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    Dataset: P3

    Full-text · Dataset · Jan 2016
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    A.N. Khan · R.K. Khar · M. Udayabanu
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    ABSTRACT: Objective: Antibiotics save millions of lives from infectious diseases worldwide. Failing treatment, serious adverse effects, and antimicrobial resistance are constantly reported mainly from developing nations due to lack of quality of antibiotics medicines. In India quality of medicines remains a major regulatory challenge and patients concern. Thus, a pilot study to explore the quality of generic amoxicillin products and associated price along with their burden on patients was evaluated. Methods: 46 amoxicillin trihydrate generic products with the label claim of 250 mg amoxicillin were procured from open market of Northern India without prescription. Identification and quantitative evaluations of these generic products were estimated using Indian Pharmacopoeia (IP) 2010 recommended High-Performance Liquid Chromatography (HPLC) method. And assay value was compared with the maximum retail price per unit dosage. Affordability was estimated in general for the population who daily live on less than Indian rupees (`) 144 and `88.6. Results: Out of 46 products, 28.26% were found to be out of IP specification, and 13.04% products were of substandard quality. Fishers’ exact test with p-value 0.87 showed products quality gaps were irrespective of their price. Ceiling price of 3.04 per unit dosage; pose a high burden on the patients who are on amoxicillin treatment. Conclusion: Situation demands the evidence of safety before approval and thereafter too. However, the situation may become worst if the price and quality could not be controlled. Thus Indian drug regulatory bodies need to be entreated to counter these critical issues. © 2016 The Authors. Published by Innovare Academic Sciences Pvt Ltd.
    Full-text · Article · Jan 2016
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    ABSTRACT: Topotecan (TPT) is indicated against a variety of solid tumors, but has restricted clinical use owing to associated pharmaceutical caveats. This study is focused at formulating a successful TPT PLGA nanosystem which ameliorates the rapid conversion of active lactone form of drug to its inactive carboxylate form and consequently improvises its efficacy. TPT PLGA nanoparticles were formulated by a double emulsion-solvent evaporation technique with sequential optimization to obtain desired particle size, PDI, zeta potential, and entrapment efficiency. Stability of TPT was ensured by maintaining an acidic pH in the drug-containing phase and the system was evaluated for in vitro-in vivo performance including cytotoxic potency. The optimized nanosystem had a particle size of 187.33 ± 7.50 nm, a PDI of 0.179 ± 0.05, and an entrapment efficiency of 56 ± 1.2%. Low pH in the interior of nanoparticles stabilized the drug to remain in its active lactone form and revealed a biphasic release pattern till 15 d. Additionally, an in vitro cytotoxicity testing as well as in vivo antitumor efficacy demonstrated a significant potential of higher proliferation inhibition as compared with neat drug (TPT). Thus, the investigation summarized an innovative simple tool for developing stable TPT NPs for effective delivery for treating solid tumors.
    No preview · Article · Nov 2015 · Drug Delivery
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    Ahmed Nawaz Khan · Anupriya Kaur · Roop Krishen Khar · Sadaf Khanam
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    ABSTRACT: Background: Indian Pharmaceutical market is well known for generic medicines and the government also promotes them due to their affordability. These medicines are manufactured by big, medium and small size companies and their quality are generally checked by analytical methods though real evaluation of medicines can only be ensure by Medical practitioners (MP) who prescribe them which is based on therapeutic responses and adverse effects they notice. Perspectives of MP about prescribed medicines, price, therapeutic responses, adverse effects and their awareness about different interactions are valuable and may initiate for better treatment and healthcare system. Method: A survey of 111 MP was conducted on one to one basis in a form of questioner. Frequency, percentage, Chi square and Friedman test were applied to check the association and rank between different attributes. Results: Branded generic is preferred over innovator branded generic and generic by 63.1% of MP because 64.9% believe it has good therapeutic response and 68% experienced it has mild adverse effects while only 0.9% assumed it has high adverse effect. Only generic considered as highly affordable but it is prescribed moderately or less preferably. Self study is the main source of medicine information for MP but all of them do not have excellent or good drug-drug and drug-food interactions knowledge. Patients only adhere to their 70-90%, 40-60% and 10-30% instructions according to 33.3%, 51% and 18% MP respectively. Conclusion: There is excessive demand of high quality generic products for better safety of patients irrespective of its affordability. Efficient training programs are required for some MP to improve average interactions knowledge. Patient non-adherence needs prior attention by implementing patient involvement in treatment decision and educating them.
