Abstract: The Ramon preparation is received from a plant; it is destined for external treatment of inflammations in post-surgery period. The Ramon is a biogenic immune stimulator accelerating metabolism, contributing to improvement of blood indexes, having general tonic, anti-inflammatory and bactericidal effect.
Abstract: Free Hemoglobin promotes the accumulation of
hydroxyl radicals by the heme iron, which can react with endogenous
hydrogen peroxide to produce free radicals which may cause severe
oxidative cell damage. Haptoglobin binds to Hemoglobin strongly
and Haptoglobin-Hemoglobin binding is irreversible. Peroxidase
activity of Haptoglobin(2-2)-Hemoglobin complex was assayed by
following increase of absorption of produced tetraguaiacol as the
second substrate of Haptoglobin-Hemoglobin complex at 470 nm and
42°C by UV-Vis spectrophotometer. The results have shown that
peroxidase activity of Haptoglobin(2-2)-Hemoglobin complex is
modulated via homotropic effect of hydrogen peroxide as allostric
substrate. On the other hand antioxidant property of Haptoglobin(2-
2)-Hemoglobin was increased via heterotropic effect of the two drugs
(especially ampicillin) on peroxidase activity of the complex. Both
drugs also have mild effect on quality of homotropic property of
peroxidase activity of Haptoglobin(2-2)-Hemoglobin complex.
Therefore, in vitro studies show that the two drugs may help Hp-Hb
complex to remove hydrogen peroxide from serum at pathologic
temperature ature (42 C).
Abstract: The worldwide prevalence of H3N2 influenza virus
and its increasing resistance to the existing drugs necessitates for the
development of an improved/better targeting anti-influenza drug.
H3N2 influenza neuraminidase is one of the two membrane-bound
proteins belonging to group-2 neuraminidases. It acts as key player
involved in viral pathogenicity and hence, is an important target of
anti-influenza drugs. Oseltamivir is one of the potent drugs targeting
this neuraminidase. In the present work, we have taken subtype N2
neuraminidase as the receptor and probable analogs of oseltamivir as
drug molecules to study the protein-drug interaction in anticipation of
finding efficient modified candidate compound. Oseltamivir analogs
were made by modifying the functional groups using Marvin Sketch
software and were docked using Schrodinger-s Glide. Oseltamivir
analog 10 was detected to have significant energy value (16% less
compared to Oseltamivir) and could be the probable lead molecule. It
infers that some of the modified compounds can interact in a novel
manner with increased hydrogen bonding at the active site of
neuraminidase and it might be better than the original drug. Further
work can be carried out such as enzymatic inhibition studies;
synthesis and crystallizing the drug-target complex to analyze the
interactions biologically.
Abstract: Most of the drugs used for pharmaceutical purposes
are poorly water-soluble drugs. About 40% of all newly discovered
drugs are lipophilic and the numbers of lipophilic drugs seem to
increase more and more. Drug delivery systems such as
nanoparticles, micelles or liposomes are applied to improve their
solubility and thus their bioavailability. Besides various techniques of
solubilization, oil-in-water emulsions are often used to incorporate
lipophilic drugs into the oil phase. To stabilize emulsions surface
active substances (surfactants) are generally used. An alternative
method to avoid the application of surfactants was of great interest.
One possibility is to develop O/W-emulsion without any addition of
surface active agents or the so called “surfactant-free emulsion or
SFE”. The aim of this study was to develop and characterize SFE as a
drug carrier by varying the production conditions. Lidocaine base
was used as a model drug. The injection method was developed.
Effects of ultrasound as well as of temperature on the properties of
the emulsion were studied. Particle sizes and release were
determined. The long-term stability up to 30 days was performed.
The results showed that the surfactant-free O/W emulsions with
pharmaceutical oil as drug carrier can be produced.
