Nigerian National Institute for Pharmaceutical Research and Development

Abuja, Nigeria

Nigerian National Institute for Pharmaceutical Research and Development

Abuja, Nigeria
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Oga E.F.,Nigerian National Institute for Pharmaceutical Research and Development
International Journal of Pharmacy and Pharmaceutical Sciences | Year: 2010

Tuberculosis cases have significantly increased within the past decade, especially among AIDS patients, hence the importance of isoniazid, a first line anti-tubercular agent. This has prompted many investigators to develope methods for the rapid determination of isoniazid in pure form as well as in pharmaceutical formulations. A method is described for the determination of isoniazid, in pure form and in pharmaceutical formulations. The method is based on the coupling of isoniazid and vanillin in an ethanolic hydrochloric acid medium and the spectrophotometric determination at the absorption maximum (405nm). A yellow coloured hydrazone was formed. Beer's law was obeyed in the concentration range of 1-12μg/ml at 405nm. The proposed method was applied in the analysis of commercially purchased brands of isoniazid tablets and showed good accuracy and precision. Excipients used in the pharmaceutical formulation showed no interference in the analysis. The method offers the advantages of rapidity, simplicity and sensitivity and low cost and can be easily applied resource-poor settings without the need for expensive instrumentation and reagents.


Adebayo A.H.,Covenant University | John-Africa L.B.,Nigerian National Institute for Pharmaceutical Research and Development | Agbafor A.G.,Covenant University | Omotosho O.E.,Covenant University | Mosaku T.O.,Covenant University
Pakistan Journal of Pharmaceutical Sciences | Year: 2014

Anchomanes difformis is a tropical plant that has been used in folklore to treat diverse complications. The leaf extract of A. difformis was investigated for possible anti-nociceptive and anti-inflammatory effects in albino wistar rats. In these independent studies, two sets of twenty five rats were divided into five groups of five rats per group. Formalin induced pain in rats was used to investigate the anti-nociceptive effect of the extract. The extract was administered orally in the treated groups at doses 200, 400, 800 and 1600 mg/kg with aspirin serving as the positive drug control while the normal control group was not given any extract but water. Studies were also carried out on the egg albumin induced anti-inflammatory activity in rats by inducing oedema on the left hind paw. The result showed a significant inhibition (p<0.05) on the later phase (800mg/kg) of formalin pain induction in rats; similarly, a significant (p<0.05) anti-inflammatory activity was observed at 60, 90 and 120 minutes. The study thus validates the ethnomedicinal usage of A. difformis in the treatment of pain and inflammation.


Chindo B.A.,Nigerian National Institute for Pharmaceutical Research and Development | Chindo B.A.,Ahmadu Bello University | Adzu B.,Nigerian National Institute for Pharmaceutical Research and Development | Yahaya T.A.,Nigerian National Institute for Pharmaceutical Research and Development | Gamaniel K.S.,Nigerian National Institute for Pharmaceutical Research and Development
Progress in Neuro-Psychopharmacology and Biological Psychiatry | Year: 2012

Schizophrenia is a chronic and highly complex psychiatric disorder characterised by cognitive dysfunctions, negative and positive symptoms. The major challenge in schizophrenia research is lack of suitable animal models that mimic the core behavioural aspects and symptoms of this devastating psychiatric disorder. In this study, we used classical and atypical antipsychotic drugs to examine the predictive validity of ketamine-enhanced immobility in forced swim test (FST) as a possible animal model for the negative symptoms of schizophrenia. We also evaluated the effects of a selective serotonin reuptake inhibitor (SSRI) on the ketamine-enhanced immobility in FST. Repeated administration of a subanaesthetic dose of ketamine (30mgkg-1, i.p., daily for 5days) enhanced the duration of immobility in FST 24h after the final injection. The effect, which persisted for at least 21days after withdrawal of the drug, was neither observed by single treatment with ketamine (30mgkg-1i.p.) nor repeated treatment with amphetamine (1 and 2mgkg-1i.p., daily for 5days). The enhancing effects of ketamine (30mgkg-1day-1i.p.) on the duration of immobility in the FST were attenuated by clozapine (1, 5 and 10mgkg-1i.p.), risperidone (0.25 and 0.5mgkg-1i.p.) and paroxetine (1 and 5mgkg-1i.p.). Haloperidol (0.25 and 0.50mgkg-1day-1i.p.) failed to attenuate the ketamine-enhanced immobility in the FST. The repeated ketamine administration neither affects locomotor activity nor motor coordination in rats under the same treatment conditions with the FST, suggesting that the effects of ketamine on the duration of immobility in this study was neither due to motor dysfunction nor peripheral neuromuscular blockade. Our results suggest that repeated treatment with subanaesthetic doses of ketamine enhance the duration of immobility in FST, which might be a useful animal model for the negative symptoms (particularly the depressive features) of schizophrenia. © 2012 Elsevier Inc.


