Original Article

Spectrophotometric determination of Eflornithine hydrochloride through schiff’s base system using pdab reagent in pharmaceutical preparation

Amit Kumar^a,*, Vijender Singh^b, Praveen Kumar^c

^aDepartment of Pharmaceutical Analysis, NKBR College of Pharmacy & Research Centre, Meerut, Uttar Pradesh, India.

^bDepartment of Pharmaceutical Analysis, BBS Institute of Pharmaceutical & Allied Sciences, Greater Noida, India.

^cMoradabad Educational Trust Group of Institutions Faculty of Pharmacy, Moradabad, Uttar Pradesh, India.

* Corresponding Author: Tel. No.: +91 9897144639, Email: amit_analysis@yahoo.co.in

A rapid, economic and highly sensitive spectrophotometric method was developed for the quantification of eflornithine hydrochloride (DFMO). The method involves the reaction DFMO with para-dimethylamino benzaldehyde (PDAB) in acidic medium (pH 5.4) which results in an orange-coloured product exhibiting maximum absorbance λmax at 563. The proposed method can be utilized as a stability indicating assay. The different experimental parameters affecting the derivatization reaction were carefully studied and incorporated into the procedure. Under the described conditions the apparent molar absorption coefficient (έ563) is 4.9 × 103 L/mol cm. The linear equation is Y= 1.60 +0.038X (μg/mL) in the range of 5–40 μg/mL of DFMO with a correlation coefficient r = 0.9992, and the detection limit (LOD) is 11.842 μg/mL. The average recovery of the target compound is 100.07% with a limit of quantification (LOQ) of 39.47 μg/mL. The mechanism of the derivatization reaction is proposed and advantages of the proposed method are discussed. The method was validated in terms of accuracy and precision and was successfully applied to the determination of DFMO in its pharmaceutical dosage form. The proposed method is useful for routine analysis of DFMO in quality control laboratories.

Keywords: Eflornithine hydrochloride, Spectrophotometry, PDAB, Validation

Original Article

Synthesis and antiangiogenic activity of some novel analogues of 2-[(Z)-2-(4-Nitrophenyl) ethenyl]furan

Anurag Chaudhary^a,*, Prince P. Sharm^b

^aDepartment of Pharmaceutical Technology, Meerut Institute of Engineering and Technology, NH-58, Meerut Bypass Road, Meerut, Uttar Pradesh, India.

^bDepartment of Pharmaceutical Science, Faculty of Medical Science and Health, Gurukul Kangri University, Haridwar, Uttar Pradesh, India

*Corresponding author: Tel. No.: +91 9917062681, Email: anurag15182@rediffmail.com

A series of 2-[(z)-2-(4-nitrophenyl)ethenyl]furan analogues were synthesized in order to obtain new compounds with potential antiangiogenic activity. Base catalysed condensation of p-nitrophenyl acetic acid (3) with furfuraldehyde (2), in the presence of triethylamine, yielded carboxylic acid derivative (4) which on esterification, with methanol, using a catalytic amount of H2 SO4 , gave corresponding ester derivative (5). Reaction of thionyl chloride with carboxylic acid derivative in refluxing benzene gave the corresponding acid chloride (6), which on subsequent reaction with appropriate amine gave compounds 7a-k. All compounds were evaluated for their antiangiogenic activity by chorioallantoic membrane (CAM) assay method. Compounds 6 and 7h showed pronounced antiangiogenic activity, however, they were less active than standard (β-1,4-galactan sulphate). All other compounds showed significant inhibition of angiogenesis when compared to control but they were much less active than standard. As some of 2-[(z)-2-(4- nitrophenyl)ethenyl]furan analogues showed significant antiangiogenic activity, this moiety may be further explored to find new antiangiogenic leads.