    Full-text · Article · Oct 2015 · Journal of Young Pharmacists
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    ABSTRACT: Due to the structure and physiological barrier of eye, only 1% of instilled dose is available for action on the corneal surface. In this work, we developed and evaluated chitosan (pH sensitive) and gellan gum (ion sensitive) in situ gel of sparfloxacin to improve precorneal residence time. A protocol for radiolabeling of sparfloxacin with Tc-99m was optimized to study the ocular retention using gamma scintigraphy technique. The clear formulation was developed. In vitro release showed a sustained and prolonged release compared to plain eye drop solution. Dynamic and static gamma scintigraphy showed better retention than plain eye drops. The ocular tolerance test (hen's egg test-chorioallantoic membrane test and infra-red study) showed that the formulation is nonirritant and can be used as ocular vehicle. Radiolabel protocol for sparfloxacin was successfully developed and evaluated on ocular retention studies of developed in situ gel. The developed in situ gel is non irritant and can go further with clinical evaluation.
    Full-text · Article · Jul 2015 · Journal of Pharmacy & Bioallied Sciences
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    ABSTRACT: A simple, accurate sensitive and stability indicating high performance thin layer chromatography (HPTLC) method for the estimation of (-)-α-bisabolol in chamomile oil and in nanoformulation was developed and validated according to ICH guidelines. The quantification of (-)-α-bisabolol was done by applying standard drug solution on precoated HPTLC plates (silica gel 60 F254) that act as stationary phase, kept in twin trough glass chamber presaturated with mobile phase consisting of toluene: chloroform: methanol: acetic acid in the ratio 9.2:0.4:0.4:0.2:0.04 (v/v/v/v). Linear ascending mode was used for the development of chromatograms and spectrodensitometric analysis was done at 430nm. The linear regression analysis data,in concentration range of 100-1000 ng per spot for (-)-α-bisabolol (Rf = 0.46±.02), showed best relationship (r2=0.99) with respect to peak area. The limit of detection (8.68 ng per spot) and limit of quantification (26.30 ng per spot) were determined by standard deviation method. Stress degradation studies confirmed that the developed method gave well resolved peaks of the drug and degradation products, hence this can be used to separate pure compounds from impurities.The developed HPTLC method was used for the estimation of (-)-α-bisabolol in bulk drug and in nanoemulsion formulation. It can also be employed for ex-vivo skin permeation and skin deposition studies as the developed method is economical, robust and time saving. Please cite this article in press as Zrien Naz et al. Determination of (-) α-bisabolol in Matricaria chamomileoil and in nanoformulation by HPTLC method: its application in ex vivo studies. Indo American Journal of Pharm Research.2015:5(06).
