Download View Contents - Pharmacophore

PHARMACOPHORE JOURNAL
USA CODEN: PHARM7
IC VALUE: 5.09
IMPACT FACTOR: 0.927
Pharmacophore
(An International Research Journal)
ISSN
2229 – 5402
Available online at http://www.pharmacophorejournal.com/
Article [1]
Vol.5, Issue-4, July-August 2014
Original Research Paper
DEVELOPMENT AND VALIDATION OF RP-HPLC METHOD FOR THE
SIMULTANEOUS ESTIMATION OF CHLORTHALIDONE AND CILNIDIPINE IN
BULK AND COMBINED TABLET DOSAGE FORM
Neelima Kudumula1* and Y. Rajendra Prasad2
1
Deparment of Medicinal Chemistry, Sarojini Naidu Vanita Pharmacy Maha Vidyalaya,
Exhibition Grounds, Nampally, Hyderabad-500 001, A.P., India
2
Department of Pharmaceutical Chemistry, Andhra University College of Pharmaceutical
Sciences, Peda Waltair, Visakhapatnam-530003, India
ABSTRACT
A simple, sensitive, linear, precise and accurate method by Gradient RP-HPLC for the simultaneous
estimation of Chlorthalidone and Cilnidipine in bulk and in their combined Tablet Dosage form was
developed and validated. The separation of the two drugs was based on Inertsil ODS 3V (250 × 4.6 mm,
i.d., 5 μm) column in a Gradient mode. The mobile phase consisting of 0.025 M Potassium dihydrogen
orthophosphate buffer whose pH was adjusted to 2.5 using dilute orthophosphoric acid (solvent A) and
Acetonitrile (solvent B), set with gradient programming for 15 min at a flow rate of 1ml/min and the
detection of the drugs at 240 nm using a variable PDA detector. The retention times of Chlorthalidone and
Cilnidipine were found to be 3.872 minutes and 7.668 minutes respectively. The assay of CHL and CIL in
bulk drug and in combined tablet dosage form was found to be 99.72% and 99.90% respectively.
Calibration curves were linear for CHL and CIL at concentration ranges of range of 200-600 μg/ml and 160480 μg/ml with the regression coefficient of 0.999 for both the drugs and precise with (% RSD < 2). The
LOD was found to be 0.50 μg/ml and 0.40 μg/ml for CHL and CIL and LOQ was 1.50 μg/ml 1.20 μg/ml for
CHL and CIL respectively. The developed method was validated by determining its linearity, accuracy,
precision, system suitability and can be employed for routine quality control analysis as per ICH guidelines.
Keywords: Chlorthalidone, Cilnidipine, RP-HPLC, Gradient mode, Validation.
[View Full Text PDF] [View as HTML]
Correspondence Author:
Neelima Kudumula
Deparment of Medicinal Chemistry, Sarojini Naidu Vanita Pharmacy Maha Vidyalaya, Exhibition Grounds, Nampally,
Hyderabad-500 001, A.P., India
Cite This Article: Neelima, Kudumula and Y, Rajendra Prasad (2014), “Development and validation
of RP-HPLC method for the simultaneous estimation of chlorthalidone and cilnidipine in bulk and
combined tablet dosage form”, Pharmacophore, Vol. 5 (4), ….-….
Submit manuscript: [email protected] or [email protected]
http://www.pharmacophorejournal.com/
PHARMACOPHORE JOURNAL
USA CODEN: PHARM7
IC VALUE: 5.09
IMPACT FACTOR: 0.927
Pharmacophore
(An International Research Journal)
ISSN
2229 – 5402
Available online at http://www.pharmacophorejournal.com/
Article [2]
Vol.5, Issue-4, July-August 2014
Original Research Paper
FORMULATION DEVELOPMENT AND IN VITRO CHARACTERIZATION OF
CARVEDILOL SUSTAIN RELEASE TABLET BY USING LIQUISOLID
TECHNIQUE
Tushar N. Patel*, Zankhana P. Sheth, Bhagirath K. Patel and Pritesh Patel
Sat Kaival College of Pharmacy, Sarsa, India
ABSTRACT
The in-vitro dissolution property of poorly water soluble Carvedilol was improved by exploring the
potential of Liquisolid system. Liquisolid technique as an approach was developed to sustain the drug
release from matrix compacts. Different Liquisolid compacts were prepared using the required quantities of
powder and liquid ingredients to produce acceptably flowable and compressible admixture. Eudragit (S, L,
RL or RS), Aerosil 200 and PVP were employed as carrier, coating material and binder respectively for
preparing Liquisolid compacts. The prepared Liquisolid compacts were evaluated for their flow properties
and compressibility. The results suggested that the presence of non-volatile cosolvent is vital to produce
slow release pattern for some of liquisolid compacts. The type of cosolvent had significant effect on drug
release and it was revealed that by changing the type of cosolvent, the desirable release profile was
achievable. PEG 400 was optimizing for this study. The sustained release action of different grade of
Eudragit i.e., S 100, L 100, RS 100 & RL 100 was studied from which Eudragit RL 121.5 mg shown better
dissolution profile till 12hr. Eudragit RL 100 resulted in fine network and matrix with lower porosity and
higher tortuosity could formed and the particle are surrounded by the polymer network resulting in the
lower diffusion of drug. This could reason for greater retardation properties. From this study it concludes
that the Liquisolid technique is a promising alternative for improvement of dissolution property of waterinsoluble drugs.
