Frequency of Osteoporosis in Black Nigerian Women Aged 50 and above with Degenerative Musculoskeletal Diseases and Fractures.

BACKGROUND AND OBJECTIVES: Osteoporosis is a bone disease characterized by reduced bone density (and microarchitecture damage) prevalent in post-menopausal women, who are prone to fragility fractures. There is paucity of data regarding the prevalence of osteoporosis in Nigerian women. This study was carried out to evaluate the frequency of osteoporosis among Nigerian women with degenerative skeletal diseases and fractures who visited our hospital so as to suggest prevention and early treatment in order to reduce the occurrence of fragility fractures. METHODS: Women aged 50 years and older, who visited the hospital with degenerative skeletal diseases and fractures during the study period were recruited. Their ages, diagnosis, Bone Mineral Density (BMD), T-score and interpretation were recorded in an anonymous database. RESULTS: The ages of the 173 patients evaluated ranged between 51 and 89 years, of which 111 (64.1%) were aged between 61 and 80 years. The most common diagnosis was degenerative lumbar spine disease in 37.0% of patients, but only 13.9% had fractures. Knee and hip osteoarthritis (OA) accounted for fewer cases (22.5% and 3.5% respectively). Using WHO criteria for diagnosing osteoporosis, 35 (20.2%) of the patients had osteoporosis, while 82 (47.4%) had low BMD, 52 (30.1%) were normal and 4 (2.3%) had high BMD. CONCLUSIONS: In this study, the frequency of osteoporosis increased with age and was higher among patients with a combination of cervical and lumbar degenerative disease, followed by fractures. We, therefore, recommend routine screening of women aged 50 and above with degenerative spine disease and fractures.

CONTEXTE ET OBJECTIFS: L'ostéoporose est une maladie osseuse caractérisée par une réduction de la densité osseuse (et des dommages à la microarchitecture) fréquente chez les femmes ménopausées, sujettes aux fractures de fragilité. Il y a peu de données sur la prévalence de l'ostéoporose chez les femmes nigérianes. Cette étude a été réalisée pour évaluer la fréquence de l'ostéoporose chez les femmes nigérianes atteintes de maladies dégénératives du squelette et de fractures qui ont visité notre hôpital afin de suggérer une prévention et un traitement précoce afin de réduire la survenue de fractures de fragilité. MÉTHODES: Des femmes âgées de 50 ans et plus, qui ont visité l'hôpital avec des maladies dégénératives du squelette et des fractures au cours de la période d'étude ont été recrutées. Leur âge, leur diagnostic, leur densité minérale osseuse (DMO), leur score T et leur interprétation ont été enregistrés dans une base de données anonyme. RÉSULTATS: L'âge des 173 patients évalués variait entre 51 et 89 ans, dont 111 (64,1%) étaient âgés de 61 à 80 ans. Le diagnostic le plus courant était la maladie dégénérative de la colonne lombaire chez 37,0% des patients, mais seulement 13,9% avaient des fractures. L'arthrose du genou et de la hanche (OA) représentait moins de cas (22,5% et 3,5% respectivement). En utilisant les critères de l'OMS pour le diagnostic de l'ostéoporose, 35 (20,2%) des patients souffraient d'ostéoporose, tandis que 82 (47,4%) avaient une faible DMO, 52 (30,1%) étaient normales et 4 (2,3%) avaient une DMO élevée. CONCLUSIONS: Dans cette étude, la fréquence de l'ostéoporose augmentait avec l'âge et était plus élevée chez les patients présentant une combinaison de maladies dégénératives cervicales et lombaires, suivies de fractures. Nous recommandons donc un dépistage systématique des femmes âgées de 50 ans et plus souffrant de maladie dégénérative de la colonne vertébrale et de fractures. MOTS CLÉS: femmes nigérianes, ostéoporose, densité minérale osseuse, fractures de fragilité.