    Full-text · Article · Jun 2015
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    Neeraj Kumar · Prof. (Dr.) R. K Khar · Dr. Bhavna
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    ABSTRACT: Cyclodextrin are the functional excipients which are useful for enhancing solubility, and are being used in an increasing way to overcome the undesirable pharmaceutical characteristics especially poor aqueous solubility. It has generally been assumed that mechanism where cyclodextrin exert their effects, especially their augmentation of solubility is via the formation of non-covalent dynamic inclusion complexes. The aim of this study was to prepare and characterization of atenolol-cyclodextrin(CDs) complex. Atenolol (ATN) is widely use as anti-hypertensive drug (beta blocker) it oral bioavailability is 46-60% such low bioavailability has been attributed to low aqueous solubility of atenolol. To increase its aqueous solubility two different type of cyclodextrins (CDs): beta Cyclodextrin (BCD) and hydroxy-propyl beta cyclodextrin (HPBCD) were used. Solubility depends on the type of CDs, increased solubility were obtained. When the more substituted CDs (HPBCD) were used instead of non-substituted cyclodextrin. Solid-ATN-CDs complex were prepared by kneeded and freeze-dried methods these complex were compared with physical mixture of ATN-CDs. The characterization of these complexes was made by Differential scanning calorimeter (DSC), FTIR, NMR, SEM and drug release studies. Drug release studies shows that freeze dried inclusion complex increase the solubility rate of ATN. A bioavailability studies on albino Wister rates was done with a formulation of ATN-BCD and ATN-HPBCD was compared with conventional ATN tablets.
    Full-text · Article · May 2015 · International Journal of Pharmacology and Pharmaceutical Sciences

  • No preview · Article · Apr 2015
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    A N Khan · R K Khar
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    ABSTRACT: Globally, every country is the victim of substandard or spurious drugs, which result in life threatening issues, financial loss of consumer and manufacturer and loss in trust on health system. The aim of this enumerative review was to probe the extent on poor quality drugs with their consequences on public health and the preventive measures taken by the Indian pharmaceutical regulatory system. Government and non-government studies, literature and news were gathered from journals and authentic websites. All data from 2000 to 2013 were compiled and interpreted to reveal the real story of poor quality drugs in India. For minimizing spurious/falsely-labelled/falsified/counterfeit drugs or not of standard quality drugs, there is urgent requirement of more stringent regulation and legal action against the problem. However, India has taken some preventive steps in the country to fight against the poor quality drugs for protecting and promoting the public health.
    Full-text · Article · Mar 2015 · Indian Journal of Pharmaceutical Sciences
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    ABSTRACT: Delivering drugs to ocular region is a challenging task. Eye physiological barriers lead to relatively less therapeutic and bioavailability effect by the conventional eye drops. This may be overcome by the use of in situ gel delivery system. The objective of our work was to formulate an ocular delivery system of levofloxacin, based on the concept of ion (sodium alginate) and pH (chitosan) activated in situ gelation concept. Due to its elastic properties, in situ gels resist the ocular drainage of drug leading to longer contact times with ocular surface. The formulation was evaluated for physicochemical characteristics, in vitro drug release. Ocular retention studies were carried out by Gamma scintigraphy. Time activity curve was plotted between marketed formulation and developed formulation for comparing drug drainage from the eye with time. Ocular tolerance test was performed by handheld infra-red camera. The formulations showed a first-order release pattern over 12 h. Both in vitro release studies and in vivo gamma scintigraphy precorneal retention studies indicated better therapeutic efficacy compared with standard eye drops. The results demonstrated that the developed in situ gel of levofloxacin is nonirritant, has prolonged action and is a better option in terms of retention, ocular bioavailability and patient compliance when compared with plain eye drops formulation.
