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Table of Contents
April-June 2009
Volume 1 | Issue 2
Page Nos. 99-190
Online since Friday, September 11, 2009
Accessed 18,780 times.
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INVITED ARTICLE
Pharmaceutical E-learning: Precepts, retrospect and prospects
p. 99
B Singh, R Kapil, OP Katare
DOI
:10.4103/0975-1483.55740
The domain of pharmaceutical sciences is a highly dynamic one with the "half-life" of pharmaceutical information declining constantly. Be it the drug industry or the academic institutes, it is mandatory to keep abreast with the latest developments, and update our curricula and training contents accordingly. The traditional "chalk and talk" methods though are satisfying the objectives, yet have proved invariably to be monotonous and resource-intensive. The judicious use of web-based e-technologies in imparting training to the university students has been found to be interesting as well as rewarding. Being interactive, e-Learning in this context, presents the material in a structured manner and permits the student to progress at one's own pace taking an individual path through the lesson. Globally, the pharmaceutical institutes and industries have already recognized the enormous potential of e-Learning, and are applying it too in the mundane training of their skilled workforce. A transition from the erstwhile "hard" educational course materials in the printed form to the current "soft" materials on CDs and DVDs has already begun. Nevertheless, the pharmaceutical institutes and corporates of India are yet to harvest completely the utility of these effective and cost-effective e-Learning tools. But of late, the winds have started blowing in the favorable direction. With an increasing proportion of the young, computer-aware and "networked" population coupled with favorable gubernatorial policies, the future of e-Learning in India seems to be quite bright.
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PHARMACEUTICS
Skin penetration enhancement techniques
p. 110
M Bharkatiya, RK Nema
DOI
:10.4103/0975-1483.55741
Transdermal drug delivery systems allow delivery of a drug into the systemic circulation via permeation through skin layers at a controlled rate. In addition to the currently marketed formulations, new drugs are being formulated using the transdermal system because of the inherent advantage of administration by this route. It offers a noninvasive route of drug administration, although its applications are limited by low skin permeability. Innovative research exploiting penetration-enhancing strategies, such as iontophoresis, electroporation, microneedles, and sonophoresis, holds promise for the successful use of these drugs as consumer-friendly, transdermal dosage forms in clinical practice. This review outlines promising new technologies involved in enhancing transdermal permeation.
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Formulation and evaluation of drug-free ophthalmic films prepared by using various synthetic polymers
p. 116
Dipti H Patel, Manish P Patel, Madhabhai M Patel
DOI
:10.4103/0975-1483.55742
An attempt has been made to formulate drug-free ophthalmic films by using different polymers in single use as well as in combinations for matrix system design for ocular use and to study the effect of various plasticizers on
physicochemical characteristics and permeability of the resultant films. Drug-free films of hydroxypropyl methyl cellulose (HPMC), polyvinyl alcohol (PVA), hydroxypropyl cellulose (HPC), polyvinyl pyrrolidone (PVP), and Eudragit RL 100 polymers were prepared by the solvent casting method on a mercury surface by employing distilled water and ethanol as solvents, and glycerol and dibutyl phthalate as plasticizers. These films were evaluated for weight variation, uniformity of thickness, tensile strength, percentage of elongation at break, folding endurance, hardness, surface pH, and water vapor permeability. Permeability characteristics of these films were studied using Ofloxacine as a model drug. Film properties of various synthetic polymers such as hydroxypropyl methyl cellulose (HPMC), polyvinyl alcohol (PVA), hydroxypropyl cellulose (HPC), polyvinyl pyrrolidone (PVP), and Eudragit RL 100 were studied for their utility in the formulation of ophthalmic inserts. Sterility test was carried out before performing an irritation study on
albino
rabbit eyes. There was no sign of any irritation, redness, swelling, or haziness in the rabbit's eyes even after 24 hours after removal of the film.
