Briefly stated, the operating depth of field for a bar code scanner, preferably a laser scanner, is increased by placing a cubic phase mask (CPM) in the scanning beam. The masked beam is then scanned and reflected off a bar code and received by a photodetector. The received signal is then processed to recover the original unperturbed representation of the bar code pattern. The processed signal has an increased depth of field over an unmasked scanner signal.

Method and apparatus for extending operating range of bar code scanner

Berberine (Ber) and its main metabolites were identified and quantified using liquid chromatography/electrospray ionization/ion trap mass spectrometry. Rat plasma contained the main metabolites, berberrubine, thalifendine, demethyleneberberine, and jatrorrhizine, as free and glucuronide conjugates after p.o. Ber administration. Moreover, the original drug, the four main metabolites, and their glucuronide conjugates were all detected in liver tissues after 0.5 h and in bile samples 1 h after p.o. Ber administration. Therefore, the metabolic site seemed to be the liver, and the metabolites and conjugates were evidently excreted into the duodenum as bile. The pharmacokinetics of Ber and the four metabolites were determined in conventional and pseudo germ-free rats (treated with antibiotics) after p.o. administration with 40 mg/kg Ber. The AUC0-limt and mean transit time values of the metabolites significantly differed between conventional and pseudo germ-free rats. The amounts of metabolites were remarkably reduced in the pseudo germ-free rats, whereas levels of Ber did not obviously differ between the two groups. The intestinal flora did not exert significant metabolic activity against Ber and its metabolites, but it played a significant role in the enterohepatic circulation of metabolites. In this sense, the liver and intestinal bacteria participate in the metabolism and disposition of Ber in vivo.

https://dmd.aspetjournals.org/content/dmd/early/2006/09/06/dmd.106.011361.full.pdf

Pharmacokinetics of Berberine and Its Main Metabolites in Conventional and Pseudo Germ-Free Rats Determined by Liquid Chromatography/Ion Trap Mass Spectrometry

The objective of the present research was to evaluate the physicochemical characteristics of berberine chloride and to assess the complexation of drug with 2-hydroxypropyl-β-cyclodextrin (HPβCD), a first step towards solution dosage form development. The parameters such as log P value were determined experimentally and compared with predicted values. The pH-dependent aqueous solubility and stability were investigated following standard protocols at 25°C and 37°C. Drug solubility enhancement was attempted utilizing both surfactants and cyclodextrins (CDs), and the drug/CD complexation was studied employing various techniques such as differential scanning calorimetry, Fourier transform infrared, nuclear magnetic resonance, and scanning electron microscopy. The experimental log P value suggested that the compound is fairly hydrophilic. Berberine chloride was found to be very stable up to 6 months at all pH and temperature conditions tested. Aqueous solubility of the drug was temperature dependent and exhibited highest solubility of 4.05 ± 0.09 mM in phosphate buffer (pH 7.0) at 25°C, demonstrating the effect of buffer salts on drug solubility. Decreased drug solubility was observed with increasing concentrations of ionic surfactants such as sodium lauryl sulfate and cetyl trimethyl ammonium bromide. Phase solubility studies demonstrated the formation of berberine chloride–HPβCD inclusion complex with 1:1 stoichiometry, and the aqueous solubility of the drug improved almost 4.5-fold in the presence of 20% HPβCD. The complexation efficiency values indicated that the drug has at least threefold greater affinity for hydroxypropyl-β-CD compared to randomly methylated-β-CD. The characterization techniques confirmed inclusion complex formation between berberine chloride and HPβCD and demonstrated the feasibility of developing an oral solution dosage form of the drug.

/pdf/physicochemical-characterization-of-berberine-chloride-a-222och7fjj.pdf

Physicochemical Characterization of Berberine Chloride: A Perspective in the Development of a Solution Dosage Form for Oral Delivery

https://iplab.ust.hk/pdf/Reviews%20pdf/2015_07%20NeurochemInt.pdf

Plant alkaloids as drug leads for Alzheimer's disease.

Iodine as a catalyst for efficient conversion of ketones to gem-dihydroperoxides by aqueous hydrogen peroxide.

Among 42 extracts, prepared from 14 medicinal plants used in Vietnamese traditional medicine to treat malaria, 24 were found to have antiplasmodial activity by inhibiting the growth of the chloroquine-resistant Plasmodium falciparumstrain FCR-3 with EC50 values less than 10g/ml. Each medicinal plant possessed at least one active extract. The methanol extract of Coscinium fenestratumhad the strongest antiplasmodial activity with EC50 value of 0.5g/ml. Activity-guided fractionation led to identification of berberine as the major active constituent.

Short communication In vitro antiplasmodial activity of antimalarial medicinal plants used in Vietnamese traditional medicine

Ozonolysis of vinyl ethers 1a–c in the presence of hydrogen peroxide in diethyl ether gave the corresponding 1,1-bis(hydroperoxide)s 2a–c. Subsequent trimethylsilylation, followed by the TMSOTf-catalyzed cyclocondensation with carbonyl compounds gave the unsymmetrically-substituted 1,2,4,5-tetroxanes 5–14. Similarly, the 1,2,4,5,7-pentoxocanes 18, 19 were prepared by the reaction of an α,α′-bis(trimethylsilylperoxy) ether 17 and carbonyl compounds. The tetroxane 14 showed notable antimalarial activity in vitro and in vivo.

Synthetic methods for unsymmetrically-substituted 1,2,4,5-tetroxanes and of 1,2,4,5,7-pentoxocanes

In this short review the methods of preparation of novel 1,2,4,5-tetraoxacycloalkanes and the related peroxides are summarized, with the emphasis on the usefulness of 1,1-bishydroperoxides as the precursor. Also, their antimalarial activities in vitro and in vivo are discussed.

1,2,4,5-Tetraoxacycloalkanes: synthesis and antimalarial activity.

Febrifugine represented by formula (A) and isofebrifugine represented by formula (B), having an extremely potent activity on Plasmodium falciparum; and total synthesis routes permitting efficient mass production of both.

Yusuke Wataya

Papers

Short communication In vitro antiplasmodial activity of antimalarial medicinal plants used in Vietnamese traditional medicine

Synthetic methods for unsymmetrically-substituted 1,2,4,5-tetroxanes and of 1,2,4,5,7-pentoxocanes

1,2,4,5-Tetraoxacycloalkanes: synthesis and antimalarial activity.

Febrifugine and isofebrifugine and processes for the preparation of both

Synthetic Methods for Unsymmetrically‐Substituted 1,2,4,5‐Tetroxanes and of 1,2,4,5,7‐Pentoxocanes.