Harinath N. More

Evaluation of antiulcer and antioxidant activity of Barleria gibsoni Dalz. leaves

Background: Peptic ulcer is a digestive disorder most commonly found in clinical practice. Given the many side effects of modern medicine, the initial acquisition of fewer side effects, and medication of indigenous drugs, it should be considered as a better alternative for the treatment of peptic ulcer. Objective: To assess antiulcer and antioxidant activity of ethanol extract of Barleria gibsoni (EBG) Dalz. leaves in ulcer-induced rats and in vitro antioxidants method, respectively. Materials and Methods: Ethanol EBG was screened for antiulcer activity in pylorus ligation-induced ulcer models in Wistar rats. In vitro antioxidant activity of the extracts was tested using 2,2-diphenyl-1-picrylhydrazyl (DPPH), nitric oxide (NO) radical scavenging activity. Total phenol and flavonoid content in the extracts were determined spectrophotometrically. Results: Oral administration of ethanol extract of leaves at doses of 250, 500 mg/kg p.o. reduced significant gastric lesions induced by pylorus ligation-induced ulcer as compared to standard omeprazole (20 mg/kg p.o.). The IC50values were found to be 150 μg/mL in leaves extract. The ethanol extracts showed good antioxidant capacity in DPPH radical scavenging assay and NO radical scavenging activity when compared to standard. The total phenolic content using Folin–Ciocalteu reagent estimated in 1 mg of leaves extracts was 368 μg and 481 μg with gallic acid equivalent and also the total flavonoid content found to be 240 and 410 μg, respectively, with quercetin equivalence. Conclusion: These findings suggest that the leaves of B. gibsoni possessed antiulcer potential and antioxidant compared to standard. This is the first ever report of antiulcer and antioxidant activities in B. gibsoni (Acanthaceae).

