Tofogliflozin Salt Cocrystals with Sodium Acetate and Potassium Acetate

Takata, Noriyuki; Tanida, Satoshi; Nakae, Shinichi; Shiraki, Koji; Tozuka, Yuichi; Ishigai, Masaki

doi:10.1248/cpb.c18-00483

Cited by 5 publications

(6 citation statements)

References 34 publications

(36 reference statements)

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“…Proses Leblanc ini didasarkan pada pemanggangan kerak garam (115)(116)(117)(118)(119)(120)(121)(122)(123)(124) dengan karbon dan gamping di dalam tanur putar dan sesudah itu dilakukan proses pengerasan hasilnya dengan air. Produk kasar dari reaksi ini dinamakan black ash (abu hitam).…”

Section: B Proses Leblancunclassified

Natrium Karbonat : Termodinamika dan Transport Ion

Jumalia¹,

Zainul²

2019

Preprint

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Natrium Karbonat merupakan salah satu garam natrium dari asam karbonat yang bersifat higroskospis. Natrium Karbonat biasanya dapat digunakan dalam pembuatan kaca. Sintesis Natrium karbonat dapat dilakukan dengan proses Leblanc dan Solvay. Tujuan dari review ini untuk mengetahui termodinamika dan transport ion pada senyawa natrium karbonat. Metode yang digunakan yaitu studi literatur menggunakan endnote X7, pemodelan komputasi menggunakan ChemOffice 15.0, dan perhitungan matematis. Metode dengan studi literatur dapat dilihat pada fishbone. Metode menggunakan ChemOffice 15.0, pada minimize energy dihasilkan energi -271.9263 kcal/mol pada suhu optimum dengan bend nya yaitu 4.4521. Pada metode perhitungan matematis ada beberapa parameter transport ion yang dapat dihitung yaitu konduktivitas, viskositas, mobilitas ion, dan kecepatan hanyut. Parameter ini selain didapatkan dari perhitungan matematis juga dari data hasil review jurnal penelitian yang berkaitan. Hasil perhitungan pada konduktivitas yaitu 0,07905 x 10-8 mho/cm. Nilai viskositas natrium karbonat yaitu . Kelarutan natrium karbonat anhidrat pada suhu 20OC yaitu 2.533 g/cm3 .Sifat termokimia pada natrium karbonat ini yaitu Cp, So, ΔfHo ,ΔfG, masing-masing bernilai 109,2 J/mol·K; 136,4 J/mol·K; -1131 kJ/mol ; -1047,5 kJ/mol.

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Section: B Proses Leblancunclassified

Natrium Karbonat : Termodinamika dan Transport Ion

Jumalia¹,

Zainul²

2019

Preprint

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“…The analysis of chloride salt anhydrate structures of these drugs performed by them reveals that the Cl – ion also acts as an H-bond acceptor to satisfy the donor–acceptor imbalance to some extent. However, the H-bond donor to acceptor ratio was found at best in the case of salt hydrates, which was argued as the reason for their high propensity to hydrate formation. − Other potential causes considered for hydrate formation include the presence of hydrophilic functional groups exposed toward crystal facets (surface anisotropy) − and an increased number of crystal defect sites induced during processing (milling, mixing, granulation, and compression). ,, …”

Section: Introductionmentioning

confidence: 99%

Crystalline Multicomponent Solids: An Alternative for Addressing the Hygroscopicity Issue in Pharmaceutical Materials

Thakur

Thakuria

2020

Crystal Growth & Design

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The ambient humidity varies with seasons and geographical altitude across the regions. A change in relative humidity during processing, storage, and transportation can cause instability to the active pharmaceutical ingredient (API) solid form, which may sometimes lead to the formation of hydrates, decomposition, and dissociation (or disproportionation) of the drug product. A thorough understanding of the interaction of crystalline solid with atmospheric water is necessary to understand this phenomenon and to develop a potential solution to this problem. In this review, we discuss various aspects of this phenomenon along with some examples from the literature wherein the physical stability enhancement of an API is addressed through the multicomponent solid form (salts, cocrystals, and eutectics) development. The review also presents an overview of computational approaches employed to predict the hydration behavior of an API, their susceptibility to form hydrates, and studies on the crystal structure prediction of hydrates. Additionally, a few representative studies highlighting the moisture-induced phase transformations to polymorphs, hydrates, and cocrystal formation and their dissociation are discussed.

