Amide prodrugs of NSAIDs: Synthesis and biological evaluation with a hydrolysis study
Asif Husain, Priyanka Ahuja, Aftab Ahmad, Shah Alam Khan
Sch Acad J Pharm | 145-152
DOI : 10.36347/sajp
Abstract
PDF
Full Texts
e-Pub
The aim of the present study was to synthesize prodrugs of commonly used NSAIDs to overcome the
gastrointestinal toxicity (irritation and bleeding) associated with their use. A total of six amide-based prodrugs (Ia-f) of
aceclofenac, diclofenac, fenbufen, indomethacin, mefenamic acid and 4-biphenyl acetic acid were synthesized through
one-pot method (single step synthesis). The structures of the synthesized prodrugs were confirmed by modern analytical
techniques. The release pattern of parent drug from prodrug Ia was also studied by reverse phase HPLC method in acidic
buffer (pH 1.2), phosphate buffer (pH 7.4), 80% plasma, 10% rat intestinal homogenate and 10% rat liver homogenate
(pH 7.4). The prodrugs were also evaluated for their anti-inflammatory and ulcerogenic actions and compared to their
corresponding parent drugs.
Principles of Toxicotherapy: General & Special Therapy
Mohammad Karami, Mohammad Reza Abdolahzadeh e Estachri
Sch Acad J Pharm | 153-156
DOI : 10.36347/sajp
Abstract
PDF
Full Texts
e-Pub
Appropriate therapies for commonly encountered poisonings, medication overdoses, and other toxicological
emergencies are reviewed, with discussion of pharmacists' role in ensuring their ready availability and proper use.
Antidotal therapy are general antidotal therapy(supportive and palliative care that palliative treatments may be used to
alleviate the side effects of curative treatments, such as relieving the nausea associated with chemotherapy and enhance
quality of life; is applicable early in the course of illness, in conjunction with other therapies that are intended to
prolong life, such as chemotherapy or radiation therapy And special antidotal therapy is the use of any chemical or
physiologic procedure used to prevent, minimize, or terminate the adverse effects associated with chemical toxicity or
aberrant pathophysiologic processes. These antidotal procedures may alter the toxicity associated with an exogenous
chemical (naloxone antagonism of opioid narcotics) or with endogenous substances (epinephrine reversal of histamineinduced anaphylaxis). The goal of this review is to provide essential information to guide the appropriate use of
antidotes. Pharmacists can play a key role in reducing poisoning and overdose injuries and deaths by assisting in the early
recognition of toxic exposures and guiding emergency personnel on the proper storage, selection, and use of antidotal
therapies.
Effects of ethanolic leaf extract of Psidium guajava Linn. on L-arginine induced obsessive compulsive disorder in mice
Krishna Mohan Chinnala, Swetha Jukanti, Madhan Mohan Elsani
Sch Acad J Pharm | 157-163
DOI : 10.36347/sajp
Abstract
PDF
Full Texts
e-Pub
Obsessive compulsive disorder (OCD) is a high-prevalence psychiatric disorder affecting 2–5% of the
population. It is a type of anxiety disorder in which people suffer from recurrent, unwanted thoughts or ideas
(obsessions), engage in repetitive, irrational behaviors or mental acts (compulsions) or both. Although its
pathophysiology remains unclear, current evidence implicates contributions of the serotonergic and dopaminergic
neurotransmitter systems and a neural circuitry that includes the orbitofrontal cortex, the thalamus and the striatum. In
this present research work the pharmacological effect of ethanolic extract of Psidium guajava Linn.(EEPG) against Larginine induced obsessions were evaluated along with in-vitro studies like estimation of serotonin and dopamine. From
the results we found that the EEPG shown significant (p<0.05 - p<0.01) improvement in behavioral parameters viz.
marble burying behavior, locomotion and memory retention. It is also identified that the EEPG treated groups had shown
the significant (p<0.01 and p<0.05) increase in levels of dopamine and serotonin which may be responsible for
behavioral functions.