Room temperature stabilization of human serum albumin by vacuum foam drying

This article characterizes the activities required to launch a new pharmaceutical molecule into the market, summarizes studies that have attempted to pinpoint the research and development costs incurred per approved new molecule, and analyzes the various critiques levied against published R&D cost estimates. It finds that by any reckoning, R&D costs per approved molecule have risen sharply over time, most likely at a rate of approximately 7 percent per year after stripping out the effects of general economic inflation.A is a newer NSAID, used in treatment of osteoarthritis, rheumatoid arthritis and ankylosing spondylitis. Aceclofenac has shorter biological half-life around 4 h which makes it suitable for modified release to improve bioavailability and to reduce dosing frequency. Present work was aimed to develop and evaluate aceclofenac modified release (Triple Layer Tablet) TLT following direct compression technique using natural and synthetic polymers. Aceclofenac TLT containing immediate-releaselayer (IM) as first layer, controlled-release-layer (CR) as second layer and ethyl cellulose layer as barrier-layer (BL) were prepared. IM was optimized by D-optimal design where 16 formulations (IM1 – IM16) were developed by using super disintegrating agents like mannitol and SSG. CR was optimized by 32 full factorial design and 9 batches (CN1–CN9 & CS1–CS9) were developed using natural and synthetic polymers like guar gum, xanthan gum and HPMC K100 CR, HPMC K100 LVCR respectively. Drugpolymers compatibility was evaluated by Infrared spectroscopy, where all compositions were found compatible without any interaction. All formulations were evaluated for various post-compression parameters like disintegration time (DT), swelling index, hardness, friability and weight variation etc., and results were found in desirable range. IM and CR formulations were evaluated for drug release behavior in pH 6.8 phosphate buffer and best release compositions among batches were chosen to prepare TLT with BL to modify the release. Among IM formulations least DT was found in IF9 with 90.86% drug release in 10 min 21 sec so, IF9 was claimed as best composition. Among CR formulations the best compositions found were CN3 and CS6 with Time at 47.38 % and 26.42% drug release around 8 h respectively and, were then developed as triple layered tablets with IF9 where drug release was extended up to 24 h.H compounds have received considerable attention owing to their variety of biological activities, especially as inhibitors of PDE5 extracted from human platelets, HIV-1 reverse transcriptase, human EPK2, cyclin-dependent kinas. Also, heterocyclic nitrogen compounds are indispensable structural units for medicinal chemists and used as antibiotics, anthelmintics, antiviral, antidepressant, and anti-inflammatory. In view of these observations we evaluate some new poly hetero cyclic compounds which were previously synthesized according to for their analgesic, anti-inflammatory and anti-microbial activities in comparison to some reference drugs. Pyrimidines present an interesting group of compounds many of which possess wide-spread pharmacological properties such as antidepressant, antimicrobial, anticancer, and anticonvulsant activitiesM drugs combination is a promising strategy in biomedical fields, such as cancer chemotherapy, tissue engineering. The multi-drug system enables to be delivered with multiply targets and exhibits the additive or synergistic effects of drugs. However, the specific distinct drug release kinetics of the multiply drugs are required to meet the clinical needs, especially in the combined therapy of tissue regeneration and tumor chemotherapy. In order to deliver the individual drug at optimal dosages, the release behaviors of each drug in multi-drug systems should be controlled independently. Therefore, two kinds of nanoparicles with core-shell structure (PVP/PLGA and PCL/PLGA) were fabricated by coaxial electrospray in this paper. Each kind of nanoparticles can both encapsulate the hydrophilic rhodamine B and hydrophobic naproxen in one single step efficiently. The monodisperse size distribution as well as the desired core-shell structure was observed. These two multi-drug systems with dual drug loaded exhibited different distinct release profiles, attributing to the distinct core-shell structures of nanoparticles and the difference of two drugs in hydrophilic properties. Meanwhile, the release profiles of encapsulated drugs with different amount were investigated as well. The drug release behaviors were dominated by the following processes: water penetration, surface drug release, outer drug diffusion with shell polymer erosion, inner drug diffusion and nanoparticle collapse. The results suggested that the distinct release kinetics of multiply drugs fabricated by coaxial electrospray can be obtained and tuned to fulfill the clinical requirement in combination therapy.Aspirin suppositories are in commercial use, suffer with side effects such as irritation, burning sensation, rectal hemorrhage. The aim of the present work is to formulate aspirin nanoparticles loaded suppositories and to perform In vitro investigation for the prepared suppositories. Initially aspirin-chitosan nanoparticles were prepared by ionic gelation method and the nanoparticles evaluated for different In vitro evaluation studies; based on results the best formulation was selected and in order to know the diffusion efficiency, different compositions of aspirin glycerogelatin suppositories were prepared and subjected to various In vitro evaluation studies and best composition was selected. From the previously performed evaluation studies best formulation from aspirin nanoparticles incorporated in to selected glycerol gelatin bases and evaluated for In vitro characteristics. The results indicates that formulation Fa9 Aspirin nanoparticles were proved to be best formulation with 88.3±1.1 % of drug release at the end of 24hr, with zero drug release. In vitro characterization performed for aspirin suppositories indicates that Fs2, Fs4, Fs9 and Fa11 was proved to be best composition with highest percentage of drug release at the end of 60 minutes with 98.06±1, 99.3±0.45, 97.6±1.8 and 97±1 drug release and other characteristic studies performed indicates that all formulation are ideal characteristics. Previously selected bases composition used for the loading of nanoparticles based on displacement value results indicates that drug release appears with a lag phase initially and controlled for a period of 24hr.Orally dissolving tablets (ODT) provides a patient compliance solution for patients swallowing difficulties. Foam granulation is a newer technique that promises better distribution of the granulating system and better properties of the produced tablets. Aceclofenac (anti-inflammatory and analgesic) was selected as the model drug. The poor hydrophilicity of the drug results in variable dissolution rate and poor bioavailability. In this study, we tried to prepare aceclofenac ODT using the newer technique and various types of disintegrants, glidants, and lubricants. The resulted tablets were evaluated for hardness, friability, weight variation, in vitro disintegration time, and wetting time. All the formulation showed acceptable disintegration time. It was concluded that the prepared aceclofenac ODT by foam granulation technique using selective range of excipients can provide a dosage form with better patient compliance and effective therapy.