Lipophilicity Descriptors Correlate Uniquely with Pharmacokinetic and Blood-Brain Barrier Penetration Parameters for Selected Antipsychotic Drugs

Lipophilicity is an important physicochemical parameter of biological relevance; although its in- vivo predictive capability is dependent on accuracy and reliability of platforms used for its determination. This work examines biomimetic attribute of isocratic chromatographic hydrophobicity index (ICHI), experimental logarithm of octanol ­ water partition coefficient (LogP) and some computed lipophilicity indices for eight (8) selected antipsychotic agents and their predictive capability in drug discovery. The retention behavior of 5 first-generation and 3 second-generation antipsychotics was determined on reversed-phase chromatographic platform using methanol-phosphate buffer (pH 6.8) mobile phase. The retardation factor obtained was transformed to Rm, and plotted against volume fraction of organic modifier in the mobile phase to generate linear graph whose x- intercept is ICHI. Experimental LogP values were curled from literature while computed LogP were obtained using respective software. The experimentally determined LogPoctanol/water and ICHI were first correlated with index of brain permeability (BBB); before all lipophilicity indices were comparatively evaluated and correlated with in-vivo-normalized pharmacokinetic parameters curled from literature. ICHI gave better correlation with BBB index (r = 0.976) compared to Log Poctanol/water (r = 0.557). Comparative lipophilicity evaluation shows clustered pattern for second generation antipsychotics compared to first generation. In vivo correlation was poorer for the 8 drugs (r < 0.7), better with subset of phenothiazine homologues (r = 0.51 to 0.97). The ALogP, LogPoctanol/water, cLogP and ICHI gave highest correlation with the pharmacokinetic parameters. The biomimetic attributes of ICHI is better than for LogPoctanol/water in predicting brain permeability, but lower for in-vivo pharmacokinetic prediction.

Ultrasonographic Volumetric Assessment of Achilles Tendons in Unilateral Congenital Clubfoot in Lagos, Nigeria.

PURPOSE: To assess cases of unilateral congenital talipes equinovarus (CTEV) and compare both Achilles tendons using [MSK USS]. METHODS: Twenty-two patients (44 feet) with unilateral CTEV presenting at the clubfoot clinic who met the inclusion criteria were recruited for the study. Biographic data was collected from the patients and both Achilles tendons scanned using high frequency ultrasound scan probe. The length, width, thickness were measured and area of the tendons estimated. RESULTS: The median age of the patients was 32.5days with a male to female ratio of 1.2:1. The right foot was involved in 15 patients while the left was affected in 7 cases giving a ratio 2.1:1. The Achilles tendons in Clubfeet with mean length of 2.44(±0.3) cm were consistently longer than in the normal feet with mean length of 2.25(±0.3) cm. The width, thickness and area of the Achilles tendons in normal feet with mean values of 0.52(±0.01) cm, 0.22(±0.03) cm and 0.030(±0.01) cm2 respectively were consistently more than in clubfeet with mean values of 0.43(±0.1) cm, 0.20(±0.03) cm and 0.020(±0.01) cm2 respectively. The disparity in length between the normal and clubfeet when compared with the Pirani scores of the affected feet revealed no statistically significant difference. This was also noted when the disparity in width, thickness and area of Achilles tendons were similarly compared with Pirani scores. CONCLUSION: The Achilles tendon of unilateral CTEV is longer but thinner and narrower than in the contralateral normal foot. The disparity in sizes of the tendon has no significant correlation with severity of the clubfeet.

Bioseparation and activity of Khaya senegalensis fractions against infective larvae of Haemonchus contortus.