Keywords: Cis-stilbene, Chorioallantoic membrane, Antitumor, Antiangiogenic, Antitubulin

Original Article

Nitazoxanide stabilizing hypsochromic shift based method for its determination in bulk and in pharmaceutical formulation

Sanjay Sharma*, Sachin Kumar

NKBR College of Pharmacy and Research Centre, Phaphunda Hapur Road, Meerut, Uttar Pradesh, India

*Corresponding author: Tel. No.: +91 9627268090, Email: sanjaysharma.qa@gmail.com

Nitazoxanide used as antiprotozal agent. There is no method for determination of the drug content in dosage form without drug was acid stabilized and Hypsochromic shift based method. Simple, fast, reliable and Hypsochromic shift based spectrophotometric method has been developed for determination of nitazoxanide in bulk and tablet dosage forms. The quantitative determination of drug was carried out using the zero order values (absorbance) measured at 343.5 nm in 20% v/v 0.1M Citric acid solutions in Methanol. Use of citric acid in solvent system shift the maximum absorbance wavelength to lower side (Hypsochromic shift) and drug was stable in the solvent system (acid stabilized drug). Drug content was determined in within the desirable confidence interval of 98-102%. The proposed method is economic, sensitive, accurate, reproducible and useful for the determination of nitazoxanide in bulk drug and tablet formulations. The method was validated as per ICH guidelines. The proposed method is economic, accurate, reproducible and useful for the determination of nitazoxanide in bulk drug, tablet formulations, biological fluids, dissolution studies, bio-equivalence studies as well as routine analysis in pharmaceutical industries.

Keywords: Nitazoxanide, Hypsochromic shift, Bulk drug, Tablet, Validation

Original Article

Synthesis and antimicrobial activity of some novel derivatives of 7-hydroxy-4- methyl coumarin

Mohit Gupta^a,*, Sushil Kumar^b, Maya K. Gupta^c

^aRadha Govind Institute of Pharmacy, Chandausi, Moradabad, Uttar Pradesh, India.

^bPharmacy Department, IFTM University, Moradabad, Uttar Pradesh, India.

^cOm Sri Sai College of Pharmacy, Aligarh, Uttar Pradesh, India

*Corresponding author: Tel. No.: +91 9358211655, Email: drmohit.mpharmphd@gmail.com

Some novel derivatives of 7-hydroxy-4-methyl coumarin were synthesized. The title compounds were obtained by the reaction of 7-hydroxy-4-methyl coumarin with ethylchloroacetate in the presence of potassium carbonate in acetone afforded ethyl-2-(4-methyl-2-oxo-2H-chromen-7-yloxy)acetate, which react with hydrazine hydrate in ethanol afforded 2-(4-methyl-2-oxo-2H-chromen-7-yloxy) acetohydrazide. Hydrazide was considered as the key intermediate for some novel compounds (MK1-MK6). The reaction of hydrazide with acetyl acetone and ethyl acetoacetate gave 7-(2-(3,5-dimethyl-1H-pyrazol-1-yl)-2-oxoethoxy)-4-methyl-2Hchromen-2-one (MK-1) and 1-(2-(4-methyl-2-oxo-2H-chromen-7-yloxy)icetyl)-3- methyl-1H-pyrazol-5(4H)-one (MK-2). Also reaction of hydrazide with isatin lead to the formation of 2-(4-methyl-2-oxo-2H-chromen-7-yloxy)-N’-(2-oxoindolin-3- ylidene) acetohydrazide (MK-3).The other derivatives MK-4, MK-5 and MK-6 were obtained by treating the hydrazide with phthalic, maleic and succinic anhydrides respectively. The structures of these compounds were established on the basis of IR and 1 H-NMR spectral analysis. Compounds (MK1-MK6) were screened for their antimicrobial activity. All compounds exhibit significant antimicrobial activity as compared to standard drug.

Keywords: 7-Hydroxy-4-Methyl Coumarin, Hydrazide, Antibacterial and Antifungal activity

Original Article

Novel interpenetrating polymer network mucoadhesive microspheres of locust bean gum and poly(vinyl alcohol) for the delivery of Famotidine
Neelam Jain*, Hitesh Kumar, Ashok K. Rajpoot, Harish C. Verma

Moradabad Educational Trust Group of Institutions Faculty of Pharmacy, Moradabad, Uttar Pradesh, India

