Development and characterization of miconazole nitrate transfersomal gel

Miconazole nitrate (MIC) is an antifungal drug used for the treatment of superficial fungal infections. However, it has low skin permeability. Hence, the basic idea behind the development of such a system, transfersomes is to maintain a sustain release of drug from the dosage form and for target delivery. Miconazole nitrate was formulated as transfersomes, half-life can be increased and the desired effect can be obtained. MIC transfersomes were prepared using a thin lipid film hydration technique. The prepared transfersomes were evaluated with respect to entrapment efficiency (EE%), particle size, and quantity of in vitro drug released to obtain an optimized formulation. The optimized formulation of MIC transfersomes was incorporated into a Carbapol 934 gel base which was for drug content, pH, spreadability, viscosity, in vitro permeation, and in vitro activity. The prepared MIC transfersomes had a high EE% ranging from 65.45% to 80.11%, with small particle sizes ranging from 368 nm to 931 nm. The in vitro release study suggested that there was an inverse relationship between EE% and in vitro release. In 24 hrs the drug release was observed ranging from 79.08% to 88.72%. The kinetic analysis of all release profiles was found to follow Higuchi’s diffusion model. All independent variables had a significant effect on the dependent variables (p-values < 0.05). Therefore, Miconazole nitrate in the form of transfersomes has the ability to penetrate the skin, overcoming the stratum corneum barrier. When the data subjected to zero order and first order kinetics model, a linear relationship was observed with high R2 values for zero order model as compared to first order model and suggested that the formulations followed zero order sustained release

Formulation and in-vitro evaluation of ciprofloxacin HCl floating matrix tablets

Oral drug delivery is the most widely utilized route of administration among all the routes that have been explored for systemic delivery of drugs via pharmaceutical products of different dosage form. Oral route is considered most natural, uncomplicated, convenient and safe due to its ease of administration, patient acceptance and cost-effective manufacturing process. Gastroretentive drug delivery system was developed in pharmacy field and drug retention for a prolonged time has been achieved. The goal of this study was to formulate and in-vitro evaluate Ciprofloxacin HCl controlled release matrix floating tablets. Ciprofloxacin HCl floating matrix tablets were prepared by wet granulation method using two polymers such as HPMC K100M (hydrophilic polymer) and HPMC K15M. All the Evaluation parameters were within the acceptable limits. FTIR spectral analysis showed that there was no interaction between the drug and polymers. In-vitro dissolution study was carried out using USP dissolution test apparatus (paddle type) at 50 rpm. The test was carried out at 37 ± 0.5 0C in 900ml of the 0.1 N HCl buffer as the medium for eight hours. HPMC K100M shows a prolonged release when compared to HPMC K15M. These findings indicated that HPMC K100M can be used to develop novel gastroretentive controlled release drug delivery systems with the double advantage of controlled drug release at GIT pH. On comparing the major criteria in evaluation such as preformulation and in vitro drug release characteristics, the formulation F8 was selected as the best formulation, as it showed the drug content as 99±0.4% and swelling index ratio was 107.14, and in-vitro drug released 61.31±0.65% up to 8 hours. Results indicated that controlled Ciprofloxacin HCl release was directly proportional to the concentration of HPMC K100M and the release of drug followed non-Fickian diffusion. Based on all the above evaluation parameters it was concluded that the formulation batch F8 was found to be best formulation among the formulations F1 to F8 were prepared

CATHARANTHUS ROSEUS: ORNAMENTAL PLANT IS NOW MEDICINAL BOUTIQUE

India possesses a rich biodiversity of the medicinal plants that were still not explored completely. Catharanthus roseus is native to the Indian Ocean island of Madagascar. This herb is now common in many tropical and subtropical regions worldwide, including the southern United States. It is a popular ornamental plant found in gardens and homes across the warmer parts of the world. The need for the novel pharmaceutical products out from the plant has attained a great interest in the present research world due to the cost and the higher side effects that are associated with the chemically manufactured drugs. Catharanthus roseus, which is a potent medicinal plant many of the pharmacological actions. That is used to treat many of the fatal diseases. Alkaloids were the major phytochemical constituent of the above medicinal plant and have different types possessing various medicinal uses. This review highlights the marvelous properties of this plant. Key words: periwinkle, vinca, alkaloids, catharanthus, MadagascarÂ