The anthelmintic constituents of Khaya senegalensis (Deser.) A. Juss (Meliaceae) bark extract, previously demonstrated to show both in vitro and in vivo activity against gastrointestinal nematodes of sheep was investigated by chromatographic separation of the crude extract and bioassay of fractions. Bioseparation of the crude ethanol (95%) extract was carried out by gradient vacuum liquid chromatographic analysis and thin layer chromatography fingerprinting of eluates. The activity of the fractions was tested by a larval development assay in vitro. The survival rate of infective larvae L3 of sheep nematodes, predominantly Haemonchus contortus, was used to assess relative bioactivity. A secondary fraction obtained from further purification by preparative thin layer chromatography of a primary active fraction was also assessed for bioactivity. The compositions of the fractions were determined by qualitative chemical tests. The extracts killed infective larvae of H. contortus in a concentration-dependent manner. Best-fit LC50 values were 80.81, 63.73, 44.03 and 63.90 microg/ml for fractions A, B, C, and D, respectively (95% CI). The fractions are composed of saponins (A), saponins and alkaloids (B), saponins, terpenoids, flavonoids, condensed tannins (C), and saponins and tannins (D). Fraction C shows the highest activity of all the fractions, however, the difference is not statistically significant (p>0.05, Kruskal-Wallis test). The secondary fraction, C1A obtained from fraction C gave best-fit LC50 value of 5.09 microg/ml (95% CI) and was identified to be condensed tannin. The anthelminthic activity of K. senegalensis appears to involve synergism between various secondary metabolites found in the extract rather than a particular group of compounds.

Hepatoprotective activity of purified fractions from Garcinia kola seeds in mice intoxicated with carbon tetrachloride.

The hepatoprotective activity of kolaviron (KV), a biflavonoid complex from Garcinia kola seeds, and its purified fractions was investigated in mice intoxicated with carbon tetrachloride (CCl(4)). The ability of vitamin E to attenuate the toxicity was also examined. KV was extracted from powdered seeds of G. kola and then separated by thin-layer chromatography into three fractions--Fraction I (FI), Fraction II (FII), and Fraction III (FIII), with ratio of fronts values of 0.48, 0.71, and 0.76, respectively. Pretreatment with KV, FI, and FII at a dose of 100 mg/kg of body weight for 2 weeks and then challenge with CCl(4) at a dose of 1.2 g/kg of body weight, three times a week for 2 consecutive weeks, decreased the CCl(4)-induced increase in activities of alanine aminotransferase (ALT) and aspartate aminotransferase (AST) by 31%, 30%, and 31% and 41%, 55%, and 42%, respectively. CCl(4) intoxication also caused a significant (P < .05) accumulation of lipid peroxidation (LPO) products as revealed by the formation of the thiobarbituric acid-reactive substances: CCl(4) induced LPO levels in serum and microsomes by 112% and 89%, respectively. However, pretreatment with KV, FI, and FII decreased LPO levels in serum by 31%, 41%, and 40% and in microsomes by 48%, 39%, and 35%, respectively. Vitamin E was protective in reducing the CCl(4)-induced increase in levels of AST, ALT, and gamma-glutamyl transferase as well as LPO. Furthermore, CCl(4) intoxication significantly (P < .05) decreased the activities of microsomal glucose-6-phosphatase, aniline hydroxylase, and cytosolic glutathione-S-transferase (GST). While pretreatments with KV, FI, and FII were able to ameliorate the levels of glucose-6-phosphatase and GST, there were no significant (P > .05) effects on the levels of aniline hydroxylase and DT-diaphorase. This study confirms that FI and FII from KV enhanced recovery from CCl(4)-induced hepatotoxicity by decreasing the extent of LPO and also inducing the levels of phase II enzyme (GST). These fractions are responsible for the observed antihepatotoxic effect of KV.

Anthelmintic activity of Spigelia anthelmia extract against gastrointestinal nematodes of sheep.

In vitro (larval development assay) and in vivo studies were conducted to determine possible direct anthelmintic effect of ethanolic and aqueous extracts of Spigelia anthelmia towards different ovine gastrointestinal nematodes. The effect of extracts on development and survival of infective larvae stage (L(3)) was assessed. Best-fit LC(50) values were computed by global model of non-linear regression curve fitting (95% confidence interval). Therapeutic efficacy of the ethanolic extracts administered orally at a dose rate of 125, 250, and 500 mg/kg, relative to a non-medicated control group of sheep harbouring naturally acquired infection of gastrointestinal nematodes, was evaluated in vivo.The presence of S. anthelmia extracts in the cultures decreased the survival of L(3) larvae. The LC(50) of aqueous extract (0.714 mg/ml) differ significantly from the LC(50) of the ethanolic extract (0.628 mg/ml) against the strongyles (p < 0.05, paired t-test). Faecal egg counts on day 12 after treatment showed that the extract is effective, relative to control (one-way analysis of variance [ANOVA], Dunnett's multiple comparison test) at 500 mg/kg against Strongyloides spp. (p < 0.01), 250 mg/kg against Oesophagostomum spp., Trichuris spp. (p < 0.05), and 125 mg/kg against Haemonchus spp. and Trichostrongylus spp. (p < 0.01). The effect of the doses is significant in all cases, the day after treatment is also extremely significant in most cases, whereas interaction between dose and day after treatment is significant (two-way ANOVA). S. anthelmia extract could, therefore, find application in the control of helminth in livestock, by the ethnoveterinary medicine approach.

