In vivo pharmacodynamic and pharmacokinetic interactions of Hibiscus sabdariffa calyces extracts with simvastatin.

WHAT IS KNOWN AND OBJECTIVES: Increasing number of patients use herbs with their medications. Such practice may result in beneficial or harmful herb-drug interactions. A recent survey reported that some participants co-administered Hibiscus sabdariffa, a widely used beverage, or tea, with their antihyperlipidaemic medications. This study therefore evaluated the effect of concomitant administration of Hibiscus sabdariffa calyces' extracts with simvastatin on hyperlipidaemia and pharmacokinetics of the drug in vivo. METHODS: Factorial experimental designs were used to evaluate the comparative effectiveness and interactions between simvastatin and aqueous extract of Hibiscus sabdariffa (AEHS) on lipid profile parameters in hyperlipidaemia-induced Wistar rats. Different combinations of low (AEHS 250 mg/kg; simvastatin 10 mg/kg) and high doses (AEHS 500 mg/kg; simvastatin 20 mg/kg) were administered individually and concurrently daily for 2 and 4 weeks. Lipid profile parameters were assessed at these treatment periods. Subsequently, the effect of aqueous beverage of Hibiscus sabdariffa (ABHS) on the pharmacokinetics of single-dose 40 mg simvastatin was also evaluated in six healthy human volunteers using two-period randomized crossover design. Blood samples were collected at predetermined times for 24 hours. The plasma obtained was analysed for simvastatin using RP-HPLC/UV method. RESULTS: Aqueous extract of Hibiscus sabdariffa reduced total cholesterol (Tc ) better than simvastatin (P = .031). Low-dose AEHS and low-dose simvastatin used concomitantly caused 38.3% and 57.4% reductions in Tc and triglyceride levels, respectively, compared with low-dose simvastatin (P < .05). Also, ABHS increased clearance and reduced peak concentration of simvastatin by 44.6% and 18.0%, respectively (P < .05). The geometric mean ratio of simvastatin AUC0-∞ with or without ABHS was 0.646 with the 90% confidence interval (0.564, 0.758) falling outside the bioequivalent range. WHAT IS NEW AND CONCLUSION: Aqueous extract of Hibiscus sabdariffa lowered Tc better than simvastatin and enhanced the antihyperlipidaemic activity of the drug when co-administered at low doses in an animal model. However, aqueous beverage of Hibiscus sabdariffa caused a significant herb-drug interaction resulting in overall reduction in exposure to simvastatin in humans. Caution should thus be placed on clinical judgement or recommendations based on the animal results. Nevertheless, co-administration of the beverage with simvastatin should be discouraged until more clinical data are available.

Les étiologies des urgences obstétricales à la maternité du centre hospitalier universitaire départemental de l'Ouémé-plateau (CHUD O/P) au Bénin

Objectif : Décrire les étiologies des urgences obstétricales dans le service de gynécologie et d'obstétrique du Centre Hospitalier Universitaire Départemental de l'Ouémé-Plateau.Patientes et Méthodes : Il s'agissait d'une étude transversale, descriptive et analytique menée à la maternité du CHUD O/P sur une période de 06 mois allant de Février 2016 à Aout 2016. Les critères d'inclusion étaient constitués de toutes les patientes admises à la maternité du CHUD O/P et traitées pour des complications de la gravido-puerpéralité. N'étaient pas inclues les urgences non obstétricales.L'analyse et les tests statistiques ont été effectués sur les logiciels CS PRO 6.2 et SPSS en comparant les moyennes et les écarts, en utilisant le chi carré de Pearson pour les variables dichotomiques en acceptant une probabilité significative p0,05. Les considérations éthiques, la confidentialité et l'anonymat étaient respectés. Résultats et conclusion : La fréquence d'admission des urgences obstétricales était de 34,8%. L'âge moyen était de 27,3 +/- 5,7 ans. Elles étaient nullipares (31,4%), aux activités professionnelles peu rémunératrices (69,3%). La référence était dans 70,4% le mode d'admission mais inadéquate. Les causes retrouvées par ordre de fréquence, étaient : les dystocies (30,7%) ; les urgences hémorragiques (25,9%) ; les urgences hypertensives (21,5%) ; les hypoxies foetales (17,8%) et les infections 4,0%). La létalité maternelle et néonatale étaient respectivement de 3,8% et 11,5%.L'anticipation des SONU s'avère indispensable dans la prise en charge des urgences obstétricales

Physicochemical properties and biological evaluation of Yoyo bitters.