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Preparation of biodegradable microspheres containing repaglinide
p. 121
S Tamizharasi, R Jagdish Chandra, R Vaishali
DOI
:10.4103/0975-1483.55743
The objective of the present study is to prepare and evaluate poly(ε-caprolactone) microspheres of repaglinide by using the solvent evaporation technique. The microspheres were prepared with different drug-to-carrier ratios: F
1
(1:3), F
2
(1:4), F
3
(1:5), and F
4
(1:6). The microspheres were then evaluated for particle size, SEM, FT-IR study, percentage yield, drug entrapment, stability studies, and for
in vitro
release kinetics. Scanning electron microscopy (SEM) revealed that microspheres were spherical with a nearly smooth surface morphology. The percentage yield and drug entrapment efficiency were high for all the formulations. Fourier Transform-Infrared spectroscopy (FT-IR) showed that there was no chemical interaction between the drug and the polymer. No appreciable difference was observed in the stability study, in the extent of degradation of the product for 60 days in the microspheres that were stored at various temperatures. The
in vitro
release study showed that replaglinide release from all the formulations was slow and sustained over 12 h. Application of the
in vitro
drug release data to various kinetic equations indicated zero order release from repaglinide microspheres.
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PHARMACOGNOSY
Anti-inflammatory activity of ethanolic leaf extracts from
Adenanthera pavonina
(L) in Rats
p. 125
C Mayuren, R Ilavarasan
DOI
:10.4103/0975-1483.55744
Ethanolic extracts from the leaves of
Adenanthera pavonina
were assessed at doses of 250 and 500mg/kg for anti-inflammatory effects using both acute and chronic inflammatory models. The anti-diarrheal activity was also evaluated to support any possible evidence of prostaglandin synthesis inhibition. It was found that the doses possessed inhibitory effects on the acute phase of inflammation as seen in carrageenan-induced hind paw edema as well as in a subacute study of cotton pellet-induced granuloma formation. The anti-inflammatory activity elicited by the leaf extracts may be due to the influence of the active constituents such as beta-sitosterol and stigmasterol. A possible mechanism may also be due to the inhibition of prostaglandin synthesis which is also evidenced by the delay in the formation of wet faeces. Further study is required to postulate the exact molecular mechanism involved in this process of inhibition of inflammation by these leaf extracts.
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Free-radical-scavenging activity in the inflorescence of European Nettle/Sisnu (
Urtica dioica
L.)
p. 129
P Mandal, TK Misra, ID Singh, JK Das, M Bhunia
DOI
:10.4103/0975-1483.55745
The inflorescence of
Urtica dioica
L. is used by ethnic people of Darjeeling Hills as therapeutics and green vegetables. As it is ethnomedicinally very important for curing several critical and emerging oxidative stress-induced diseases, the inflorescence of this plant may be considered as a potential source of antioxidants. In the present study,
U. dioica
inflorescences were successively extracted and purified with nine different solvents by using silica gel column chromatography to study their antioxidant properties and polyphenol contents. Ethyl acetate:acetone::1:3 fraction was found (91.50% inhibition) to be the best scavenger of DPPH at a dose of 100 µg/ml among 33 extracts, which was comparable with standard quercetin (44.77% inhibition). An NBT-NADH-PMS-based highest superoxide-scavenging activity (53.30% inhibition) was observed in acetone:ethanol::1:1 fraction, which was also comparable with the same standard (72.30%). Optimum anti-lipid peroxidation of 55.27% inhibition was detected in diethyl ether:ethyl acetate::1:1 fraction. TLC fingerprint of ethyl acetate:acetone::1:3 extract after derivatization with DPPH showed maximum number of separated components with the highest diameter at R
f
= 0.907. Phenols and flavonoids were mostly concentrated in the same fraction with a concentration of 24.22 ± 0.26 and 43.34 ± 1.02 mg/g of dry mass, respectively. Significant correlations were found among phenolic phytochemicals and radical-scavenging activity through which it may be assumed that the antioxidants present in
U. dioica
inflorescence are polyphenolic in nature. The observations suggest the importance of ethnomedicinal use of
U. dioica
, which could be commercially exploited by the pharmaceutical industry as a natural antioxidant.