Keywords: Liquisolid compacts, Eudragit, Drug Release, Physico mechanical property, Dissolution
parameters
[View Full Text PDF] [View as HTML]
Correspondence Author:
Tushar N. Patel
Sat Kaival College of Pharmacy, Sarsa, India
Cite This Article: Tushar, N Patel; Zankhana, P Sheth; Bhagirath, K Patel and Pritesh, Patel (2014),
“Formulation development & in vitro characterization of carvedilol sustain release tablet by using liquisolid
technique”, Pharmacophore, Vol. 5 (4), …-….
Submit manuscript: [email protected] or [email protected]
http://www.pharmacophorejournal.com/
PHARMACOPHORE JOURNAL
USA CODEN: PHARM7
IC VALUE: 5.09
IMPACT FACTOR: 0.927
Pharmacophore
(An International Research Journal)
ISSN
2229 – 5402
Available online at http://www.pharmacophorejournal.com/
Article [3]
Vol.5, Issue-4, July-August 2014
Original Research Paper
DESIGN AND CHARACTERIZATION OF FLOATING TABLET OF
ONDANSETRON HYDROCHLORIDE FOR GASTRICRETENTION
S. Yadav*, S. Padhi and P. Kumar
Department of Pharmaceutical Technology, Noida Institute of Engineering and Technology,
Plot No.19, Knowledge Park-II, Greater Noida, Uttar Pradesh-201306, India
ABSTRACT
Floating drug delivery system is the gastro retentive systems can remain in the stomach for many hours and
can significantly prolong the gastric residence time of drugs. The aim of the work is to design floating
tablets of Ondansetron for gastric retention by using 32 factorial designs. Chitosan and Sodium Bicarbonate
is used as independent variables were as time taken to release 50% and floating lag time is dependent
variables. Floating tablets of Ondansetron were prepared by direct compression method using polymers and
sodium bicarbonate. Floating tablets were evaluated for floating time, floating lag time, drug content and in
vitro dissolution profile. The lag time is between 25-10 sec and floating time of the formulations stopped on
12 hrs, Drug release percentage is upto 90-94 % and kinetic studies were carried out and best batch is F9,
The best fit model is Korsemeyer Peppas Model. From the study it is proof that the sustain release by
floating tablets of Ondansetron can be develop.
Keywords: Floating tablets, Sustained release, Gastric retention time, Ondansetron, Factorial design.
[View Full Text PDF] [View as HTML]
Correspondence Author:
S. Yadav
Department of Pharmaceutical Technology, Noida Institute of Engineering and Technology, Plot No.19, Knowledge ParkII, Greater Noida, Uttar Pradesh-201306, India
Cite This Article: S, Yadav; S, Padhi and P, Kumar (2014), “Design and characterization of floating
tablet of ondansetron hydrochloride for gastric retention”, Pharmacophore, Vol. 5 (4), …-…..
Submit manuscript: [email protected] or [email protected]
http://www.pharmacophorejournal.com/
PHARMACOPHORE JOURNAL
USA CODEN: PHARM7
IC VALUE: 5.09
IMPACT FACTOR: 0.927
Pharmacophore
(An International Research Journal)
ISSN
2229 – 5402
Available online at http://www.pharmacophorejournal.com/
Article [4]
Vol.5, Issue-4, July-August 2014
Original Research Paper
A PROSPECTIVE AND OBSERVATIONAL STUDY OF USE AND FREQUENCY
OF VARIOUS ERYTHROPOIETIN (EPO) CONGENERS AND ANALYSING
THEIR EFFECTIVENESS IN THREE FORMS: DARBEPOETIN ALFA, EPOETIN
ALPHA AND PEGYLATED ERYTHROPOIETIN ON DIALYSIS PATIENTS AT
MAX SUPER SPECIALITY HOSPITAL, PATPARGANJ, DELHI
Anamika Singh1*, Avijit Majumdar1, Sanjita Das1, Satish Chhabra2,
Aditya Jayaraman2 and Sourabh Bharadwaj2
1
NIET School of Pharmacy, 19, Knowledge Park 2, Greater Noida-201306, UP
2
Max Super Speciality Hospital Patparganj-110092, Delhi
ABSTRACT
Erythropoietin or EPO is a glycoprotein hormone that controls Erythropoiesis, or red blood cell production.
Human EPO has a molecular weight of 34 kDa. Erythropoietin has been shown to exert its effects
by binding to the erythropoietin receptor (EpoR). EPO is highly glycosylated (40% of total molecular
weight), with half-life in blood around five hours. EPO's half-life may vary between endogenous and
various recombinant versions. In this study we will consider following epo on (n=105 patients) 35 patients
in each arm. This study compared effectiveness between Darbepoetin alfa, Epoetin alpha and Pegylated
Erythropoietin, by calculating their hemoglobin level of the patient on dialysis. A voluntary written consent
will be obtained from all eligible patients who fulfill all inclusion criteria and do not meet any exclusion
criteria. An average level of Hb for group of patients was recorded as: Darbepoetin alfa (before and after 7.8
and 10.9), Epoetin alfa (before and after 8.6 and 11.7) and Pegylated erythropoietin (Before and after 8.7
and 12.7). Based on the study, and observing the detailed pattern of results produced by various
Erythropoietins on various patients, it can be concluded from our study Pegylated Erythropoietin showed
the maximum erythropoietin effect followed by Epoetin alpha and Darbepoetin alpha.
Keywords: Erythropoietin, Darbepoetin alpha, Epoetin alpha, Pegylated erythropoietin, Haemoglobin.
