MOSP - Macao Scientific Publishers

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Impact of Starch Gel on Granule and Tablet Characteristics of the Potent Herbal Extract AM-1

Philip F. Builders*, Patricia Ogwuche, Yetunde Isimi and Olobayo O. Kunle

Abstract: The ability to convert potent herbal medicines into robust tablet will require a good understanding of certain critical factors such as effect of binder concentration on granule particles and tablets properties. In this study, granules of AM-1, a prototype herbal extract has been produced by the wet granulation process of massing and screening using different concentrations of maize starch gel as binder. The effect of the binder concentrations and granule particles’ size on the granules’ flow and moisture uptake characteristics as well as, their effect on the friability and tensile strength of tablets produced with the granules were investigated. The AM-1 granules prepared with the different concentrations of maize starch gel as binder were of variable particulate dimensions. The particle size and size distribution of the granules showed a remarkable binder concentration sensitivity with a shift to larger particles with increasing binder concentrations. The flow of the granules as determined by evaluating their angle of repose and Carr compressibility indices showed enhanced flow relative to the unformulated AM-1. At simulated tropical humidity and temperature conditions, the AM-1 granules exhibited binder concentration sensitivity to moisture uptake. There was also a reduction in the moisture uptake ability of the granulated AM-1 relative to the ungranulated sample. The tensile strength and friability of the AM-1 tablets showed binder concentration and granule particle size sensitivity: the duo increased with increase in binder concentrations as swell as particle size. This study has shown the effects of granulation as well as starch gel concentration on some critical formulation properties of an herbal extract AM-1, obtained by freeze drying the aqueous decoction of a powdered root material. Keywords: Herbal extract AM-1, starch gel, binder concentration, granule properties, tablet properties. [...] Read More.

Keywords: Herbal extract AM-1, starch gel, binder concentration, granule properties, tablet properties.

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Comparative Analysis of Aggressive vs. Conventional Atorvastatin Doses on IL-6 and NO Levels in Acute Myocardial Infarction Patients

Mustafa Kemal BASARALI, Sadık BUYUKBAS, Hayrullah YAZAR*, Aysel KIYICI, Mehmet KAYRAK and Sıddık ULGEN

Abstract: High dose statin medication in acute coronary syndrome cases is a therapy which lowers mortality and morbidity rates. Interleukin-6 (IL-6) is produced in higher amounts in acute myocardial infarction (MI) and facilitates myocardial damage. However, secretion of nitric oxide (NO) is depleted. We aimed to compare the effects of conventional dose (10-40 mg/day) and aggressive dose (80 mg/day) atorvastatin medications on IL- 6 and NO levels in patients with primary percutaneous transluminal coronary angioplasty (PTCA) intervention after acute MI. 50 patients (8 females, 42 males) with the diagnosis of acute MI with ST segment elevation enrolled to the study. Primary PTCA intervention was performed on these patients and consequently either conventional dose (10 to 40 mg/day) or aggressive dose (80 mg/day) atorvastatin medications were given to the patients. Three months later, plasma IL-6 and NO levels were determined and alterations in the groups were evaluated. IL-6 levels decreased from 24.34 ± 12.04 to 11.40 ± 5.79 pg/ ml and from 29.62 ± 17.38 to 12.51 ± 8.95 pg/ml in conventional dose and aggressive dose regimens respectively (p[...] Read More.

Keywords: Atorvastatin, interleukin-6, nitric oxide, myocardial infarction.

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Utilizing Fluorine-19 NMR for Accurate Measurement of Efavirenz in Serum and Pharmaceuticals

Mojtaba Shamsipur*, Masoumeh Sarkouhi, Jalal Hassan and Soheila Haghgoo

Abstract: 19F NMR provided a highly specific tool for identification of efavirenz in human serum and pharmaceutical preparations as well as a suitable analytical technique for their absolute quantification. The method is based on the integration of appropriate signals of efavirenz and potassium fluoride, as an internal standard. The proposed method is simple and reliable, but when it is used without any sample pretreatment, there is a manipulation of large sample volumes and lengthy analysis time. The calibration curve for efavirenz in human serum was linear over the range of 0.8 to 1000 mg L−1, with detection limit of 0.3 mg L−1. The mean error on human serum samples ranged from about - 4 to -6%, with relative standard deviations of[...] Read More.

Keywords: Efavirenz, 19F NMR analyses, HIV, serum, pharmaceuticals.