SIMULTANEOUS ESTIMATION OF DESLORATADINE AND MONTELUKAST IN BULK AND PHARMACEUTICAL FORMULATIONS BY RP-HPLC

A new, simple, precise, accurate and reproducible RP-HPLC method for Simultaneous estimation of Desloratadine and Montelukast in bulk and pharmaceutical formulations. Separation of Desloratadine and Montelukast was successfully achieved on a ECLEPSE XDB C8 (4.6 x 150mm, 5 mm, Make: Waters) or equivalent in an isocratic mode utilizing K2HPO4 buffer (pH: 8.6) Methanol (60:40%v/v) at a flow rate of 0.8 mL/min and elute was monitored at 261 nm, with a retention time of 2.485 and 3.800 minutes for Desloratadine and Montelukast. The method was validated and the response was found to be linear in the drug concentration range of 50 µg/mL to 150 µg/mL for Desloratadine and 50 µg/mL to 150 µg/mL for Montelukast. The LOD and LOQ for Desloratadine were found to be 2.759, 9.195 respectivly. The LOD and LOQ for Montelukast were found to be 2.9091, 9.6970 respectively. This method was found to be good percentage recovery for Desloratadine and Montelukast were found to be 100.00% and 100.00% respectively indicates that the proposed method is highly accurate. The specificity of the method shows good correlation between retention times of standard with the sample so, the method specifically determines the analyte in the sample without interference from excipients of tablet dosage forms. The method was extensively validated according to ICH guidelines for Linearity, Range, Accuacy, Precesion, Specificity and Robustness

Phytochemical Analysis, Antioxidant, Antistress, and Nootropic Activities of Aqueous and Methanolic Seed Extracts of Ladies Finger ( Abelmoschus esculentus

Abelmoschus esculentus L. (ladies finger, okra) is a well-known tropical vegetable, widely planted from Africa to Asia and from South Europe to America. In the present study, we investigated the in vitro antioxidant capacity and in vivo protective effect of the aqueous and methanolic seed extracts of Abelmoschus esculentus against scopolamine-induced cognitive impairment using passive avoidance task and acute restraining stress-induced behavioural and biochemical changes using elevated plus maze (EPM) and forced swimming test (FST) in mice. Our results demonstrated that the pretreatment of mice with aqueous and methanolic seed extracts of Abelmoschus esculentus (200 mg/kg, p.o.) for seven days significantly (P< 0.01) attenuated scopolamine-induced cognitive impairment in the passive avoidance test. In addition, these extracts significantly reduced the blood glucose, corticosterone, cholesterol, and triglyceride levels elevated by acute restraint stress and also significantly increased the time spent in open arm in EPM and decreased the immobility time in FST. It has also been revealed that these extracts showed a significant antioxidant activity and no signs of toxicity or death up to a dose of 2000 mg/kg, p.o. These results suggest that the seed extracts of Abelmoschus esculentus L. possess antioxidant, antistress, and nootropic activities which promisingly support the medicinal values of ladies finger as a vegetable

FORMULATION AND IN-VITRO EVALUATION OF A NOVEL BIODEGRADABLE POLYMER BASED MICROPARTICULATE SYSTEM FOR POTENTIAL COLON TARGETED DRUG DELIVERY