Obidike I.C.,Nigerian National Institute for Pharmaceutical Research and Development | Emeje M.O.,Nigerian National Institute for Pharmaceutical Research and Development | Emeje M.O.,CSIR - National Chemical Laboratory
Journal of Ethnopharmacology | Year: 2011

Ethnopharmacological relevance: The antiulcer potentials of most plants still remain largely unexplored, despite their prospects evidenced by their use as ethnomedicine. Entada africana (Mimosaceae) has been widely used in Africa for the treatment of skin infections, wounds, tonic for stomach troubles and against diphtheria-like throat complaints. The aim of the present study was to evaluate the anti-ulcer properties of Entada africana (EA) ethanol leaf extract and to obtain a novel multiparticulate pharmaceutical formulation (ACE) with it. Materials and methods: Ethanol or Indomethacin was administered to rats after oral administration of EA (200, 400 and 800 mg extract/kg b.w), ACE (400 and 800 mg/kg bw), cimetidine (100 mg/kg bw), misoprostol (40 μg/kg bw) or distilled water/saline (vehicle). Anti ulcer property was evaluated by examining and scoring stomach lesions. Results: The extract exhibited significant (P < 0.01) cytoprotective effect against ethanol and indomethacin induced gastro ulceration. The microcapsules showed enhanced cytoprotective effect against ethanol and indomethacin induced gastro ulceration. Histopathologically, the effects of EA and ACE on mucus epithelia were mild with reduced neutrophil, eosinophil and lymphocytic infiltration in stomach tissues of rats ulcerated with ethanol. Conclusions: Our current findings show that EA and its multiparticulate formulation may be a useful preparation in peptic ulcer disease. © 2011 Elsevier Ireland Ltd All rights reserved.


Builders P.F.,Nigerian National Institute for Pharmaceutical Research and Development | Bonaventure A.M.,Nigerian National Institute for Pharmaceutical Research and Development | Tiwalade A.,Nigerian National Institute for Pharmaceutical Research and Development | Okpako L.C.,University of Bradford | Attama A.A.,University of Nigeria
International Journal of Pharmaceutics | Year: 2010

The choice of excipients remains a critical factor in pharmaceutical formulations. Microcrystalline cellulose-maize starch composites (MCC-Mst) have been prepared by mixing colloidal dispersions of microcrystalline cellulose (MCC) with 10% (w/w) of chemically gelatinized maize starch (Mst) at controlled temperature conditions for use as multifunctional excipients with direct compression and enhanced disintegration abilities. The novel excipient was evaluated for its direct compression and enhanced disintegrant properties and the result compared with the properties of the individual components. Some of its physicochemical and thermal properties were also determined together with effects of freeze-thaw cycles of processing on the functional and physicochemical properties. The scanning electron micrograph (SEM) shows that the particles of the MCC-Mst were irregular in shape and multiparticulate with a marked degree of asperity. The indirect assessment of the powder flow properties as determined by Carr's compressibility index and angle of repose showed that the MCC-Mst possesses better flow compared with MCC and Mst. MCC-Mst is moderately hygroscopic and shows a Type III moisture sorption isotherm. The FT-IR spectra and DSC thermograms of the composite were different from those of MCC and Mst. The hardness of aspirin tablets was enhanced by incorporating MCC-Mst and MCC, but was reduced by Mst. While the tablets prepared with MCC-Mst and Mst disintegrated within 7 min, aspirin compacts devoid of any excipient and those prepared with MCC did not disintegrate even after 2 h. Acetaminophen compacts prepared with MCC and MCC-Mst showed similar compact hardness characteristics and loading properties. The loading capacity of the different samples of the composite decreased with increase in the freeze-thaw cycles. The loading capacity of the different materials as assessed by their compact hardness efficiency can be represented as follows (MCC > T0 > T1 > T4 > T3 > T2 > Mst). Generally, the different samples of MCC-Mst are characterized by physicochemical and functional properties that are similar at different degrees to MCC and Mst. © 2010 Elsevier B.V. All rights reserved.