    Full-text · Article · Feb 2015 · Journal of Pharmacy & Bioallied Sciences
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    ABSTRACT: In the present study, toxicity of nanoparticles is evaluated for assessing their effect on liver and kidney. We have synthesized highly mono-disperse spherical and rod-shaped silver nanoparticles using reverse microemulsion and aqueous phase methods. These were characterized by UV–vis spectrophotometer, dynamic light scattering, and transmission electron microscope confirming the formation of different sizes of spherical-shaped and rod-shaped silver nanoparticles (Ag NPs). Acute toxicity of different shapes and sizes of Ag NPs and their modulations by using Withania somnifera were evaluated through biochemical and histopathological changes in liver and kidney tissues of Wistar rats. We also evaluated cytotoxicity in specific murin macrophages through confocal microscopy. Cytotoxicity analysis indicates that median lethal dose (LD50) for 20, 50, and 100-nm size spherical and 100-nm rod-shaped Ag NPs was 0.25, 0.35, 0.35, and 0.35 mg/ml, respectively. We also calculated clinically important protein concentration to illustrate the efficacy of Ag nanomaterials. These studies indicated that 20, 50, and 100-nm spherical Ag NPs (35 mg/kg, 23 days) increased the biochemically important enzymes and substrate levels glutamate oxaloacetate transaminase (GOT), glutamate pyruvate transaminase (GPT), alkaline phosphatase (ALP), creatinine, and urea concentration in serum, showing liver and kidney tissue damage. After 23 days of treatment of Ag NPs (20, 50, and 100 nm spherical), along with W. somnifera, toxicity of Ag NPs significantly decreased and marginalized. However, no significant changes were observed for 100-nm rod-shaped Ag NPs on normal liver and kidney architecture. Given their low toxic effects and high uptake efficiency, these have a promising potential as to lower the toxicity of Ag NPs.
    No preview · Article · Sep 2014 · Protoplasma
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    ABSTRACT: Poor drug penetration and rapid clearance after topical instillation of a drug formulation into the eyes are the major causes for the lower ocular bioavailability from conventional eye drops. Along with this, poor encapsulation efficiency of hydrophilic drug in polymeric nanoparticles remains a major formulation challenge. Taking this perspective into consideration, dorzolamide (DZ)-loaded PLGA nanoparticles were developed employing two different emulsifiers (PVA and vitamin E TPGS) and the effects of various formulation and process variables on particle size and encapsulation efficiency were assessed. Nanoparticles emulsified with vitamin E TPGS (DZ-T-NPs) were found to possess enhanced drug encapsulation (59.8±6.1%) as compared to those developed with PVA as emulsifier (DZ-P-NPs). Transcorneal permeation study revealed a significant enhancement in permeation (1.8-2.5 fold) as compared to solution. In addition, ex vivo biodistribution study showed a higher concentration of drug in the aqueous humour (1.5-2.3 fold). Histological and IR-camera studies proved the non-irritant potential of the formulations. Pharmacoscintigraphic studies revealed the reduced corneal clearance, as well as naso-lachrymal drainage in comparison to drug solution. Furthermore, efficacy study revealed that DZ-P-NPs and DZ-T-NPs significantly reduced the intraocular pressure by 22.81% and 29.12%, respectively, after a single topical instillation into the eye.
    Full-text · Article · Jul 2014 · Colloids and surfaces B: Biointerfaces
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    ABSTRACT: In the present work we developed and optimized moxifloxacin loaded PLGA nanodispersions for enhanced ocular delivery of moxifloxacin. The optimized nanodispersions were prepared by double emulsification solvent evaporation method using high pressure homogenizer (500 bar pressure, 2 cycles) to homogenize primary emulsion. Particle size of nanodispersion was found to be dependent on PLGA concentration, PLGA:drug ratio, PVA concentration and W:O phase volume ratio whereas drug encapsulation was related to PLGA concentration and PLGA:drug ratio. Encapsulation efficiency of optimized nanodispersion was 62.5% with a mean particle size of around 118.5 nm which makes them a suitable candidate for ocular administration. Drug release kinetic studies indicate a sustained release profile of moxifloxacin from nanodispersions. In addition, in vitro and in vivo studies have revealed that PLGA nanodispersions were non irritant, prevent ocular drainage of moxifloxacin with enhanced ocular bioavailability by 3-fold.
