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Table of Contents
January-March 2012
Volume 4 | Issue 1
Page Nos. 1-58
Online since Monday, March 12, 2012
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EDITORIAL
Introduction of APCs in
J. Young Pharm.
p. 1
KK Mueen Ahmed
DOI
:10.4103/0975-1483.93567
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PHARMACEUTICS
Formulation and evaluation of cephalexin extended-release matrix tablets using hydroxy propyl methyl cellulose as rate-controlling polymer
p. 3
J Vijay, JT Sahadevan, R Prabhakaran, R Mehra Gilhotra
DOI
:10.4103/0975-1483.93570
The present investigation reports the design and evaluation of six-hour extended release film-coated matrix tablets of cephalexin using different grades of hydrophilic polymer hydroxypropylmethylcellulose (HPMC) employing direct compression method. The preformulation studies performed included the physical compatibility studies, Differential Scanning Calorimetry analysis, drug characterization using Fourier Transform Infra Red spectroscopic analysis and particle size analysis using sieve method. The tablets were evaluated for weight variation, hardness, thickness and friability. Results of the studies indicate that the polymers used have significant release-retarding effect on the formulation. The dissolution profile comparison of the prepared batches P1 to P8 and market preparation (Sporidex AF 375) was done by using Food and Drug Administration-recommended similarity factor (f
2
) determination. The formulation P8 (10% HPMC K4M, 15% HPMC 15cps) with a similarity factor (f
2
) of 77.75 was selected as the optimized formulae for scale-up batches. The dissolution data of the best formulation P8 was fitted into zero order, first order, Higuchi and Korsemeyer-Peppas models to identify the pharmacokinetics and mechanism of drug release. The results of the accelerated stability study of best formulation P8 for three months revealed that storage conditions were not found to have made any significant changes in final formulation F3. The release of cephalexin was prolonged for 6 h by using polymer combinations of HPMC and a twice daily matrix tablet was formulated.
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Formulation development and evaluation of alginate microspheres of ibuprofen
p. 13
M Nagpal, DK Maheshwari, P Rakha, H Dureja, S Goyal, G Dhingra
DOI
:10.4103/0975-1483.93573
The present study was designed to investigate the effects of different variables on the release profile of ibuprofen microspheres formulated using modified emulsification method. Eight batches of microspheres (F1-F8) were prepared by applying 2
3
factorial design. The amount of sodium alginate, amount of calcium chloride, and amount of magnesium stearate were selected as formulation variables. All the batches were evaluated in terms of percentage yield, percentage encapsulation efficiency and
in vitro
release characteristics. The batch F7 was found to be optimum batch and was further characterized via scanning electron microscopy (SEM) and particle size analysis. Multiple linear regression was applied to confirm significant effect of each variable on release characteristics. The model developed in the present study can be effectively utilized to achieve the formulation with desired release characteristics.
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PHARMACOGNOSY
Assessment of
In vitro
sun protection factor of
Calendula officinalis
L. (asteraceae) essential oil formulation
p. 17
AK Mishra, A Mishra, P Chattopadhyay
DOI
:10.4103/0975-1483.93575
The present study was undertaken to study the sunscreen activity of herbal formulation. There is no evidence of the sun protection factor (SPF) studies on essential oil of Calendula flowers (
Calendula officinalis
L., Asteraceae). The study investigates the
in vitro
SPF by ultraviolet specrtophotometry method of Calendula flower oil in a cream formulation. Calendula oil was isolated by Clavenger's apparatus, compositions were identified by GC-MS and the cream of calendula flower oil was prepared by homogenization method followed by evaluation for physical parameters. The sun protection factor of cream was evaluated by
in vitro
method employing UV-visible spectrophotometer (Shimazdu-1600). The SPF of Calendula oil in cream formulation exhibited good activity (SPF = 14.84 ± 0.16). Finding of this study suggested that calendula oil cream can be used to protect the skin from UV radiations in form of sunscreen cream and to maintain the natural pigmentation of the skin.