Farida T.,Ahmadu Bello University | Salawu O.A.,Nigerian National Institute for Pharmaceutical Research and Development | Tijani A.Y.,Nigerian National Institute for Pharmaceutical Research and Development | Ejiofor J.I.,Ahmadu Bello University
Journal of Ethnopharmacology | Year: 2012

Ethnopharmacological relevance: Ipomoeaasarifolia (Desr.) Roem. and Schult. is used traditionally in some parts of Africa for the treatment of a variety of diseases. This study attempts to validate its hepatoprotective activity by evaluating the prophylactic and curative properties of the methanolic extract of Ipomoea asarifolia (IA) leaves. Materials and Methods: Liver damage was induced by administering 0.5 ml/kg of an equal mixture of carbon tetrachloride (CCl4) in olive oil intraperitoneally on alternate days, for 5 days and the plant extract was given orally daily, for 7 days at doses of 100, 200 and 400 mg/kg. Results: Pre-treatment with the extract significantly (P<0.05) decreased CCl4-induced elevation in serum levels of alanine transaminase, aspartate transaminase, alkaline phosphatase, triglycerides, bilirubin and cholesterol, better than the standard drug silymarin at 100 mg/kg. In the curative study, IA significantly (P<0.05) reversed CCl 4-induced liver damage, comparable to silymarin. Hepatoprotective potential was further supported by decrease in pentobarbitone sleeping time and improved hepatic tissue histopathology. Conclusion: These results indicate that I. asarifolia leaves have potent hepatoprotective activity against CCl 4-induced hepatic damage in rats. © 2012 Elsevier Ireland Ltd.


Mbah C.C.,Nigerian National Institute for Pharmaceutical Research and Development | Mbah C.C.,University of Nigeria | Builders P.F.,Nigerian National Institute for Pharmaceutical Research and Development | Attama A.A.,University of Nigeria
Expert Opinion on Drug Delivery | Year: 2014

Introduction: The application of vesicular carrier formulations has generated promise of overcoming some problems associated with drug delivery arising from not only the physicochemical properties of the drug but also those of the biological barriers, such as the membrane linings of various body tissues and the skin. This review article discusses the importance of various vesicular carriers, namely liposomes, niosomes, transfersomes and ethosomes in drug delivery with greater emphasis on ethosomes. Areas covered: The nature, mechanism of drug delivery, methods of preparation as well as characterization of vesicular carriers was discussed with a focus on ethosomes. An overview of their potential applications was provided with discussions on the future prospects and challenges of achieving enhanced drug delivery using ethosomes. Expert opinion: Vesicular carriers offer controlled and sustained drug release, improved permeability and protection of the encapsulated bioactives. Ethosomes offer more efficient and enhanced bioavailability better than the older dosage forms owing to the high ethanol content. Ethosomes have potential applications in the development of nanomedicines, including phytomedicines, for the treatment of challenging diseases ravaging the world today. The future holds great prospects in the utilization of vesicular carriers, especially ethosomes, in overcoming peculiar problems of drug delivery. © 2014 Informa UK, Ltd.