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Comparative evaluation of extracts of
Citrus limon
burm peel for antioxidant activity
p. 136
S Akhila, AR Bindu, K Bindu, NA Aleykutty
DOI
:10.4103/0975-1483.55746
Cellular damage arising from free radicals is one of the fundamental mechanisms underlying a number of human neurodegenerative disorders like diabetes, inflammation, Alzheimer's disease, autoimmune pathologies, and digestive system disorders. Thus, antioxidants play an important role in the treatment of such diseases. Natural sources of antioxidants, free of carcinogenicity unlike synthetic ones, are being tapped for antioxidant formulations. The present study aims at a comparative evaluation of hexane, alcoholic, and aqueous extracts of fresh lemon peel for antioxidant activity. All extracts were subjected to phenolic content estimation by the Folin-Ciocalteau method and flavonoid content estimation by the aluminium chloride colorimetric method. Results revealed that the alcoholic extract had the maximaml content of both phenolics and flavanoids. Antioxidant activity was evaluated by using the beta-carotene bleaching method, the nitric oxide radical scavenging and the hydrogen peroxide scavenging assays. The alcoholic extract was found to have good free radical inhibitory property as well as nitric oxide radical scavenging activity. The hexane extract, however, showed only good hydrogen peroxide scavenging activity. Thus, the higher antioxidant activity of the alcoholic and hexane extracts of
Citrus limon
peel could have wide therapeutic utility against various diseases.
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PHARMACOLOGY
Pharmacology of recombinant or genetically engineered drugs
p. 141
Kamal Kishore, Pawan Krishan
DOI
:10.4103/0975-1483.55747
Recombinant technology or genetic engineering is a modern method used for the synthesis of therapeutic agents. The central theme of recombinant technology is the process of "gene cloning" which consists of the production of a defined fragment of DNA and its propagation and amplification in a suitable host cell. Drugs developed by recombinant technology or genetic engineering are known as biologics, biopharmaceuticals, recombinant DNA expressed products, bioengineered, or genetically engineered drugs. A current list of various products developed by recombinant technology includes erythropoietin, coagulation modulators, enzymes, hormones, interferons, interleukins, granulocyte colony-stimulating factors, anti-rheumatoid drugs, and various other agents like TNF, becaplermin, hepatitis-B vaccine, antibodies etc. This article provides general as well as recent pharmacological information on different aspects of recombinant drugs that may be useful for their better understanding by users and health care professionals.
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Diabetes type-II exaggerates renal ischemia reperfusion injury by elevation of oxidative stress and inflammatory response
p. 151
J Vaghasiya, N Sheth, Y Bhalodia, N Jivani
DOI
:10.4103/0975-1483.55748
Objective:
The present work was designed to investigate the role of Diabetes Mellitus Type-II (DM-II) on renal ischemia reperfusion (I/R)-associated pathophysiology in renal damage.
Materials and Methods:
DM-II in rats was induced by the administration of nicotinamide (230 mg /kg, i.p.), 15 min prior to a single dose of streptozotocin (65mg/ kg, i.v.).
In vivo
renal I/R was performed in both DM-II and normal rats.
Results and Discussions:
Lipid peroxidation, xanthine oxidase activity, and nitric oxide levels were significantly increased in renal tissue after I/R in diabetic rats compared to I/R in normal rats. Levels of antioxidant enzymes such as glutathione, superoxide dismutase, catalase, and glutathione peroxidase were significantly reduced after I/R in diabetic rats compared to normal rats. Serum TNF-α levels, renal tissue myeloperoxidase activity, and apoptosis were also significantly increased after I/R in DM-II rats. Furthermore, DM-II rats that underwent I/R, showed severe tubular cell swelling, interstitial edema, tubular dilatation, hyaline casts, and moderate to severe necrosis.
Conclusion:
In conclusion, DM-II rats showed exaggerated renal I/R injury. These findings have a major implication in ischemic injury that is prone to develop in DM-II.