Pharmacognostical and Pharmaceutical Evaluation of Devdarvyadi Vati-A Compound Ayurvedic Formulation
Vhora Maleka, Patel KS, Harisha , Rajagopala S, Shukla
Sch Acad J Pharm | 164-167
DOI : 10.36347/sajp
Abstract
PDF
Full Texts
e-Pub
Childhood period is a crucial stage for rapid growth and development. All the phases of growth and
development are easily affected by unfavorable conditions like use of contaminated foods and water, faulty food habits
etc. In day to day practice, pediatricians come across with good number of patients suffering from diseases related to
gastrointestinal tract i.e. loss of appetite, abdominal pain, vomiting, bowel disturbances (diarrhea, constipation) etc. If
these problems are ignored, they lead to malnutrition and its complications. The changed lifestyle is responsible
forvitiation of Agni, improper Agni especially Mandagni results in Grahani Dosha, which is a precursor stage of
malabsoption syndrome. Devdarvyadi Churna is indicated in such condition. Devdarvyadi Churna converted into Vati
form due to easy palatability in pediatrics patients and drugs were selected in the present study. The present work was
carried out to standardize the finished product Devdarvyadi Vati to conform its identity, quality and purity. The
pharmacognostical work reveals that presence of lignified fibers of Devadaru (Cedrusdeodara (Roxb.) Loud),starch with
oiliores in content of Vacha (Acoruscalamus Linn.), starch grain in Musta(Cyperusrotundus Linn.), starch with oiliores in
contentin Shunthi (Zingiberofficinale Roscoe.)prismatic crystal of Ativisha(Aconitum heterophyllum Wall. ex Royal),
epicarpe cells of Haritaki (Terminalia chebula Retz.) were observed microscopically. Organoleptic features of coarse
powder made out of the crude drugs were within the standard range as per mention in classic. The pH value
ofDevdarvyadiVatiis4, Water soluble extract is 11.07%w/w, Loss on drying is 5.73 %w/wand High Performance Thin
Layer Chromatography (HPTLC) at 254nm and 366nm resulted into 5 and 6 spots respectively
Changes in the Amounts of Amoxicillin and Metronidazole Used for Helicobacter pylori Eradication Therapy in the Stomach after Their Oral Administration to Rats
Mai Kubodera, Tadakazu Tokumura, Yoshiharu Machida
Sch Acad J Pharm | 168-171
DOI : 10.36347/sajp
Abstract
PDF
Full Texts
e-Pub
In the eradication therapy of Helicobacter pylori, the changes of the amounts and concentrations of antibiotics
in the stomach after oral administration were unclear. Amoxicillin (AMX) and metronidazole (MTZ), which are used for
such therapy, were selected for this study. The levels of these drugs in homogenate of the stomach after their oral
administration to rats were determined by HPLC. The doses of AMX and MTZ to the rats were 15 mg/kg and 5 mg/kg,
respectively. The proportions of these drugs remaining in the stomach decreased according to first-order kinetics. The
rate constants for AMX and MTZ were 0.512 and 0.436 h-1, respectively. The decrease of the stomach volume was also
expressed as first-order kinetics, with a rate constant of 0.184 h-1. These data are useful for the design of intragastric
buoyant sustained-release preparations for the eradication therapy of H. pylori.
Formulation and Evaluation of Herbal Gel Containing Terminalia chebula Retz., Leaves Extract
R. Bhramaramba¸ I. Sudheer Babu, Ch. Divya Naga Deepthi
Sch Acad J Pharm | 172-176
DOI : 10.36347/sajp
Abstract
PDF
Full Texts
e-Pub
In this context a technique was employed for the formulation of herbal gel by using Terminalia chebula
Retz.,. The plant is commonly referred as ‘King of Medicine’ in Tibet, which is widely grown at places up to a height of
about 2000 m from the sea level, and in areas with an annual rainfall 100-150 cm and temperature 0-17° C in tropical and
subtropical regions of East Asia. It mainly contains active constituents like steroids, flavonoids, tannins, reducing sugar,
belleric acid, bellericoside, chebulinic acid, gallic acid, ethyl gallate,punicalagin, terflavin A, terchebin, luteolin, and
tannic acid . It is mainly used as antibacterial and antifungal, analgesic, anti-inflammatoy, sun burns and wound healing.
Various formulations were prepared with different concentrations of the plant extract and it was evaluated for physical
parameters, viscosity, Skin Irritation and Spreadibility. Out of the three formulations the 5% was found to be better in all
aspects. Thus it can be used as an alternative for the treatments and drug delivery systems.
