MOSP - Macao Scientific Publishers

Research Article

Cross-linked Nanoparticles of Cytarabine: Encapsulation, Storage and In-vitro Release

Nisha Mary Joseph*, Pramod Kumar Sharma

Abstract: This work presents results of the preparation and characterization of nanoparticles for entrapping cytarabine, a chemotherapeutic agent. The particle size analysis indicated a uniform particle size. The study of the release of drug from nanoparticles exhibited a prolonged release profile as studied over a period of 16 hours. The drug release was constant from the 10th to the 16th hours, which showed that the formulation was successful for long-term treatment. The drug entrapment efficiency of the nanoparticles having the same ratio of polymer and drug was about 90.2%. The physical stability of the nanoparticles was good as studied over a period of 4 weeks. These results are promising for producing nanoparticles by entrapping cytarabine, which can be useful for cancer therapy.[...] Read More.

Keywords: Cytarabine, Nanoparticles, In-vitro Release, Sodium Tripolyphosphate

Int. J. Pharm. & Pharmacol. 2010, 1(1), 1-6;

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Research Article

Efficacy of hibitaneÂ® on Some Nosocomial Isolates of S. aureus, E. coli and C. albicans

El Mahmood, A. M.*, Doughari, J. H.

Abstract: The effectiveness of the disinfectant hibitane on some microorganisms associated with nosocomial infections were assessed at various use-dilutions of 1: 10, 1: 100, 1: 200 and 1: 2000 constituted using aqueous ethanol and 10% serum solutions. The shapes of the death curves were qualitatively similar for all the organisms exhibiting an initial shoulder (lag), the duration of which depended on hibitane® concentration used and this was closely followed by an exponential order of death. Alcoholic solutions were much more potent than aqueous solutions. Activity of the disinfectant was maintained in the presence of potable water and serum though to a lesser extent than deionized water. The order of resistance to the disinfectant was Escherichia coli (MBC 0.00008 - 0.0003) > Staphyloccocus aureus (MBC 0.00007 - 0.00026) > Candida albicans MBC 0.00006 - 0.00022).[...] Read More.

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Int. J. Pharm. & Pharmacol. 2010, 1(1), 1-6;

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Research Article

Effect of Grewia Gum on The Mechanical Properties of Paracetamol Tablet Formulations

Emeje Martins*, Isimi Christiana, Kunle Olobayo

Abstract: Grewia gum has been evaluated as a binder in paracetamol tablet formulations. Compressional properties of the formulations were analyzed using density measurements and the compression equations of Heckel and Kawakita as assessment parameters. Formulations containing Grewia gum as a binder show a slower onset and lower amount of plastic deformation than those containing PVP. The Db values for formulations containing Grewia gum, increased with increased concentration up to 4% w/w. Formulations containing Grewia gum were also found to exhibit higher degree of packing than those containing PVP. Yield values for formulations containing Grewia gum was found to be at variance with the binder concentration. The values increased between 1 and 2% w/w and decreased between 2 and 4% w/w. A linear relationship was found to exist between N/C and N for formulations containing Grewia gum at all concentrations. Grewia gum was found to improve the fluidity of paracetamol granulation better than PVP. This study suggests that Grewia gum compares favorably with the standard binder PVP used hence could be a useful substitute binder in paracetamol tablet formulations.[...] Read More.

Keywords: Grewia gum, PVP, paracetamol, Heckel equation, Kawakita equation, compaction characteristics.

Int. J. Pharm. & Pharmacol. 2010, 1(1), 1-6;

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Research Article

Antimicrobial Activity of Leaf Extracts of Senna Obtusifolia (L)

Doughari, J. H*, El-mahmood, A. M. and Tyoyina, I

Abstract: Antimicrobial properties of leaf extracts of Senna obtusifolia (L) were investigated against both clinical and laboratory isolates of both bacteria and fungi using the disc diffusion method. Acetone extracts (12 mm zone diameter of inhibition, MIC 200 g/mL and MBC 300 g/mL) demonstrated the highest activity, followed by dichloromethane (8 mm zone diameter of inhibition, MIC 300 g/mL and MBC 400 g/mL), methane (7 mm zone diameter of inhibition, MIC 400 g/mL and MBC 400 g/mL) and hexane (6 mm zone diameter of inhibition, MIC 800 g/mL and MBC 1000 g/mL). Water extracts demonstrated the least activity against the test bacteria and fungi (4 mm zone diameter of inhibition, MIC 800 g/mL and MBC 800 g/mL). Phytotoconstituents present included Saponins, Tannins, Alkaloids and Flavonoids. S. obtusifolia (L) can be used to source antibiotic substances for possible treatment of bacterial and fungal infections including gonorrhea, pneumonia, urinary tract and some mycotic infections.[...] Read More.