    No preview · Article · May 2014 · Science of Advanced Materials
  • Roop Krishen Khar Kilam

    No preview · Article · Dec 2013
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    ABSTRACT: Abstract Availability of proper concentration of medicament on to the corneal surface is a challenging task. Many novel formulations, i.e. hydrogels, nanoparticles, ocuserts, etc. had been tested to improve ocular bioavailability, out of which our group found, in situ gel and polymeric nanoparticle are the most interesting approach to achieve ocular retention. We found that in situ gel stay only for 12 h and poly(lactic-co-glycolic acid (PLGA) nanoparticles are non mucoadhesive in nature so we try to combine both these formulations and termed it as "Nanoparticle laden in situ gel". Here we prepare nanoparticle laden in situ gel containing levofloxacin encapsulated PLGA nanoparticle, incorporated in chitosan in situ gel and evaluated its ocular retention by gamma scintigraphy in rabbits. The observations of acquired gamma camera images showed good retention over the entire precorneal area. From static and dynamic gamma scintigraphy evaluation, we can be interpret that developed nanoparticle laden in situ gel formulation cleared at a very slow rate and remained at corneal surface for longer duration than marketed formulation, in situ gel and nanosuspension alone.
    No preview · Article · Sep 2013 · Drug Delivery
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    Naseem Akhtar · Sushama Talegaonkar · Roop Kishan Khar · Manu Jaggi
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    ABSTRACT: The present investigation was aimed to establish a validated stability-indicating liquid chromatographic method for the estimation of etoposide (ETP) in bulk drug and self-nano emulsifying formulation. ETP was successfully separated from the degradation products formed under stress conditions on LiChrospher 100 C18 reverse-phase column (a 250 mm × 4.6 mm i.d., 5-μm particle size) using 55:45 (v/v) acetonitrile-phosphate buffer saline (pH 4.5) as the mobile phase, at a flow rate of 1.0 mL min(-1) and detection at 283 nm. The response was a linear function of analyte concentration (R(2) > 0.9997) over the concentration range of 0.05-50 μg mL(-1). The method was validated for precision, accuracy, robustness, sensitivity and specificity. The % recovery of ETP at three different levels (50%, 100% and 150%) ranged between 93.84% and 100.06% in optimized self-nano emulsifying formulation, Etosid® soft-gelatin capsule and Fytosid® injection. First-order degradation kinetics of ETP were observed under acidic and alkaline conditions. The method was also applied for the stability assessment of self-nano emulsifying formulation under accelerated conditions, the formulation was found to be stable at all storage conditions with the shelf-life of 2.37 years at 25 °C. The method holds promise for routine quality control of ETP in bulk, pharmaceutical formulations as well as in stability-indicating studies.
    Full-text · Article · Aug 2013 · Saudi Pharmaceutical Journal
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    ABSTRACT: The purpose of this work is intended to investigate the potential of self-nanoemulsifying (SNE) drug delivery system for enhanced oral bioavailability of etoposide by P-glycoprotein (P-gp) modulation. The components of SNE formulation were optimized by their solubilization and emulsification efficiency. The ternary phase diagrams provided nanoemulsion existence ranges and the corresponding formulations were developed and evaluated via thermodynamic and dispersibility tests. The successful formulations were characterized for various parameters including time required for self-emulsification, percentage transmittance, droplet size, surface morphology, zeta potential and in vitro release. The etoposide loaded SNE9 formulation showed 2.6- and 11-fold higher permeability coefficient in apical to basolateral direction across Caco-2 monolayers as compared to the Etosid and plain drug solution, respectively. The etoposide loaded SNE9 formulation showed a higher cytotoxicity at the highest tested concentration compared to the blank SNE9 formulation and the free etoposide. Furthermore, an in vivo pharmacokinetic study of etoposide in SNE9 formulation showed 3.2- and 7.9-fold increase in relative oral bioavailability compared with that of etoposide in Etosid and drug suspension, respectively. Thus, the developed SNE drug delivery system could be a valuable tool for the effective oral delivery of etoposide.