Abstract: Chikungunya virus (CHICKV) is an arboviruses belonging to family Tagoviridae and is transmitted to human through by mosquito (Aedes aegypti and Aedes albopictus) bite. A large outbreak of chikungunya has been reported in India between 2006 and 2007, along with several other countries from South-East Asia and for the first time in Europe. It was for the first time that the CHICKV outbreak has been reported with mortality from Reunion Island and increased mortality from Asian countries. CHICKV affects all age groups, and currently there are no specific drugs or vaccine to cure the disease. The need of antiviral agents for the treatment of CHICKV infection and the success of virtual screening against many therapeutically valuable targets led us to carry out the structure based drug design against Chikungunya nSP2 protease (PDB: 3TRK). Highthroughput virtual screening of publicly available databases, ZINC12 and BindingDB, has been carried out using the Openeye tools and Schrodinger LLC software packages. Openeye Filter program has been used to filter the database and the filtered outputs were docked using HTVS protocol implemented in GLIDE package of Schrodinger LLC. The top HITS were further used for enriching the similar molecules from the database through vROCS; a shape based screening protocol implemented in Openeye. The approach adopted has provided different scaffolds as HITS against CHICKV protease. Three scaffolds: Indole, Pyrazole and Sulphone derivatives were selected based on the docking score and synthetic feasibility. Derivatives of Pyrazole were synthesized and submitted for antiviral screening against CHICKV.
Abstract: Antifungal activities of ether and methanolic extracts of volatiles oils of Nigella Sativa seeds were tested against pathogenic bacterias and fungies strains.The volatile oil were found to have significant antifungal and antibacterial activities compare to tetracycline, cefuroxime and ciprofloxacin positive controls.The ether and methanolic esxtracts were compared to each other for antifungal and antibacterial activities and ether extracts showed stonger activity than methanolic one.
Abstract: The objective of this study was to develop vaginal
suppository containing lactobacillus. Four kinds of vaginal
suppositories containing Lactobacillus paracasei HL32 were
formulated: 1) a conventional suppository with Witepsol H-15 as a
base, 2) a conventional suppository with mixed polyethylene glycols
(PEGs) as a base, 3) a hollow-type suppository with Witepsol H-15
as a base and 4) a hollow-type suppository with mixed PEGs as a
base. The release studies demonstrated that the hollow-type
suppository with mixed PEGs as the base gave the highest release of
L. paracasei HL32 and was microbiological stable after storage at 2-
8°C over the period of 3 months.
Abstract: This article demonstrated development of
controlled release system of an NSAID drug, Diclofenac
sodium employing different ratios of Ethyl cellulose.
Diclofenac sodium and ethyl cellulose in different proportions
were processed by microencapsulation based on phase
separation technique to formulate microcapsules. The
prepared microcapsules were then compressed into tablets to
obtain controlled release oral formulations. In-vitro evaluation
was performed by dissolution test of each preparation was
conducted in 900 ml of phosphate buffer solution of pH 7.2
maintained at 37 ± 0.5 °C and stirred at 50 rpm. At predetermined
time intervals (0, 0.5, 1.0, 1.5, 2, 3, 4, 6, 8, 10, 12,
16, 20 and 24 hrs). The drug concentration in the collected
samples was determined by UV spectrophotometer at 276 nm.
The physical characteristics of diclofenac sodium
microcapsules were according to accepted range. These were
off-white, free flowing and spherical in shape. The release
profile of diclofenac sodium from microcapsules was found to
be directly proportional to the proportion of ethylcellulose and
coat thickness. The in-vitro release pattern showed that with
ratio of 1:1 and 1:2 (drug: polymer), the percentage release of
drug at first hour was 16.91 and 11.52 %, respectively as
compared to 1:3 which is only 6.87 % with in this time. The
release mechanism followed higuchi model for its release
pattern. Tablet Formulation (F2) of present study was found
comparable in release profile the marketed brand Phlogin-SR,
microcapsules showed an extended release beyond 24 h.
Further, a good correlation was found between drug release
and proportion of ethylcellulose in the microcapsules.
Microencapsulation based on coacervation found as good
technique to control release of diclofenac sodium for making
the controlled release formulations.