BACKGROUND: The current widespread distribution and use of Yoyo bitters; an herbal bitters made in Nigeria calls for an assessment of its content, efficacy and extent to which this product achieves the labelled claim of being an herbal cleanser. METHODS: The pH, analysis for trace metal and preliminary phytochemicals screening were assessed. In addition, the total phenolic acid content, antioxidant activity using DPPH inhibition and microbiological assay were evaluated using standard procedures. The biological effect of different doses on weight, blood glucose, haematological parameters, liver function and tissues pathology were investigated in healthy Wistar rats over a 28-day period. RESULTS: Yoyo bitters is a slightly acidic liquid (pH 5.46), containing 0.110 µg/L of zinc, little quantities of saponins, alkaloids, anthraquinones and cardenolides. Low total phenolic acid content (537.7 ± 22.38 mgGAE/mL), poor radical scavenging activity; DPPH IC50 of 855.27 ± 85.8 mg/mL compared with 1.27 ± 0.03 and 1.24 ± 0.02 mg/nL for gallic acid and ascorbic acid respectively. There was lack of antibacterial activity. The weight, blood glucose level and liver function were not affected, while only WBC and platelet levels were increased significantly (p = 0.003). Gut associated lymphoid tissues (GALT) was observed in the intestine as well as hepatic lesions with some of the treated groups. CONCLUSION: Yoyo bitters has a weak antioxidant activity, thus may not possess significant effect on the enhancement of general body health. It has immune-potentiating effect with the risk of development of hepatic degeneration.

Synergistic effect of aqueous extract of Telfaria occidentalis on the biological activities of artesunate in Plasmodium berghei infected mice.

BACKGROUND: Resistance to most antimalarial drugs has encouraged the use of herbal preparations along with prescribed orthodox drugs. OBJECTIVE: To investigate effect of co-administration of aqueous extract of T. occidentalis leaves; commonly used as antimalarial and haematinic agent in Nigeria and artesunate using P. berghei animal model. METHODS: In vivo curative antiplasmodial effect of T. occidentalis (200mg/kg) alone and combination with artesunate (2mg/kg) were evaluated using albino mice infected with 10(6) parasitized erythrocytes of P. berghei intraperitoneally. The haematological parameters: haemoglobin level, red blood cells and white blood cells and packed cell volume were monitored using standard methods. RESULTS: Aqueous extract of T. occidentalis, artesunate and the combination gave 72.17±4.07%, 70.43± 4.27% and 85.43±3.65% reduction in parasitaemia after 48hours respectively. A significant enhancement of the PCV was obtained with the coadministration of artesunate and aqueous extract (p< 0.01). Similar trends were also observed with heamatological parameters at 72hours of administration. CONCLUSION: This study revealed a synergistic effect of the co-administration on parasite clearance rate of P. berghei infection in mice, with a significant enhancement of haematological parameters within 48 hours of administration. This indicates a rapid rate of recovery from plasmodial infections with the co-administration.

Evaluation of the physicochemical equivalence of three brands of commercially available quinine sulphate tablets from South Western part of Nigeria.

BACKGROUND: The relatively little resistance to quinine globally has led to an increase in its use in P. falciparum malaria especially in multi-drug resistant strains. OBJECTIVE: To evaluate the physicochemical and equivalency of three brands of quinine sulphate tablets available in South Western region of Nigeria. METHODS: The pharmaceutical and chemical equivalence of three brands of quinine sulphate tablets were assessed through the evaluation of some biopharmaceutical parameters and active drug content. RESULTS: All the brands complied with the official specification for uniformity of weight. Two of the brands (A & B) gave similar crushing strengths while the third brand (C) gave a much lower value. Similarly all the brands complied with the official specification of disintegration test but the obtained values were statistically different (p<0.05). The T(70) obtained from the dissolution rate profile was less than 45 minutes for the three brands, although A and B were not statistically different but C was statistically from A and B. The quinine content of brands B and C are within the official specification however brand A with percentage content of 110±1.3%w/w, is above the specification while it is statistically different from the other brands. CONCLUSION: Brands B and C could be regarded as chemical equivalent, but they are not biopharmaceutical equivalents, on the other hand, brands A and B may be regarded as biopharmaceutical equivalents but not chemical equivalent.

