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Chemistry, Pharmaceutical (1):
Recent article
Chemistry, Pharmaceutical
Nature Chemical Biology (7)11 2011
Abstract
Cyclooxygenase-2 (COX-2) catalyzes the oxygenation of arachidonic acid and the endocannabinoids 2-arachidonoylglycerol and arachidonoylethanolamide. Evaluation of a series of COX-2 inhibitors revealed that many weak competitive inhibitors of arachidonic acid oxygenation are potent in...
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PMID: 22053353
PDF is available here.
PDF is available here.
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Abstract
Interest in use of the polysaccharide chitosan as a pharmaceutical excipient by different dose routes and for a number of applications is not new but it still does not appear to be present in any marketed drugs. Also a novel excipient in a new formulation requires a lot of safety consideration. Publi...
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PMID: 21928704
PDF is available here.
PDF is available here.
Abstract
The present investigation concerns with the development and optimization of a bipolymeric delivery device for the treatment of colonic diseases. Prednisolone - a popular glucorticoid was used a model drug. The formulations were designed with an objective to deliver the drug to the large bowel with a...
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PMID: 21928719
PDF is available here.
PDF is available here.
Abstract
Abstract
Sulfurous compounds: sodium sulfite Na2SO3 (E 221), sodium bisulfite NaHSO, (E 222), and sodium metabisulfite Na2S2O5 (E 223) are largely used as antioxidants in many pharmaceutical formulations. A method for determination of sodium metabisulfite in parenteral formulations containing tartrate ions wa...
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PMID: 21928707
PDF is available here.
PDF is available here.
Abstract
The purpose of this research was to develop oro-dispersible tablets of metformin by direct compression method using super disintegrants approach, effervescent approach and sublimation approach. Powder blend was evaluated for angle of repose, bulk density, tapped density, compressibility index, Hausne...
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PMID: 21928717
PDF is available here.
PDF is available here.
Abstract
The aim of this study was to evaluate the effects of newly formulated topical cream of Calendula officinalis extract on the mechanical parameters of the skin by using the cutometer. The Cutometer 580 MPA is a device that is designed to measure the mechanical properties of the skin in response to the...
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PMID: 21928714
PDF is available here.
PDF is available here.
Abstract
Abstract
We present a data mining approach that enables the identification of alternative analog series with different core structures, corresponding substitution patterns, and comparable potency progression. Scaffolds can be exchanged between these series and new analogs suggested that incorporate preferred...
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PMID: 21774471
PDF is available here.
PDF is available here.
Abstract
We present an extension of the activity cliff concept by introducing "activity ridges" that are formed by overlapping "combinatorial" activity cliffs between participating compounds, giving rise to ridge-like structures in activity landscapes. Activity ridges are rich in SAR information. In a system...
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PMID: 21761918
PDF is available here.
PDF is available here.
Abstract
Abstract
A large-scale similarity search investigation has been carried out on 266 well-defined compound activity classes extracted from the ChEMBL database. The analysis was performed using two widely applied two-dimensional (2D) fingerprints that mark opposite ends of the current performanc...
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PMID: 21728295
PDF is available here.
PDF is available here.
Abstract
We sought to develop an appropriate method to examine large sets of GPCR ligand information for both screening collection enhancement and hit expansion. To this end, we have implemented a modified version of BDACCS that removes highly correlated descriptors (rBDACCS). To test the hypothesis that a s...
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PMID: 21761904
PDF is available here.
PDF is available here.
Abstract
We describe the potential of estimating melting temperature (T(m)) for nonstandard oligonucleotides by using the correlation of the experimental T(m) with the calculated duplex binding energy (BE) for oligonucleotides of a given length. This method has been automated into a standardized molecular dy...
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PMID: 21702481
PDF is available here.
PDF is available here.
Abstract
The mechanism of action of non-steroidal anti-inflammatory drugs (NSAIDs), to which ketoprofen belongs, is based on their cyclo-oxigenase (COX) inhibiting action, concerning both subtype COX-1 constitutive isoform and COX-2 inducible isoform. Ketoprofen administration may be carried out by oral and p...
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PMID: 21780552
PDF is available here.
PDF is available here.
Abstract
Our study concludes that cellular uptake and cytotoxicity of DOX can be improved in MES-SA/Dx5 cells by loading DOX into PLGA NPs. DNPs targeted to membrane receptors may enhance cellular uptake and cytotoxicity in SKOV-3 cells. FROM THE CLINICAL EDITOR: The authors of this study compare the cellula...
