Objective: The aim of the study was to determine the content of polyphenols and flavonoids from sixteen selected medicinal plants from the spontaneous Romanian flora and fifteen tinctures obtained with propylene glycol.
Methods: The polyphenols were determined by the Folin-Ciocalteu method while the flavonoids by using a colorimetric method from the 10th edition of the Romanian Pharmacopoeia. The antioxidant activities of the most common nine medicinal plants and fifteen tinctures were determined by DPPH and ABTS methods.
Results: The results highlighted that the phenolic compounds and flavonoids have contributed to their antioxidant activities and the medicinal plants and tinctures included in the study are rich sources of natural antioxidants.
Conclusions: There are a wide variety of extraction methods for the determination of phenolics and flavonoids. The study confirms a correlation between phenolic and flavonoid contents obtained by using the DPPH and ABTS tests.
Objective: Analgesic medicines containing combinations of nonsteroidal anti-inflammatory drugs and codeine are available without prescription. Codeine, in these combinations can not be used recreationally due to the high toxicity profile of the nonsteroidal anti-inflammatory drugs. However, methods for extracting codeine from these types of medication are available on the internet. The purpose of this work is to evaluate if codeine can be extracted from codeine containing analgesics sold without prescription.
Methods: High Performance Liquid Chromatography (HPLC) with UV detection was used to measure the amounts of codeine and nonsteroidal anti-inflammatory drugs recovered after applying an extraction method described on the internet.
Results: The results show that codeine can be very easily separated from NSAID as aspirin, acetaminophen, ibuprofen using the cold water extraction method. However, very large differences (20 to 90%) were recorded for the recovery of codeine depending on the OTC product that was used. That large difference increases the risk of potentially lethal overdoses when the user switches between “similar” products.
Conclusions: Our work shows that analgesic medication with codeine content can be recreationally used after the extraction of codeine. In order to prevent this, the sell of this type of products should be regulated or products that do not allow the extraction of codeine should be developed.
Prodrugs are chemically modified derivatives introduced in therapy due to their advantageous physico-chemical properties (greater stability, improved solubility, increased permeability), used in inactive form. Biological effect is exerted by the active derivatives formed in organism through chemical transformation (biotransformation). Currently, 10% of pharmaceutical products are used as prodrugs, nearly half of them being converted to active form by hydrolysis, mainly by ester hydrolysis. The use of prodrugs aims to improve the bioavailability of compounds in order to resolve some unfavorable characteristics and to reduce first-pass metabolism. Other objectives are to increase drug absorption, to extend duration of action or to achieve a better tissue/organ selective transport in case of non-oral drug delivery forms. Prodrugs can be characterized by chemical structure, activation mechanism or through the presence of certain functional groups suitable for their preparation. Currently we distinguish in therapy traditional prodrugs prepared by chemical derivatisation, bioprecursors and targeted delivery systems. The present article is a review regarding the introduction and applications of prodrug design in various areas of drug development.
Objective: the number of alkaloids like morphine and codeine found in poppy seeds used in food industry are monitored by a directive given by European Food Safety Authority. Based on this regulation the aim of the study was to determine the quantity of morphine and codeine from several brands of poppy seeds. Methods: an HPLC-UV method (205 nm) was developed to measure the quantity of morphine and codeine. Sample preparation was made using recipes posted on Drugs Forum by some users. Limits of detection were not determined because the lowest concentration from the reference (0.1 μg/ml) detected morphine concentrations that are far lower than a limit of toxicological concern. Results: The concentrations, which were found, ranged between Below the Level of Toxicological Concern (BLTC) - 243.26 mg/kg for morphine and BLTC - 88.58 mg/kg for codeine using several methods of preparation. Conclusions: one can observe that there are some brands of poppy seeds which do not respect the regulation about the amount of morphine and codeine. The high amount of morphine in some samples suggests that there are different varieties of poppy seeds, which can be used for an illicit purpose and can lead to addiction or even overdose in some cases.
A 62 year-old caucasian male was admitted in our pulmonary hypertension expert center with initial diagnosis of pulmonary veno-occlusive disease for validation and specific treatment approach. Routine examinations revealed no apparent cause of pulmonary hypertension. Patient was referred for a thorax contrast enhanced multi-slice computed tomography which revealed extensive bilateral thrombi in pulmonary lower lobe arteries, pleading for chronic post embolic lesions. A right heart catheterization and pulmonary angiography confirmed the diagnosis of chronic thromboembolic pulmonary hypertension (CTEPH). Following the local regulations, the patient underwent thrombophilia screening including molecular genetic testing, with positive findings for heterozygous for VCORK1 -1639G>A gene single nucleotide polymorphism, PAI-1 4G/5G and factor II G20210A gene. With heterozygous genetic profile of 3 mutations he has a genetic predisposition for developing a thrombophilic disease which could be involved in the etiology of CTEPH. Familial screening was extended to descendants; the unique son was tested with positive results for the same three genes. Supportive pulmonary hypertension drug therapy was initiated together with patient self-monitoring management of oral anticoagulation therapy. For optimal control of targeted anticoagulation due to a very high risk of thrombotic state the patient used a point-of-care device (CoaguChek®XS System, Roche Diagnostics) for coagulation self-monitoring.