West African Journal of Pharmacology and Drug Research

Pharmacokinetic evaluation of aqueous solution of enrofloxacin after single intramuscular injection in layers

2021-12-06T14:40:44+00:00

The effective use of enrofloxacin (ENX) in control of bacterial diseases of commercial egg layers is dependent on knowledge of pharmacokinetics (PK) and use of appropriate drug dosage formulation that guarantee sustainable and adequate drug delivery. This study aside from determining PK indices of aqueous ENX preparation administered to hens intramuscularly will also investigate the capacity of this dosage formulation in delivering therapeutic and sustainable serum drug levels against common pathogenic bacteria of chickens in our environment. A total of 108 hens assigned to 3 groups of 36 birds each were administered with 10mg/kg aqueous ENX intramuscularly. A parallel sampling technique involving one blood draw from each bird at each of the 12 time points was used. Therefore 3 birds were sampled at each time point. This was repeated in each of the experimental groups. The serum ENX concentration was determined using enzyme linked immuno-sorbent assay (ELISA). The peak serum concentration (Cmax), time to achieve peak serum concentration (Tmax), area under curve _0-24hrs (AUC), area under the first moment curve (AUMC), clearance (CL), volume of distribution (V_D), mean residence time (MRT) and elimination half-life (t_1/2) were obtained from Non-compartmental analysis of concentration-time data. The Mean ± SEM of AUC, AUMC, CL, V_D, t_1/2, MRT, Cmax and T max were; 5.32 ± 0.10, 64.99 ± 2.15, 0.12 ± 0.03, 1.52 ± 0.25, 8.46 ± 0.92, 12.20 ± 0.34, 0.23±0.01, 6.12 ± 0.22 respectively. In conclusion, bolus intramuscular administration of aqueous ENX to hens is capable of achieving therapeutic and sustainable drug concentrations against highly sensitive pathogenic bacteria. This formulation may prove useful in chemoprophylaxis but not in treating acute bacterial infections.

Xylopia aethiopica (Annonaceae) seeds enhance male reproductive functions during ethanol-induced oxidative conditions in adult Wistar rats

2021-12-09T14:03:59+00:00

Prolonged alcohol intake exerts damaging effects on the functions of male reproductive organs. This study was designed to investigate the activities of Xylopia aethiopica aqueous seed extract (XA) on oxidative states in male reproductive organ of adult rats exposed to ethanol (30 % v/v) orally for 14 days. The phyto-components were extracted via cold maceration in distilled water for 72h. After 14 days of everyday treatment with an oral dose of 300 mg/kg/p.o with ethanol (30 % v/v), and 10% Tween 80 as controls, the effects of XA on antioxidant enzymes, hematological profile, and semen were examined. Results revealed that XA significantly elevated the concentrations of catalase (CAT) (p < 0.0001) in normal rats; whereas in oxidative state, it increased both CAT (p < 0.001) and superoxide dismutase (SOD) (p< 0.0001) levels and had negligible effect on malondialdehyde (MDA). Conversely, ethanol only raised the levels of MDA (p < 0.01). For hematological profiles, XA had negligible effects in normal condition however in ethanol-induced oxidative state, it significantly (p < 0.05) raised the percentages of granulocytes (GR) and hematocrit (HCT) but lowered significantly (p < 0.05) the level of lymphocytes (LY). For semen examination; XA had negligible effects on sperm pH and morphology, but significantly increased sperm concentration, count and motility (p < 0.05) respectively in oxidative state. These put forward that XA could have useful effects by preventing oxidative damage in male reproductive organs and enhance male reproductive functions which may well contribute in the treatment and management of male infertility.

Evaluation of phytochemical constituents and antimicrobial activity of Vernonia amygdalina leaf extracts

2021-12-08T12:55:30+00:00

Vernonia amygdalina is a shrub found in Nigeria, growing in backyard gardens and farmlands where it is popularly used as vegetable. The decoction has been used for bowel ailments and fresh cuts injuries. Aqueous, ethanolic, methanolic extracts of Vernonia amygdalina were examined for the phytochemical constituents and antimicrobial activities against Escherichia coli, Staphylococcus aureus, Klebsiella pneumoniae and Salmonella typhi. Leaf extracts of the plant contained glycosides, alkaloids, saponins and tannins. The minimum inhibitory concentration (MIC) of the extracts against the test organisms is in the range of 15mg/ml to 45mg/ml. MIC values of 15mg/ml, 20mg/ml, 30mg/ml and 35mg/ml were recorded against methanol extract when the extract was assayed against E. coli, S. aureus, K. pneumonia and S. typhi respectively. The results of this study suggests that extracts of Vernonia amygdalina could serve as a source of chemotherapeutic agent against the infections associated with Escherichia coli, Staphylococcus aureus, Klebsiella pneumoniae and Salmonella typhi.

Effect of Neocarya macrophylla root on Naja nigricollis venom

2021-12-08T13:04:24+00:00

Background and objective: Snake envenomation remain a public health problem, causing considerable morbidity and mortality especially in South Asia and sub-Saharan Africa. The study evaluated the antisnake venom activity of the methanol root extract, ethylacetate and n-butanol fractions of Neocarya macrophylla against Naja nigricollis venom.

Materials and Methods: The powdered plant material was macerated in 90% methanol and the extract was fractionated into n-hexane, chloroform, ethylacetate and n-butanol fractions. Preliminary phytochemical screening was conducted using standard procedures and acute toxicity was conducted according to Lorke's method. The antivenom studies was evaluated using both in vitro and in vivo studies in mice.