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PMID: 21094277
PDF is available here.
PDF is available here.
Abstract
Nevirapine is a poorly water-soluble antiretroviral drug. Intravenous nevirapine nanosuspensions (NS) (457 ± 10 nm) were prepared by high-pressure homogenization. NS were surface modified by stabilizer adsorption, e.g., serum albumin, polysaccharide and polyethylene glycol (PEG) 1000. The NS were ch...
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PMID: 21094278
PDF is available here.
PDF is available here.
Abstract
Nifedipine is a dihydropyridine calcium channel antagonist effective in the clinical management of cardiovascular disease. Due to nifedipine's poor water solubility and erratic bioavailability, complexation with selected cyclodextrins was studied in order to overcome these limitation...
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PMID: 21091429
PDF is available here.
PDF is available here.
Abstract
The 90% confidence intervals for Test/Reference ratios of the pharmacokinetic parameters (Cmax, AUC0-t and AUC0-∞) of both risperidone and its active metabolite (9-hydroxyrisperidone) fell within the acceptable bioequivalence range (80 - 125%) according to ASEAN guideline. Conclusion: The two risp...
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PMID: 21612749
PDF is available here.
PDF is available here.
Abstract
These results indicated that solvent emulsification evaporation is a simple, easy, available and effective method for preparing SYR-SLN....
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PMID: 21699077
PDF is available here.
PDF is available here.
Abstract
The three main pillars of drug evaluation are quality, safety and efficacy. Each marketing authorization dossier has to demonstrate conformity with quality, safety and efficacy requirements separately. While this is justifiable, it may nevertheless lead to some important problems being overlooked. Th...
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PMID: 21699091
PDF is available here.
PDF is available here.
Abstract
This study was done to prepare thymopentin (TP5)-loaded poly (butyl cyanoacrylate) nanoparticles (TP5-PBCA-NPs) and evaluate thier efficacy for oral delivery. TP5-PBCA-NPs were prepared by emulsion polymerization, and the formulation was optimized based on Box-Behnken experimental design. The physico...
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PMID: 21699067
PDF is available here.
PDF is available here.
Abstract
PX-18 and PX-13 are secretory phospholipase A2-IIA (sPLA2-IIA) inhibitors. An increased expression of sPLA2 in psoriatic skin has been reported. The selective inhibition of this enzyme is a new therapeutic approach. For dermal application PX-18 and PX-13 have been loaded to Nanostructured lipid carri...
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PMID: 21699069
PDF is available here.
PDF is available here.
Abstract
Melittin liposomes surface modified with poloxamer 188 were developed, and the effect of poloxamer 188 was investigated with regard to anti-cancer effect and vascular stimulation. Melittin liposomes surface modified with poloxamer 188 at different concentrations (0%, 2%, and 5%) were prepared using t...
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PMID: 21699070
PDF is available here.
PDF is available here.
Abstract
The object of this study was to investigate the influence of static and dynamic forces on mechanical properties of the biocompatible polymer ethyl cellulose. Similar polymeric films containing 40% (w/w) of the plasticizer dibutyl sebacate were subjected to tensile forces at different velocities. The...
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PMID: 21095223
PDF is available here.
PDF is available here.
Abstract
I drugs, IND salts could be considered for possible waivers of bioequivalence....
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PMID: 21453261
PDF is available here.
PDF is available here.
Abstract
A comparative pharmacokinetic study of three enrofloxacin injectable solutions was carried out in six healthy Barky rams after intramuscular injection according to a single dose, randomized, crossover experimental design. The three formulations were enrofloxacin 10% (Baytril(®)), enrofloxacin 10% pl...
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PMID: 21457136
PDF is available here.
PDF is available here.
Ceska a Slovenska farmacie : casopis Ceske farmaceuticke spolecnosti a Slovenske farmaceuticke spolecnosti (60)2 2011
Abstract
During the second half of the last century, pelletization methods based on wetting were developed, e.g. agglomeration in coating pans, pelletization plates or fluid-bed equipment, layering of the drug in solution or suspension on inactive spherical cores, extrusion/spheronization and later on also ro...
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PMID: 21650006
PDF is available here.
PDF is available here.
Abstract
To summarize a standard formulary decision process and provide recommendations for the integration of pharmacogenomic (PGx) information within the formulary decision-making process.
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PMID: 21487085
PDF is available here.
PDF is available here.