[View Full Text PDF] [View as HTML]
Correspondence Author:
Anamika Singh
NIET School of Pharmacy, 19, Knowledge Park 2, Greater Noida-201306, UP
Cite This Article: Anamika, Singh; Avijit, Majumdar; Sanjita, Das; Satish, Chhabra; Aditya,
Jayaraman and Sourabh, Bharadwaj (2014), “A prospective and observational study of use and frequency of
various erythropoietin (Epo) congeners and analyzing their effectiveness in three forms: darbepoetin alfa,
epoetin alpha and pegylated erythropoietin on dialysis patients at max super speciality hospital, patparganj,
Delhi”, Pharmacophore, Vol. 5 (4), ..-..
Submit manuscript: [email protected] or [email protected]
http://www.pharmacophorejournal.com/
PHARMACOPHORE JOURNAL
USA CODEN: PHARM7
IC VALUE: 5.09
IMPACT FACTOR: 0.927
Pharmacophore
(An International Research Journal)
ISSN
2229 – 5402
Available online at http://www.pharmacophorejournal.com/
Article [5]
Vol. 5, Issue-4, July-August 2014
Original Research Paper
PREPARATION AND EVALUATION OF THE ANTIVIRAL ACTIVITY OF
ACYCLOVIR LOADED NANO-NIOSOMES AGAINST HERPES SIMPLEX
VIRUS TYPE 1
1
Mirzaei Parsa Mohamad Javad , Monavari S. Hamid Reza2*, Dadashzadeh Simin3,
Ebrahimi S. Ahmed4, Bolouri Bahram5 and Haeri Azadeh3
1
School of Advanced Medical Technologies, Tehran University of Medical Sciences, Tehran, Iran
Department of Virology, School of Medicine, Iran University of Medical Sciences, Tehran, Iran
3
School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran
4
Department of Pharmacology, School of Medicine, Tehran University of Medical Sciences, Tehran, Iran
5
Department of Medical Physics and Engineering, Tehran University of Medical Sciences, Tehran, Iran
2
ABSTRACT
Acyclovir (ACV), analog of 2′-deoxyguanosine, is known for its antiviral activity against Herpes
simplex virus (HSV). A major limitation of treatment with acyclovir is high distribution and low
half-life that leads to taking high doses of acyclovir. Recent studies have shown that entrapment of
acyclovir in nano-carriers can increase effectiveness and also decrease side effects of the drug.
Therefore, in the present study the preparation and characterization of acyclovir loaded nanoniosomes was investigated. The non-ionic surfactant vesicles were prepared by thin film hydration
method. The lipid composition in optimal formulation consisted of Span, cholesterol and D-tocopheryl polyethylene glycol succinate (TPGS) in the molar ratio of 55 : 30 : 15, respectively.
Physical characteristics of optimized niosomes such as particle size, encapsulation efficiency (EE)
and in vitro drug release were evaluated. Furthermore, the in vitro cytotoxicity study of empty
niosomes (E-N), acyclovir loaded niosomes (ACV-N) and ACV as a free drug against Hela cell
line was performed by MTT assay. The average of particle size and EE for optimized niosomes
were 122.6 ± 0.2 nm and 24 % respectively. The drug release profiles proved the efficacy of
optimized niosomes in prolonged release of ACV, so that the percent drug release for 1h was
recorded as approximately 11.7 %. The prepared niosomes also showed significant stability with
regard to particle size and EE when stored at least for seven days at 5˚C. The results of this study
revealed ACV-N (F5) have a higher antiviral activity compared with free drug, and could be a
suitable carrier for delivery of acyclovir in the treatment of HSV-1 infections.
Keywords: Acyclovir, Nano-niosomes, Herpes simplex virus.
[View Full Text PDF] [View as HTML]
Correspondence Author:
Monavari S. Hamid Reza
Department of Virology, School of Medicine, Iran University of Medical Sciences, Tehran, Iran
o
Cite This Article: Mirzaei. Parsa Mohamad Javad; Monavari, S Hamid Reza; Dadashzadeh, Simin;
Ebrahimi, S Ahmed; Bolouri, Bahram and Haeri, Azadeh (2014), “Preparation and evaluation of the
Submit manuscript: [email protected] or [email protected]
http://www.pharmacophorejournal.com/
PHARMACOPHORE JOURNAL
USA CODEN: PHARM7
IC VALUE: 5.09
IMPACT FACTOR: 0.927
antiviral activity of acyclovir loaded nano-niosomes against herpes simplex virus type 1”,
Pharmacophore, Vol. 5 (4), ..-...
Submit manuscript: [email protected] or [email protected]
http://www.pharmacophorejournal.com/
PHARMACOPHORE JOURNAL
USA CODEN: PHARM7
IC VALUE: 5.09
IMPACT FACTOR: 0.927
Pharmacophore
(An International Research Journal)
ISSN
2229 – 5402
Available online at http://www.pharmacophorejournal.com/
Article [6]
Vol.5, Issue-4, July-August 2014
Original Research Paper
FORMULATION AND IN VITRO EVALUATION OF ORAL FLOATING
NICARDIPINE HYDROCHLORIDE TABLETS USING POLYETHYLENE
GLYCOL 6000 AND VARIOUS HPMC GRADES
Chabria N. B.1* and Narayanan N.2
1
Pharmacy Department, Higher College of Technology, Ministry of Manpower, Muscat,
Sultanate of Oman
2
Department of Pharmaceutics, Jaya College of Pharmacy, Thiruninravur -262024, Chennai,
Tamilnadu, India
ABSTRACT
The purpose of this research was to formulate floating tablets of Nicardipine hydrochloride so as to prolong
its gastric residence time and increase its bioavailability as it has good solubility at low pH values. Melt
granulation technique was used for preparing the floating tablets using polyethylene glycol 6000 as
bioadhesive hydrophilic meltable polymer and different viscosity grades of direct compressible polymer like
hydroxyl propyl methylcellulose, and gas generating agent like sodium bicarbonate and ethyl cellulose as
floating enhancer material. Pre-compressional and post compressional parameters were evaluated. The
mechanisms of drug release were analyzed using different kinetic models. The concentrations of PEG 6000,
HPMC K4M, were selected as independent variables and drug release values at t50% and t80% as dependent
variables. Formulation P6 was selected as an optimum formulation as it showed more similarity in
dissolution profile with theoretical profile (similarity factor, f2 = 0.98). It was also observed that increase in
viscosity of the HPMC grade resulted in increased floating lag time with simultaneous increase in floating
duration. The in vivo studies in albino rabbit showed good floating duration for the optimized formulation.