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The Role of Glycyrrhizin in Modulating Secretory Component Expression in Caco-2 Cells

Jin-long Fu, Yu-rong Wang, Ying Zhou and Pei Liu*

Abstract: The aim of this study was to investigate whether glycyrrhizin, with steroid hormone-like effects, can upregulate expression of secretory component (SC) in human colonic epithelial Caco-2 and to explore its underlying mechanism. Cultures of Caco-2 were exposed to glycyrrhizin. Free SC in culture supernatants, SC protein, and SC mRNA expression were measured by enzyme-linked immunosorbent assay (ELISA), western blot, real-time PCR, respectively. Cultures of Caco- 2 were exposed to RU486, a glucocorticoid receptor (GR) antagonist, combined with glycyrrhizin or dexamethasone (DEX), SC protein and SC mRNA expression were examined. Glycyrrhizin dose-dependently upregulated free SC in culture supernatants, SC mRNA and protein expression of SC (p[...] Read More.

Keywords: Licorice, glucocorticoid, polymeric Ig receptor, glucocorticoid receptor.

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Factors Influencing Potential Drug-Drug Interactions in Pulmonology Patients: Age, Hospital Stay, and Polypharmacy

Mohammad Ismail, Zafar Iqbal*, Muhammad Bilal Khattak, Arshad Javaid and Tahir Mehmood Khan

Abstract: The objective of the study was to identify prevalence, types and predictors of potential drug-drug interactions (pDDIs) in pulmonology ward and to report common interactions. Medical records of 400 randomly-selected patients were reviewed for pDDIs using Micromedex Drug-Reax software. Logistic-regression was applied to determine predictors of pDDIs. We identified 126 interacting-combinations that encountered in total 558 pDDIs with median number of 01 pDDI per patient. Overall 45% patients had at least one pDDI; 24.25% were having at least one major pDDI, and 36% patients had at least one moderate pDDI. Among 558 identified pDDIs, most were of moderate (53.6%) or major severity (34%); good (74.2%) or fair (16.3%) type of scientific-evidence; and delayed onset (70%). Top 15 common pDDIs included 6 major, 7 moderate and 2 minor interactions. There was significant association of the occurrence of pDDIs with patient with age of 60 years or more (p[...] Read More.

Keywords: Drug-drug interactions, potential drug-drug interaction, prescriptions screening, drug related problems, clinical pharmacy.

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Understanding the Knowledge Gap in Antimalarial Treatments: A Study of Self-Medication Trends Among Women in Nigeria

Jombo G. T. A.*, Mbaawuaga E. M. , Denen Akaa P., Alao O. O., Peters E. J., Dauda M. A., Okwori E. E., Akosu T. J., Etukumana E. A. and Yaakugh J. B

Abstract: Correct knowledge of current antimalarial drugs available for malaria treatment by Nigerians has a significant impact on the overall success of the ongoing national malaria control programme. This is as a result of a large segment of the communities, who more often than not, rely on self medications or as care givers influence the choice drugs for malaria treatment for their wards. The study was therefore set up to ascertain the types of drugs used for self medication of malaria among adult women in Makurdi city. The study was cross-sectional in nature involving adult women who were selected from households using systematic sampling methods. Quantitative information such as age, educational level, marital status, occupation and knowledge of malaria were obtained using structured and semi structured questionnaires, while qualitative information was obtained using focussed and in-depth group discussions to complement quantitative data. Those aware of existence of malaria were 97% (2,013/2075) with no significant age difference (P > 0.05) while 3.0% (62/2,075) with no knowledge of malaria all had no education (P < 0.001). There was a strong correlation between low economic status, low educational level and unemployment, and self medications for malaria (RR = 1.4 - 1.55). Several drugs with no antimalarial properties were mentioned by the respondents with the factors earlier stated still playing significant roles; and little or no mention was made of the artemisinin-based combination therapy (ACT) by the same group (P < 0.05). There should be a renewed sensitization and public awareness about the current trend in the control of malaria with special emphasis on the use of ACT; also introduction of home managers of malaria for commencement of intermittent preventive treatment should be considered a priority.[...] Read More.

Keywords: Drugs, self-medication, malaria, adult women.

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Chemical Composition and Antifungal Properties of Mentha piperita Essential Oil: Insights from Capillary Gas Chromatography Analysis

M. Moghtader

Abstract: The antifungal activity of Mentha piperita L. essential oil and its comparison with synthetic menthol on Aspergillus niger growth have been determined in vitro. The chemical compositions of essential oil of M. piperita provided from the aerial parts of plants grown in a village in Kerman Province in June 2012 were determined. The sample was cleaned and then dried in the shade. Essential oil was made by hydro-distillation method and analyzed by capillary gas chromatography (GC) using flame ionization (FID) and capillary gas chromatography coupled mass spectrometry (GC/MS). The main oil content from the plants of M. piperita was 3.26% (v/w). Twenty three (23) compounds were identified in the essential oil of M. piperita, making 96.25% of the total oil. The major components were menthol (38.33%), menthone (21.45%) and menthyl acetate (12.49%). For study of antifungal activity, the essential oil was tested against A. niger (strain PTCC = 5223) by disc diffusion method via average inhibition zone. The results showed that essential oil from M. piperita at 1 and 1/2 oil dilutions exhibited a strong antifungal activity than gentamycin (8 mg/ml) antibiotic on A. niger and exhibited a strong synthetic menthol at 10% dilution. The relative high amount of menthol and menthone in the M. piperita essential oil showed that they could display antifungal activity.[...] Read More.

