Modeling of quantitative relationships between physicochemical properties of active pharmaceutical ingredients and tensile strength of tablets using a boosted tree

Hayashi, Yoshihiro; Oishi, Takuya; Shirotori, Kaede; Marumo, Yuki; Kosugi, Atsushi; Kumada, Shungo; Hirai, Daijiro; Takayama, Kozo; Onuki, Yoshinori

doi:10.1080/03639045.2018.1434195

Cited by 25 publications

(8 citation statements)

References 31 publications

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“…The TS of tablets is affected by several API properties, such as particle size [ 27 ], moisture content [ 28 ], and elastic recovery [ 29 ]. In our previous study [ 30 ], we established that one of the most crucial factors is the particle size. In general, there is a negative correlation between particle size and TS [ 31 , 32 ] because the compaction of smaller primary particles provides a larger total area for bonding than in the case of larger particles.…”

Section: Resultsmentioning

confidence: 99%

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A Precise Prediction Method for the Properties of API-Containing Tablets Based on Data from Placebo Tablets

et al. 2020

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We previously reported a novel method for the precise prediction of tablet properties (e.g., tensile strength (TS)) using a small number of experimental data. The key technique of this method is to compensate for the lack of experimental data by using data of placebo tablets collected in a database. This study provides further technical knowledge to discuss the usefulness of this prediction method. Placebo tablets consisting of microcrystalline cellulose, lactose, and cornstarch were prepared using the design of an experimental method, and their TS and disintegration time (DT) were measured. The response surfaces representing the relationship between the formulation and the tablet properties were then created. This study investigated tablets containing four different active pharmaceutical ingredients (APIs) with a drug load ranging from 20–60%. Overall, the TS of API-containing tablets could be precisely predicted by this method, while the prediction accuracy of the DT was much lower than that of the TS. These results suggested that the mode of action of APIs on the DT was more complicated than that on the TS. Our prediction method could be valuable for the development of tablet formulations.

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Section: Resultsmentioning

confidence: 99%

“…It is known that numerous API properties have a significant impact on the TS. They include particle size, bulk density, moisture content, and others [ 30 ]. However, these effects are thought to be independent from the effects of the formulation factors of the model tablet, and a high prediction accuracy could be achieved.…”

Section: Resultsmentioning

confidence: 99%

A Precise Prediction Method for the Properties of API-Containing Tablets Based on Data from Placebo Tablets

et al. 2020

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“…Mechanical property of loratadine and loratadine-succinic acid cocrystal is described as tensile strength curve shown in Figure 2. Tensile strength is an important parameter in tablet dosage form production as it represents the ability of a component or mixture of components to withstand the compression force applied and form compacted tablet without failure [14]. Both samples exhibited the same trend, that tensile strength increased with higher compression force.…”

Section: Mechanical Propertymentioning

confidence: 99%

Compression force effect on characteristics of loratadine-succinic acid cocrystal prepared by slurry method

Setyawan¹,

Paramanandana²,

Erfadrin³

et al. 2020

jrp

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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.

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“…Nilai kekuatan tarik dapat dihitung dari gaya yang diperlukan untuk memecah tablet (harga kekerasan) dan luas area yang diberi gaya kompresi (diameter tablet). Secara umum, peningkatan gaya kompresi akan meningkatkan nilai kekuatan tarik [8,9].…”

Section: Kurva Kekuatan Tarikunclassified

Pengaruh Komponen Hidrofobik Elastis terhadap Karakteristik Fisik dan Laju Disolusi Tablet Eritromisin Stearat

Paramita

Setyawan

2019

J Sains Farm Klin

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Eritromisin stearat (ERS) telah diketahui menunjukkan fenomena sintering ketika dikempa dan ini berpotensi menyebabkan masalah pada kualitas sediaan mengingat ERS umum dipasarkan sebagai tablet. Pembuatan campuran biner ERS dengan parasetamol (PRS) dan asam mefenamat (ASM) dilakukan untuk menelaah pengaruh karakter hidrofobik elastis kedua senyawa tersebut terhadap sintering dari ERS. Karakterisasi fisik tablet campuran biner meliputi uji kekuatan mekanis, difraksi sinar-X serbuk (DSXS), scanning electron microscope (SEM), differential thermal analysis (DTA), spektrofotometri inframerah, dan terakhir dilakukan uji disolusi. Keberadaan PRS dan ASM meningkatkan nilai kekuatan tarik tablet ERS dan ASM memberikan peningkatan yang lebih tinggi. Superimposisi pola difraksi ERS dengan PRS maupun ASM teramati dari difraktogram sinar-X campuran biner. Fotomikrograf SEM memperlihatkan batas-batas antarpartikel pada permukaan dan patahan tablet campuran biner yang lebih jelas terlihat pada tablet ERS-ASM. Spektra inframerah dan termogram DTA tidak menunjukkan adanya puncak baru akibat interaksi pada sampel campuran biner, hanya teramati transformasi polimorfik dari PRS. Tablet campuran biner ERS-PRS dan ERS-ASM menghasilkan profil disolusi lebih baik dari pada tablet ERS. Berdasarkan hasil karakterisasi tersebut di atas dapat disimpulkan bahwa kemampuan PRS dan ASM dalam mencegah fenomena sintering dari ERS tidak melibatkan adanya interaksi dan dapat memengaruhi profil disolusinya.

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Modeling of quantitative relationships between physicochemical properties of active pharmaceutical ingredients and tensile strength of tablets using a boosted tree

Abstract: This study demonstrates that BT model could provide comprehensive understanding of the latent structure underlying APIs and TS of tablets.

Cited by 25 publications

References 31 publications

A Precise Prediction Method for the Properties of API-Containing Tablets Based on Data from Placebo Tablets

A Precise Prediction Method for the Properties of API-Containing Tablets Based on Data from Placebo Tablets

Compression force effect on characteristics of loratadine-succinic acid cocrystal prepared by slurry method

Pengaruh Komponen Hidrofobik Elastis terhadap Karakteristik Fisik dan Laju Disolusi Tablet Eritromisin Stearat

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