Keywords: Senna obtusifolia (L), antimicrobial property, extract antibiotic.

Int. J. Pharm. & Pharmacol. 2010, 1(1), 1-6;

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Research Article

Characterization of Rat Liver Mitochondrial Permeability Transition Pore by Using Mitochondrial Swelling Assay

Manash K. Paul* , Rajinder K, Anup K. Mukhopadhyay

Abstract: The mitochondrial permeability transition (MPT) is considered to contribute substantially to the regulation of normal mitochondrial metabolism and plays as an important mediator of cell death. MPT is regulated in a tissue specific manner. The importance of this work is highlighted by the fact that knowledge regarding liver MPT may serve as important determinants of the physiological state of the liver. Our results suggest that liver mitochondria exhibit a cyclosporin A sensitive, exogenous calcium mediated full scale MPT opening, indicative of classical MPT. Transmission electron microscopy suggests a homogeneous mitochondrial population. Complex II substrate (succinate) in comparison to complex I substrate (NADH) induces increased MPT opening. Reactive Oxygen Species induces liver mitochondrial MPT opening and is abrogated by ascorbic acid and -tocopherol. Liver MPT is sensitive to redox modulation. Reducing and oxidizing agents decrease and increase MPT opening respectively. MPT of liver mitochondria show typical pH dependence, acidic and alkaline pH induces MPT closure while, maximal MPT opening and calcium sensitivity was achieved at a pH range of ~7.2-7.4. ATP inhibited, while ADP activated MPT opening. Thus, our study demonstrates that all the major MPT functions in normal liver mitochondria could be determined by simple mitochondrial swelling assay under well-defined conditions, thereby suggesting its application in therapeutic diagnostics.[...] Read More.

Keywords: Mitochondria, mitochondrial permeability transition, swelling assay, oxidants, reductants, calcium, cyclosporin A, pH.

Int. J. Pharm. & Pharmacol. 2010, 1(1), 1-6;

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Research Article

Quality of Brands of Atorvastatin Calcium Tablets marketed in Lagos, Nigeria

Moshood O. Akinleye, Oladipo Idris*, Patricia N. Nwachukwu and Olubukola O. Oyetunde

Abstract: This study investigated the quality of atorvastatin calcium tablets marketed in Lagos, Nigeria, by evaluating and comparing their physico-chemical profiles. Evaluation of physico-chemical parameters viz: uniformity of weight, hardness, friability and disintegration test was carried out according to British Pharmacopoeia. Assay of active ingredient and in-vitro dissolution evaluation were conducted using USP Apparatus 2 satisfying the general conditions for film tablets as stipulated in official books. Tablets and dissolution samples were analyzed using a modification of the validated High performance liquid chromatographic method developed by Stanisz and Lukas. All the three brands met the standards for the physical qualities of a satisfactory tablet, and all had percentage purities within the 90 to 110% range. Only brands AT and CT had released ≥75% of label claim of atorvastatin calcium within 45 min, as specified in the B.P for conventional tablets. Thus, brand BT which had barely released 70% of its label claim at 60 min failed dissolution test. We concluded that out of the 3 brands of immediate-release atorvastatin calcium tablets available in the market at the time of the study, only 2 passed all the pharmacopoeia tests for satisfactory quality. Thus, only these can be interchanged in clinical practice.[...] Read More.

Keywords: Atorvastatin, in-vitro bioequivalence, switch ability, quality, safety.