Abstract: The occurrence and removal of trace organic
contaminants in the aquatic environment has become a focus of
environmental concern. For the selective removal of carbamazepine
from loaded waters molecularly imprinted polymers (MIPs) were
synthesized with carbamazepine as template. Parameters varied were
the type of monomer, crosslinker, and porogen, the ratio of starting
materials, and the synthesis temperature. Best results were obtained
with a template to crosslinker ratio of 1:20, toluene as porogen, and
methacrylic acid (MAA) as monomer. MIPs were then capable to
recover carbamazepine by 93% from a 10-5 M landfill leachate
solution containing also caffeine and salicylic acid. By comparison,
carbamazepine recoveries of 75% were achieved using a nonimprinted
polymer (NIP) synthesized under the same conditions, but
without template. In landfill leachate containing solutions
carbamazepine was adsorbed by 93-96% compared with an uptake of
73% by activated carbon. The best solvent for desorption was
acetonitrile, with which the amount of solvent necessary and dilution
with water was tested. Selected MIPs were tested for their reusability
and showed good results for at least five cycles. Adsorption
isotherms were prepared with carbamazepine solutions in the
concentration range of 0.01 M to 5*10-6 M. The heterogeneity index
showed a more homogenous binding site distribution.
Abstract: A new reverse phase-high performance liquid chromatography (RP-HPLC) method with fluorescent detector (FLD) was developed and optimized for Norfloxacin determination in human plasma. Mobile phase specifications, extraction method and excitation and emission wavelengths were varied for optimization. HPLC system contained a reverse phase C18 (5 μm, 4.6 mm×150 mm) column with FLD operated at excitation 330 nm and emission 440 nm. The optimized mobile phase consisted of 14% acetonitrile in buffer solution. The aqueous phase was prepared by mixing 2g of citric acid, 2g sodium acetate and 1 ml of triethylamine in 1 L of Milli-Q water was run at a flow rate of 1.2 mL/min. The standard curve was linear for the range tested (0.156–20 μg/mL) and the coefficient of determination was 0.9978. Aceclofenac sodium was used as internal standard. A detection limit of 0.078 μg/mL was achieved. Run time was set at 10 minutes because retention time of norfloxacin was 0.99 min. which shows the rapidness of this method of analysis. The present assay showed good accuracy, precision and sensitivity for Norfloxacin determination in human plasma with a new internal standard and can be applied pharmacokinetic evaluation of Norfloxacin tablets after oral administration in human.
Abstract: Severe acute respiratory syndrome (SARS) is a respiratory disease in humans which is caused by the SARS coronavirus. The treatment of coronavirus-associated SARS has been evolving and so far there is no consensus on an optimal regimen. The mainstream therapeutic interventions for SARS involve broad-spectrum antibiotics and supportive care, as well as antiviral agents and immunomodulatory therapy. The Protein- Ligand interaction plays a significant role in structural based drug designing. In the present work we have taken the receptor Angiotensin converting enzyme 2 and identified the drugs that are commonly used against SARS. They are Lopinavir, Ritonavir, Ribavirin, and Oseltamivir. The receptor Angiotensin converting enzyme 2 (ACE-2) was docked with above said drugs and the energy value obtained are as follows, Lopinavir (-292.3), Ritonavir (-325.6), Oseltamivir (- 229.1), Ribavirin (-208.8). Depending on the least energy value we have chosen the best two drugs out of the four conventional drugs. We tried to improve the binding efficiency and steric compatibility of the two drugs namely Ritonavir and Lopinavir. Several modifications were made to the probable functional groups (phenylic, ketonic groups in case of Ritonavir and carboxylic groups in case of Lopinavir respectively) which were interacting with the receptor molecule. Analogs were prepared by Marvin Sketch software and were docked using HEX docking software. Lopinavir analog 8 and Ritonavir analog 11 were detected with significant energy values and are probable lead molecule. It infers that some of the modified drugs are better than the original drugs. Further work can be carried out to improve the steric compatibility of the drug based upon the work done above for a more energy efficient binding of the drugs to the receptor.
Abstract: The purpose of this work was to inspect the potential
of vincristine-dextran complex loaded solid lipid nanoparticles for
drug delivery to the brain.
The nanoparticles were stained with a fluorescence dye and their
plasma pharmacokinetic and brain concentrations were investigated
following injection to rats.
