Quality Control Tests on Andrographis paniculata Nees (Family: Acanthaceae) – an Indian ‘Wonder’ Plant Grown in Nigeria

Purpose: To characterize the aerial parts of Andrographis paniculata, a bitter Indian herb grown in Nigeria, for the purpose of quality control.Methods: The determination of bitterness value and of various physicochemical characteristics; tests for key phytochemicals; and thin layer chromatography (TLC) of the air-dried herb, were carried out as prescribed in standard texts. Results: The mean bitterness value of the herb for both men and women was 2.86 ± 1.74 x 103 unitsper g. The male value (2.07 ± 1.42 x 103) appeared to be lower than the female’s (3.52 ± 1.82 x 103) but the difference was not statistically significant. The results (% w/w) of loss on drying (10.64 ± 0.36), totalash (14.10 ± 4.49), water extractive value (30.37 ± 2.63) and acid insoluble ash (1.00 ± 0.06) were similar to those reported for the Asian plant. The phytochemical tests revealed the presence of glycosides, saponins, tannins and alkaloids, but not of anthraquinones. Normal phase TLC of the drug yielded 5 spots as against 6 spots yielded by reverse TLC. Conclusion: The results provide useful quantitative and descriptive data that are essential for identifying and characterizing the Nigerian grown herb for the purpose of quality control; and confirm keysimilarities between the Nigerian and the Asian plant.Keywords:  Andrographis paniculata, Quality control, Bitterness value, Physicochemical, Phytochemical, Chromatography

Rapid, cost-effective liquid chromatograghic method for the determination of metronidazole in biological fluids

A rapid and cost effective method for the analysis of metronidazole in biological samples was developed. The extraction method is a simple single-step liquid-liquid process that has eliminated the need for costly extraction and evaporation equipment. The mobile phase consists largely of water, making the method cheap to run with less than 6 min total analytical time per sample. The calibration curve was linear from 0 to 2.00 ìg/ml. The regression coefficient was 0.99. The method is highly sensitive, with limit of detection of 1 ng/ml. The coefficient of variation for within-day run was less than 4% while that of day-to-day run was less than 6%. There were no interfering peaks from endogenous materials in the serum. The method was validated and used for pharmacokinetic studie

The efficacy of urine data in comparative bioavailability of proguanil after oral and rectal administration in man

The bioavailability of proguanil formulated as suppository, was compared to the tablet formulation in a bid to evaluate the utility of the suppository dosage form as means of administering proguanil in children and high-risk groups, such as sickle cell patients, who may not tolerate oral route of administration. The study was a completely randomized cross over involving administration of 200 mg of proguanil suppository and tablet to twelve healthy volunteers. Biological fluids such as urine and blood were collected before and at predetermined time intervals following administration of the drug. The biological samples were analyzed for the unchanged proguanil using an earlier reported method. The relative bioavailability of proguanil suppository as compared to the tablet dosage form was found to be about 61% from both urine and plasma data. The findings showed for the first time that proguanil suppository could be sufficiently bioavailable and may therefore be useful in chemoprophylaxis of malaria in sickle cell patients and children, particularly under such conditions that made oral route become impracticable.Key words: Proguanil, tablets, suppositories, plasma and urine data, bioavailability

Sensitive high performance liquid chromatographic method for the determination of proguanil and its metabolites, cycloguanil and 4-chlorophenylbiguanide in biological fluids

A new simple, sensitive, cost-effective and reproducible high performance liquid chromatographic (HPLC) method for the determination of proguanil (PG) and its metabolites, cycloguanil (CG) and 4-chlorophenylbiguanide (4-CPB) in urine and plasma is described. The extraction procedure is a simple three-step process that has eliminated the need for costly extraction and evaporation equipment. The mobile phase consisted largely of buffer, making the method cheap to run. The calibration plots were linear over the concentration range up to 3.0 &#181g/ml PG, CG and 4-CPB in urine and concentration range up to 1000 ng/ml in plasma. The correlation coefficients (r) were of the order of 0.99 and above for PG and 4-CPB and 0.98 for CG. The ion pair method was carried out on a 5 &#181 reversed-phase C-18 column, using perchlorate ion as the counter ion and ultra violet detection at 254 nm. The method was reproducible with coefficient of variation for PG, CG and 4-CPB, being less than 10% in urine and plasma. PG was well resolved from its metabolites, CG and 4-CPB, and the internal standard, pyrimethamine. The limit of detection of PG was 10 ng/ml and the recovery was greater than 90% in urine and plasma. The analytical method therefore, exhibits good precision and sensitivity and is one of the few methods that can detect PG and the two metabolites CG and 4-CPB. The analytical method developed in this study was used to determine PG bioavailability after rectal administration in humans. Key words: Proguanil, HPLC, metabolites, biological fluids.African Journal of Biotechnology Vol. 4 (8), pp. 856-56

Clostridium Difficile Infection Risk With Important Antibiotic Classes: An Analysis of the FDA Adverse Event Reporting System