Chime S.A.,University of Nigeria | Attama A.A.,University of Nigeria | Builders P.F.,Nigerian National Institute for Pharmaceutical Research and Development | Onunkwo G.C.,University of Nigeria
Journal of Microencapsulation | Year: 2013

Objective: To formulate sustained-release diclofenac potassium-loaded solid lipid microparticles (SLMs) based on solidified reverse micellar solution (SRMS) and to evaluate the in vitro and in vivo properties. Methods: SRMS consisting of mixtures of Phospholipon® 90H and Softisan® 154 were used to formulate diclofenac potassium-loaded SLMs. Characterization based on the particle size and morphology, stability and encapsulation efficiency (EE%) were carried out on the SLMs. In vitro release was carried out in simulated intestinal fluid (pH 7.5). Anti-inflammatory and ulcerogenic properties were studied using rats. Results: Maximum EE% of 95%, 94% and 93% were obtained for SLMs formulated with SRMS 1:1, 2:1 and 1:2, respectively. In vitro release showed about 85-90% drug release at 13h. Diclofenac potassium-loaded SLMs showed good anti-inflammatory and gastro-protective properties. Conclusion: Diclofenac potassium-loaded SLMs based on SRMS could be used orally or parenterally under controlled conditions, for once daily administration. © 2013 Informa UK Ltd.


Ohwoavworhua F.O.,Nigerian National Institute for Pharmaceutical Research and Development | Adelakun T.A.,Nigerian National Institute for Pharmaceutical Research and Development
Indian Journal of Pharmaceutical Sciences | Year: 2010

The microcrystalline cellulose is an important ingredient in pharmaceutical, food, cosmetic and other industries. In this study, the microcrystalline cellulose, obtained from the stalk of Sorghum caudatum was evaluated for its physical and tableting characteristics with a view to assessing its usefulness in pharmaceutical tableting. The microcrystalline cellulose, obtained from the stalk of Sorghum caudatum, obtained by sodium hydroxide delignification followed by sodium hypochlorite bleaching and acid hydrolysis was examined for its physicochemical and tableting properties in comparison with those of the well-known commercial microcrystalline cellulose grade, Avicel PH 101. The extraction yield of this microcrystalline cellulose, obtained from the stalk of Sorghum caudatum was approximately 19%. The cellulose material was composed of irregularly shaped fibrous cellulose particles and had a moisture content of 6.2% and total ash of 0.28%. The true density was 1.46. The flow indices showed that the microcrystalline cellulose, obtained from the stalk of Sorghum caudatum flowed poorly. The hydration, swelling and moisture sorption capacities were 3.9, 85 and 24%, respectively. Tablets resulting from these cellulose materials were found to be without surface defects, sufficiently hard and having disintegration time within 15 min. The study revealed that the microcrystalline cellulose, obtained from the stalk of Sorghum caudatum compares favourably with Avicel PH 101 and conformed to official requirement specified in the British Pharmacopoeia 1993 for microcrystalline cellulose.


Rodrigues A.,CSIR - National Chemical Laboratory | Emeje M.,CSIR - National Chemical Laboratory | Emeje M.,Nigerian National Institute for Pharmaceutical Research and Development
Carbohydrate Polymers | Year: 2012

Starch has found use in industries as diverse as food, textiles, cosmetics, plastics, adhesives, paper, and pharmaceuticals. From a pharmaceutical standpoint, starch finds its value in solid-oral dosage forms, where it has been used as a binder, diluent, and disintegrant. However, only recently has the use of starch in nanotechnology started to make significant advances in biomedical applications, including newer drug delivery techniques. There has been a considerable effort to develop biodegradable nanoparticles as effective drug delivery systems. Being cheap, non-toxic, renewable, biodegradable and compatible with many other materials for industrial applications, starch is attracting the interest of drug delivery scientists. We have put together in a short and concise format, recent applications of starch derivatives in the emerging field of nanodrug delivery with the conclusion that a lot still needs to be done. © 2011 Elsevier Ltd. All rights reserved.

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