The FTIR/DSC studies revealed no interaction between the drugs and excipients. It can be concluded from
this study that the combined matrix system containing combination of high molecular weight hydrophilic
polymers with increased viscosity minimized the burst release of drug from the tablet and achieved a
controlled drug release which is otherwise difficult to achieve with only single polymer matrix.
Keywords: Nicardipine HCl, Melt granulation technique, HPMC, PEG6000, In vitro buoyancy, Kinetic
models.
[View Full Text PDF]
[View as HTML]
Correspondence Author:
Chabria N. B.
Pharmacy Department, Higher College of Technology, Ministry of Manpower, Muscat, Sultanate of Oman
Cite This Article: Chabria, NB and Narayanan, N (2014), “Formulation and in vitro evaluation of oral
floating nicardipine hydrochloride tablets using polyethylene glycol 6000 and various HPMC grades”,
Pharmacophore, Vol. 5 (4), ..-..
Submit manuscript: [email protected] or [email protected]
http://www.pharmacophorejournal.com/
PHARMACOPHORE JOURNAL
USA CODEN: PHARM7
IC VALUE: 5.09
IMPACT FACTOR: 0.927
Pharmacophore
(An International Research Journal)
ISSN
2229 – 5402
Available online at http://www.pharmacophorejournal.com/
Article [7]
Vol.5, Issue-4, July-August 2014
Original Research Paper
MOLECULAR DOCKING STUDIES OF WATTAKAKA VOLUBILIS FLAVONIDS
AS INSULIN RECEPTOR TYROSIN KINASE ACTIVATOR AS CURE FOR
DIABETES MELLITUS
M. Priya and J. Caroline Rose*
Department of Biotechnology, Arignar Anna College (Arts and Science), Krishnagiri,
Tamil Nadu, India
ABSTRACT
The studies on molecular docking have emerged during last three decades and now are becoming the
integral part in drug discovery and development. In silico approach was used to access the use flavonids
compounds of nutritionally enriched plant Wattakaka volubilis. Flavonids are potential agents that could act
as insulin receptor tyrosin kinase activators and reduce the harmful effects of diabetes. Insulin binds to its
receptors that are present on different cells of the body and mediates the absorption of glucose into the cell
and they belong to the class of tyrosine kinase receptor. The three dimensional structure of Insulin receptor
was obtained from PDB database and biocomponents of isoflovones and flavonones of the Wattakaka
volubilis were downloaded from USDA database. Docking studies of Insulin receptor with Wattakaka
volubilis biocomponents for isoflovones and flavonones were performed using HEX 6.3 software. Analysis
of the docking results suggested that the flavonones sub category compound hesperidins can act as a potent
insulin receptor activator than the other component.
Keywords: Diabetes, Insulin receptor, Isoflovones, Flavonones, Wattakaka volubilis, Docking HEX 6.3.
[View Full Text PDF] [View as HTML]
Correspondence Author:
J. Caroline Rose
Department of Biotechnology, Arignar Anna College (Arts and Science), Krishnagiri, Tamil Nadu, India
Cite This Article: M, Priya and J, Caroline Rose (2014), “Molecular docking studies of Wattakaka
volubilis flavonids as insulin receptor tyrosin kinase activator as cure for diabetes mellitus”,
Pharmacophore, Vol. 5 (4), ..-...
Submit manuscript: [email protected] or [email protected]
http://www.pharmacophorejournal.com/
PHARMACOPHORE JOURNAL
USA CODEN: PHARM7
IC VALUE: 5.09
IMPACT FACTOR: 0.927
Pharmacophore
(An International Research Journal)
ISSN
2229 – 5402
Available online at http://www.pharmacophorejournal.com/
Article [8]
Vol.5, Issue-4, July-August 2014
Original Research Paper
DESIGNING, SYNTHESIS AND BIOLOGICAL EVALUATION OF NOVEL
PYRIDAZINONE DERIVATIVES
Sukhbir Lal Khokra1*, Sonakshi Seth1, Baljit Saharan2 and Ankita2
1
Institute of Pharmaceutical Sciences, Kurukshetra University, Kurukshetra-136119, Haryana, India
2
Department of Microbiology, Kurukshetra University, Kurukshetra-136119, Haryana, India
ABSTRACT
The designing and synthesis of selected 6-(4-methylphenyl)-4,5-dihydropyridazin-3(2H)-one, 6-(4benzylphenyl)-4,5-dihydropyridazin-3(2H)-one and 6-(4-phenoxyphenyl)-4,5-dihydropyridazin-3(2H)-one
derivatives was carried out starting from succinic anhydride and aroylpropionic acids using substituted
phenylhydrazines guide by computational approach. Estimation of pharmacotherapeutic potential, possible
molecular mechanism of action, toxic/side effects and interaction with drug-metabolizing enzymes was also
achieved by computational & suitable in-vitro studies. The in-silico docking results showed that compound
no. III l & III c were best with analgesic potential while III u & III l were found to be best for antiinflammatory activity. The results of in-vivo anti-inflammatory studies by carrageenan induced rat paw
edema method also revealed that the compound no. III u showed maximum inhibition in paw edema volume
followed by compound no. III l while the compound no. III l showed maximum analgesic effect determined
by Acetic acid induced writhing method and inhibited the wriths to 69.99 % followed by the compound no.
