LIQUID CHROMATOGRAPHY TANDEM MASS SPECTROMETRY DETERMINATION METHOD OF BENCYCLOQUIDIUM BROMIDE: APPLICATION TO DRUG INTERACTION STUDY IN HUMAN

Objective: This study was conducted to develop a sensitive and effective LC-MS/MS method for the determination of bencycloquidium bromide (BCQB) and its application in pharmacokinetic drug interaction study between BCQB and paroxetine. Methods: The chromatographic separation was performed on Hedera ODS-2 C18 column with a mobile phase consisted of acetonitrile-10 mmol/l ammonium acetate containing 0.2% acetic acid (33:67, v/v) at 550 μl/min, and the plasma samples were processed using solid-phase extraction. The MS/MS transitions were m/z 330.2 → 142.0 for BCQB and m/z 344.2 → 156.1 for the I. S in positive ESI mode. Results: The validated method was linear over the concentration range of 2-1200 pg/ml with the correlation coefficient r2>0.998. The intra-and inter-batch precisions of the assay were lower than 8.2% and 9.1%, respectively. The lower limit of quantification (LLOQ) was 2 pg/ml. The stability data at different storage conditions of BCQB were within±5% RE. The mean AUC0-36 of BCQB was increased by approximately 33%, after the administration of BCQB alone and upon co-administration with paroxetine during the drug interaction study. Conclusion: The LC-MS/MS method validated in this study was robust, reproducible, accurate, precise and reliable and was successfully applied in the pharmacokinetic drug interaction studies

IDENTIFICATION AND QUANTIFICATION OF PHOSPHODIESTERASE-5 INHIBITOR AS FALSIFIED IN ‘‘NATURAL’’ MALAYSIAN HERBAL APHRODISIACS SOLD IN SOME BENINESE MARKETS

Objective: Nowadays, there have been several reports of herbal products falsified with well-known synthetic molecules, leading to harmful health consequences for the consumer. The aim of this study was to assess the profile of ‘natural' herbal aphrodisiacs in the local markets of the municipalities of Cotonou and Abomey-Calavi in Benin and to screen some of them for the presence of additives such as sildenafil and tadalafil. Methods: A non-probability survey was conducted to identify the available aphrodisiacs and their characteristics. Some of them were then selected for analysis. Thin Layer Chromatography (TLC) was adopted for qualitative detection. The TLC positive extracts were then analyzed by HPLC on a C18 column with a mobile phase consisting of a mixture of 0.05M phosphate buffer (pH 5.8), acetonitrile and methanol (30:50:20). The Detection was performed at 290 nm. Results: Seventy-seven aphrodisiacs were identified and from these, 18 were selected for analysis. Six of them were adulterated with tadalafil. The concentration of tadalafil in the samples was 1.7 to 4.6 times higher than the recommended dose of 20 mg. Conclusion: This work opens the door to the need to control ‘‘natural’’ labeled products in order to ensure their quality

Simple LC Isocratic Methods Development, Validation, and Application in the Analysis of Poor Quality Antimalarial Medicines

peer reviewedLiquid chromatographic methods in isocratic mode for the analysis of poor quality medicines are privileged due to their simplicity and facility in methods development. They are generally fast; do not need to be re-equilibrated between sample injections; have larger flexibility with acceptable changes on different column dimensions; and are applicable to LC systems equipped with simple or high developed pumps. In this study, we focused on developing simple isocratic methods using classical mobile phase composed by methanol and ammonium formate buffer for the analysis of most common antimalarial medicines marketed in malaria endemic countries and susceptible of being counterfeit/falsified, substandard and degraded. The selected medicines were quinine and related cinchona alkaloids in tablets and injectable forms; artemether/ lumefantrine tablets; and artemisinin compounds (arteether, artemether, and artesunate) in injectable forms. The current methods were developed thanks to simple methodological approach consisting in sequential isocratic runs through adjustment or adaptation of existing methods to obtain optimal analytical conditions without complex design of experiments that might be long and costly. Then, the new methods presented shorter analysis time; allowed increase of sample analysis throughput; and obviously consumed little mobile phase solvents on classical analytical columns: 50 - 250 mm of length (L), 4.6 mm of internal diameter (I.D.), and 3.5 - 5.0 μm of particle size (dp)

Quality assessment of three imidazole antiparasitics (albendazole, mebendazole and metronidazole) sold in Benin

peer reviewedIllicit circuit of medicines disrupts the quality assurance system and the rational use of medicines. Substandard and falsified (SF) medicines present a major risk for the public health, due to lack of active ingredient and/or toxicity of certain components. The purpose of this study was to evaluate the quality of three imidazole antiparasitic medicines (albendazole, mebendazole and metronidazole tablets) sold in Benin, to describe the different forms of non-compliances of the medicines sold in the illicit circuit. The samples were collected in the formal and illicit (informal) circuits. The results appeared as follows: irregularities of packaging (25.5% of samples from the illicit circuit); mass uniformity test (14.7% of samples from the illicit circuit were noncompliant); disintegration test (2.1% of samples from the illicit circuit and 3.5% from the formal circuit were non-compliant); identification (all samples were compliant) and assay (47.1% of samples from the informal circuit were non-compliant among which 26.5% of under-dosing and 20.6% of overdose). In sum, there were respectively 38.3% (i.e. 18/47) and 3.5% (i.e. 2/58) of non–compliance in the illicit and formal circuit