The objective of present study is to design a novel multiparticulate system for colon targeting drug delivery system of cyclophosphamide (CPM) using biodegradable Konjac glucomannan (KGM) as a carrier for colorectal cancer treatment. Glucomannan is a high-molecular weight, water-soluble, non-ionic polysaccharide extracted from the tuber or root of the elephant yam, also known as konjac (Amorphophallus konjac or Amorphophallus rivieri). cyclophosphamide (CPM) has been the only agent with clinically active against colorectal cancer. Different batches of CPM granules were prepared and coated with KGM. Optimized CPM granules (KGM-STMP) were evaluated for flow properties, granular parameters, weight variation and content uniformity. The prepared formulations were subjected for in-vitro drug release studies in simulated gastric and intestinal fluids. It was found that during 2 hr at pH 1.2 HCl (SGF), 3 hr at pH 7.4 phosphate buffer (SIF) only less than 20% of drug was released. The drug release studies was also carried out in simulated colonic fluid (SCF) of pH 6.8 containing β-mannanase in order to mimic the conditions from mouth to colon. Drug release from 5-FU granules coated with KGM-STMP followed diffusion dependent zero order kinetics. Further, report suggested that konjac glucomannan (KGM) was biodegradable and susceptible to the colonic microfloras under anaerobic environments. Spectroscopic, (FTIR), X-ray Diffraction (X-RD) and DSC studies concluded that no polymer-drug interaction was concluded. Accelerated stability studies indicated that no significant changes, in drug release and micrometric patterns for observed when stored at 40± 2ºC / 75±5% RH. Therefore, it was concluded that konjac glucomannan (KGM) is a promising potential carrier for targeting CPM in the vicinity of colon in order to treat colon cancer effectively. Key words: Cyclophosphamide (CPM), Konjac glucomannan (KGM), multiparticulate system, colon targeted

Quantification of sibutramine and its two metabolites in human plasma by LCâESI-MS/MS and its application in a bioequivalence study

Obesity can be considered as a chronic illness of epidemic proportion and its incidents have increased exponentially in recent years. The use of anti-obesity drugs such as sibutramine is somewhat helpful. There is a need to quantify such drugs in biological samples, which is generally quite difficult. In this report, we developed and validated a simple, sensitive and specific liquid chromatographyâtandem mass spectrometry (LCâMS/MS) method for the quantification of sibutramine (SB) and its two metabolites N-des methyl sibutramine (DSB) and N-di desmethyl sibutramine (DDSB) in human plasma. Zorbax SB-C18 (4.6 mmÃ75 mm, 3.5 μm, 80 Ã) analytical column and 5 mM ammonium formate:acetonitrile (10:90, v/v) mobile phase were used for chromatographic separation of SB, DSB and DDSB. Multiple reaction monitoring (MRM) in the positive mode was used to detect SB, DSB and DDSB at m/z 280.3/124.9, 266.3/125.3 and 252.2/124.9, respectively. Liquidâliquid extraction was used for the extraction of analytes and internal standard from human plasma. This method was validated over a linear concentration range of 10.0â10,000.0 pg/mL for SB, DSB and DDSB with correlation coefficients (r) of â¥0.9997. The drug and the two metabolites were stable in plasma samples. The validated method was successfully applied in a bioequivalence and pharmacokinetic study with human volunteers under fasting condition. Keywords: LCâESI-MS/MS, Sibutramine, Human plasma, Bioequivalence, Pharmacokinetic stud

Quantification of desloratadine in human plasma by LC-ESI-MS/MS and application to a pharmacokinetic study

A simple, sensitive, and specific liquid chromatography tandem mass spectrometry (LC-MS/MS) method was developed for the quantification of desloratadine (DL) in human plasma using desloratadine-d5 (DLD5) as an internal standard (IS). Chromatographic separation was performed using an Xbridge C18 column (50 mmÃ4.6 mm, 5 μm) with an isocratic mobile phase composed of 10 mM ammonium formate: methanol (20:80, v/v), at a flow rate of 0.7 mL/min. DL and DLD5 were detected with proton adducts at m/z 311.2â259.2 and 316.2â264.3 in multiple reaction monitoring (MRM) positive modes, respectively. Liquidâliquid extraction (LLE) method was used to extract the drug and the IS. The method was validated over a linear concentration range of 5.0â5000.0 pg/mL with a correlation coefficient of (r2)â¥0.9994. This method demonstrated intra- and inter-day precision within 0.7â2.0% and 0.7â2.7%, and an accuracy within 101.4â102.4%, and 99.5â104.8%. DL was found to be stable throughout the freezeâthaw cycles, bench-top, and postoperative stability studies. This method was successfully applied in the analysis of plasma samples following oral administration of DL (5 mg) in 35 healthy Indian male human volunteers under fasting conditions. Keywords: Mass spectrometry, Desloratadine, Bioequivalence, Pharmacokinetic stud