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PHARMACOLOGY
Evaluation and quantification of angiogenesis activity of
Terminalia bellirica roxb
, by mice sponge implantation method
p. 22
V Vinoth Prabhu, N Chidambaranathan, V Gopal
DOI
:10.4103/0975-1483.93577
Angiogenesis represents an excellent therapeutic target for the treatment of cardiovascular diseases. It is a potent physiological process that underlies the natural manner in which our bodies respond to a diminution of blood supply to vital organs, namely the production of new collateral vessels to overcome the ischemic state. This present study is aimed to evaluate and quantify the Angiogenic potential of
Terminalia bellirica
Roxb
, by
in vivo
mice sponge implantation assay. Here, gelatin sponge with or without Ethanolic extract of
Terminalia bellirica
leaf (EETB - 0.3 mg and 0.5 mg, respectively) were subcutaneously injected into Swiss albino mice, and 14 days later, the implanted sponges was excised and histologically examined. The stained section showed that sponge containing EETB had produced more vessels in gels than sponges alone. The new vessels were abundantly filled with intact Red blood corpuscles (RBCs), which indicate the formation of a functional vasculature inside the sponges and blood circulation in newly formed vessels by angiogenesis which is induced by EETB. It also measured that the hemoglobin content inside the sponges: Whereas, hemoglobin in control was nearly 0.3 μg, EETB cases the hemoglobin quantity was markedly enhanced to about 17 μg. Taken together, it demonstrated that Ethanolic extract of
Terminalia bellirica
leaf exhibited a profound angiogenic activity
in vivo.
The phytochemical screening and qualitative instrumental analysis of EETB reveals the presence of proteins and Phytosterols. The promising angiogenic potential may be due to the presence of the above chemical constituents. Further study is required to define more precisely the molecular mechanisms by which Ethanolic extract of
Terminalia bellirica
leaf modulates endothelial cell function and gene expression, as well as the pathological relevance of these findings.
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Investigation of the mechanisms underlying the gastroprotective effect of
Cymbopogon citratus
essential oil
p. 28
CN Fernandes, HF De Souza, G De Oliveria, JGM Costa, MR Kerntopf, AR Campos
DOI
:10.4103/0975-1483.93578
Cymbopogon citratus
is a medicinal plant popularly used in Brazil for the treatment of various diseases, and the research interest in this plant is justifiable because of its potential medicinal value in stomachache and gastric ulcer. This study was aimed to test the validity of this practice by using experimental models of gastric ulcer and to clarify the mechanisms of gastroprotection by
C. citratus
leaves essential oil (EOCC). EOCC was evaluated for the ability to protect the gastric mucosa against injuries caused by necrotizing agents (absolute ethanol and aspirin) in rodents. The results of this study revealed that EOCC posses a dose-independent anti-ulcer effect against the different experimental models. EOCC pretreatment depicted a higher preventive index in ethanol-(88%) and aspirin-induced (76%) acute ulceration. On pretreatment of mice with indomethacin, the cyclooxygenase inhibitor slightly suppressed the gastroprotective effect of EOCC (48.5%). Furthermore, EOCC gastroprotection was not attenuated in mice pretreated with L-NAME (85.2%), glibenclamide (100%), or yohimbine (79.7%), the respective inhibitors of nitric oxide synthase, K
+
ATP
channel activation, and α
2
receptors. These results confirmed the traditional use of
C. citratus
for the treatment of gastric ulcer. Thus, we provide the first evidence that EOCC reduces gastric damage induced by ethanol, at least in part, by mechanisms that involve endogenous prostaglandins.
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PHARMACEUTICAL CHEMISTRY
Design and microwave-assisted synthesis of 1,3,4-oxadiazole derivatives for analgesic and anti-inflammatory activity
p. 33
CR Biju, K Ilango, Manju Prathap, K Rekha
DOI
:10.4103/0975-1483.93576
1,3,4-Oxadizoles form a biologically important group of compounds having activities like analgesic, anti-inflammatory, bactericidal, antifungal, anticonvulsant, psychotropic, plant growth regulating and mono amino oxidase inhibition. This research has focused on the incorporation of the oxadiazole moiety into isoniazid because of their versatile biological action, to get 2-aryl-5-(4-pyridyl)-1,3,4-oxadiazole to explore the possibilities of some altered biological action. 1,3,4-Oxadiazole derivatives were synthesized by microwave-assisted synthesis and screened for their analgesic, anti-inflammatory activities. The synthesized compounds were characterized by Melting point, Thin layer chromatographyInfra red, Nuclear magnetic resonance spectroscopy, etc. Almost all the synthesized compounds possessed good activity as compared to the standard.