Keywords: Mentha piperita L., Aspergillus niger, menthol, antifungal activity.

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Evaluating the Efficacy of Xylazine, Ketamine, and Atropine in Sheep for Veterinary Pharmacology Instruction

Rogelio Cruz Cruz*, Armando Cuesta Guillen and Daniel Hussien

Abstract: The current research was conducted with the objective of developing a practical laboratory of Veterinary Pharmacology course, specifically for the purpose of evolving a practical part of the theory in the chapter of general anesthetics. The practice of the evaluation of drugs acting on the central nervous system in this discipline has difficulty with the choice of experimental model, because sometimes there are no laboratory animals such as rats, mice or rabbits; however, it is possible to use larger animals such as sheep. In this paper, we demonstrated that sheep is a suitable experimental model for demonstrating the action of drugs that produce sedation and anesthesia. The effects by the action of xylazine, ketamine and atropine can be produced in about 60 min which corresponds to time allotted in a teaching practice. Therefore, the authors recommended other sister colleges in Ethiopia and elsewhere in the world to use sheep as experimental model for demonstration of general anesthesia for their students.[...] Read More.

Keywords: Anesthetics, drugs, central nervous system, sheep.

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Formulation and Pharmacological Assessment of Indomethacin Tablets Using Solidified Reverse Micellar Solutions: Implications for Pain Management

Salome Amarachi Chime*, Ikechukwu V. Onyishi, Mumuni A. Momoh and Anthony A. Attama

Abstract: The aim of the present study was to evaluate in vivo the anti-inflammatory, antinociceptive and ulcerogenic properties of indomethacin tablets based on solidified reverse micellar solution (SRMS). SRMS consisting of mixtures of phospholipid (Phospholipon® 90H) and triglyceride (Softisan® 154) were prepared in the ratios of 1:1, 2:1 and 1:2, respectively. SRMS based tablets containing 75 mg of indomethacin each were prepared using validated plastic mould. The physicochemical properties of the tablet formulations were studied using both official and unofficial tests. Anti-inflammatory, analgesic/antinociceptive and ulcerogenic properties of indomethacin tablets based on SRMS were studied. The results showed that the physicochemical properties of the tablet formulations were significantly affected by the composition/ratio of the lipid matrix used. The softening time in SIF ranged from 53.7 ± 0.5 to 102.6 ± 0.5 min. Results of analgesic/antinociceptive properties showed that indomethacin tablets formulated with the SRMS 1:1 had an increase in pain reaction time at 7 h significantly (p < 0.05) different from the results exhibited by tablets formulated with the lipid matrices, SRMS 1:2 and 2:1 and the reference, which showed a decrease in pain reaction time at 7 h. Indomethacin tablets based on SRMS had good anti-inflammatory properties and also inhibited the ulcerogenicity of indomethacin by 70 to 80%. Therefore, indomethacin tablets based on SRMS could be used for improved oral bioavailability of indomethacin and to enhance patient’s compliance due to inhibition of gastric irritation effect of this drug.[...] Read More.

Keywords: Non steroidal anti-inflammatory drugs (NSAIDS), solidified reverse micellar solutions (SRMS), tablets, ulcerogenicity, antinociception, lipids.

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Toxicity Assessment and Blood Glucose Regulation by Cissampelos mucronata Leaf Extracts in Wistar Rats with Streptozocin-Induced Diabetes

Tanko, Y. *, Yaro, A. H., Isa, A. I, Yerima, M., Saleh, M. I. A. and Mohammed, A.

Abstract: Preliminary phytochemical screening of the ethanol leaves of Cissampelos mucronata revealed the presence of reducing sugars, cardiac glycosides, resin, tannins, saponins, glycosides, flavonoids, glycerin and steroids. The median lethal dose (LD50) in rats is greater than 5000 mg/kg body weight intaperitoneally. The hypoglycemic effect of ethanol extract of C. mucronata was also investigated in Streptozocin - induced diabetic rats. Single intraperitoneally administration of the extract at the doses of 200, 400 and 800 mg/kg. There was a significant decreased (p[...] Read More.

Keywords: Cissampelos mucronata, hypoglycemic activity, streptozocin, diabetes.

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