    No preview · Article · Jul 2013 · Journal of Biomedical Nanotechnology
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    ABSTRACT: Abstract Collagen, a high molecular weight, hydrophilic and highly abundant protein is known to have anti-ageing, anti-wrinkle, anti-acne, anti-scar and wound healing properties. High molecular weight and hydrophilic nature hinder its effective topical delivery. So, the objective of present study was to develop effective topical nano-surfactant dispersion (NSD) for collagen delivery. NSD was prepared from sorbitan monostearate (Span60) and cholesterol using ethanol injection method followed by probe sonication. NSD was characterized for entrapment efficiency (%EE), size and size distribution (Z-avg and polydispersity index (PDI)), shape, zeta-potential (ζ), in vitro drug release, skin hydration and skin irritation test and histopathological examination. Optimized NSD (NSD3) had %EE, z-avg, PDI and ζ-potential of 77.56% ± 1.09%, 158.1 ± 2.31 nm, 0.211 and -17.2 ± 0.64 mV, respectively. In in vivo skin hydration test, NSD treatment showed nearly 2.5-fold and 3-fold increase in the thickness of stratum corneum (SC) as compared to the collagen gel treated and untreated skin, respectively. The mean scores of skin irritation test in two animal species, rats and rabbits, were found to be 1.42 ± 1.01 and 1.71 ± 0.29, respectively, indicating the non-irritant nature of collagen loaded NSD. Histopathology of the skin after application of developed NSD showed non-significant changes in skin anatomy indicating its safe nature.
    Full-text · Article · May 2013 · Pharmaceutical Development and Technology
  • Ahmad I · Akhter S · Ahmad MZ · Shamim M · Rizvi MA · Khar RK · Ahmad FJ
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    ABSTRACT: Collagen, a high molecular weight, hydrophilic and highly abundant protein is known to have anti-ageing, anti-wrinkle, anti-acne, anti-scar and wound healing properties. High molecular weight and hydrophilic nature hinder its effective topical delivery. So, the objective of present study was to develop effective topical nano-surfactant dispersion (NSD) for collagen delivery. NSD was prepared from sorbitan monostearate (Span60) and cholesterol using ethanol injection method followed by probe sonication. NSD was characterized for entrapment efficiency (%EE), size and size distribution (Z-avg and polydispersity index (PDI)), shape, zeta-potential (ζ), in vitro drug release, skin hydration and skin irritation test and histopathological examination. Optimized NSD (NSD3) had %EE, z-avg, PDI and ζ-potential of 77.56% ± 1.09%, 158.1 ± 2.31 nm, 0.211 and -17.2 ± 0.64 mV, respectively. In in vivo skin hydration test, NSD treatment showed nearly 2.5-fold and 3-fold increase in the thickness of stratum corneum (SC) as compared to the collagen gel treated and untreated skin, respectively. The mean scores of skin irritation test in two animal species, rats and rabbits, were found to be 1.42 ± 1.01 and 1.71 ± 0.29, respectively, indicating the non-irritant nature of collagen loaded NSD. Histopathology of the skin after application of developed NSD showed non-significant changes in skin anatomy indicating its safe nature
    No preview · Article · May 2013 · Pharmaceutical Development and Technology
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    ABSTRACT: Proper availability of drug on to corneal surface is a challenging task. However, due to ocular physiological barriers, conventional eye drops display poor ocular bioavailability of drugs (< 1%). To improve precorneal residence time and ocular penetration, earlier our group developed and evaluated in situ gel and nanoparticles for ocular delivery. In interest to evaluate the combined effect of in situ gel and nanoparticles on ocular retention, we combined them. We are the first to term this combination as "nanoparticle laden in situ gel", that is, poly lactic co glycolic acid nanoparticle incorporated in chitosan in situ gel for sparfloxacin ophthalmic delivery. The formulation was tested for various physicochemical properties. It showed gelation pH near pH 7.2. The observation of acquired gamma camera images showed good retention over the entire precorneal area for sparfloxacin nanoparticle laden in situ gel (SNG) as compared to marketed formulation. SNG formulation cleared at a very slow rate and remained at corneal surface for longer duration as no radioactivity was observed in systemic circulation. The developed formulation was found to be better in combination and can go up to the clinical evaluation and application.
    Full-text · Article · Apr 2013 · Journal of Pharmacy & Bioallied Sciences

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