Evaluation of the physicochemical equivalence of three brands of commercially available quinine sulphate tablets from South Western part of Nigeria

BACKGROUND:The relatively little resistance to quinine globally has led to an increase in its use in P. falciparum malaria especially in multi-drug resistant strains.OBJECTIVE:To evaluate the physicochemical and equivalency of three brands of quinine sulphate tablets available in South Western region of Nigeria.METHODS:The pharmaceutical and chemical equivalence of three brands of quinine sulphate tablets were assessed through the evaluation of some biopharmaceutical parameters and active drug content. RESULTS:All the brands complied with the official specification for uniformity of weight. Two of the brands (A & B) gave similar crushing strengths while the third brand (C) gave a much lower value. Similarly all the brands complied with the official specification of disintegration test but the obtained values were statistically different (p<0.05). The T(70) obtained from the dissolution rate profile was less than 45 minutes for the three brands, although A and B were not statistically different but C was statistically from A and B. The quinine content of brands B and C are within the official specification however brand A with percentage content of 110±1.3%w/w, is above the specification while it is statistically different from the other brands. CONCLUSION:Brands B and C could be regarded as chemical equivalent, but they are not biopharmaceutical equivalents, on the other hand, brands A and B may be regarded as biopharmaceutical equivalents but not chemical equivalent

Physicochemical equivalence evaluation of some piroxicam capsule brands in Nigeria.

Comparative chemical and pharmaceutical equivalence study on ten brands of piroxicam capsules was carried out. The aim of the study was to determine whether the brands are comparable with each other on the basis of their physico-chemical properties. The chemical and pharmaceutical equivalences of ten brands of piroxicam capsules were assessed by evaluating the uniformity of weight, dissolution rate, content identification and the chemical assay of the capsules. All the ten brands complied with British Pharmacopoiea standard for uniformity of weight. The thin layer chromatographic test for content identification showed that nine of the brands contain only piroxicam while one brand contains an additional compound apart from the labeled piroxicam. The ultraviolet procedure for content identification showed that only two brands complied with the official specification. Five brands complied with specification for the content assay of the active ingredient. However, only two brands complied with the official specification of 70% w/v dissolution at 45 minutes. The result obtained from this study showed that only the innovator brand meets all the specifications. Moreover, only five of the other brands can be regarded as chemical equivalent of the innovator. The result obtained in this study underscores the need for registration and post market surveillance of products circulating in the drug market.

Additive effects of ciprofloxacin on the in-vitro activity of chloroquine against a clinical isolate of Plasmodium falciparum.

As chloroquine and ciprofloxacin each possess substantial inhibitory activity against the schizonts of Plasmodium falciparum, it seems possible that a combination of the two drugs may be clinically useful. The effects on the erythrocytic stages of P. falciparum of combined treatment with chloroquine and ciprofloxacin were therefore evaluated in vitro, using the World Health Organization's standardized micro test. When used alone, the median inhibitory concentration (IC(50)) of chloroquine against the schizonts in the assay mixtures was found to be 7.75 microg/ml, whereas the corresponding value for ciprofloxacin was markedly lower, at 3.35 microg/ml. When they were used together, however, there was marked and statistically significant mutual enhancement of schizont inhibition by the two drugs, indicating that a chloroquine-ciprofloxacin combination may be useful clinically, in the treatment and management of P. falciparum malaria.

Comparative determination of halofantrine tablets by titrimetry, spectrophotometry and liquid chromatography.

Comparative determination of halofantrine tablets by titrimetry, ultraviolet spectrophotometry and liquid chromatography (LC) is described. Non-aqueous titrimetry on halofantrine hydrochloride tablets was carried out using glacial acetic acid as solvent, perchloric acid as titrant and crystal violet as indicator. Simultaneous potentiometric monitoring of end point delineated an exact color shade of indicator at the end point. Direct measurement of methanol solution, at 254 nm, was adopted for UV spectrophotometric method while reversed-phase liquid chromatographic (LC) method employed a C8 column (4.6 mm x 25 cm) with mobile phase consisting of methanol / 0.05 M NaH2PO4 (76:24, v/v) containing 55 mmol/L perchloric acid (pH 3.4) at a flow rate of 1 ml / min. The three methods gave precise and accurate results. Mean percentage recovery were obtained respectively as 100.73 +/- 0.41, 100.36 +/- 0.79 and 99.93 +/- 3.74% while coefficient of variation were 0.41, 1.36 and 3.74% for non-aqueous. UV spectrophotometry and LC. The three methods were successfully applied to analysis of halofantrine tablets (Halfan) and showed no statistically significant difference in accuracy (P > 0.05, ANOVA). Validated assay methods for halofantrine tablets have been developed. The titrimetric and spectrophotometric methods are of equivalent accuracy with the liquid chromatographic method and could be used for routine quality control of halofantrine tablets where LC method is not readily available.