Journal of Pharmacy Research最新文献

Background

Famotidine (FMD) is a histamine H₂-receptor antagonist that inhibits stomach acid production, and it is commonly used in the treatment of peptic ulcer disease and gastro esophageal reflux disease. The main objective of the present investigation is to develop a rapid, precise and accurate stability indicating ultra performance liquid chromatographic method for the analysis of pharmaceutical formulations.

Methods

Waters-Alliance Ultra Performance Liquid Chromatographic system equipped with Auto Sampler, PDA detector, detection at a wavelength of 297 nm, Symmetry C18 (2.1 × 50 mm, 1.7 μm, Make: BEH) column and mobile phase of potassium dihydrogen phosphate buffer of pH = 7.0 and acetonitrile in the ratio 40:60 v/v at a flow rate of 0.2 per minute was used for the assay of famotidine in tablets by a reverse phase ultra performance liquid chromatographic method (RP-UPLC).

Results and discussion

The system suitable parameters such as tailing factor and theoretical plate count were found to 1.48 and 8896 respectively under the optimized experimental conditions. The retention time of the compound was observed to be 0.595 min. The developed method was proved to be precise and accurate by calculating percent of relative standard deviation (% RSD is equal to 0.900%) for six replicate injections and mean recovery (99.8%) of famotidine at three different concentration levels. Linearity between peak area and concentration was found to be 5.0–20.0 μg/mL. The limit of detection (LOD) and limit of quantitation (LOQ) values were found to be 0.006 μg/mL and 0.02 μg/mL respectively. The drug was found to be stable (81.37%–93.44%) under different degradation conditions like acid (0.1 N HCl), alkali (0.1 N NaOH), peroxide (3% H₂O₂), photolytic and thermal.

Conclusions

The developed method was found to be simple, rapid, repeatable, reproducible, robust, rugged and economic hence it can be used as a new analytical method for the analysis of pharmaceutical formulations in any pharmaceutical industries.

Objective

To develop a simple, sensitive and selective LC–MS–MS method for the simultaneous determination of amoxicillin and clavulanic acid in human plasma using amoxicillin D4 and ampicillin as internal standard (IS).

Method

Amoxicillin and clavulanic acid in plasma were concentrated by solid phase extraction and chromatographed on a C18 column using a mobile phase of acetonitrile: 2 mM ammonium acetate (80:20 v/v) under isocratic condition. Quantitation was performed on a triple quadrupole mass spectrometer by employing electrospray ionization technique and operating in multiple reaction monitoring (MRM) and negative ion mode with mass transitions 364.00/223.00, 198.00/136.00, 368.00/227.00 and 347.90/304.00 for Amoxicillin, Clavulanic acid, Amoxicillin D4 and Ampicillin respectively.

Results

The method was validated over a linear range of 50.43–31500.68 and 25.28–6185.18 ng/mL for amoxicillin and clavulanic acid respectively. The Lower Limit of Quantitation (LLOQ) were 50.43 and 25.28 ng/mL for amoxicillin and clavulanic acid respectively. Inter-batch and intra-batch coefficient of variation across three validation runs (LLOQ, LQC, MQC1, MQC and HQC) was less than 3.55% and 3.07% for amoxicillin and clavulanic acid respectively.

Conclusion

The method was validated and was suitable for the quantitation of amoxicillin and clavulanic acid from plasma samples in a pharmacokinetic study.

Aims

The work is aimed to formulate aqueous nanodispersion of aceclofenac Nanostructured Lipid Carriers (NLC) by using modified hot sonication method and to prepare NLC based gel for topical delivery of aceclofenac.

Methods

The lipids incorporated in the study were Compritol 888 ATO and Miglyol and the emulsifier/stabilizer used was Polysorbate 80. The formulations were optimized by using 3 factor, 3 levels, Box–Behenken design. The independent variables were combination of lipids (% w/w), concentration of emulsifier (% w/v), lipid drug ratio and the response variables were particle size, percentage entrapment and drug release after 12 h. The formulations were also characterized for particle size, entrapment efficiency, drug loading and depression in melting point.

Results

The DSC, FTIR analyses were performed to characterize the state of drug and lipid modification. Shape and surface morphology were determined by SEM which showed spherical shape of the formulations. Further the formulations were evaluated for in vitro drug permeability study, rheological properties, skin irritation, pharmacodynamic and stability studies.

Conclusion

The pharmacodynamic characteristics of aceclofenac NLC gel with reference to the conventional gel were compared by using Carrageenan induced rat paw edema method. The study showed the promising and stable alternative form for the aceclofenac for topical application.

Background

Jawarish-e-Jalinoos is a Unani poly herbal compound formulations listed under the Majooniath category in National Formulary of Unani Medicine (NFUM), Part-I. It is used in various ailments such as Zof-e-Aza-Raeesa (weakness of the principle organs like brain, heart and liver), Zof-e-Meda (weakness of the stomach), Nafkh-e-Shikam (flatulence in the stomach) and Khafqan (palpitation).