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Glucose-lowering, hepatoprotective and hypolipidemic activities of stem bark of
Ficus racemosa
in streptozotocin-induced diabetic Rats
p. 160
F Ahmed, A Urooj
DOI
:10.4103/0975-1483.55749
The present study evaluated the antihyperglycemic, hepatoprotective, and hypolipidemic effects of
F. racemosa
bark powder and aqueous extract in streptozotocin-induced diabetic rats. Streptozotocin-induced diabetic rats (
n
= 6) were treated with
F. racemosa
Linn (Moraceae) bark powder (FRP) and aqueous extract (FRAE) for six weeks. Blood glucose was determined every 15 days using a portable glucometer. At the end of the study period, the rats were sacrificed and levels of serum glucose, protein, total cholesterol, triglycerides, AST, ALT, TBARS, and glutathione were determined as indicators of antihyperglycemic, hypolipidemic, and hepatoprotective activities, as well as of antioxidant potential. TBARS and glutathione levels were determined in the liver and the kidneys also. Both the
bark powder and aqueous extract of
F. racemosa
bark caused a significant reduction (
P
≤ 0.05) in blood glucose (54 and 66% respectively). A significant reduction (
P
≤ 0.05) was also observed in serum cholesterol and triglyceride levels to the control levels. The aqueous extract was more effective and caused a significant reduction (
P
≤ 0.05) in TBARS, AST, ALT levels compared to untreated diabetic rats. However, it did not reach control levels. A significant increase in glutathione concentrations over the control levels was also observed in rats treated with
F. racemosa
bark. It is concluded that
F. racemosa
bark has a significant hypolipidemic and hepatoprotective effect besides being a potent antihyperglycemic agent.
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PHARMACEUTICAL CHEMISTRY
Synthesis and characterization of pyrazine-2-carbohydrazide derivatives as antimicrobial agents
p. 165
PB Miniyar, SJ Makhija
DOI
:10.4103/0975-1483.55750
A series of pyrazine-2-carbohydrazide derivatives has been synthesized and assessed for their
in vitro
antimicrobial activity against Gram-positive and Gram-negative strains of bacteria. In the present study, pyrazinamide was hydrolyzed and esterified to obtain ethyl-pyrazinoate and was reacted with hydrazine hydrate to yield the pyrazinoic acid hydrazide. This pyrazinoic acid hydrazide was then condensed with various substituted aromatic aldehydes to obtain different derivatives of pyrazine-2-carbohydrazide. The newly synthesized compounds were characterized by IR, 1HNMR and MS spectral data. The antimicrobial activity of the synthesized compounds was found to be potent against the selected strains of Gram-positive bacteria as compared with Gram-negative bacteria.
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Synthesis and screening for analgesic and anti-inflammatory activities of some novel amino acid-containing bicyclo compounds
p. 170
CS Sharma, RK Nema, VK Sharma
DOI
:10.4103/0975-1483.55751
Diazabicyclo[4.3.1]decane derivatives are well known opioid receptor ligands, hence, we have developed a novel and simple method for the synthesis of 3, 4-diphenyl-2,5-diaza-bicyclo[4.3.1]deca-1(9),2,4,6(10),7-pentaene-8-carbonyl chloride derivatives containing amino acid moieties. The compounds were structurally confirmed with the help of TLC, IR, NMR, and LCMS spectra. All the title compounds were screened for analgesic activity by using the tail-flick method and for anti-inflammatory activity by using the carrageenan-induced paw edema method using diclofenac sodium as a standard.
