Publisher SummaryOrganic impurities, often called related, ordinary or synthesis-related impurities can originate from various sources and from various phases of the synthesis of bulk drugs and the preparation of pharmaceutical dosage forms. A sharp differentiation between synthesis-related or p...

The degradation pattern of hydrocortisone in aqueous solution was investigated utilizing an HPLC procedure capable of separating and quantitating hydrocortisone and its major degradation products. The product distribution was characterized qualitatively and quantitatively as a function of pH in ...

Hydrocortisone pretreatment of male rats daily for five days (2 or 10 mg/kg, s.c.) had no significant effect on the total inactivation of prostaglandin E2 in isolated perfused rat lungs or on the activity of NAD+-dependent 15-hydroxyprostaglandin dehydrogenase in the 100.000 × g supernatant fra...

A new stability indicating reversed phase high performance liquid chromatography (RP-HPLC) method was developed and validated under current International Conference of Harmonisation (ICH) guidance for the determination of prednisolone acetate (PAC) and impurities in an ophthalmic suspension. The...

The influence of hydroxypropyl methylcellulose (HPMC), methylcellulose (MC), polyvinyl pyrrolidone (PVP) and polyethylene glycol (PEG400) on the crystallization of hydrocortisone acetate (HA) was studied. Supersaturation was created by the cosolvent technique. Spontaneous nucleation was observed...

The crystal morphology of zinc lactate trihydrate in the absence or presence of impurities (viz. succinic acid, L-malic acid and D-malic acid) is investigated by molecular simulation based on surface docking model and COMPASS force field. Combing simulation results with our previous experimental...

In this work, the possibility of bottom-up creation of a relatively stable aqueous hydrocortisone nanosuspension using microfluidic reactors was examined. The first part of the work involved a study of the parameters of the microfluidic precipitation process that affect the size of generated dru...

Hydrocortisone degradation products 1, 2, 3, and 4 along with hemiacetal derivatives 5, 6, 7, and 8 were observed through stressed hydrocortisone in solution. Their structures were identified based on HPLC-UV, HPLC–MS, and HPLC-HRMS (high resolution/high accuracy mass spectrometry) analyses as ...

Hydrocortisone, the endogenously expressed steroidal, hormonal ligand for glucocorticoid receptor (GR), is body's natural anti-inflammatory and xenobiotic metabolizing agent. It has both palliative as well as adverse effects in different cancer patients. Herein, we show that conjugation pro...

The chemo- and stereoselectivity in reactions with E and Z isomers of ethyl 3-[(S)-2,2-dimethyl-1,3-dioxolan-4-yl]acrylate, 1 and 2, are strongly dependent on the composition of the organocopper reagent. Synthetically useful yields and stereoselectivities are obtained with reagents of good nucle...

Hydrogenation of 1-benzyl-aziridine-2-carboxylic acid ethyl ester 1 yielded the enantiomerically pure 1H-aziridine 2 or the β-amino acid ester 3 as main products depending on the reaction time. The Z-protected derivatives of 2 and 3 were transformed into the γ-lactones 4 and 5, respectively.

The reactions of chiral 3-(2,2-dimethyl-1,3-dioxolan-4-yl)-2-propenoate esters 2–5 with NsONHCO2Et and CaO, produce the aziridine derivatives by addition of (ethoxycarbonyl)amino group on the double bond. The stereoselectivity is good for trans substrates. Products are precursors to polyhydroxy...

Carboxyacyl derivatives of phosphatidylethanolamine with different chain length were synthesized. These compounds were generally prepared by conversion of an appropriate dicarboxylic acid to its anhydride with dicyclohexylcarbodiimide, then reaction with phosphatidylethanolamine (PE) and triethy...

5-Iodotbercidin (Itu) and proglycosyn (Pro) have similar glycogenic properties. To compare their mechanisms of action, we tested them in hepatocytes from fasted rats. We show that both compounds are similar in that they stimulated glycogen synthesis, increased the concentration of synthase a, de...

Proglycosyn (LY177507) belongs to a series of powerful agents that stabilize liver glycogen stores by promoting glycogen synthesis from different precursors and inhibiting glycogenolysis and glycolysis. In the present study we have examined the effects of proglycosyn on fatty acid metabolism in ...

Proglycosyn, a phenylacyl imidazolium compound that lowers blood glucose levels, was demonstrated previously to promote hepatic glycogen synthesis, stabilize hepatic glycogen stores, activate glycogen synthase, inactivate glycogen phosphorylase, and inhibit glycolysis. In the present study progl...

Key factors in C 1s photoelectron spectroscopy for realistic samples of single crystal diamonds are remarked. Basic equations for angle-dependent photoelectron spectroscopy applied to single crystal diamond samples are described in Appendix A. Carbon 1s photoelectron spectroscopic works so far r...

A novel side-chain-sulfonated aromatic diamine of bis[4-(4-aminophenoxy)-2-(3-sulfobenzoyl)]phenyl sulfone (BAPSBPS) was synthesized. Sulfonated copolyimides were synthesized by random and sequenced block copolymerization of 1,4,5,8-naphthalene tetracarboxylic dianhydride, BAPSBPS and nonsulfona...

A new kind of pyridine-containing aromatic diamine monomer, 4-phenyl-2, 6-bis [3-(4-aminophenoxy)phenyl]-pyridine(m-PAPP),was synthesized by a modified Chichibabin reaction of benzaldehyde and a substituted acetophenone, 3-(4-nitrophenoxy)-acetophenone(m-NPAP), and a reduction of the resulting d...

A new series of thermoplastic polyimides derived from 2,2-dimethyl-1,3-bis(4-aminophenoxy)propane (MD) and a new diamine 2-methyl-2-propyl-1,3-bis(4-aminophenoxy)propane (MPPD) have been prepared and characterized. These materials were selected on the basis of their potential to serve as low-cos...