FORMULATION AND BIOPHARMACEUTICAL EVALUATION OF SUSTAINED RELEASE PELLETS OF BOSENTAN BY PANCOATING METHOD

Objective: The aim of the present study was to formulate sustained release pellets of bosentan by eudragit RL 100 and RS 100, which are the polymers used in the pan coating technique. Methods: The sustained release pellets of bosentan were formulated by pan coating method. The drug was coated on nonpareil seeds along with EudragitRL100 by solution layering technique. Drug loaded pellets were coated with EudragitRS100. The prepared pellets were evaluated for moisture content, drug content, particle size, and in vitro drug release. Stability studies were carried out on the optimised formulations for a period of 6 months. Results: The drug content was in the range of 98.89±0.32. The mean particle size of the drug loaded pellets was in the range of 835 μm. The drug release rate decreased as the concentration of eudragit increased in the pellet formulations. Among the prepared formulations, PC 4 showed 89.35±0.52 drug release in 12 h from a good linear relationship was established between model independent approaches (T25%, T50%, and T100%) and weight gain in coating. This indicated the possibility of extending the drug release by increasing the weight gain in the coating, and hence, it was proposed to extend the drug release for 24 hours. From the prepared pellets, the optimised formulation PC 12 showed a 100.02±0.03 drug release in 24 hours. Furthermore, these pellets were filled into capsules and compared the dissolution studies. The compatibility between drugs and polymers in the drug loaded pellets was confirmed by DSC and FTIR studies. Stability studies indicated that the pellets were stable. Conclusion: The prepared pellets were capable of releasing the drug for 24 hrs to treat the Pulmonary Arterial Hypertension

NEPHROPROTECTIVE, NEPHROCURATIVE ACTIVITY OF MIMOSA PUDICA ROOT AGAINST GENTAMICIN INDUCED NEPHROTOXICITY

Objective: To study nephroprotective effect of ethanolic extract of Mimosa pudica root against Gentamicin induced nephrotoxicity in rats. Methods: After the treatment scheduled period of 21 days, the extent of nephrotoxicity with gentamicin (40 mg/kg), nephroprotection, nephrocurative activity of ethanolic extract of Mimosapudica root was estimated by serum, urine samples. In this study, we assess the serum creatinine, blood urea nitrogen (BUN), total proteins, urine volume, creatinine clearance, in vivo antioxidant parameters like MDA GSH, CAT also.Results: Plant extract of 200 mg/kg, 400 mg/kg and 600 mg/kg in serum creatinine has shown significant decrease ie., up to p&lt;0.001 but had less significant in curative dose (600 mg/kg) ie., p&lt;0.01. Plant extract of 400 mg/kg, 600 mg/kg and curative treatment (600 mg/kg) had shown significanct decrease in BUN and total proteins ie., up to p&lt;0.001 but had less significance in 200 mg/kg ie., p&lt;0.01. Plant extract 200 mg/kg, 400 mg/kg, 600 mg/kg and Curative treatment had shown increased creatinine clearence significance ie., p&lt;0.01. All doses of ethanolic extract of Mimosa pudica root had shown significant decrease in MDA and significant increase in GSH, ie., p&lt;0.001, Plant extract of 200 mg/kg, 400 mg/kg, 600 mg/kg has shown significant increase in catalase up to p&lt;0.05 p&lt;0.01 p&lt;0.001 with respective doses. The histopathology findings supported the results.Conclusion: It is proposed that the nephroprotective, nephrocurative effect of Mimosapudica root ethanolic extract in gentamicin-induced nephrotoxicity may involve its antioxidant and oxidative radical scavenging activities.Â