Novel determination of nabumetone, a cox-2 inhibitor precursor via its 4-carboxyl-2,6-dinitrobenzene diazonium (CDNBD) derived AZO dye.

A novel colorimetric determination ofnabumetone in tablets has been developed. The assay is based on chemical derivatization (aromatic ring derivatization technique) using newly developed 4-carboxyl-2,6-dinitrobenzene diazonium (CDNBD) ion as the chromogenic derivatizing reagent and resultant formation of azo dye.Optimization studies established an optimal reaction time of 10 minutes at 30 degrees C after mixing the drug/reagent mixture in a vortex mixer for 10 sec. A new absorption maximum (ë(max)) was found at 470 nm, which was selected as analytical wavelength. The assays were linear over 1-6 microg/ml of nabumetone and the optimal reaction required a 2:1 reagent/drug stoichiometric ratio. The developed method has a low limit of detection of 0.39 microg/ml, and is reproducible (1.81% RSD). It has been applied successfully to the assay of nabumetone tablets and is of equivalent accuracy (p > 0.05) with the official (B.P) HPLC method. The new method is simple, has the main advantage of employing a more affordable instrumentation and could find application in routine in-process quality control of nabumetone tablets.

Anthelmintic efficay of nauclea latifolia extract against gastrointestinal nematodes of sheep: in vitro and vivo studies

Direct effects of Nauclea latifolia extracts on different gastrointestinal nematodes of sheep is described. In vivo and in vitro studies were conducted to determine possible anthelmintic effect of leaf extracts of Nauclea latifolia toward different ovine gastro intestinal nematodes. A larval development assay was used to investigate in vitro; the effect of aqueous and ethanolic extracts of N. latifolia towards strongyles larvae. The development and survival of infective larvae (L3) was assessed and best-fit LC50 values were computed by global model of non-linear regression analysis curve-fitting (95CI). Twenty sheep harbouring naturally acquired gastrointestinal nematodes were treated with oral administration of ethanolic extracts at a dose rate of 125 mg/kg; 250 mg/kg and 500mg/kg to evaluate therapeutic efficacy; in vivo. The presence of the extracts in the cultures decreased the survival of larvae. The LC50 of aqueous and ethanolic extract were 0.704 and 0.650 mg/ml respectively and differ significantly (P0.05; paired t test). Faecal egg counts (FEC) on day 12 after treatment showed that the extract is effective; relative to control (1-way ANOVA; Dunnett's multiple comparison test); at 500mg/kg against Haemonchus spp; Trichostrongylus spp (p0.05); Strongyloides spp (P 0.01); at 250mg/kg against Trichuris spp (P 0.01) and ineffective against Oesophagostomum spp (p0.05). The effect of doses is extremely significant; the day after treatment is sometimes significant while interaction between dose and day after treatment is insignificant (2-way ANOVA). N. latifolia extract could therefore find application in the control of helminth in livestock; by the ethnoveterinary medicine approach

Anthelmintic efficacy of Nauclea latifolia extract against gastrointestinal nematodes of sheep: in vitro and in vivo studies.