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“…24 With regard to safety, salt counters and amino acids that have been approved or are listed in generally recognized as safe (GRAS) 25 and everything added to food in the United States (EAFUS) 26 are selected as the coformers for cocrystals, ionic cocrystals, and salt cocrystals. 15,27,28 Sugars are neutral, safe, and inexpensive coformers, and many studies on ionic cocrystals with sugars have been reported. The formation of a complex with D-glucose with sodium chloride (NaCl) was reported in the early 1800s.…”

Section: ■ Introductionmentioning

confidence: 99%

“…In a salt cocrystal of metoclopramide hydrochloride with oxalic acid, oxalic acid reduces the hygroscopicity owing to the use of all proton donors and acceptors of metoclopramide for hydrogen bonding . With regard to safety, salt counters and amino acids that have been approved or are listed in generally recognized as safe (GRAS) and everything added to food in the United States (EAFUS) are selected as the coformers for cocrystals, ionic cocrystals, and salt cocrystals. ,, …”

Section: Introductionmentioning

confidence: 99%

Salt Cocrystallization of Loxoprofen Sodium with Sugar: Reduction of the Propensity for Hydrate Formation by Forming a Continuous One-Dimensional Chain Structure of Sodium and Sugar

Fujito

Oshima

Higashi

et al. 2021

Crystal Growth & Design

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Compared to free base forms, salt forms are more frequently obtained as hydrates during solid form screening, although physically unstable hydrates are difficult to select for drug development. In this study, loxoprofen sodium dihydrate (LOXNa-2H2O), a widely used anti-inflammatory drug, was selected as a model drug to investigate the potential use of sugar as a coformer for cocrystallization with Na salts and the effect of salt cocrystallization with sugars on hydrate formation. In a screening study by liquid-assisted grinding with ethanol, two sugars, ribose (RIB) and fructose (FRU), formed new salt cocrystals with LOXNa. Differential scanning calorimetry, thermogravimetry, temperature-programmed powder X-ray diffraction, and water vapor sorption/desorption isotherm measurements revealed that the LOXNa·RIB and LOXNa·FRU salt cocrystals were a monohydrate and anhydrate, respectively. Single-crystal X-ray structural analysis of both salt cocrystals showed that direct ionic interaction did not occur between the Na cation and the carboxylate anion of LOX. Instead, sugars were coordinated around a Na cation, and a consecutive alternating structure of Na cations and sugars with a one-dimensional chain was formed along the b-axis. These characteristic chain structures prevented water molecules from approaching the Na cation and reduced the propensity for hydrate formation. FRU possesses one more hydroxyl group than the RIB molecule. The resulting strong hydrogen bonding network stabilized the LOXNa-FRU as an anhydrate without water molecules. Since sugars are safe and inexpensive excipients with various species, they can be useful coformers for salt cocrystals with various drug Na salts.

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Tofogliflozin Salt Cocrystals with Sodium Acetate and Potassium Acetate

Cited by 5 publications

References 34 publications

Natrium Karbonat : Termodinamika dan Transport Ion

Natrium Karbonat : Termodinamika dan Transport Ion

Crystalline Multicomponent Solids: An Alternative for Addressing the Hygroscopicity Issue in Pharmaceutical Materials

Salt Cocrystallization of Loxoprofen Sodium with Sugar: Reduction of the Propensity for Hydrate Formation by Forming a Continuous One-Dimensional Chain Structure of Sodium and Sugar

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