III c. The compound no. III l also showed good analgesic effect determined by Tail immersion method and
increased the reaction time to 90 minutes followed by the compound no. III c. In in-vitro anti-bacterial
studies, compound no. III j was found to be most effective against Gram positive strain S. aureus and B.
cereus showing the maximum zone of inhibition of 32 mm and 33 mm, respectively whereas compound no.
III n was found to be most effective against Gram negative strain E. coli and S. flexveri showing maximum
zone of inhibition of 29 mm and 30 mm respectively. The compound no. III u was found to have maximum
anti-oxidant potential i.e. 89.393 % at concentrations of 1000, 500 and 250 μg/ml. From above results, it is
concluded that compound III u has maximum anti-inflammatory and anti-oxidant potential followed by III l.
Also anti-oxidant activity has a parallel association with inflammatory process and can be regarded base for
anti-inflammatory activity. So, in-vitro results along with in-silico findings strengthens the research findings
of these studies.
Keywords: Pyridazinones, Analgesic, Anti-inflammatory, Antimicrobial activity, Molegro virtual docker.
[View Full Text PDF] [View as HTML]
Correspondence Author:
Sukhbir Lal Khokra
Institute of Pharmaceutical Sciences, Kurukshetra University, Kurukshetra-136119, Haryana, India
Cite This Article: Sukhbir, Lal Khokra; Sonakshi, Seth; Baljit, Saharan and Ankita (2014), “Designing,
synthesis and biological evaluation of novel pyridazinone derivatives”, Pharmacophore, Vol. 5 (4), ..-..
Submit manuscript: [email protected] or [email protected]
http://www.pharmacophorejournal.com/
PHARMACOPHORE JOURNAL
USA CODEN: PHARM7
IC VALUE: 5.09
IMPACT FACTOR: 0.927
Pharmacophore
(An International Research Journal)
ISSN
2229 – 5402
Available online at http://www.pharmacophorejournal.com/
Article [9]
Vol.5, Issue-4, July-August 2014
Review Article
CHEMISTRY AND BIOLOGICAL ACTIVITY OF SOME ALANTOLOIDS FROM
INULA SPECIES - A REVIEW
Ramandeep Kaur, Dalvir Kataria and K K Chahal*
Department of Chemistry, Punjab Agricultural University, Ludhiana, Punjab-141004, India
ABSTRACT
The compounds present in plants of genus Inula exhibit wide spectrum of biological and medicinal
activities. These plants are rich source of wide variety of bioactive secondary metabolites such as tannins,
terpenoids, alkaloids, and flavonoids. Alantolactone and Isoalantolactone are the major compounds present
in Inula plants. The selection of the plants in the present study is primarily based on their chemistry,
biological and medicinal properties reported. This review attempts to summarize the current status of
reported various activities of Inula species. Some very interesting findings have been observed and thus
recorded and reported in this review.
Keywords: Inula, Sesquiterpenoids, Secondary metabolites, Alantolactone, Isoalantolactone.
[View Full Text PDF] [View as HTML]
Correspondence Author:
K K Chahal
Department of Chemistry, Punjab Agricultural University, Ludhiana, Punjab-141004, India
Cite This Article: Ramandeep, Kaur; Dalvir, Kataria and KK, Chahal (2014), “Chemistry and
biological activity of some alantoloids from inula species - A review”, Pharmacophore, Vol. 5 (4), ..-..
Submit manuscript: [email protected] or [email protected]
http://www.pharmacophorejournal.com/
PHARMACOPHORE JOURNAL
USA CODEN: PHARM7
IC VALUE: 5.09
IMPACT FACTOR: 0.927
Pharmacophore
(An International Research Journal)
ISSN
2229 – 5402
Available online at http://www.pharmacophorejournal.com/
Article [10]
Vol.5, Issue-4, July-August 2014
Original Research Paper
ISOLATION, CHARACTERIZATION OF BIOACTIVE MOLECULES FROM
XANTHIUM SPINOSIUM AND THEIR BIOLOGICAL EVALUATION
Sadath Ali1*, Amit Kumar Verma2 and Abdul Baseer Khan1
1
Azad Institute of Pharmacy and Research, Lucknow, India
2
Himalayan Institute of Pharmacy and Research, Dehradun, India
ABSTRACT
Two sesquiterpene lactones; xanthanolides, isolated and their structures were established by spectroscopic
methods (IR, 1H – NMR, 13C – NMR and Lc-Ms spectra). Antisuppresent activity and antimicrobial study,
Were carried out the isolated isoxanthanol has got significant antisuppresent activity as compared to control
and standard were as xanthanol has got moderate activity compared to control and standard. But the isolated
compounds does not show any significant antimicrobial activity compared to control and standard.
Keywords: Xanthium spinosum, Compositae, Sesquiterpene lactones, Xanthanolides, Isolation,
antisuppresent activity and Antimicrobial study.
[View Full Text PDF] [View as HTML]
Correspondence Author:
Sadath Ali
Azad Institute of Pharmacy and Research, Lucknow, India
Cite This Article: Sadath, Ali; Amit, Kumar Verma and Abdul, Baseer Khan (2014),
“Isolation, characterization of bioactive molecules from xanthium spinosium and their
biological evaluation”, Pharmacophore, Vol. 5 (4), ..-..