Direct effects of Nauclea latifolia extracts on different gastrointestinal nematodes of sheep is described. In vivo and in vitro studies were conducted to determine possible anthelmintic effect of leaf extracts of Nauclea latifolia toward different ovine gastro intestinal nematodes. A larval development assay was used to investigate in vitro, the effect of aqueous and ethanolic extracts of N. latifolia towards strongyles larvae. The development and survival of infective larvae (L(3)) was assessed and best-fit LC(50) values were computed by global model of non-linear regression analysis curve-fitting (95% CI). Twenty sheep harbouring naturally acquired gastrointestinal nematodes were treated with oral administration of ethanolic extracts at a dose rate of 125 mg/kg, 250 mg/kg and 500 mg/kg to evaluate therapeutic efficacy, in vivo.The presence of the extracts in the cultures decreased the survival of larvae. The LC(50) of aqueous and ethanolic extract were 0.704 and 0.650 mg/ml respectively and differ significantly (P<0.05, paired t test). Faecal egg counts (FEC) on day 12 after treatment showed that the extract is effective, relative to control (1-way ANOVA, Dunnett's multiple comparison test), at 500 mg/kg against Haemonchus spp, Trichostrongylus spp (p<0.05), Strongyloides spp (P < 0.01); at 250 mg/kg against Trichuris spp (P < 0.01) and ineffective against Oesophagostomum spp (p>0.05). The effect of doses is extremely significant; the day after treatment is sometimes significant while interaction between dose and day after treatment is insignificant (2-way ANOVA). N. latifolia extract could therefore find application in the control of helminth in livestock, by the ethnoveterinary medicine approach.

Toxic effects of chromatographic fractions of Phyllanthus amarus on the serum biochemistry of rats.

Chromatographic fractions obtained from Phyllanthus amarus were tested for toxicity on the serum biochemistry of rats. The results revealed that some fractions of P. amarus had potentially deleterious effects on the blood and therefore caution should be exercised in the use of P. amarus as a medicinal plant.

Anthelmintic activity of extracts of Spondias mombin against gastrointestinal nematodes of sheep: studies in vitro and in vivo.

This study was carried out to validate the efficacy of Spondias mombin, used locally as an anthelmintic, and to standardize the effective dose of the plant extract required for worm control in livestock. In vitro and in vivo studies were conducted to determine the direct anthelmintic effect of ethanolic and aqueous extracts of S. mombin towards different ovine gastrointestinal nematodes. A larval development assay (LDA) was used to investigate the in vitro effect of extracts on strongyle larvae. Another study was conducted in vivo to evaluate the therapeutic efficacy of the extracts administered orally at dose rates of 125, 250, 500 mg/kg to sheep naturally infected with gastrointestinal nematodes. Twenty sheep were selected on the basis of positive faecal egg counts (750 epg). The sheep were allocated randomly to a non-medicated control group (A) or to groups given 125 mg/kg (B), 250 mg/kg (C) or 500 mg/kg (D) of extract, respectively. Sheep in groups B-D were given extracts orally on two days. Individual faecal egg counts were performed on days 0, 3, 6, 9 and 12. The presence of S. mombin extracts in in vitro cultures of larvae decreased the survival of L3 larvae. The LC50 of the aqueous extract of S. mombin was 0.907 mg/ml, while the LC50 of the ethanolic extract was 0.456 mg/ml. This difference in LC50 was statistically significant (p > 0.05). The mean percentage faecal egg reduction of sheep drenched with 500 mg/kg S. mombin extracts was 15.0%, 27.5%, 65.0%, 65.0%, 100.0% against Haenmonchus spp., Trichostrongylus spp., Oesophagostomunm spp., Strongyloides spp. and Trichuris spp. respectively, on day 12. Extracts of S. mombin could find application in the control of helminths in livestock.

Evaluation of the anthelmintic activity of Khaya senegalensis extract against gastrointestinal nematodes of sheep: in vitro and in vivo studies.