Ceska a Slovenska farmacie : casopis Ceske farmaceuticke spolecnosti a Slovenske farmaceuticke spolecnosti (60)2 2011
Abstract
The present paper deals with a complex spectral and physicochemical evaluation of mono[{3-[4-(2-etoxyetoxy)-benzoyloxy]-2-hydroxypropyl}-isopropylammonium]fumarate, a potential ultrashort acting beta1-blocker. The identity of the substance under study (labelled as UPB-1) was confirmed by 1H- and 13C-...
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PMID: 21650011
PDF is available here.
PDF is available here.
Ceska a Slovenska farmacie : casopis Ceske farmaceuticke spolecnosti a Slovenske farmaceuticke spolecnosti (60)2 2011
Univerzita Komenského Bratislava, Farmaceutická fakulta, Katedra galenickej farmácie, Slovenská republika.
Abstract
The objective of this article is to describe the formulation and evaluation of dermal semisolid drugs--carbopol hydrogels containing the solution of Bukofit, zinc chloride and the local anaesthetic lidocaine. The hydrogels were evaluated after 2, 7, 14 and 28 days after their preparation and stored a...
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PMID: 21650010
PDF is available here.
PDF is available here.
Abstract
Enalapril maleate, one of the Angiotensin converting enzyme (ACE) inhibitor is effective in the treatment of hypertension. Enalapril maleate is selected for the present study. The aim of this study was to develop a new formulation of Enalapril maleate tablet and its comparative evalu...
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PMID: 21454172
PDF is available here.
PDF is available here.
Abstract
Betulinic acid (3beta, hydroxy-lup-20(29)-en-28-oic acid, BA), a pentacyclic triterpenoid, is derived from a widely distributed natural anticancer compound betulin. It has selective anticancer activity against several tumor cells, and recently it was shown that it also possess anti-a...
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PMID: 21702370
PDF is available here.
PDF is available here.
Abstract
The objective of the present investigation was to prepare mucoadhesive microspheres of ketorolac for nasal administration by means of a solvent evaporation technique using carbopol (CP), polycarbophil (PL) and chitosan (CS) as mucoadhesive polymers. The prepared microspheres were cha...
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PMID: 21612151
PDF is available here.
PDF is available here.
Abstract
A randomized study comparing efficacy and safety of a new 75 mg/1 ml formulation of injectable diclofenac sodium designed for intra-deltoid use with the conventional 75 mg/3 ml formulation given by the intra-gluteal route. Design: This was an open-label, multicentric, randomized clinical trial.
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PMID: 21429443
PDF is available here.
PDF is available here.
Abstract
Formulation of the contact allergens dinitrochlorobenzene and isoeugenol in ethanolic liposomes (ethosomes) increases their sensitizing properties in the local lymph node assay compared with an ethanol-water formulation of the allergens. Likewise, isoeugenol and methyldibromo-glutaronitrile formulate...
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PMID: 21091289
PDF is available here.
PDF is available here.
Abstract
Due to the eye's specific anatomical and physiological conformation, the treatment of eye diseases is a real challenge for pharmaceutical therapy. The presence of efficient protective barriers (i.e., the conjunctival and corneal membranes) and protective mechanisms (i.e., blinking and nasolachrymal d...
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PMID: 21440104
PDF is available here.
PDF is available here.
Abstract
Revue d histoire de la pharmacie (58)368 2011
Abstract
Theriaca, after the Greco-Roman antiquity, survived centuries with some continuity. The formula used during the 17th century, inherited from the tradition of Hippocrates and Galen is closed to what it was centuries earlier, despite the difficulties of supply of raw materials. It is considered a mains...
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PMID: 21661227
PDF is available here.
PDF is available here.
Abstract
The objective of the present study was to develop a nanocarrier based formulation of nadifloxacin and to investigate its in vitro antimicrobial effect against Propionibacterium acnes. Nanocarrier based microemulsion formulations were prepared by aqueous titration method, using oleic...
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PMID: 21434572
PDF is available here.
PDF is available here.
Abstract
Budesonide is a potent glucocorticoid with high affinity for the glucocorticoid receptor, which is used for the treatment of inflammatory bowel diseases. Current oral formulations of budesonide present low efficacy against ulcerative colitis because of the premature drug release in t...
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PMID: 21434575
PDF is available here.
PDF is available here.
YAKUGAKU ZASSHI (131)2 2011
Abstract
Sperminated pullulans (SP) having different molecular weights (MWs) were prepared, and the enhancing effect on the pulmonary absorption of insulin in rats was examined. SP acted as enhancers of insulin absorption when a 0.1% solution was applied with insulin simultaneously and their enhancing effects...