Aim

Present study was undertaken to develop the Standard Operating Procedure for the preparation of drug Jawarish-e-Jalinoos and to evaluate its pharmacopoeial standards.

Methods

To prepare the drug in different batches at laboratory scale using 18 single drugs were used. The drug was prepared as per the method prescribed in NFUM. To evaluate the pharmacopoeial standards and quality control parameters pharmacognostical, physico-chemical and WHO methods were followed.

Results

Microscopical studies show the presence of various characteristic features of single drugs used in the preparation viz., vessels elements with reticulate, scalariform, pitted; perisperm cells with angular and bulbous projections; pollen grains; fibre like sclereids; septate fibres; starch grains of various shapes and sizes; stone cells with horse shoe shaped thickening; druses of calcium oxalate crystals. The physico-chemical study shows presence of moisture content 19.87%, ash content 0.8% and acid insoluble ash 0.20%. Alcohol and water soluble extractive value of the drug obtained were 40.80% and 62.78% respectively. Other parameters such as heavy metals, microbial load, aflatoxins and pesticidal residues were found within the permissible limit.

Conclusion

The evaluated data from this study will be helpful in laying down the SOP's and pharmacopoeial standards for the drug Jawarish-e-Jalinoos.

A bioassay-guided fractionation and chemical investigation of the whole plant of Premna tomentosa resulted in the isolation and characterization of premnalin (1), along with the known compounds coniferaldehyde (2), syrangaldehyde (3), acetoxy syrangaldehyde (4), lupeol (5), betulin (6), 2-(4-methoxyphenyl)-2-butanone (7), icetexatriene-1 (8), icetexatriene-2 (9). Their structures were established on the basis of extensive spectroscopic such as (IR, MS, 2D NMR) data analysis and by comparison with the spectroscopic data reported in the literature, premnalin (IC₅₀: 12.11 μg/mL) & (SC₅₀: 20.58 μg/mL), acetoxy syrangaldehyde (IC₅₀: 18.41 μg/mL) & (SC₅₀: 20.83 μg/mL) displayed potent α-glucosidase inhibition and free radical scavengers (DPPH).

Background/Objectives

Bitter melon (Momordica charantia L., MC) has been used as a traditional remedy in diabetics due to its hypoglycemic activity. However, its anti-hyperglycemic effect and antiglycation activity have been demonstrated in vitro and in animal experiments, but not in a long-term clinical study. The aim of this study was to investigate the effect of bitter melon on long-term glycemic control and glycation status in type 2 diabetic patients.

Methods

This study was a two-arm, parallel, randomized, double-blinded, placebo-controlled trial in which type 2 diabetic patients were randomized to continuously take either 6 g/day of MC dried-fruit pulp containing 6.26 ± 0.28 mg of charantin (N = 19) or placebo (N = 19) for 16 weeks.

Results

After 8 and 16 weeks of the treatment, the reduction of A1C from baseline in the MC group was greater than that of the placebo group (0.25 ± 0.12%, P = 0.042 and 0.31 ± 0.15%, P = 0.044, respectively). In addition, the MC group showed a significant decline of total advanced glycation endproducts (AGEs) in serum after 16 weeks of the intervention. The mean difference between both groups was 8.22 ± 3.58 × 10³ AU/g protein (P = 0.028). The levels of alanine aminotransferase (ALT), aspartate aminotransferase (AST) and serum creatinine (Cr) did not change from baseline in each group and were not different between the two groups. None of participants experienced serious adverse events.

Conclusions

It is possible that this herb is beneficial not only on glycemic control, but also on potential systemic complications of type 2 diabetes mellitus.

Novel exploiting to the understanding of conventional medicine was followed by the findings of many unique secondary metabolites and its biological property and is highly required for treating of many endemic diseases. The plants have been a long background in ethno pharmacological knowledge for treatment of endemic and non-endemic diseases. Such plants are traditionally used in different form of paste, extraction and powder to treat seasonal diseases. Nowadays main uses of some medicinal plants have been a great deal with cure and control various chronic diseases such as cancer, AIDS, hepatitis, neurogenic disorders and acute kidney diseases. Cancer is molecular dysfunction and disarrangement in DNA base pairs it leads to change the human physiological and biochemical behavior of the system. Apoptotic mechanisms are regulating by two distinct pathways in which basic creeds perform in common to all eukaryotes. The key components in apoptosis especially mitochondrial intracellular organelles are identified (DNA, protein and ATP, Ca²⁺). These components control the next cellular binder step and participate in effecting cell suicide mechanisms. The diverse aspects of mitochondria involved in apoptosis include dealing with other proceedings such as release of protein or enzymes to effective for cell death. In these mechanism plants and related natural products using alternative therapeutic management, very less toxicity and cost benefits. Plant extracts and its biomass has revealed the existing of various pharmacologically active compounds like steroids, polyphenols, polysaccharides, saponins, alkaloids, tannins and terpenoids. The reliable natural products are acting as high sources for anticancer drugs. The natural derived compounds are the prolongation of life span of the zeolites and decrease of malignancy cell formation in the cellular system.