Introduction: Antibiotic use is an important risk factor for Clostridium difficile infection (CDI). Prior meta-analyses have identified antibiotics and antibiotic classes that pose the greatest risk for CDI; however, CDI epidemiology is constantly changing and contemporary analyses are needed. Objectives: The objective of this study was to evaluate the association between CDI and important antibiotic classes in recent years using the FDA Adverse Event Report System (FAERS). Methods: FAERS reports from January 1, 2015 to December 31, 2017 were analyzed. The Medical Dictionary for Regulatory Activities (MedDRA) was used to identify CDI cases. We computed the Reporting Odds Ratios (RORs) and corresponding 95% confidence intervals (95%CI) for the association between antibiotics and CDI. An association was considered statistically significant when the lower limit of the 95%CI was greater than 1. Results: A total of 2,042,801 reports (including 5,187 CDI reports) were considered, after inclusion criteria were applied. Lincosamides (e.g., clindamycin) had the greatest proportion of CDI reports, representing 10.4% of all lincosamide reports. CDI RORs (95%CI) for the antibiotic classes were (in descending order): lincosamides 46.95 (39.49-55.82), monobactams 29.97 (14.60-61.54), penicillin combinations 20.05 (17.39-23.12), carbapenems 19.16 (15.52-23.67), cephalosporins/ monobactams/carbapenems 17.28 (14.95-19.97), cephalosporins 15.33 (12.60-18.65), tetracyclines 7.54 (5.42-10.50), macrolides 5.80 (4.48-7.51), fluoroquinolones 4.94 (4.20-5.81), and trimethoprim-sulfonamides 3.32 (2.03-5.43). Conclusion: All antibiotic classes included in the study were significantly associated with CDI. Lincosamides (e.g., clindamycin) had the highest CDI ROR among the antibiotics evaluated in this study

Torsades de Pointes and Qt Prolongation Associations With Antibiotics: A Pharmacovigilance Study of the FDA Adverse Event Reporting System

Introduction: Macrolides, linezolid, imipenem-cilastatin, fluoroquinolones, penicillin combinations, and ceftriaxone are known to be associated with Torsades de pointes/QT prolongation (TdP/QTP). Other antibiotics may also lead to TdP/QTP, but no study has systemically compared TdP/QTP associations for many available antibiotics. Objectives: The objective of this study was to evaluate the association between TdP/QTP and many available antibiotics using the FDA Adverse Event Report System (FAERS). Methods: FAERS reports from January 1, 2015 to December 31, 2017 were analyzed. The Medical Dictionary for Regulatory Activities (MedDRA) was used to identify TdP/QTP cases. We calculated the Reporting Odds Ratios (RORs) and corresponding 95% confidence intervals (95%CI) for the association between antibiotics and TdP/QTP. An association was considered to be statistically significant when the lower limit of the 95%CI was greater than 1.0. Results: A total of 2,042,801 reports (including 3,960 TdP/QTP reports) were considered, after inclusion criteria were applied. Macrolides had the greatest proportion of TdP/QTP reports. Of the 4,092 reports associated with macrolides, 108 reports (2.6%) were associated with TdP/QTP. Significant TdP/QTP RORs (95%CI) for the antibiotics were (in descending order): macrolides 14.32 (11.80-17.38), linezolid 12.41 (8.52-18.08), amikacin 11.80 (5.57-24.97), imipenem-cilastatin 6.61 (3.13-13.94), fluoroquinolones 5.68 (4.78-6.76), penicillin combinations 3.42 (2.35-4.96), and ceftriaxone 2.55 (1.41-4.62). Conclusion: This study confirms prior evidence for TdP/QTP associations with macrolides, linezolid, imipenem-cilastatin, fluoroquinolones, penicillin combinations, and ceftriaxone. This study also identifies a new association between amikacin and TdP/QTP

Interstitial lung disease; a need for oxygen concentrator rental business in Nigeria?

Background: Patients with chronic obstructive airway diseases often need domiciliary oxygen supply. Case report: We report an elderly woman with interstitial lung disease that was dependent on intranasal oxygen. We discuss the need for rental oxygen concentrator business in Nigeria. Key Message: Rental oxygen concentrator business will make oxygen concentrators affordable in Nigeri

The efficacy of urine data in comparative bioavailability of proguanil after oral and rectal administration in man

The bioavailability of proguanil formulated as suppository, was compared to the tablet formulation in a bid to evaluate the utility of the suppository dosage form as means of administering proguanil in children and high-risk groups, such as sickle cell patients, who may not tolerate oral route of administration. The study was a completely randomized cross over involving administration of 200 mg of proguanil suppository and tablet to twelve healthy volunteers. Biological fluids such as urine and blood were collected before and at predetermined time intervals following administration of the drug. The biological samples were analyzed for the unchanged proguanil using an earlier reported method. The relative bioavailability of proguanil suppository as compared to the tablet dosage form was found to be about 61% from both urine and plasma data. The findings showed for the first time that proguanil suppository could be sufficiently bioavailable and may therefore be useful in chemoprophylaxis of malaria in sickle cell patients and children, particularly under such conditions that made oral route become impracticable