Submit manuscript: [email protected] or [email protected]
http://www.pharmacophorejournal.com/
PHARMACOPHORE JOURNAL
USA CODEN: PHARM7
IC VALUE: 5.09
IMPACT FACTOR: 0.927
Pharmacophore
(An International Research Journal)
ISSN
2229 – 5402
Available online at http://www.pharmacophorejournal.com/
Article [11]
Vol.5, Issue-4, July-August 2014
Original Research Paper
SOLUBILITY ENHANCEMENT OF POORLY WATER SOLUBLE DRUG
ATORVASTATIN CALCIUM BY SOLID DISPERSION TECHNIQUE USING
NATURAL CARRIER
S. J. Wadher*, S. S. Martande and T. M. Kalyankar
School of Pharmacy, Swami Ramanand Teerth Marathwada University, Nanded, India
ABSTRACT
Atorvastatin calcium (ATC) is an oral anticholesteremic agent. ATC belongs to BCS class II drug having
high permeability but low aqueous solubility. In order to get beneficial therapeutic effects, its water
solubility needs to be increased. In the present study, attempt was made to improve solubility and
dissolution rate of ATC by formulating it into solid dispersion using maltose monohydrate as a highly water
soluble carrier. Three methods were used for preparing solid dispersion, namely, physical mixture, kneading
and solvent evaporation method in 1:1, 1:3 and 1:5 drug-carrier ratios. The FTIR study of ATC, its
combination with the carrier, and of the sold dispersion indicated no interaction between drug, carrier and
other excipients used. The prepared solid dispersion showed improved solubility and dissolution rate as
compared to pure drug. The improvement in solubility may be attributed to the improved wettability of ATC
due to uniform dispersion into the carrier. The optimized batch was K2, which was prepared by kneading
method in 1:3 ratios. The optimized batch released 99.59 % drug within 60 min and had solubility almost
five folds higher than pure ATC. From the solubility values it was clear that kneading method was more
suitable than the other two methods used for preparing solid dispersion. The XRD studies revealed that the
crystalline nature of ATC was reduced when formulated into solid dispersion. The optimized batch of solid
dispersion was chosen for formulating immediate release tablet into three batches by direct compression
method by varying the concentration of superdisintegrant, crosscarmellose sodium. Tablet prepared with
20% cross carmellose sodium showed 99.41% drug release in 60 min, this drug release was higher
compared to the other two batches of tablet prepared.
Keywords: Atorvastatin calcium (ATC), Solid dispersion, Solubility, Dissolution.
[View Full Text PDF] [View as HTML]
Correspondence Author:
S. J. Wadher
School of Pharmacy, Swami Ramanand Teerth Marathwada University, Nanded, India
Cite This Article: SJ, Wadher; SS, Martande and TM, Kalyankar (2014), “Solubility enhancement of
poorly water soluble drug atorvastatin calcium by solid dispersion technique using natural carrier”,
Pharmacophore, Vol. 5 (4), ..-..
Submit manuscript: [email protected] or [email protected]
http://www.pharmacophorejournal.com/
PHARMACOPHORE JOURNAL
USA CODEN: PHARM7
IC VALUE: 5.09
IMPACT FACTOR: 0.927
Pharmacophore
(An International Research Journal)
ISSN
2229 – 5402
Available online at http://www.pharmacophorejournal.com/
Article [12]
Vol.5, Issue-4, July-August 2014
Review Article
PHYTOPHARMACOLOGICAL USES OF TEPHROSIA PURPUREA - A REVIEW
Baranwal Akanksha*, Mazumder Avijit, Chakraborthy G.S., Gupta Seema
Department of Pharmaceutical Technology, Noida Institute of Engineering & Technology
(NIET), Greater Noida, India
ABSTRACT
Tephrosia purpurea (Linn.) Pers (Fabaceae) is a perennial herb. In the Ayurveda system, Tephrosia
purpurea is referred to as Sarwa wran vishapaha which implies that it can heal any type of wound.
Tephrosia purpurea has played an important role in the traditional medicine. Thus, the modern
pharmacological and clinical investigation of Tephrosia purpurea is a valuable herbal therapy that has an
antioxidant, antimicrobial, anti-inflammatory, anti-viral and antiulcer properties. Whole plant has been used
to cure tumors, ulcers, leprosy, allergic and inflammatory conditions such as rheumatism, asthma and
bronchitis. The aqueous extract of Tephrosia purpurea seeds has shown significant in vivo hypoglycemic
activity in diabetic rabbits. The flavanoids isolated from the plant has been reported to have antimicrobial
activity. It has also been reported to acquire hepatoprotective, mast cell stabilizing and erythrocyte
membrane integrity enhancing effect in various animal models. Phytochemical investigations on Tephrosia
purpurea have revealed the presence of various phytoactive constituents such as glycosides, rotenoids,
isoflavones, flavanones.
Keywords: Tephrosia purpurea, Herb, Antioxidant, Antimicrobial, Anti-inflammatory, Anti-viral and
antiulcer.
[View Full Text PDF] [View as HTML]
Correspondence Author:
Baranwal Akanksha
Department of Pharmaceutical Technology, Noida Institute of Engineering & Technology (NIET), Greater Noida, India
Cite This Article: Baranwal, Akanksha; Mazumder, Avijit; Chakraborthy, GS and Gupta, Seema
(2014), “Phytopharmacological uses of tephrosia purpurea -A review”, Pharmacophore, Vol. 5 (4), ..-..