The anthelmintic effect of Khaya senegalensis is described. In vitro and in vivo studies were conducted to determine possible direct anthelmintic effects of ethanolic and aqueous extracts of K. senegalensis towards different ovine gastrointestinal nematode. A larval development assay was used to investigate in vitro, the effect of aqueous and ethanolic extracts towards larvae of strongyles. The LC50 values of the effects of both the aqueous and ethanolic extracts were calculated. Another study was conducted in vivo to evaluate the therapeutic efficacy of the extracts administered orally at a dose rate of 125, 250 and 500 mg/kg of sheep harbouring naturally acquired infection of gastrointestinal nematodes. The presence of K. senegalensis extracts in the cultures decreased the viability of larvae. The LC50 of the aqueous extract (0.69 mg/ml) is not significantly different (P >0.05, t-test) from the ethanolic extract (0.51 mg/ml). The activity of the extract is concentration dependent in vivo. Sheep drenched with 500 mg/kg K. senegalensis ethanolic extract had a mean faecal egg count (FEC) reduction of 88.82%. The extract of K. senegalensis could find application in anthelmintic therapy in veterinary practice.

Morphometric and histopathological studies on the effects of some chromatographic fractions of Phyllanthus amarus and Euphorbia hirta on the male reproductive organs of rats.

The aqueous crude extracts of P. amarus and E. hirta were administered to thirty eight-week old sexually mature male albino to determine the effects of these extracts on the male reproductive organs of these animals. The results from this study revealed that the aqueous crude extracts of P. amarus and E. hirta caused varying degrees of testicular degeneration as well as reduction in the mean seminiferous tubular diameter (STD) in the treated rats. It thus shows that the aqueous crude extracts of P. amarus and E. hirta have potentially deleterious effects on the testes and accessory organs of rats. Great caution should therefore be exercised in the use of these plants for medicinal purpose.

Some physicochemical properties of 4-amino-3,5-dinitrobenzoic acid (ADBA).

Some physicochemical properties of the aromatic amino acid 4-amino-3,5-dinitrobenzoic acid (ADBA) were determined. This provides, for the first time, quantitative data about this chemical of current pharmaceutical and biomedical interest. The analytical reagent grade of ADBA has 100% purity, determined by potentiometry. The ionization constant (pKa) is 4.00 +/- 0.04. The specific absorbance of ADBA [A(1%, 1 cm)] was determined as 389.42 +/- 51.33 and 381.67 +/- 38.99 (p = 0.05) in water (435 nm) and octanol (415 nm), respectively. The lipophilicity of ADBA is described by its octanol/water partition coefficient (Log P) of -1.50. An analogous parameter descriptive of lipophilicity, the chromatographic hydrophobicity index (Rm), was determined as -0.84 on reversed phase thin layer chromatography (RPTLC). ADBA is more acidic thanp-amino benzoic acid (PABA), the prototype aromatic amino acid of which ADBA is an analogue. It is also about thirty-two times more water soluble than in n-octanol. These findings have a predictive value with respect to absorption and distribution of this compound in living organisms.

Evaluation of diazotized 4-amino-3,5-dinitrobenzoic acid (ADBA) as a new derivatizing reagent.

A preliminary evaluation of the reactivity of diazotized 4-amino-3,5-dinitrobenzoic acid (ADBA) towards selected aromatic compounds has been described. Successful diazo coupling of pharmaceuticals possessing aromatic rings of varying reactivities was achieved with the arenediazonium ion of ADBA at room (30 degrees C) or elevated temperature (80 degrees C). The adducts formed in spot-test reactions were coloured for some compounds (e.g, cloxacillin and chloroxylenol), others showed colour at elevated temperature of reaction (e.g., salicylic acid and aspirin), while others showed no detectable change in colour of reaction mixture, even at elevated temperature (e.g., imidazole and tinidazole). The coloured product formed at room temperature decomposed and the colour discharged at elevated temperature in some cases (e.g., beta-naphthol). However, thin layer chromatographic analysis suggested that a more lipophilic derivative, relative to the original compound was formed for some of the compounds studied which did not show any detectable colour change in the spot test reactions. The diazotized ADBA is thus shown to be a reactive coupling reagent with which a suitable derivatization methodology could be developed for a wide range of pharmaceuticals in ultraviolet/visible spectrophotometry and high performance liquid chromatographic (HPLC) analysis.