Isolation, characterization, and evaluation of Cassia fistula Linn. seed and pulp polymer for pharmaceutical application.

Introduction: Present work, is an effort toward exploring the potential of Cassia fistula Linn. seed gum as an extended release polymer and laxative. While, C. fistula pulp polymer has evaluated as suspending agent. Materials and Methods: For extended release application, total five batches (F1-F5) were prepared by varying the ratio of drug:polymer as 1:1, 1:2, 1:3, 1:4, and 1:5, respectively. The granules were prepared by wet granulation method and further evaluated for micromeritic properties such as angle of repose (θ), Carrs compressibility index (CCI), and Hausners ratio. Further compacts were evaluated by hardness, thickness, swelling index, in-vitro dissolution, and so on. Laxative activity was evaluated by administration of seed polymer (100 mg/kg) alone or in combination with bisacodyl (2.5 mg/kg) in 1% Tween 80. Zinc oxide suspension was prepared by varying the concentration of C. fistula pulp polymer and compared with suspension made by use of tragacanth, sodium carboxymethyl cellulose and bentonite. Results: Result showed that granules were free flowing, while the compact extended the drug release up to 10 h (72.84 ± 0.98; batch F5) and followed Higuchi matrix release kinetics. This extended release might be due to the formation of polyelectrolyte complex because of gluco-mannose in seed gum. Result of in-vivo laxative activity showed that seed polymer reduced faeces weight after 24 h compared to control (P < 0.01). Conclusions: Pulp polymer showed good sedimentation volume, but alone fails to stabilize the suspension for a longer period, so it could be useful in combination with other suspending agents and can be useful as novel excipient.

Lung delivery of nanoliposomal salbutamol sulphate dry powder inhalation for facilitated asthma therapy

Abstract The motive behind present work was to discover a solution for overcoming the problems allied with a deprived oral bioavailability of salbutamol sulfate (SS) due to its first pass hepatic metabolism, shorter half-life, and systemic toxicity at high doses. Pulmonary delivery provides an alternative route of administration to avoid hepatic metabolism of SS, moreover facilitated diffusion and prolonged retention can be achieved by incorporation into liposomes. Liposomes were prepared by thin film hydration technique using 32 full factorial design and formulation was optimized based on the vesicle size and percent drug entrapment (PDE) of liposomes. Optimized liposomal formulation exhibited an average size of about 167.2u2009±u20090.170u2009nm, with 80.68u2009±u20090.74% drug entrapment, and 9.74u2009±u20091.10u2009mV zeta potential. The liposomal dispersion was then spray dried and further characterized for in-vitro aerosol performance using Andersen Cascade Impactor. Optimized liposomal formulation revealed prolonged in-vitro drug release of more than 90% up to 14u2009h following Higuchi’s controlled release model. Thus, the proposed new-fangled liposomal formulation would be a propitious alternative to conventional therapy for efficient and methodical treatment of asthma and alike respiratory ailments.

Formulation and Evaluation of Herbal Lipstick using Lycopene Extracted from Solanum lycopersicum L

Herbal cosmetics are gaining popularity as nowadays most women prefer natural products over chemicals for their personal care and to enhance their beauty. Compared to other beauty products, natural cosmetics are safe to use. Synthetic colouring agents may cause allergic reactions and were found to be carcinogenic. Aim of present study was to formulate and evaluate herbal lipstick using lycopene extracted from Solanum lycopersicum L. as a colouring agent. Along with lycopene different natural ingredients such as bees wax, carnuba wax, white soft paraffin, castor oil, strawberry essence and lemon juice were used to formulate herbal lipstick. Prepared herbal lipstick were evaluated for different evaluation test such as colour, texture, pH, melting point, breaking point, softening point, surface anomalies, ageing and perfume stability and also compared with marketed standard formulation. Results showed that, different evaluation parameters of prepared herbal lipstick were resembled with standard values and with marketed formulation. Study concluded that, lycopene extracted from Solanum lycopersicum L. may be better option for synthetic colouring agent.