Submit manuscript: [email protected] or [email protected]
http://www.pharmacophorejournal.com/
PHARMACOPHORE JOURNAL
USA CODEN: PHARM7
IC VALUE: 5.09
IMPACT FACTOR: 0.927
Pharmacophore
(An International Research Journal)
ISSN
2229 – 5402
Available online at http://www.pharmacophorejournal.com/
Article [13]
Vol.5, Issue-4, July-August 2014
Original Research Paper
SYNTHESIS, BIOLOGICAL EVALUATION AND DOCKING STUDIES OF DGLUCOSE DERIVED ARYL 1, 2, 3-TRIAZOLES
Thatipamula Ranjith Kumar, Sirassu Narsimha, Satheesh Kumar Nukala and Sudhakar
Lavudya and Nagavelli Vasudeva Reddy*
Department of Chemistry, Kakatiya University, Warangal-506009, Telangana, India
ABSTRACT
Synthesis, characterization, antimicrobial activity and docking studies of 1, 2, 3-triazoles comprising a
glucose and aryl moieties were reported. Majority of the compounds found to be active and few of them
exhibited strong in vitro antimicrobial activity against S. aureus, B. subtilis, E. coli, P. aeruginosa, B.
proteus, C. albicans and A. fumigatus. All the compounds were subjected to docking studies against S.
aureus tyrosyl tRNA synthetase and Lanosterol-14-demethylase (CYP51). The docking study results
demonstrated that, all are having considerable binding energies and have good affinity toward the active
sites of the protein, thus, they may be considered as good inhibitors of tyrosyl tRNA synthetase and CYP51.
Keywords: O-Propargyl Glucoside, Arylazide, Click chemistry, Glucotriazoles, Antimicrobial activity,
Molecular docking.
[View Full Text PDF] [View as HTML]
Correspondence Author:
Nagavelli Vasudeva Reddy*,
Department of Chemistry, Kakatiya University, Warangal-506009, Telangana, India
Cite This Article: Thatipamula, Ranjith Kumar; Sirassu, Narsimha; Satheesh, Kumar Nukala;
Sudhakar, Lavudya and Nagavelli, Vasudeva Reddy (2014), “Synthesis, biological evaluation and docking
studies of d-glucose derived aryl 1, 2, 3-triazoles”, Pharmacophore, Vol. 5 (4), ..-..
Submit manuscript: [email protected] or [email protected]
http://www.pharmacophorejournal.com/
PHARMACOPHORE JOURNAL
USA CODEN: PHARM7
IC VALUE: 5.09
IMPACT FACTOR: 0.927
Pharmacophore
(An International Research Journal)
ISSN
2229 – 5402
Available online at http://www.pharmacophorejournal.com/
Article [14]
Vol.5, Issue-4, July-August 2014
Original Research Paper
FORMULATION AND EVALUATION OF FLOATING MICROSPHERE OF
AMLODIPINE BESYLATE BY USING ETHYLCELLULOSE AND HPMC
R. Mazumder, M. Sharma and A. Mishra*
Department of Pharmaceutical Technology, Noida Institute of Engineering and Technology,
Plot No.19, Knowledge Park-II, Greater Noida, Uttar Pradesh-201306, India
ABSTRACT
The purpose of this research work was to develop a novel gastro retentive floating microsphere of
Amlodipine Besylate. Amlodipine besylate has maximum solubility in acidic pH and thus most suitable to
prolong release of drug in stomach so an attempt has been made to sustain the drug release by incorporation
oh hydrophilic swellable polymers such as HPMC and ethylcellulose and present it in the form of gastro
retentive floating microspheres which after oral administration are designed to provide the desired
controlled and complete release of drug for prolonged period of time in the treatment of hypertension.
Floating microsphere of Amlodipine Besylate were formulate using various material HPMC, ethylcellulose,
ethanol, dichloromethane, SLS. The concentration of these agents was also optimized to get desired
controlled release of drug. The floating microsphere were evaluated for physical characterization, size of
microsphere, entrapment efficiency, swelling index, buoyancy studies and in vitro release studies. The result
indicated that the optimized intragastric floating microsphere (F8) composed of 1g Amlodipine Besylate, 4g
ethylcellulose, 0.3g HPMC exhibited 97% release in 8 hrs, while the buoyancy lag time was 20 sec and the
intragastric floating microsphere remain buoyant for 20 hrs. In vitro drug release kinetics evaluated using
the linear regression methods was using found to follow the Zero order kinetics. Optimized intragastric
floating microsphere showed no significant change in physical appearance, drug content, total buoyancy
time or in vitro dissolution pattern after storage at 40oC/75% relative humidity for 1 month.
Keywords: Amlodipine besylate, Floating microspheres, Gastro retentive, Intragastric floating, Floating
drug delivery, Controlled release.
[View Full Text PDF] [View as HTML]
Correspondence Author:
A. Mishra
Department of Pharmaceutical Technology, Noida Institute of Engineering and Technology, Plot No.19, Knowledge ParkII, Greater Noida, Uttar Pradesh-201306, India
Cite This Article: R, Mazumder; M, Sharma and A, Mishra (2014), “Formulation and evaluation of
floating microsphere of amlodipine besylate by using ethylcellulose and HPMC”, Pharmacophore, Vol. 5
(4), ..-..