The result revealed a significant improvement in the plasma
concentration profile of the SLN injected animals as well as a sharp
increased concentration in the brains.
Abstract: This presentation narrates the comparative analysis of
the dissolution data nimesulide microparticles prepared with
ethylcellulose, hydroxypropyl methylcellulose, chitosan and
Poly(D,L-lactide-co-glycolide) as polymers. The analysis of release
profiles showed that the variations noted in the release behavior of
nimesulide from various microparticulate formulations are due to the
nature of used polymer. In addition, maximum retardation in the
nimesulide release was observed with HPMC (floating particles).
Thus HPMC miacroparticles may be preferably employed for
sustained release dosage form development.
Abstract: A new and cost effective RP-HPLC method was
developed and validated for simultaneous analysis of non steroidal
anti inflammatory dugs Diclofenac sodium (DFS), Flurbiprofen
(FLP) and an opioid analgesic Tramadol (TMD) in advanced drug
delivery systems (Liposome and Microcapsules), marketed brands
and human plasma. Isocratic system was employed for the flow of
mobile phase consisting of 10 mM sodium dihydrogen phosphate
buffer and acetonitrile in molar ratio of 67: 33 with adjusted pH of
3.2. The stationary phase was hypersil ODS column (C18, 250×4.6
mm i.d., 5 μm) with controlled temperature of 30 C°. DFS in
liposomes, microcapsules and marketed drug products was
determined in range of 99.76-99.84%. FLP and TMD in
microcapsules and brands formulation were 99.78 - 99.94 % and
99.80 - 99.82 %, respectively. Single step liquid-liquid extraction
procedure using combination of acetonitrile and trichloroacetic acid
(TCA) as protein precipitating agent was employed. The detection
limits (at S/N ratio 3) of quality control solutions and plasma samples
were 10, 20, and 20 ng/ml for DFS, FLP and TMD, respectively.
The Assay was acceptable in linear dynamic range. All other
validation parameters were found in limits of FDA and ICH method
validation guidelines. The proposed method is sensitive, accurate and
precise and could be applicable for routine analysis in
pharmaceutical industry as well as in human plasma samples for
bioequivalence and pharmacokinetics studies.
Abstract: Antioxidants contribute to endogenous photoprotection
and are important for the maintenance of skin health. The study was carried out to compare the skin hydration and transepidermal
water loss (TEWL) effects of a stable cosmetic preparation
containing flavonoids, following two applications a day over a period
of tenth week. The skin trans-epidermal water loss and skin hydration
effect was measured at the beginning and up to the end of study period of ten weeks. Any effect produced was measured by Corneometer and TEWA meter (Non-invasive probe).
Two formulations were developed for this study design. Formulation one the control formulation in which no apple juice
extract( Flavonoids) was incorporated while second one was the active formulation in which the apple juice extract (3%) containing
flavonoids was incorporated into water in oil emulsion using Abil EM 90 as an emulsifier. Stable formulations (control and Active)
were applied on human cheeks (n = 12) for a study period of 10 weeks. Result of each volunteer of skin hydration and TEWL was
measured by corneometer and TEWA meter. By using ANOVA and Paired sample t test as a statistical evaluation, result of both base and
formulation were compared. Statistical significant results (p≤0.05)
were observed regarding skin hydration and TEWL when two creams, control and Formulation were compared. It showed that
desired formulation (Active) may have interesting application as an
active moisturizing cream on healthy skin.
Abstract: L-asparaginase was extracted from pathogenic
Escherichia coli which was isolated from urinary tract infection
patients. L-asparaginase was purified 96-fold by ultrafiltration, ion
exchange and gel filtration giving 39.19% yield with final specific
activity of 178.57 IU/mg. L-asparaginase showed 138,356±1,000
Dalton molecular weight with 31024±100 Dalton molecular mass.
Kinetic properties of enzyme resulting 1.25×10-5 mM Km and
2.5×10-3 M/min Vmax. L-asparaginase showed a maximum activity
at pH 7.5 when incubated at 37 ºC for 30 min and illustrated its full
activity (100%) after 15 min incubation at 20-37 ºC, while 70% of its
activity was lost when incubated at 60 ºC. L-asparaginase showed
cytotoxicity to U937 cell line with IC50 0.5±0.19 IU/ml, and
selectivity index (SI=7.6) about 8 time higher selectivity over the
lymphocyte cells. Therefore, the local pathogenic E. coli strains may
be used as a source of high yield of L-asparaginase to produce anti
cancer agent with high selectivity.