Antioxidant Potentials of Marine Red and Green Algae Extracts In-vitro
Yanti, Fendy Heryanto Koesnoto, Andre Sutanto, Jae-Kwan Hwang
Sch Acad J Pharm | 177-180
DOI : 10.36347/sajp
Abstract
PDF
Full Texts
e-Pub
Reactive oxygen species (ROS) is normally found in balance with antioxidant molecules within all aerobic
cells. The unbalance condition between ROS and antioxidant molecules will cause oxidative stress that may lead to any
damages on nucleic acid, protein, and fatty acid. In this study, we investigated the antioxidant potentials of Indonesian
marine algae extracts, including red algae (Botryocladia sp. and Gracilaria sp.) and green algae (Caulerpa sertulaioides,
C. racemosa, Codium sp., Enteromorpha sp., and Halimeda opuntia) in vitro. Seven marine algae were dried and
extracted with ethanol, followed by evaporating and freeze-drying treatments to obtain algae extracts. The antioxidant
activity was referred to the 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay. Our results demonstrated that both red algae
(Botryoclardia sp. and Gracilaria sp.) and green algae (C. sertulaioides and Codium sp.) at 100 µg/mL significantly
possessed 35-40% antioxidant activity, indicating that these marine algae extracts may exert potential natural antioxidant
properties.
Hepatoprotective activity of tagetes erecta Linn. in ethanol induced hepatotoxicity in rats
Gauri Karwani, Siddhraj S. Sisodia
Sch Acad J Pharm | 181-189
DOI : 10.36347/sajp
Abstract
PDF
Full Texts
e-Pub
The plant Tagetes erecta Linn., locally known as Genda Phul (Marigold) belongs to the family Asteraceae
(Compositaeis). Current study focus on hepatoprotective activity of the roots in ethanol extract by ethanol induced
hepatotoxicity model. Physical parameters, liver functioning, antioxidant levels and histopathological study of the liver
were studied to find out hepatoprotective action of Tagetes erecta. Treatment with Tagetes erecta root extracts has
protected liver from induced hepatotoxicity. This was demonstrated by reducing the elevated levels of biochemical
markers and additional histopathological observations have shown that there is an improvement in the structural design
of liver due to induced hepatotoxicity
Inhibition of Matrix Metalloproteinase-2 Expression by Ethanolic Extracts of Zingiberaceae Rhizomes in Artery Endothelial Cells
Yanti, Andre Wiharja, Nikodemus Steven, Surya Fajarianto
Sch Acad J Pharm | 190-194
DOI : 10.36347/sajp
Abstract
PDF
Full Texts
e-Pub
Atherosclerosis belongs to inflammation-related vascular diseases due to bacterial infection and causes lipid
accumulation in artery wall that lead to heart attack and stroke. Matrix metalloproteinase (MMP)-2 and -9 are grouped to
zinc-dependent proteases that act in degradation of extracellular matrix in atherosclerotic plaque. Instead of traditional
foods, the rhizomes of Zingiberaceae have been empirically used in folk medicines purposes, including natural vascular
protection. This study was aimed to test the inhibitory effect of 10 Zingiberaceae rhizomes on the expression of MMP-2
activity in lipopolysaccharide-induced artery endothelial cells by conducting gelatin zymogram. At 1 µg/ml, selected
Zingiberaceae rhizomes, i.e. Kaempferia pandurata, Curcuma xanthorrhiza, Alpinia galanga, Zingiberaceae officinale,
and Z. officinale Var Rubra, were found to attenuate MMP-2 activity up to 50% compared with LPS-treated cells. In
summary, these data suggest that selected Zingiberaceae rhizomes may be applied for potential therapeutics in vascular
protection and therapy, in particular atherotherapy
Effect of Xanthium strumarium L. extract on Glucose Metabolism in HeLa cervical cancer cells
Khanjan Vaishnav, Linz-Buoy George, H. N. Highland
Sch Acad J Pharm | 195-198
DOI : 10.36347/sajp
Abstract
PDF
Full Texts
e-Pub
Cancer cells exhibit increased glucose metabolism and pentose phosphate cycle activity compared to normal
untransformed cells. Glucose metabolism plays an important role in hydroperoxide detoxification and the inhibition of
glucose metabolism has been shown to increase prooxidant production and cytotoxicity in cancer cells. There are reports
showing that inhibition of the Akt pathway which is responsible for cell growth and survival, inhibits glucose
consumption and induces parameters indicative of oxidative stress such as glutathione disulfide (%GSSG) and
thioredoxin reductase (TR) activity in certain cancer cells. Hence after the treatment with a drug, when the levels of
glucose consumption are decreased cancer cells, it could indicate increase in oxidative stress resulting in cell death and
that the drug is effective against that particular cancer. In our previous studies, we have already shown that the
hydroalcoholic extract of an annual herb Xanthium strumarium induced cell death and generated oxidative stress in HeLa
cervical cancer cell line. In our current study, we have performed the test for glucose consumption to support our study
further.
