukan kokristal dan ball milling yang dilakukan secara in-situ dan ex-situ. Optimasi dilakukan dengan memvariasikan waktu penggilingan dan jenis stabilizer. Jenis stabilizer yang digunakan meliputi Tween 80 (ETX-OXA-BM-T), Poloxamer 188 (ETX-OXA-BM-P), dan kombinasi Tween 80-sodium lauryl sulfate (SLS) (ETX-OXA-BM-T-S). Percobaan secara in-situ memberikan jumlah rendemen yang sangat rendah (<10%) serta tidak mampu menghasilkan kokristal sehingga tidak layak dilanjutkan. Sementara proses ex-situ memberikan proses yang lebih potensial, sehingga hasil dilanjutkan evaluasi menggunakan Differential Scanning Calorimetry (DSC), Powder X-Ray Diffractometry (PXRD), dan Scanning Electron Microscope (SEM). Analisis DSC dari ETX memberikan puncak endotermik pada 130°C, sementara untuk ETX-OXA, ETX-OXA-BM-T, ETX-OXA-BM-P, dan ETX-OXA-BM-T-S memberikan puncak endotermik pada rentang 179 - 180°C. Difraktogram PXRD untuk ETX-OXA, ETX-OXA-BM-T, ETX-OXA-BM-P, ETX-OXA-BM-T-S memberikan puncak yang sama; dan berbeda dengan ETX. Hasil analisis SEM menunjukkan bahwa ETX-OXA-BM-T dengan waktu milling 60 menit memberikan partikel dalam rentang nanometer yang tidak terindividualiasi. Sementara penggunaan Poloxamer 188 serta kombinasi Tween 80-SLS menghasilkan ukuran partikel > 1 µm. ETX-OXA-BM-T menunjukkan peningkatan kelarutan yang paling tinggi pada semua media. Hasil disolusi ETX-OXA-BM-T menunjukkan adanya peningkatan pada media dapar fosfat pH 6,8. Sementara hasil disolusi pada media dapar pH 1,2 dan dapar pH 4,5 tidak memberikan perbedaan yang signifikan. Pada penelitian ini dapat dibuktikan bahwa kombinasi teknik pembentukan kokristal dan ball milling secara ex-situ merupakan salah satu pendekatan yang potensial untuk meningkatkan laju disolusi dari etoricoxib.

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Section: Pendahuluanunclassified

Kombinasi Teknik Pembentukan Kokristal dan Ball milling untuk Peningkatan Disolusi Etoricoxib

Susanto,

Wikarsa,

Nugraha

2024

JINTO

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“…Pharmaceutical cocrystals are defined as crystalline molecular complexes of fixed stoichiometry between an active pharmaceutical ingredient (API) with other pharmaceutically acceptable molecules [ 1 , 2 , 3 ]. Cocrystals can improve the physicochemical properties (e.g., stability, solubility, dissolution rate, and/or permeability) of compounds [ 4 , 5 , 6 , 7 , 8 ] and can also be tuned with pharmaceutically acceptable co-formers without altering the chemical structure of the API [ 1 ]. Especially, cocrystals are known to be superior to conventional formulations in in vivo pharmacokinetic properties such as absorption and bioavailability ( F ) [ 9 , 10 , 11 ].…”

Section: Introductionmentioning

confidence: 99%

Evaluation of Pharmacokinetic Feasibility of Febuxostat/L-pyroglutamic Acid Cocrystals in Rats and Mice

Yu,

You,

Bae

et al. 2023

Pharmaceutics

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Febuxostat (FBX), a selective xanthine oxidase inhibitor, belongs to BCS class II, showing low solubility and high permeability with a moderate F value (<49%). Recently, FBX/L-pyroglutamic acid cocrystal (FBX-PG) was developed with an improving 4-fold increase of FBX solubility. Nevertheless, the in vivo pharmacokinetic properties of FBX-PG have not been evaluated yet. Therefore, the pharmacokinetic feasibility of FBX in FBX- and FBX-PG-treated rats and mice was compared in this study. The results showed that the bioavailability (F) values of FBX were 210% and 159% in FBX-PG-treated rats and mice, respectively. The 2.10-fold greater total area under the plasma concentration–time curve from time zero to infinity (AUC0-inf) of FBX was due to the increased absorption [i.e., 2.60-fold higher the first peak plasma concentration (Cmax,1) at 15 min] and entero-hepatic circulation of FBX [i.e., 1.68-fold higher the second peak plasma concentration (Cmax,2) at 600 min] in FBX-PG-treated rats compared to the FBX-treated rats. The 1.59-fold greater AUC0-inf of FBX was due to a 1.65-fold higher Cmax,1 at 5 min, and a 1.15-fold higher Cmax,2 at 720 min of FBX in FBX-PG-treated mice compared to those in FBX-treated mice. FBX was highly distributed in the liver, stomach, small intestine, and lungs in both groups of mice, and the FBX distributions to the liver and lungs were increased in FBX-PG-treated mice compared to FBX-treated mice. The results suggest the FBX-PG has a suitable pharmacokinetic profile of FBX for improving its oral F value.

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Drug-like properties of tyrosine kinase inhibitors in ophthalmology: Formulation and topical availability

Jansook,

Loftsson,

Stefánsson

2024

International Journal of Pharmaceutics

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Preparation of pazopanib-fumarate disodium glycyrrhizinate nanocrystalline micelles by liquid-assisted ball milling

Cited by 5 publications

References 23 publications

Kombinasi Teknik Pembentukan Kokristal dan Ball milling untuk Peningkatan Disolusi Etoricoxib

Kombinasi Teknik Pembentukan Kokristal dan Ball milling untuk Peningkatan Disolusi Etoricoxib

Evaluation of Pharmacokinetic Feasibility of Febuxostat/L-pyroglutamic Acid Cocrystals in Rats and Mice

Drug-like properties of tyrosine kinase inhibitors in ophthalmology: Formulation and topical availability

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