Int. J. Pharm. & Pharmacol. 2010, 1(1), 1-6;

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Research Article

Synthesis and Biological Properties of Enantiomers of 1-Allyl-4-Hydroxy-6,7-Dimethoxy-2-Oxo-1,2-Dihydroquinoline-3-Carboxylic Acid (1-Ethylpyrrolidin-2-Ylmethyl)-Amide Hydrochloride

Igor V. Ukrainets*, Olga V. Gorokhova, Nidal Amin Jaradat, Ludmila V. Sidorenko

Abstract: Being guided by the methodological principles of "chiral switches", the synthesis of S- and R-enantiomers of 1-allyl-4-hydroxy-6,7-dimethoxy-2-oxo-1,2-dihydroquinoline-3-carboxylic acid (1-ethylpyrrolidin-2-ylmethyl)-amide hydrochloride has been carried out. According to the results of the biological research, it has been found that the ability of the optical isomers obtained to block opioid receptors remains at the racemate level. It is important for future research conclusion – the asymmetrical carbon atom in these compounds is not the site of binding with the target receptor.[...] Read More.

Keywords: amidation, 4-hydroxy-2-oxo-1,2-dihydroquinoline-3-carboxamides, opioid receptors antagonists, "chiral switch"

Int. J. Pharm. & Pharmacol. 2010, 1(1), 1-6;

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Research Article

Synthesis, Structure and Analgesic Activity of 1-(2-Cyanoethyl)- 4-Hydroxy-2-Oxo-1,2-Dihydroquinoline-3-Carboxylic Acid Hydroxy-Alkylamides and Their Derivatives

Igor V. Ukrainets*, Olga V. Gorokhova, Xeniya V. Andreeva, Galina Sim

Abstract: The simple methods for obtaining have been suggested and the synthesis of new hydroxyalkylamides of 1-(2-cyanoethyl)-4-hydroxy-2-oxo-1,2-dihydroquinoline-3-carboxylic acid and their derivatives has been carried out by alcoholic hydroxyl. The peculiarities of the spatial structure of the given group of substances have been considered by an example of 3-isopropoxypropylamide. The research results of the analgesic activity of all the compounds synthesized are given; they confirm the expediency of searching new painkillers among quinoline-3-carboxamides. According to the results of pharmacological tests for in-depth study recommended (3-chloropropyl)-amide of 1-(2-cyanoethyl)-4-hydroxy-2-oxo-1,2-dihydroquinoline-3-carboxylic acid.[...] Read More.

Keywords: 3-aminopropanenitrile, 4-hydroxy-2-oxo-1,2-dihydroquinoline-3-carbox-amides, triethyl methanetricarboxylate, analgesia, pain syndrome.

Int. J. Pharm. & Pharmacol. 2010, 1(1), 1-6;

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Research Article

Antibacterial Screening of Leaves of Wild and Cultivated Olive of Azad Kashmir

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Abstract: Wild and cultivated olive has been used in the treatment of many diseases ethnopharmacologically in Pakistan. In the present manuscript we have demonstrated the antimicrobial effects of various fractions of leaves of Olea cuspidata and Olea europaea. The leaves of O. cuspidata Wall and O. europaea L. (Family: Oleaceae) were extracted successively with four different organic solvents. These crude extracts were assessed for antibacterial activities against eight different bacterial human pathogens that is, Staphylococcus aureus, Bacillus subtilis, Salmonella typhi, Pseudomonas aeruginosa, Klebsiela pneumoniae, Proteus vulgaris, Citrobacter freundii and Streptococcus pneumoniae by using disc diffusion method. The chloroform, ethanol, and methanol crude extracts of leaves of wild and cultivated olive had significant antimicrobial activities on all the bacterial strains tested. The standard reference antibiotic discs, Ciprofloxacin (5 µg) and Erythrocin (30 µg) were used as positive control. The capacity of the extracts and antibiotics were evaluated on the basis of their capacity to inhibit the growth of pathogenic bacteria measured as zone of inhibition. Almost all bacteria showed to be sensible against the antibiotics with the value of zone of inhibition ranging from 25 to 35 mm, while the effectiveness of olive leaves extracts varied from one species to other with zone of inhibition values of 10 to 30 mm. The ethanol and methanol crude extracts of leaves of wild and cultivated olive exhibited prominent activities against all bacteria used in comparison to chloroform extract which had moderate activity against the tested bacteria. Petroleum ether extract have no effect on any of the bacteria tested. Extract obtained with ethanol appeared to be the most effective against all pathogenic bacteria compared to those obtained with other solvents.[...] Read More.

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Int. J. Pharm. & Pharmacol. 2010, 1(1), 1-6;

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