RP-HPLC Method for Simultaneous Estimation of Cilnidipine and Chlorthalidone

Aim of present study was development of RP-HPLC method for simultaneous estimation of cilnidipine and chlorthalidone. RP-HPLC method for simultaneous estimation of Cilnidipine and Chlorthalidone was carried out by using methanol: water (80:20 v/v) at a flow rate of 1 ml min-1 with UV detection at 231.6 nm. Both drugs showed linearity in the concentration range of 10-70 µg ml-1.for CIL and 10-70 µg ml-1.for CHLT. When marketed pharmaceutical preparations were analyzed, the result obtained by the proposed method was found in good agreement with labeled claims. Recoveries in all these method were in the range of 99.60-100.18%. Results obtained were statistically validated and were found to be reproducible. These methods can be applied for routine analysis of formulations containing these drugs. For analytical methods validation parameters such as linearity, precision, accuracy, specificity, limit of detection, limit of quantization and robustness were determined according to ICH Q2B guidelines.

Analytical and Bio Analytical Method for Quantification of Pure Azilsartan, Not its Salts by RP-HPLC

A simple, specific and accurate reverse phase liquid chromatographic method was developed for determination of Azilsartan in its tablet dosage form as well as from biological fluid like plasma. The determination was carried out on ODS Hypersil C18 column (4.6 mm x 250 mm 5µm) column using a mobile phase of acetonitrile: water (pH 4) [60: 40 %v/v]. The flow rate was 1 mL/min with detection at 249 nm. The linearity response of the HPLC system for Azilsartan was obtained over the range 1-64 µg/mL. Ambroxol (25µg/mL) was used as internal standard. Retention time for Azilsartan and ambroxol were found to be 3.74 and 1.84 minutes respectively. The correlation co-efficient (R2 value) for Azilsartan was found to be 0.992. The proposed method was successfully used for quantification of Azilsartan in Azilva tablets and plasma. The method was validated as per ICH Q2B (Analytical) and USFDA (Bio-analytical) guidelines. The results of analysis have been validated statistically and by recovery studies. The method is found useful for quantification of Azilsartan in marketed formulations as well as from biological fluids and can be applied for quantification of Azilsartan in preclinical and clinical studies.

Development and Validation of RP-HPLC Method for Determination of Doxorubicin Hydrochloride from Vacuum Foam Dried Formulation

A rapid reversed phase (RP) high performance liquid chromatography (HPLC) method was developed and validated for quantitative estimation of Doxorubicin hydrochloride (Dox) from the prepared vacuum foam dried formulation. Chromatographic runs were performed on C18 column with mobile phase comprising of acetonitrile: 0.01M o-phosphoric acid (40: 60) pH 2 at a flow rate of 0.75mL.min−1. Dox was detected at a wavelength of 234nm. The method was shown to be specific, linear in the range of 0–10μg.mL−1 with correlation coefficient of 0.9999, precise at the intra-day level as reflected by relative standard deviation, accurate at recovery rate 99.60±0.13 and robust to change mobile phase and column brand. The detection and quantitation limits were 0.091μg.mL−1 and 0.2758μg.mL−1, respectively. The proposed method could be advantageous in estimation of Dox quantitation in pharmaceutical dosage form in the presence of excipients.