Identification et étude phytochimique de plantes utilisées dans le traitement traditionnel de l’ulcère de Buruli au Bénin

Le traitement traditionnel de l’ulcère de Buruli (UB) au Bénin se fait principalement à base de plantes. L’enquête ethnobotanique menée auprès de 17 tradipraticiens dans la commune de Ouinhi (département du Zou) a répertorié 49 plantes différentes utilisées pour traiter cette maladie. Deux de ces plantes présentent un fort taux d’utilisation : Erythrophleum suaveolens (Guill. et Perr.) Brenan et Strophanthus hispidus DC. L’étude phytochimique de dix-sept de ces plantes révèle la présence de grands groupes chimiques dont de nombreux composés possèdent diverses propriétés notamment anti-oedémateuses, anti-inflammatoires, antibactériennes, antiseptiques, sédatives, analgésiques, anesthésiques, cicatrisantes qui pourraient intervenir dans le traitement de l’UB. Des recherches complémentaires sont nécessaires pour identifier, isoler et purifier les composés de ces groupes chimiques présents dans les plantes et étudier leur place relative dans le traitement de l’UB

A comparative study of Caesalpinia bonduc (L.) Roxb. root extracts on sexual behaviour in male Wistar rats

International audienc

Antibiotic Usage in Patients Having Undergone Caesarean Section: A Three-Level Study in Benin

The intense use and misuse of antibiotics is undoubtedly the main factor associated with the high numbers of antibiotic-resistant pathogenic and commensal bacteria worldwide. In low-income countries, this misuse and overuse is widespread, with great consequences at the personal and global levels. In the context of user fee exemptions in caesarean sections, we performed a descriptive study in women to assess the use of antibiotics on three levels—antenatal, during caesarean section, and postpartum—in four Beninese hospitals. Out of the 141 women included, 56.7% were using antibiotics. More than the half (71.3%) were taking more than one antibiotic, either for a long time or in acute treatment. In prophylaxis, the timing, dose, and duration of administration were not correctly achieved. Only 31.2% of women received optimal antibiotic prophylaxis. Various antibiotics including broad-spectrum molecules were used in the patients after caesarean section. The use of antibiotics was improper on the three levels studied. The high rate of self-administered antibiotics, the poor achievement of antibiotic prophylaxis, and the postpartum overuse of antibiotics showed a poor quality of care provided in pregnancy. A national policy is essential to improve the use of antibiotics by the general public as well as by professionals

Formulation and Optimization of Matrix Tablets Based on Spirulina and Vitamin C

Spirulina is a type of algae widely consumed around the world as a dietary supplement due to its great nutritional potential. However, it does not contain vitamin C, a vital vitamin for the proper functioning of the human body, particularly given its immunostimulant potential. The objective of this work was to formulate sustained release spirulina–vitamin C matrix tablets that would enhance particularly a prolonged release and better absorption of vitamin C. A galenic formula based only on vitamin C was made, and then the proportion of vitamin C was reduced in favor of spirulina powder. The manufactured tablets were then subjected to various pharmacopeial quality control tests. The results of these tests showed a good distribution of the powder mixtures in the formulated tablets (i.e., mass uniformity test) and satisfactory outcomes were found for the content uniformity, disintegration and dissolution tests (with 45 % of vitamin C dissolved after 4 hours). Only the results for the friability test were unsatisfactory, indicating the need to improve the physical properties of the powders before compression. These findings open a new area for developing supplementary dietary.            Keywords: Spirulina, Vitamin C, Matrix tablet, Quality control

C42 - Optimisation d’une formule de comprime matriciel à base de spiruline enrichi en vitamine C

La spiruline est une algue fortement consommée dans le monde comme complément alimentaire en raison de son grand potentiel nutritionnel. Elle se trouve toutefois exempte de vitamine C, une vitamine capitale pour le bon fonctionnement de l’organisme humain compte tenu notamment de son pouvoir immunostimulant. L’objectif de notre travail était de formuler des comprimés matriciels de spiruline et de la vitamine C, qui assureront une libération prolongée et une meilleure absorption de la vitamine C ; cette dernière étant sujette à un mécanisme de saturation lors de son absorption. Nous sommes donc partis d’une formule galénique uniquement à base de vitamine C (A1), pour ensuite réduire la proportion de vitamine C au profit de la poudre de spiruline (S). Les comprimés fabriqués ont subi les différents tests pharmaco-techniques pour le contrôle de leur qualité. Les résultats de ce contrôle ont montré une bonne distribution des mélanges de poudres dans nos comprimés à l’issue du test d’uniformité de masse (A1 : 405±8,8 mg ; S : 665±9,4 mg), des résultats également satisfaisants pour les tests d’uniformité de teneur (A1 :175 ± 15,7 mg S : 41 ± 3,4 mg), de désagrégation (300 minutes) et de dissolution avec 45 % de la vitamine C dissoute au bout de 4 h de test (Comprimé S) contre 85% pour A1. Seul le test de friabilité était non satisfaisant témoignant la nécessité d’améliorer les propriétés physiques de nos poudres avant la compression. Ce travail sera approfondi en vue de l’installation sur place d’une unité de production desdits comprimés pour leur mise sur le marché.