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Synthesis of some new isoxazoline derivatives of chalconised indoline 2-one as a potential analgesic, antibacterial and anthelmimtic agents
p. 38
P Mondal, S Jana, A Balaji, R Ramakrishna, LK Kanthal
DOI
:10.4103/0975-1483.93574
A series of novel 1[5''-(2'''-substituted phenyl)-4'',5'''-dihydro isoxazole-3''-yl]-3-[(4 substituted phenyl)imino]1-3-dihydro-2
H
-indole-2-one were synthesized from different substituted chalconised indole-2,3-dione was prepared from the different chalconised Isatin. The structures of the compounds were elucidated by elemental and spectral (IR,
1
H NMR, and MS) analysis. The synthesized compounds were screened for their analgesic activity by the acetic acid induced Writhing method and
in vitro
antimicrobial activity against the Gram-positive bacteria-
Staphylococcus aureus
and the Gram-negative bacteria-
Pseudomonas auroginosa
,
Pseudomonas mirabilis
, and
E. coli
by the cup plate agar diffusion method. Compounds 6a
1
, 6a
3
, 6b
3
, and 6b
2
were found to be active against bacteria. The compounds 6a
1
, 6b
3
, and 6a
3
show a significant analgesic activity. Synthesized compounds also screened for anthelmintic activity against
Pheretima posthuma
. Compounds 6a
1
, 6b
1
, and 6b
3
show significant anthelmintic activity.
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PHARMACEUTICAL ANALYSIS
Extractive spectrophotometric method for the determination of tropicamide
p. 42
ZA Shoaibi, AA Gouda
DOI
:10.4103/0975-1483.93572
Two simple, rapid, and extractive spectrophotometric methods were developed for the determination of tropicamide (TPC). These methods are based on the formation of ionpair complexes between the basic nitrogen of the drug with bromocresol purple (BCP) and methyl orange (MO) in acidic buffer solution. The formed complexes were extracted with chloroform and measured at 408 and 427 nm using BCP and MO, respectively. Beer's law was obeyed in the range 1.0-16 μg ml
−1
with correlation coefficient (
n=
6) ≥0.9991. The molar absorpitivity, Sandell sensitivity, detection, and quantification limits were also calculated. The composition of the ion pairs was found 1:1 by Job's method. The proposed methods have been applied successfully for the analysis of TPC in pure and in its eye drops.
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GENERAL PHARMACY
Occurrence and treatment of common health problems in a Nigerian community
p. 49
A Auta, SB Banwat, DW Dayom, D Shalkur, MO Avu
DOI
:10.4103/0975-1483.93571
Medicines are cost-effective interventions for the treatment and management of health problems. This research was carried out to determine the common health problems and medicine-use practices in treating health problems in Lamingo, Jos, Nigeria. A total of 109 households covering 676 individuals were recruited and followed up for a period of one month between 6 November 2010 and 11 December 2010. A structured interview was conducted on weekly visits to households to identify illnesses suffered by household members and treatment given. The results showed that 146 common health problems representing 1.3 cases per household per month were found. The cost of treatment per household per month was found to be $14.7. Infectious and parasitic diseases (44.6%), diseases of the digestive (11.0%) and respiratory system (9.6%) were common in the community. Self-medication was common (34.6%) and the patent medicine stores were the most common sources of medicines. Common classes of medicines used by community members were analgesics (23.6%), antimalarials (17.9%) and antibiotics (14.2%). Factors that influenced choice of treatment were previous knowledge and experience of family members with service provider and treatment (44.4%), cost (18.9%) and severity of condition (16.7%). There is, therefore, high occurrence of health problems and self-medication practices in the Lamingo community.
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LETTERS TO THE EDITOR
Health-related quality of life measurement
p. 54
PM Muragundi, AM Tumkur, RK Shetty, AN Naik
DOI
:10.4103/0975-1483.93568
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Evolutionarily conserved essential genes from arctic bacteria: A tool for vaccination
p. 55
MM Shanmugam, S Parasuraman
DOI
:10.4103/0975-1483.93569
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