Insight into the Phase Transformation among Various Solid Forms of Baicalein

A new polymorph and three hydrates of baicalein, a widely prescribed anti-inflammatory TCM drug, were discovered through comprehensive polymorph screening experiments. The forms were fully characterized by a range of analytical techniques, including PXRD, Raman spectra, FTIR, HSM, SEM, TGA, DSC, and DVS. Single crystal structures and the transformation pathways among different polymorphs and hydrates are discussed in detail. Single-crystal-to-single-crystal transformation behavior between monohydrate and hemihydrate was revealed. Thermodynamic stability, hygroscopicity, and powder dissolution behavior were investigated. The results show that the newly discovered form γ presents better dissolution behavior and remarkably greater apparent solubility compared with the current widely used marketed drug substance

Insight into the Phase Transformation among Various Solid Forms of Baicalein

A new polymorph and three hydrates of baicalein, a widely prescribed anti-inflammatory TCM drug, were discovered through comprehensive polymorph screening experiments. The forms were fully characterized by a range of analytical techniques, including PXRD, Raman spectra, FTIR, HSM, SEM, TGA, DSC, and DVS. Single crystal structures and the transformation pathways among different polymorphs and hydrates are discussed in detail. Single-crystal-to-single-crystal transformation behavior between monohydrate and hemihydrate was revealed. Thermodynamic stability, hygroscopicity, and powder dissolution behavior were investigated. The results show that the newly discovered form γ presents better dissolution behavior and remarkably greater apparent solubility compared with the current widely used marketed drug substance

Insight into the Phase Transformation among Various Solid Forms of Baicalein

A new polymorph and three hydrates of baicalein, a widely prescribed anti-inflammatory TCM drug, were discovered through comprehensive polymorph screening experiments. The forms were fully characterized by a range of analytical techniques, including PXRD, Raman spectra, FTIR, HSM, SEM, TGA, DSC, and DVS. Single crystal structures and the transformation pathways among different polymorphs and hydrates are discussed in detail. Single-crystal-to-single-crystal transformation behavior between monohydrate and hemihydrate was revealed. Thermodynamic stability, hygroscopicity, and powder dissolution behavior were investigated. The results show that the newly discovered form γ presents better dissolution behavior and remarkably greater apparent solubility compared with the current widely used marketed drug substance

Improving Dissolution and Photostability of Vitamin K3 via Cocrystallization with Naphthoic Acids and Sulfamerazine

Menadione (MD), also known as vitamin K3, has been widely applied in fortified food, feed, and the nutrition industry for its antihemorrhagic activity. However, the poor photostability in the solid state has greatly affected its biological performance and limited its applications. With the objective to alter the topochemical photoreactivity, a cocrystallization approach was employed, and three MD cocrystals with naphthoic acids and sulfamerazine were designed and prepared. Single crystal structures were determined, and solid-state characterization were performed. Solid-state UV–vis spectra revealed a significant red-shift of UV absorption in the cocrystal solids resulting in variant color differences. These physicochemical changes may be attributed to the enhanced π···π interactions and change-transfer interactions within these molecular complexes. More importantly, the newly synthesized cocrystals displayed better dissolution behavior and superior photostability with respect to MD itself. No obvious degradation was observed under stressed photoirradiation conditions. These findings may provide new possibilities to the application of this key vitamin

Cocrystals of Baicalein with Higher Solubility and Enhanced Bioavailability

Baicalein (<b>Bai</b>) is one of the most important bioactive flavonoids isolated from the well-known traditional Chinese medicine called “Huang Qin”. Though it has broad therapeutic capability, the bioavailability is limited due to its poor solubility. In this study, we aimed to modulate its solubility through cocrystallization. Cocrystals of <b>Bai</b> with isoniazide (<b>Inia</b>), isonicotinamide (<b>Inam</b>), caffeine (<b>Caf</b>), and theophylline (<b>Tph</b>) were obtained. And different cocrystallization methods lead to different cocrystal phases for <b>Inam</b> and <b>Tph</b>. These cocrystals were characterized using powder X-ray diffraction, thermogravimetric analysis, differential scanning calorimetry, dynamic vapor sorption, and Fourier transform infrared spectroscopy. Among all the cocrystals studied, <b>BaiCaf</b> is found to be superior in powder dissolution and pharmacokinetic behavior. Area under the curve values of <b>BaiCaf</b> is improved by a factor of 4.1, and the bioavailability of baicalein is thus expected to be accordingly increased. Given that <b>Caf</b> is a central nervous system stimulant available in many prescription and nonprescription medications, <b>BaiCaf</b> can be a promising alternative solid form of <b>Bai</b> to be developed

Minimum spanning tree analysis of <i>Neisseria meningitidis</i> serogroup C ST-4821 strains according to subtypes by MLVA.

<p>(a) The relationships of all 118 strains isolated from seventeen provinces of China; (b) the relationships of 29 strains isolated from Anhui Province; and (c) the relationships of 25 Shandong strains, including 18 isolates from an outbreak. In the minimum spanning tree, each circle denotes a particular subtype by MLVA, and the size of each circle indicates the number of isolates of that particular subtype. Strains from different provinces are represented by different colors. Thick, solid lines represent single-locus variants (SLV); thin, solid lines represent double-locus variants (DLV); lines for double, triple and more loci difference were omitted. MLVA grouping was achieved if neighbors differed by no more than one of five VNTR loci; these are marked with a dark gray shadow.</p

Characteristics of the <i>N. meningitidis</i> strains used in this study.

<p>Characteristics of the <i>N. meningitidis</i> strains used in this study.</p

Sequences and Primers Used for MLVA of <i>N. meningitidis</i>.

<p>Sequences and Primers Used for MLVA of <i>N. meningitidis</i>.</p

Main characteristics of the selected VNTR loci in <i>N. meningitidis</i> strains.

<p><b>Diversity Index</b> (for the VNTR data)  =  A measure of the variation in the number of repeats at each locus ranging from 0.0 (no diversity) to 1.0 (complete diversity).</p><p><b>Confidence Interval</b>  =  Precision of the Diversity Index, expressed as the 95% upper and lower boundaries.</p><p><b>K</b> =  Number of different repeats present at this locus in this sample set.</p><p><b>Max(pi)</b>  =  Fraction of samples that demonstrate the most frequent repeat number at this locus (range: 0.0 to 1.0).</p><p>*V is the abbreviation for VNTR.</p><p>Main characteristics of the selected VNTR loci in <i>N. meningitidis</i> strains.</p