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PHARMACEUTICAL ANALYSIS
Quantitative analysis of manidipine dihydrochloride in bulk and synthetic mixtures by visible spectrophotometry
p. 175
Lakshmi Sivasubramanian, K Manikandan, M Venkatesan, KS Lakshmi
DOI
:10.4103/0975-1483.55752
The present work describes three visible spectrophotometric methods for the quantitative estimation of Manidipine in bulk and synthetic mixtures. Method A is based on the reaction of the drug with
para
-dimethylaminobenzaldehyde (PDAB) and methanolic sulfuric acid at room temperature to form a green chromogen measured at 436.97 nm. Method B is based on the reaction of the diazotized drug with
N
-napthylethylenediamine dihydrochloride (NEDD) to form a pink chromogen measured at 550.20 nm. Method C utilizes the reaction of manidipine with 3-methyl-2-benzothiazoniumhydrazone hydrochloride (MBTH) in the presence of ferric chloride to form a product measured at 480.21 nm. Under optimized reaction conditions, the proposed methods were validated as per ICH guidelines. Linearity was obeyed in the concentration ranges of 25-125 ìg/ml
with the following linear regression equations for methods A, B, and C, respectively: Y = 0.002829 X + 0.01319, Y = 0.002325 X + 0.004275, Y = 0.0035 X + 0.001039. The limits of detection and limits of quantification for methods A, B and C were 1.2024 and 1.212 µg/mL; 0.9798 and 3.6451 µg/mL, and 3.672 and 2.969 µg/mL respectively. Recovery studies were carried out by using the standard addition method and the results were found to be satisfactory. All methods have been applied successfully for the estimation of manidipine dihydrochloride in bulk and synthetic mixtures.
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GENERAL ARTICLES
Drug utilization and prescription monitoring of asthma patients
p. 180
S Vijaya Kumar, M Sasi Kala, TS Mohamed Saleem, K Gauthaman
DOI
:10.4103/0975-1483.55753
The present study was conducted to establish prescription trends of anti-asthmatic drugs at the Central Referral Hospital, Tadong and Gangtok, Sikkim. The study was conducted using WHO-based prescription-auditing performa. Data were recorded from the patients attending the hospital outpatient department (OPD) through a chance, random sampling method. Methylxanthine (40%) was the most frequently prescribed drug among anti-asthmatics, followed by â2-agonists (27%), corticosteroids (23%), and mucolytics (09%). which were the least prescribed. Our study further found that combination therapy (80%) was given to a significant number of patients as compared to monotherapy (20%). In combination therapy, the two-drug combination was the most often prescribed (57.69%). Further, anti-asthmatic drugs were mostly given (68.18%) by the oral route, followed by the inhalation route (27.27%) and injection route (4.55%). The asthmatic problem was more prevalent in grade III employees that includes drivers and laborers. It has been concluded that a study may be more meaningful to further improve the prescribing as well as dispensing practices of the pharmacist through successful implementation of interventional programs in health centers.
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Relevance of the use of alternative medicine for bronchial asthma: A review
p. 184
M Sasi Kala, S Vijaya Kumar, K Gauthaman
DOI
:10.4103/0975-1483.55754
Alternative systems of medicine include Chinese medicine, Ayurveda, homeopathic, and naturopathic medicine. Chinese medicine emphasizes the balance of qi ("chee") or vital energy. Within this system, illness is defined as a disturbance in the balance of vital energy. Ayurveda is a system of healing which evolved from teachings in ancient India. Our review mainly focuses on the importance of the severity and control of asthma in the evaluation of patients and their response to treatment. We searched MEDLINE, EMBASE, The Cochrane Library, and the National / International abstracts to identify relevant articles. We limited evidence to alternative medicine for asthma, but we also reviewed observational evidence for safety. Outcomes of interest were overall mortality, exacerbations, quality of life, functional capacity, and primary health care. Lifestyle modifications that effectively lower asthma are: i) increased physical activity, ii) reduction of the impact of environmental factors on asthma such as smoking, air pollution, hazards in schools, day care, the work place, and home, as well as other environmental triggers. Our review suggests that alternative systems of medicine reduce adverse effects and the need for high-impact, high-cost intervention. It is the best way for self-healing and health promotion (salutogenesis rather than pathogenesis) that makes alternative medicine approaches to chronic disease especially attractive.
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BOOK REVIEW
Topics in the history of pharmacology
p. 190
Chetna Patel
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