Results: The intraperitoneal LD₅₀ of the methanol root extract, ethylacetate and n-butanol fractions was found to be 118, 565 and 282 mg/kg, respectively. The extract and the two fractions exhibited significant in vitro antivenom activity with 100 % survival rate in mice. The extract and fractions were also able to inhibit the hydrolytic action of phospholipase A₂ enzyme activity. Minimal in vivo activity was observed for the methanol extract and ethylacetate fraction with 20 % survival rate and no protection was observed for the n-butanol fraction.

Conclusion: The results indicated that the root of Neocarya macrophylla possess antisnake venom activity thereby validating the ethnomedicinal claim of the use of the plant in the treatment of snakebite.

Validation of antihypertensive drug requirement to measure the severity of hypertension and the efficacy of lifestyle intervention

2021-12-08T15:12:47+00:00

Background/objective: The ongoing pandemic of non-communicable diseases, with systemic arterial hypertension at the forefront, mandates urgent attention to the aetiopathogenic mechanism rather than continuing to rely on suppressive drug therapies. Lifestyle interventions (such as diet, sleep and exercise) may have substantial impact on blood pressure control in hypertension. However this may not be evident in clinical trials of lifestyle intervention if the blood pressure was previously controlled by drugs. We therefore sought to develop an alternative method of measuring the impact of lifestyle intervention, rather than rely on blood pressure measurement alone.

Methods: The open trial of a personalized food avoidance dietary approach to stop hypertension was approved by the UNTH ethics committee. The Antihypertensive Drug Treatment Requirement (ADTR) score was calculated as the total number of defined unitary dosages of antihypertensive drugs times adherence +/- 0.1 accordingly for each mm Hg that average systolic pressure either exceeds 120 mm Hg (AOBP or home BP, whichever higher) or goes below 100 mm Hg Hg (AOBP or home BP, whichever lower). The dietary compliance score was based on the frequency of major/ minor dietary indiscretion (as per the PFADASH guidelines) i.e. less than (= GOOD) or more than (= POOR) once a month/ once a fortnight, respectively. Normality of data distribution was assessed by computing Shapiro-Wilk statistics. Cronbach's alpha reliability coefficient was used to assess internal consistency of ADTR measurements.

Results: Bi-quarterly Shapiro – Wilk statistics for AdhRx scores and ADTR scores showed more than 80% likelihood of being normally distributed at 5% significance level (i.e. 13 out of 16 data sets tested). Cronbach's alpha reliability coefficient was 0.980. This confirmed consistency of the ADTR measurement scale. For three study participants who improved to Good compliance (after dietary counseling) and four participants who failed to improve, Good compliance was associated with lower ADTR scores, but the differences between Good (mean ADTR of 1.07+0.82) and Poor (3.81+3.15) were not statistically significant (p = 0.210). For the three study participants who transited from Poor to Good compliance (in response to counseling), there was a high degree of negative correlation (i.e. decline of drug requirement) which was statistically significant in two of them (p<0.05). However, in the study participants who failed to improve their dietary compliance, there was a relative lack of correlation (with higher p values). The overall pattern is consistent with a negative association between dietary compliance and ADTR score.

Conclusion: We conclude that ADTR scores are useful and valid tools to assess the impact of dietary interventions which address the aetiopathogenic mechanism in essential hypertension. This enables differentiation between blood pressure lowering by drugs and that due to dietary intervention.

Toxicity study of DHFCOP-A, chemical derived from empty oil palm bunch ash in mice

2021-12-09T13:59:18+00:00

Background: Deseeded Fruit Head Chemical of the Oil Palm – Fractionate A (DFHCOP-A) an anhydrous chemical, has a remarkable high pH 12-14 hence an alkali. DFHCOP-A is commonly used to prepare food delicacies native to the South-East part of Nigeria. Reports has shown cancer thrives in low pH. Cancer aggressiveness has been linked to the acidic extracellular microenvironment of tumour. The high pH of DFHCOP-A may have potentials to inhibit cancer growth.

Objective: In this study we investigated the LD₅₀ of DFHCOP-A in mice which will suggest doses for subsequent studies on its effect on tumour microenvironment.

Methods: Two methods were used, Lorke's method and the up and down procedure (UDP). The tests were carried out in male and female mice which involved subcutaneous and oral administration. In the Lorke's method, female and male mice were divided in groups of three (n=3) for subcutaneous and oral administration. Varying doses 10mg/kg, 100mg/kg and 1000mg/kg were given. In the second phase, two groups (n=3), were administered 2000mg/kg and 5000mg/kg subcutaneously and Orally. For UDP, 5000mg/kg was administered subcutaneously (sc) to each male and female mouse in the limit test. In the main test, 7 and 12 male mice; 7 and 8 female mice were respectively treated subcutaneously and orally with up and down doses of 550mg/kg, 1750mg/kg, 2000mg/ and 5000mg/kg.

Results: By Lorke's method, LD₅₀ of 3,162mg/kg was obtained for both female and male mice by both routes. UDP estimated LD₅₀ is 2000mg/kg for female and LD₅₀ is greater than 2000mg/kg for male mice administered subcutaneously. LD50 for the orally administered female and male mice gave 5000mg/kg.

Conclusion: UDP appears better than Lorkes methods because it highlighted the differential sensitivities of the male and female mice to DFHCOP-A, where female mice are more sensitive which reflected in LD₅₀sc.