*Corresponding author: Tel. No.: +91 8859275258, Email: neelamnj02@gmail.com

Novel interpenetrating polymer network (IPN) of locust bean gum (LBG) and poly vinyl alcohol (PVA) were prepared and crosslinked with glutaraldehyde (GA) to form mucoadhesive microspheres by emulsion cross-linking method to deliver model anti-ulcer drug, famotidine. Various formulations were prepared by changing the ratio of LBG: PVA, extent of cross-linking in order to optimize the formulation variables on drug encapsulation efficiency and release rate. FTIR spectroscopy was done to confirm the formation of interpenetrating network and the chemical stability of famotidine after penetration of microspheres. Microspheres formed were spherical with smooth surfaces as revealed by SEM and mean particle size as measured by optical microscopy ranged between 10.83±0.75μm to 21.13±0.74μm. Drug entrapment efficiency was ranges between 65.44±2.57% to 84.67±2.58%. Percentage mucoadhesion of the microspheres was found to be in the range between 63.33±2.57% to 86.66±3.65%. Equilibrium and dynamic swelling studies were performed in 0.1N HCl buffer solution of pH 1.2 and diffusion coefficients were calculated by considering the spherical geometry of the matrices. In vitro release studies were performed in pH 1.2 media. Release data indicated that a drug release which depends on the extent of cross-linking and the ratio of LBG: PVA present in the microsphere. The release data were fitted to an empirical equation to estimate the transport parameters, which indicated that the release follows Super Case II transport mechanism. Based on the results of in-vitro studies it was concluded that these IPN mucoadhesive microspheres provided oral controlled release of famotidine.

Keywords: Interpenetrating polymer network, Locust bean gum, Poly vinyl alcohol, Mucoadhesive microspheres, Famotidine

Original Article

Design and characterization of solid dispersion based fast dissolving tablet of Cetirizine hydrochloride

Anupam K. Sachana^a,*, Ankita Gupta^a, Lovi Nigam^a, Ranjana Sharma^b, Sudhir S. Gangwar^b

^aDayanand Dinanath College, Institute of Pharmacy, Ramaipur, Kanpur, India.

^bDepartment of Pharmacy, G.S.V.M. Medical College, Kanpur, India.

*Corresponding author: Tel. No.: +91 9936273358, Email: anupamkrsachan@gmail.com

The aim of present investigation was to prepare fast dissolving tablets (FDT) of an antiallergic drug Cetirizine hydrochloride to increase its clinical effects and bioavailability through pre-gastric absorption. The solubility of this poorly soluble drug was enhanced by preparing its solid dispersions with colloidal Silicon dioxide in various ratios. The surface morphology (SEM) of solid dispersion revealed its amorphous form compared to needle shape crystals of pure drug.The optimized batch of solid dispersions (SD3) were characterized by DSC and XRD studies and further developed into FDT by using different concentration of super disintegrants like Sodium starch glycolate and Crosscarmellose sodium via direct compression method. The pre-compression and post-compressive parameters for the designed tablets were evaluated. All formulations showed desired pre and post-compressive characteristics. FTIR study revealed that there was no drug excipient interaction. Formulation (F3) was selected as the best formulation with maximum amount of drug release i.e. 99.98± 0.14% in 6 min and minimum disintegration time of 2.76±0.1 sec. Stability studies of optimized formulation revealed that formulation is stable. Hence, efficacious allergic treatment anywhere and anytime particularly for geriatric, pediatric, mentally ill, bed ridden and patients who do not have easy access to water could be possible.

Keywords: Fast Dissolving Tablets, Colloidal Silicon Dioxide, Scanning Electron Microscopy, Cetirizine HCl, Solid Dispersion, PXRD studies

Original Article

Development and evaluation of fast mouth dissolving tablets of Terbutaline sulphate using two different techniques

Vikas Saxenaa^a,*, M. Hoque^b

^aRakshpal Bahadur College of Pharmacy, Bareilly , Uttar Pradesh, India.

^bIndian Veterinary Research Institute, Izatnagar Uttar Pradesh, India.

*Corresponding author: Tel. No.: +91 9412809121, Email: vikas@rbmi.in

Fast mouth dissolving tablets constitute an innovative dosage form that overcomes the problems of swallowing and provides a quick onset of action. In view of enhancing bioavailability an attempt has been made to study two different methods direct compression and sublimation in formulation of mouth dissolving tablets of Terbutaline Sulphate. Total four formulations using various superdisintegrants and subliming agents were prepared. All prepared formulations were evaluated for physico-chemical parameters. The formulations exhibited good disintegration properties with total disintegration time in the range of 25 to 35 s. Comparative evaluation of two methods showed direct compression method is a better alternative to sublimation method as its formulations rapidly disintegrate in oral cavity. In vitro cumulative percentage drug release for formulations prepared by direct compression with explotab superdisintegrants shows 99.79 while sublimation method using camphor 93.58 release in 12 min. Kinetic studies indicated that all the formulations followed first order release with diffusion mechanism.

