High-dose modified-release formulation of a poorly soluble drug via twin-screw melt coating and granulation.

Favipiravir, a high dose antiviral drug effective for oral treatment for COVID-19, with poor water solubility is formulated using a simple, low-cost melt coating and granulation methodology. High-dose (82.5 % w/w API) tablets (600 mg and 800 mg) with desired release profiles are developed while minimizing excipient burden.

Statistical data treatment for residence time distribution studies in pharmaceutical manufacturing.

Residence time distribution (RTD) method has been widely used in the pharmaceutical manufacturing for understanding powder dynamics within unit operations and continuous integrated manufacturing lines. The dynamics thus captured is then used to develop predictive models for unit operations and important RTD-based applications ensuring product quality assurance. Despite thorough efforts in tracer selection, data acquisition, and calibration model development to obtain tracer concentration profiles for RTD studies, there can exist significant noise in these profiles.

Palladium-Catalyzed Direct C-H Glycosylation of Free (-H) Indole and Tryptophan by Norbornene-Mediated Regioselective C-H Activation.

We describe the palladium-catalyzed direct C-H glycosylation of free -H indole or tryptophan for the stereoselective synthesis of 2-glycosylindoles and tryptophan--glycosides. This reaction relies on the -directing transient mediator norbornene, which underwent regioselective C-H functionalization at the indole or tryptophan ring, providing high chemoselectivity. This method offers a more straightforward, step-economical, and cost-effective route to construct -glycosides.

Homogeneous distribution of phosphor particles inside resin using a vertical vibration method for efficient laser-based white light illumination.

We report what we believe to be an innovative method for the homogeneous distribution of phosphor particles inside the optical resin-based layer using a vertical vibrational technique for efficient laser-based white light illumination. In this method, single-stage vibration energy was efficiently used against phosphor sedimentation with the help of a mechanical vibrator system. The vertical vibrational energy was transferred to negate the downward gravitational effect acting on each phosphor particle.

Tris(pentafluorophenyl)borane-Catalyzed Stereoselective -Glycosylation of Indoles with Glycosyl Trichloroacetimidates: Access to 3-Indolyl--glycosides.

An efficient and highly regioselective method for the synthesis of 3-indolyl--glycosides has been developed through coupling of glycosyl trichloroacetimidates with a wide range of substituted indoles in the presence of catalytic amounts of B(CF) within a few minutes. This methodology has a wide scope of substrates under mild reaction conditions and provides exclusively β-stereoselective 3-indolyl--glycosides in 64-87% yields.

Intramolecular 6-- Post-Ugi Cyclization of N-Substituted 2-Alkynamides: Direct Access to Functionalized Morpholinone Glycoconjugates.

We herein report a chemo- and regioselective 6- catalytic cyclization of Ugi adducts N-substituted 2-alkynamides to access functionalized morpholinone glycoconjugates in the presence of triphenylphosphine. This array allows an interesting multicomponent access to a library of functionalized morpholinone glycoconjugates under mild reaction conditions with regeneration of catalyst triphenylphosphine, supported by P nuclear magnetic resonance studies. Density functional theory shows the 6- oxocyclization pathway is preferred, which supports our experimental observation.

The strategic use of para-quinone methides to access synthetically challenging and chemoselective α,α'-diarylmethyl N-glycosides from unprotected carbohydrate amines.

Reported herein is a practical route to access synthetically challenging and chemoselective α,α'-diarylmethyl N-glycosides via Sc(OTf)3-catalyzed 1,6-conjugate addition of amino sugars with para-quinone methides (p-QMs). The reactions proceed smoothly without a base and under mild reaction conditions with a broad substrate scope and moderate to good yields.

An eco-friendly N-benzoylglycine/thiourea cooperative catalyzed stereoselective synthesis of β-L-rhamnopyranosides.

A new practical utility for β-stereoselective L-rhamnopyranosylations are conducted using rhamnosyl trichloroacetimidate donors in the presence of N-benzoylglycine/thiourea cooperative catalysis. This method represents the first instance where amino acid derivative N-benzoylglycine is used as a catalyst for β-L-rhamnopyranosylations. This method represents the first instance where environmentally benign amino acid derivative, such as N-benzoylglycine which is reported as less toxic and can be used as efficient catalyst for smooth transformation under eco friendly conditions.

Laser-line-driven phosphor-converted extended white light source with uniform illumination.

We report the development of laser-driven extended white light source designed as a light sheet for general illumination. This light sheet is made of two large diffused glass plates. A Ce:YAG phosphor layer was coated and sandwiched between the two diffusing sheets.

Synthesis of Structurally Diverse Substituted Aziridinyl Glycoconjugates via Base-Mediated One-Pot Post-Ugi Cyclization.

The base-promoted intramolecular cyclization of Ugi-azide adduct has been demonstrated for the synthesis of highly substituted aziridinyl glycoconjugates in one pot. The reactions are scalable and efficient and have an operationally simple broad substrate scope. To gain insight into the mechanism of aziridine formation, DFT and control experiments show that the cyclization of the aziridine glycoconjugate pathway was preferred, as it proceeds with a low activation energy barrier (0.

Improvement of tablet coating uniformity using a quality by design approach.

A combination of analytical and statistical methods is used to improve a tablet coating process guided by quality by design (QbD) principles. A solid dosage form product was found to intermittently exhibit bad taste. A suspected cause was the variability in coating thickness which could lead to the subject tasting the active ingredient in some tablets.