Submit manuscript: [email protected] or [email protected]
http://www.pharmacophorejournal.com/
PHARMACOPHORE JOURNAL
USA CODEN: PHARM7
IC VALUE: 5.09
IMPACT FACTOR: 0.927
Pharmacophore
(An International Research Journal)
ISSN
2229 – 5402
Available online at http://www.pharmacophorejournal.com/
Article [15]
Vol.5, Issue-4, July-August 2014
Original Research Paper
FORMULATION AND OPTIMIZATION OF THERMOREVERSIBLE IN-SITU
GEL OF VENLAFAXINE HCL
Shete Prathmesh M* and Shinde Ajay D
SVPM’s College of Pharmacy, Malegaon (Bk.), Baramati, Pune, Maharashtra-413015, India
ABSTRACT
The purpose of this research was to study the in-situ nasal gel system containing Venlafaxine HCl suitable
for administration in nose was formulated by cold method using combination of Poloxamer 407 and
Polyvinyl pyrrolidone (PVP). Thermoreversible, bioadhesive polymers such as Poloxamer 407 and PVP in
the form of in situ gel by cold technique. To modulate the gel strength and bioadhesive force for
Venlafaxine HCl nasal gel, bioadhesive polymers PVP were investigated. The gels were evaluated for
gelation temperature, bioadhesive force, gel strength, viscosity, Drug content and in-vitro release. A 2factor, 2-level full factorial design (22) was employed for optimization of Venlafaxine HCl gels with
Poloxamer 407 amount (%, X1) and polymers (PVP %, X2) as the prime selected independent variables,
which were varied at 2 different levels (low and high). The effect of formulation variables on the response
variables were statistically evaluated by using a commercially available software package Design-Expert®
version 8.0.1. The results revealed that as the increase of bioadhesive polymer PVP concentration, decrease
in gelation temperature (T). pH of all formulation were found to be within the range between 6 to 6.5. The
drug content for all formulation was found to be 96%-100%. The mucoadhesive test indicates that the level
of PVP increases, the mucoadhesive strength also increases. The developed formulations had optimum
viscosity. The optimized formulation shows the controlled drug release. This study further demonstrates that
administration of Venlafaxine Hcl intranasal in gel form is a pleasant and painless alternative.
Keywords: Nasal drug delivery, Venlafaxine HCl, Gel, Poloxamer 407, PVP, Factorial design.
[View Full Text PDF] [View as HTML]
Correspondence Author:
Shete Prathmesh M
SVPM’s College of Pharmacy, Malegaon (Bk.), Baramati, Pune, Maharashtra-413015, India
Cite This Article: Shete, Prathmesh M and Shinde, Ajay D (2014), “Formulation and optimization of
thermoreversible in-situ gel of venlafaxine HCL”, Pharmacophore, Vol. 5 (4), ..-..
Submit manuscript: [email protected] or [email protected]
http://www.pharmacophorejournal.com/
PHARMACOPHORE JOURNAL
USA CODEN: PHARM7
IC VALUE: 5.09
IMPACT FACTOR: 0.927
Pharmacophore
(An International Research Journal)
ISSN
2229 – 5402
Available online at http://www.pharmacophorejournal.com/
Article [16]
Vol.5, Issue-4, July-August 2014
Original Research Paper
ANTIOXIDANT POTENTIAL OF SOME MEDICINAL PLANTS
(Ocimum sanctum, Azadirachta indica and Nigella sativa)
Mohammed Shariq Iqbal1, Mahammad Israil Ansari1, Shehroz Jafri1, Sudhakar Padmesh1,
Iqbal Ahmad2 and Brijesh Pandey1*
1
Amity Institute of Biotechnology, Amity University Uttar Pradesh, Lucknow Campus,
Uttar Pradesh-226028 India
2
Aligarh Muslim University, Aligarh, Uttar Pradesh, India
ABSTRACT
The extracts of leaf, stem and root of Ocimum sanctum, Azadirachta indica and Nigella sativa, were used in
the comparative study of total carotene, flavonoids, phenolics and total antioxidant potential. Leaves of
Ocimum sanctum, exhibited maximum total carotene content (2.17±0.272 mg /gram fresh weight ±S.D),
while root of Nigella sativa exhibited the lowest (0.29±0.088 mg /gram fresh weight ±S.D). Flavonoids
were found to be maximum in the leaf of Nigella sativa (4.93±0.702 mg equivalent QE /gram of tissue
±S.D), while minimum in the root of Azadirachta indica (0.16±0.033 mg equivalent QE /gram of tissue
±S.D). A trend similar to total carotene content was exhibited by phenolics with (34.9±2.427 mg equivalent
GA /gram of tissue ±S.D) in the leaf of Ocimum sanctum as maximum and (6.85±2.005 mg equivalent GA
/gram of tissue ±S.D) in the root of Nigella sativa as minimum. Total antioxidant potential was observed to
be maximum in the root of Ocimum sanctum (0.69±0.013 mM equivalent ascorbic acid/g tissue ±S.D),
while minimum was recorded in the leaf of Nigella sativa (0.22±0.028 mM equivalent ascorbic acid/g tissue
±S.D). The variability when analyzed statistically by two way ANOVA it was found significant with (Pvalue < 0.05). The present study showed Ocimum sanctum to be an excellent source of antioxidants which
can be utilized for therapeutic purposes. However, the specific plant part need to be optimally utilized for
specific pharmaceutical/ neutraceutical formulation.
Keywords: Antioxidant, Azadirachta indica, Carotene, Flavonoid, Nigella sativa, Ocimum sanctum,
phenolics.
[View Full Text PDF] [View as HTML]
Correspondence Author:
Brijesh Pandey
Amity Institute of Biotechnology, Amity University Uttar Pradesh, Lucknow Campus, Uttar Pradesh- 226028 India
Cite This Article: Mohammed, Shariq Iqbal; Mahammad, Israil Ansari; Shehroz, Jafri; Sudhakar,
Padmesh1; Iqbal, Ahmad and Brijesh, Pandey (2014), “Antioxidant potential of some medicinal plants:
(Ocimum sanctum, Azadirachta indica and Nigella sativa)”, Pharmacophore, Vol. 5 (4), ..-..
Submit manuscript: [email protected] or [email protected]
http://www.pharmacophorejournal.com/