Keywords: Terbutaline Sulphate, Direct compression, Sublimation, Mouth dissolving

Original Article

Azathioprine induced hepatotoxicity due to oxidative stress, protective aspect of Quercetin in rats

Sunil Kumara^a,*, Vijay K. Sharma^b, Amit Kumar^c

^aDepartment of Pharmaceutical Sciences, Kharvel Subharti College of Pharmacy, Subharti University, Meerut, Uttar Pradesh, India.

^bDepartment of Pharmaceutical Sciences, Dr. K N Modi Institute of Pharmaceutical Education and Research, Modi Nagar, Ghaziabad, Uttar Pradesh, India.

^cDepartment of Biotechnology, Dr. K N Modi Institute of Pharmaceutical Education and Research, Modi Nagar, Ghaziabad, Uttar Pradesh, India.

*Corresponding author: Tel. No.: +91 9012406375, Email: sunilak2813@gmail.com

Mitochondrion plays the most prominent role in the production of energy and cell cycle regulation. Administration of immunosuppressant drug AZA (azathioprine) adversely affects the hepatic mitochondria, which may culminate in hepatotoxicity. The present study is aimed at evaluating the role of QE (quercetin) in AZA provoked hepatic injury. Male Wister rats were used for the experimentation. AZA was administered as a single intraperitoneal injection (50 mg/kg body weight) on the 7th day of the experiment. A prominent depletion in the levels of mitochondrial antioxidants such as MnSOD (manganese Superoxide dismutase), GPx (glutathione peroxidase) and GSH (reduced glutathione) was observed in AZA induced rats. There was a poignant deterioration noticed in mitochondrial membrane, which was observed by measuring levels of MDA (malondialdehyde). Simultaneous decrease in the levels of TCA (tricarboxylic acid) enzymes such as ICDH (isocitrate dehydrogenase) α-KGDH (α-ketoglutarate dehydrogenase) SDH (succinate dehydrogenase) and MDH (malate dehydrogenase) were observed. Decrease in the levels of these enzymes suggests a loss in mitochondrial function and integrity. The supplementation of QE (50 mg/kg body weight) restored the depleted levels of enzymes and above hepatic mitochondrial abnormalities to near normalcy. Thus, our study emphasizes on antioxidant property of QE in improving the mitochondrial functions in AZA induced hepatic degradation.

Keywords: Oxidative stress,Antioxidant, Azathioprine, Quercetin

Original Article

Aphrodisiac activity and curative effects of ethanolic extracts of Ipomoea carnea against sexual behavior on prolonged immobilization-induced stress in rodents

Rajnish K. Singh^a,b,*, Vaishalia^a, Vaibhav Rathore^a, Rajan Kaushik^a, Arun Mishra^c, Arun K. Mauryad^d

^aMoradabad Educational Trust Group of Institution Faculty of Pharmacy, Moradabad, Uttar Pradesh, India.

^bDepartment of Pharmacology, Luqman College of Pharmacy, Gulbarga, Karnataka, India.

^cDepartment of Pharmacognosy, IFTM, University, Moradabad, Uttar Pradesh, India.

^dDoon College of Education, Sundarpur, Saharanpur, Uttar Pradesh, India.

*Corresponding author: Tel. No.: +91 7417574977, Email: rajnishsingh4u@gmail.com

The present study was designed to investigate the aphrodisiac activity of the ethanolic extract of Ipomoea carnea leaves. Aphrodisiacs can be categorized according to their mode of action into three groups: substances that increase libido (i.e., sexual desire, arousal), substances that increase sexual potency (i.e., effectiveness of erection) and substances that increase sexual pleasure. Therefore, the search for a better tolerated aphrodisiac agent appears to be a necessity. The aphrodisiac activity was evaluated in various experimental animal models like Effect on fertility in mice, Effect on sperm properties in mice and Sexual behaviour on prolonged immobilization stress in rats. The ethanolic extract of Ipomoea carnea leaves even up to the dose level of 2000mg/kg. It has not produced any lethal effect. In Effect on fertility model, ethanolic extract of Ipomoea carnea leaves only 200 & 400 mg/kg dose treated groups but not 100 mg/kg dose had shown a significant increase in litter size but no effect on M/F ratio. Ethanolic extract of Ipomoea carnea leaves was tested for its effect on sperm properties with different dose levels and all doses (100,200 & 400 mg/kg) have shown a significant increase in spermatogenic activity with scant intertubular spaces between the tubules. Sexual behaviour in prolonged immobilization stress induced model, a significant increase in number of mounts and thrusting and decrease in mounting latency were recorded with 200 & 400 mg/kg treated doses only but not with 100 mg/kg treated group. The present investigation revealed that the ethanolic extract of Ipomoea carnea leaves was found to possess aphrodisiac activity.