Aim

The present study was aimed to evaluate the antioxidant property and hypoglycemic activity of aqueous and ethanolic extracts of aerial parts of Grewia serrulata DC (AEGS & EEGS) in normal and hyperglycemic male Wistar Albino rats.

Methods

The antioxidant property was evaluated both in vitro and in vivo model using standard procedures. The hypoglycemic activity was evaluated by normal glucose and oral glucose tolerance test (NG-OGTT) method and by acute administration of AEGS and EEGS extracts at doses 200 and 400 mg/kg body wt p.o in Streptozotocin (STZ) induced hyperglycemic rats.

Results

The ethanolic extract of Grewia serrulata DC exhibited strong free radical scavenging activity as evidenced by their low IC₅₀ values in DPPH (1,1-diphenyl-2-picryl-hydrazyl) (9.16 ± 1.05 μg/ml), Superoxide (35.59 ± 1.6805 μg/ml) and nitric oxide (151.80 ± 1.79 μg/ml) methods. In in vivo study, treatment with ethanolic extract at both doses shows a significant dose dependent increase (p < 0.05 to p < 0.001) in the levels of superoxide dismutase (SOD) and Catalase (CAT) and a significant decrease (p < 0.05 to p < 0.001) in the levels of Thiobarbituric acid reactive substances (TBARS), when compared to CCl₄ treated control in both liver and kidney. In NG-OGTT method EEGS shows reduction in glucose levels in normal rats and glucose loaded hyperglycemic rats and in STZ-induced hyperglycemic rats.

Conclusion

EEGS was found to possess strong antioxidant activity and good hypoglycemic activity compared to that of AEGS.

Objective

In the present study series of selected coumarin derivatives (CDs) were assessed for their inhibition of growth of Helicobacter pylori (H. pylori) and its related urease. The selected CDs were docked in-silico onto the ligand binding site of H. pylori urease.

Methods

The anti-H. pylori studies were carried out using agar diffusion assay and minimum inhibitory concentrations (MICs) were calculated by microbroth dilution method. Urease inhibitory activity of H. pylori using selected CDs was determined by Berthelot reaction and their IC₅₀ values were calculated using GraphPad Prism version 6.00 while, docking studies were performed by ArgusLab 4.0.1.

Result

The results obtained indicate that, most of the CDs showed considerable anti-H. pylori activity (MIC range of 10–40 μg/ml) as well as significant inhibition of H. pylori urease (IC₅₀ of 48.90–72.56 μM). To a greater extent, the in-silico results were in agreement with in-vitro results of inhibition of H. pylori urease.

Conclusion

The present investigation may find applications in designing and developing a novel, safe and effective anti-H. pylori agents using coumarin scaffold.

Aim

Scrutinize the phytochemical, antioxidant and acute toxicity of Agaricus bisporus extract (ABE) and A. bisporus loaded chitosan nanoparticles (ABCNPs).

Methods

Phytochemical such as total phenol and flavonoid, and terpenoid, alkaloid, steroid, carbohydrate, tannins and proteins where determined. The antioxidant activity such as DPPH, ABTS and reducing power of ABE and ABCNPs where estimated by spectrophotometry assay. The estimation of total phenolic content was determined by Folin–Ciocalteu method. The acute toxicity studies of ABE and ABCNPs were investigated in male Sprague Dawley rats. Results: In the DPPH, ABTS^•+ and reducing power scavenging assays, of ABE displayed significant antioxidant activities with the inhibition values of 27.78, 27.62 and 81.97% and ABCNPs inhibition values 27.78, 27.62 and 78.13% respectively. The reducing power of the extract increased dose-dependently, and the ABE and ABCNPs reduced the most Fe³⁺ ions. The amount of total phenolics was reported 1 g of sample contains 8.19±1 mg of gallic acid and total flavonoid analysis by the assay of aluminum chloride spectrophotometric reported 1 g of sample contains 10.3 ± 1 mg of quercetin in ABE and ABCNPs. The acute toxicity was found bellow 2747.25 mg/kg b.w. in ABE and 3178.86 mg/kg b.w. of ABCNPs.

Conclusion

The white button mushroom A. bisporus could be considered as a dietary natural food products with antioxidant activity. Thus our results provide evidence that AB and ABCNPs proves to have a potent antioxidant and intermittent therapy against cancer.