Abstract: Preparation of hydrogel based on carrageenan
extracted from Kappaphycus alvarezii was conducted with film
immersion in glutaraldehyde solution (GA 4%w/w) for 2min and
then followed by thermal curing at 110°C for 25min. The method of
carrageenan recovery strongly determines the properties of
crosslinked carrageenan. Hydrogel obtained from alkali treated
carrageenan showed higher swelling ability compared to hydrogel
from nonalkali treated carrageenan. Hydrogel from alkali treated
showed the ability of sensitive to pH media.
Abstract: This study was conducted to formulate diclofenac sodium-loaded chitosan nanoparticles and to study the effect of formulation compositions on particle size and zeta potential of chitosan nanoparticles (CSN) containing diclofenac sodium (DC) prepared by ionotropic gelation method. It was found that the formulations containing chitosan, DC and tripolyphosphate (TPP) at a weight ratio of 4:1:1, respectively, with various pH provided various systems. At pH 5.0 and 6.0, the obtained systems were turbid because of precipitation of DC and chitosan, respectively. However, the dispersed system of CSN possessing diameter of 108±1 nm and zeta potential of 19±1 mV could be obtained at pH 5.5. These CSN also showed spherical morphology observed via a transmission scanning electron microscope. Change in weight ratio of chitosan:DC:TPP i.e. 1:1:1, 2:1:1, 3:1:1 and 4:1:1 showed that these ratios led to precipitation of particles except for the ratio of 4:1:1 providing CSN properly. The effect of Tween 80 as a stabilizer was also determined. It suggested that increment of Tween 80 concentration to 0.02% w/v could stabilize CSN at least 48 hours. However, increment of Tween 80 to 0.03% w/v led to quick precipitation of particles. The study of effect of TPP suggested that increment of TPP concentration increased particle size but decreased zeta potential. The excess TPP caused precipitation of CSN. Therefore, the optimized CSN was the CSN containing chitosan, DC and TPP at the ratio of 4:1:1and 0.02% w/v Tween 80 prepared at pH 5.5. Their particle size, zeta potential and entrapment efficiency were 128±1 nm, 15±1 mV and 45.8±2.6%, respectively.
Abstract: The present invention relates to multiple-unit tablet dosage forms, which is composed of several subunits (multiparticulates/pellets). Each small multiparticulate further composed of many layers. Some layer contains drug substance; others are rate controlling polymer. The resulting multiple-unit tablet dosage forms of pantoprazole were satisfactory fabricated. Pelletization technique has some advantages over coated tablet formulation. In coated tablet the coating may be damaged and a pinhole possibly formed that would result in increased release of drug in stomach and may be deactivated in stomach juices. If the coat of some pellets may be damaged that would not affect the release properties of the multiple-unit tablet. Hence they are beneficial in this aspect. The results confirmed the successful preparation of stable and bioequivalent once daily controlled release multiple-unit tablets of pantoprazole.
Abstract: Aims: To evaluate the application of non-invasive diabetes risk assessment tool in community pharmacy setting. Methods: Thai diabetes risk score was applied to assess individuals at risk of developing type 2 diabetes. Interactive computer-based risk screening (IT) and paper-based risk screening (PT) tools were applied. Participants aged over 25 years with no known diabetes were recruited in six participating pharmacies. Results: A total of 187 clients, mean aged (+SD) was 48.6 (+10.9) years. 35% were at high risk. The mean value of willingness-to-pay for the service fee in IT group was significantly higher than PT group (p=0.013). No significant difference observed for the satisfaction between groups. Conclusions: Non-invasive risk assessment tool, whether paper-based or computerized-based can be applied in community pharmacy to support the enhancing role of pharmacists in chronic disease management. Long term follow up is needed to determine the impact of its application in clinical, humanistic and economic outcomes.