Keywords: Aphrodisiac activity, Ipomoea carnea leaves, Ethanolic extract, Mice, Rats

Original Article

Isolation of a sterol from root of Mucuna pruriens

Pramod Kumar^a,*, Vijay Juyal^b, Showkat R. Mir^c

^aDepartment of Pharmaceutical Sciences, H.N.B. Garhwal University, Srinagar, Garhwal, Uttarakhand, India

^bDepartment of Pharmaceutical Sciences, Kumaun University Bhimtal, Nainital, Uttarakhand, India.

^cDepartment of Pharmacognosy & Phytochemistry, Jamia Hamdard University, New Delhi, India.

*Corresponding Author. Tel.: +91 9456532849, E-mail address: pramodhnbgu@gmail

Mucuna pruriens belongs to the family Fabaceae significantly used in Indian traditional system for their aphrodisic, antidiabetic, antioxidant, antihyperlipidimic, anticancer and various other human ailments. The biological activity of mucuna roots has been reported in various research papers. The present paper reveals the isolation of a sterol. On the basis of spectral data and chemical reactions, the structure of compound was elucidated as 3β-benzoxy-stigmast 5-ene.

Keywords: FTIR, NMR, Column Chromatography, Soxhlet apparatus

Review Article

A new era of pharmacognosy – “Molecular Pharmacognosy”
Himesh Soni*, Priyanka Narwani, A. K. Singhai

Lakshmi Narain College of Pharmacy, Bhopal, Madhya Pradesh, India.

*Corresponding Author. Tel.: +91 9826386065, E-mail address: himeshsoni@rediffmail.com

At the edge between Pharmacognosy and molecular biology, molecular Pharmacognosy has developed as a new intermediate branch. This article reviews the methods, relevance and scene of molecular pharmacognosy. The main background focus in this manuscript including the molecular identification of medicinal raw materials, phylogenetic evolution of medicinal plants/animals, evaluation and preservation of germplasm resources for medicinal plants, etiology of endangered medicinal plants species, biosynthesis and bio-regulation of alleopatic substances. A recent advancement in herbal drug discovery involves a comprehensive approach including molecular techniques.

Keywords: DNA marker, Genetic diversity, Molecular biology, Molecular pharmacognosy, Pharmacognosy

Review Article

Physicochemical evaluation of Triphala churna

Rajan Kaushika^a,*, Praveen Kumar^a, Vaibhav Rathore^a, Gauranga S. Roy^b

^aMoradabad Educational Trust Group of Institutions Faculty of Pharmacy, Moradabad, Uttar Pradesh, India.

^bDepartment of Pharmacognosy, B.I.S. College of Pharmacy, Gagra, Moga, Punjab, India.

*Corresponding Author. Tel.: +91 9456808035, E-mail address: rajankaushik96@gmail.com.

Standardization of herbal formulation is essential in order to assess the quality of drugs for therapeutic value. In the present study the marketed formulation has been standardized in order to assess the quality of marketed formulation based on the physiochemical characters (loss on drying, extractive values, ash values and pH), physical characters viz. (bulk density, tapped density, angle of repose, hausner’s ratio and carr’s index), phytoconstituents and HPTLC analysis according to pharmacopoeial and standard methods. The set parameters viz. loss on drying (12% w/w), water soluble extractive (46.2% w/w), alcohol soluble extractive (8.6% w/w), total ash (10.2% w/w), pH value (6.2), bulk density (0.4879 gm/ml), tapped density (0.6455 gm/ml), angle of repose (22.3◦), hausner’s ratio (1.3230) and carr’s index (24.415) were found to be sufficient to standardize the Triphla Churna and can be used as reference standards for the quality control/quality assurance study. HPTLC analysis of the formulation showed an Rf value, 0.54 for gallic acid which confirmed the presence of tannins in the formulation. The results obtained may also be considered as tools for assistance to the regulatory authorities, scientific organization and manufacturers for developing standard formulation of great efficacy.

Keywords: HPTLC, Standardization, Physical evaluation