Anthelmintic activities of Barleria Gibsoni Dalz. extracts

To optimize a nanostructured lipid carriers system (NLC) for the per-oral delivery of valsartan (Val), a model BCS class II drug, in an attempt to enhance its therapeutic performance by increasing both solubility and dissolution. Val-loaded NLCs were prepared using ultrasonic melt-emulsification method. Number of formulation factors including the type of oil/lipid, Val to lipid ratio, and surfactant ratio were investigated. The prepared NLC were evaluated for their particle size and shape, polydispersity index, zeta potential, and drug entrapment efficiency. The in vitro drug release profiles were evaluated using a dialysis bags with cut-off 12KD. The prepared NLCs showed average sizes between 423.99±12.73 and 805.53±39.5 nm, and polydispersity index in the range of 0.287 to 0.361. The zeta-potential values were between -3.34 and -10.59 mV. The entrapment efficiency was not very high between 27.3 to 75.04%. The scanning electron images showed almost spherical shapes with sizes lower than those obtained by light scattering. The in vitro release followed a bi-phasic pattern with an initial rapid Val release followed by a slow release varying according to the composition. Two formulations F2 and F4 showed complete drug release within the first two hours. The optimum surfactant ratio was 37.5% by weight of the total lipid. NLC successfully enhanced the Val release rate and dissolution with high potential to enhance its bioavailability.Results: Of 1435 citation reviewed, 22 studies published in 26 papers were appraised. These studies mainly focused on factors affecting patients reporting of ADRs. None of these studies conducted at North America. Sixteen out of 22 reviewed studies described barriers to the reporting process included: Poor awareness of ADR reporting systems; difficulties with reporting procedure and forms; lack of feedback to ADRs submitted by the patients; confusion as to who reports ADRs and to whom they are reported; poor economic status; ADRs resolved; and prior negative reporting experience. Another 11 out of the 22 reviews studies described the motives for reporting ADRs by patients and those included: prevent others from similar ADRs; inform regulatory bodies, drug manufacturer, HCPs, and public; improve drug safety and medication leaflet and enhance scientific knowledge; improve HCP practices; failure of HCPs to report their ADRs; asked to report ADRs by HCPs; it was serious ADRs; and desire for personal feedback and want more information about the ADRs.W are unfortunately subject to an optimistic bias when we evaluate how, and to what extent, drugs and other medical therapies will become available and accessible to patients on the global level in which pharmaceutical enterprises operate. In developed countries, the pricing and affordability of medicines is a controversial issue that highlights health and economic inequalities, and great challenges for the future. According to the New York Times article Lawmakers Look for Ways to Provide Relief for Rising Cost of Generic Drugs (November 24th 2014), “the cost of many generic medications has increased so much over the past year that prices for many common generic drugs in the USA have surpassed those of their brandname equivalents in other developed countries”. The issue of unaffordable healthcare is more challenging with technological advances and the demographic growth of the geriatric population, including those with cancer and cardiac disease. Legislation can be instrumental in the creation of equitable solutions. The EU member state’s management of healthcare access and drug entry; the implementation of regulatory requirements aimed at ensuring quality, safety, and efficacy of medicines and vaccines for human use; and the European Transparency Directive (Council Directive 89/105) which defines procedural requirements for pricing and reimbursement of medicinal products will be discussed. These issues must be taken into account since few of the hundreds of drugs in clinical development ever reach the stage of final approval, having failed to produce the anticipated results expected by the investigators. These trials can take up to 20 years to complete, and several billion dollars to reach the stage of approval or denial by the regulatory agency involved. When failing to demonstrate viability, preexisting expenditures are allowed to be passed onto the price the pharmaceutical company charges patients. In the cancer industry for example, most new drugs require the patient or insurance company to pay 50-100,000 dollars for a course of treatment which may not offer more than several months of improvement in the clinical response. It is essential that the legislators in each of the countries where the drug is to be introduced be able to negotiate a fee arrangement where the patient will not be denied treatment and the drug company be compensated reasonably for development costs.Copyright:

Optimization of Method for Determination of Swelling Factor of IspaghulaSeeds

An endeavour of present study is to optimize the method for determination of swelling factor of Ispaghula seeds, so it can be determined correctly with minimum errors which will be reproducible. The polysaccharides in the mucilage of Plantago seeds constitute a diverse class of biological macromolecules with a broad range of physiochemical properties which are widely used for applications in Pharmacy and medicine. Many official and unofficial sources described different methods for determination of swelling factor with variable results. The present work is undertaken to determine the effect of parameters such as quantity of seed, volume and nature of solvent, time interval of agitation, time of measurement of result, Effect of quantity of seeds on swelling factor determination. Swelling factor of different seeds like Lepodium sativum, Althia officinalis and Occimum sanctum has been evaluated by IP method and optimised method for 24 h. Optimized method gives superlative results over IP method. Plantago seeds moistened with 1ml of 90% alcohol followed by addition of distilled water at room temperature along with every 3 h agitation shows exceptional swelling as compared to other methods and conditions.