Design and Development of Sustained Release Matrix Tablets of Tramadol Hydrochloride are using Gum kondagogu as a Natural polymer
V. Kamalakkannan, R.Sivaprakash, P.Venkatraman, R. Sambath kumar, K.S.G.Arul kumaran
Sch Acad J Pharm | 199-207
DOI : 10.36347/sajp
Abstract
PDF
Full Texts
e-Pub
The main objective of the present work was to develop sustained release matrix tablets of water soluble
Tramadol hydrochloride using different polymers viz. Hydroxy propyl methyl cellulose (HPMC) and natural gums like
gumkodangogu. drug and polymer for control the release of drug up to desired time, the release rates were modulated by
combination of two different rates controlling material and triple mixture of three different rate controlling material.
After evaluation of physical properties of tablet, the in vitro release study was performed in0.1 N HCl . The effect of
polymer concentration and polymer blend concentration were studied. .Dissolution data was analyzed by KorsmeyerPeppas power law expression and modified power law expression. It was observed that matrix tablets contained polymer
blend of kodangogu/HPMC were successfully sustained the release of drug upto 10 hrs. Among all the formulations,
formulation F6 which contains HPMC K15M and of kodangogu release the drug which follow Zero order kinetics via,
swelling, diffusion and erosion and the release profile of formulation F6 was comparable with the marketed product.
Stability studies (40±2ºC/75±5%RH) for 3 months indicated that Tramadol hydrochloride was stable in the matrix
tablets. The FTIR study revealed that there was no chemical interaction between drug and excipients.
Effects of Cholinesterase Inhibitors on Experimental Model of Retrograde Amnesia
Darinka Dimitrova, Zlatilina Dimitrova, Vanja Nalbantova, Gergana Durleva, Damianka Getova
Sch Acad J Pharm | 208-211
DOI : 10.36347/sajp
Abstract
PDF
Full Texts
e-Pub
The Tacrine and Galantamine are cholinesterase inhibitors for treatment of Alzheimer’s disease. The
pentylentetrazole model of retrograde amnesia is suitable for studying of learning and memory impairments. The aim of
present study was to compare the effects of the cholinesterase inhibitors Tacrine and Galantamine on pentilentetrazole
amnesia model in mice using passive avoidance test. The 32 male albino mice 21-26g was used, n=8. The groups were:
Saline 0.1ml/10g body weight; Saline + Pentylentetrazole (PTZ) 45mg/kg; Tacrine 1mg/kg + PTZ 45 mg/kg;
Galantamine 0.1mg/kg + PTZ 45 mg/kg. The mice were treated subcutaneously with PTZ immediately after testing in
Step-down apparatus (Ugo Basile, Italy). The cholinesterase inhibitors ware applied intraperitoneally 30 minutes before
testing. The latency of reaction (60 seconds) was a criterion for learning and memory. A two-way ANOVA for repeated
measurements was used to compare different groups with the respective controls. In step-down passive avoidance test
controls significantly increased the latency of reactions on learning session and on short and long memory tests. The
mice with PTZ decreased the latency of reaction compared to the same day controls. The group with Tacrine and PTZ
lowery increased the latency in comparison with PTZ group. The animals with Galantamine and PTZ significantly
increased the latency of reactions on lerning and memory tests. Our results allow us to conclude that PTZ had small
impairing effect on cognitive functions in mice. The Galantamine in low dose antagonizes inhibitory effect of PTZ on
brain functions better than Tacrine.
Management and Role of diet and exercise in diabetes mellitus: A Review
Saini K, Asija R, Sharma P.K
Sch Acad J Pharm | 212-216
DOI : 10.36347/sajp
Abstract
PDF
Full Texts
e-Pub
Diabetes is chronic hyperglycaemia together with other metabolic abnormalities. It is due to insulin resistance
or deficiency as well as increased output of hepatic glucose. It is a risk factor for CVD. Currently there is no known cure
but the disease can be controlled enabling the person to lead a healthy and productive life. The aim of management is
directed at reducing complications. Many studies have shown the benefit of healthy dietary habits and regular exercise in
the prevention and management of diabetes mellitus. Adherence to prescribed lifestyle changes have also been shown to
improve glucose levels, and decreased blood pressure and to correct lipid abnormalities, which are factors associated
with e micro and macro-vascular complications of diabetes.