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PMID: 21297376
PDF is available here.
PDF is available here.
Abstract
UV filters are traditionally classified as chemical absorbers and physical blockers depending on their mechanism of action. In this study, one of the most important chemical UVB absorber, octocrylene, was incorporated into Solid Lipid Nanoparticle (SLN) systems which themselves have...
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PMID: 21434571
PDF is available here.
PDF is available here.
Natural Product Reports (28)1 2011
Abstract
I explain why chemists should be aware of the essentials of plant naming, and describe some easy quality checks that can be performed to avoid errors being perpetuated....
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PMID: 21057691
PDF is available here.
PDF is available here.
Journal of Antibiotics (64)1 2011
Abstract
Abstract
The aim of the studies was to determine with HPLC method the stability of ceftazidime in buffered 1% and 5% eye drops of proposed formulary composition, which were stored for 30 days at the temperature of 4 degrees C and 20 degrees C and protected from light. The 1% and 5% eye drops were prepared und...
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PMID: 21485707
PDF is available here.
PDF is available here.
Abstract
The release of diclofenac sodium and papaverine hydrochloride from tablets and pellets using the flow-through cell apparatus was studied. The influence of excipients and of a size of the solid dosage forms on the amount of the released substances at the intervals of time using the different rates of...
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PMID: 21485300
PDF is available here.
PDF is available here.
Abstract
The aim of the studies was to determine the stability of metronidazole using UV spectrophotometric method in 0.5% w/w eye drops which were prepared under aseptic conditions and thermally sterilized. 0.9% solution of NaCl, 5% glucose and phosphate buffers of pH 6.97 and 6.81 were used as the solvents...
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PMID: 21485708
PDF is available here.
PDF is available here.
Abstract
The objective of present investigation was to evaluate the entrapment efficiency of the anti-HIV drug, zidovudine, using two Eudragit polymers of different permeability characteristics and to study the effect of this entrapment on the drug release properties. In order to increase the entrapment effic...
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PMID: 21648196
PDF is available here.
PDF is available here.
Abstract
Evaluation of in vitro-in vivo correlation (IVIVC) plays important role in securing therapeutic effect if a dosage form undergoes technological modifications. Similarity (closeness) of dissolution profiles of the original and modified dosage forms has been traditionally considered to be sufficient fo...
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PMID: 21648197
PDF is available here.
PDF is available here.
Abstract
Abstract
The aim of the studies was to develop formulary technologies of 1% and 5% eye drops containing cefuroxime with stability of at least 10-12 days. The stability was defined as the time required to reach the cutoff value of 10% degradation of cefuroxime in the drops, as determined using an HPLC assay. T...
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PMID: 21796938
PDF is available here.
PDF is available here.
Abstract
The objective of the present work was to optimize the formulation of fast disintegrating tablets (FDTs) of ondansetron HCl containing novel superdisintegrants, possessing sufficient mechanical strength and disintegration time comparable to those containing crospovidone or croscarmellose sodium. The F...
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PMID: 21796940
PDF is available here.
PDF is available here.
Abstract
The objective of this work was to develop and evaluate reconstitutable suspensions of ibuprofen-loaded microspheres prepared with an acrylic polymer (Eudragit RS-PM). The microspheres were prepared by the quasi-emulsion solvent diffusion technique. To prepare reconstitutable suspension formulation, t...
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PMID: 21796942
PDF is available here.
PDF is available here.
Abstract
The purpose of the study was to develop a simple, versatile HPLC method for the identification and quantification of praziquantel and ivermectin (in Equimax) or praziquantel and abamectin (in Abamitel Plus). A satisfactory separation was obtained using the Supelcosil LC-ABZ+ column in gradient system...
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PMID: 21796928
PDF is available here.
PDF is available here.
Abstract
The present investigation outlays the host-guest penetration of hydrophobic selective Cox-II chemopreventive agent, celecoxib (CXB), with hydroxypropyl-beta-cyclodextrin (HP-beta-CD) using inclusion complexation phenomena. Phase solubility studies conducted at 37 degrees C and 25 degrees C revealed t...
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PMID: 21796941
PDF is available here.
PDF is available here.
Abstract
Alginate based mineral oil entrapped emulsion gel (MOEG) buoyant beads of domperidone were prepared by emulsion gelation technique. The prepared beads were evaluated for particle size, surface morphology, buoyancy, actual drug content and entrapment efficiency. Effect of different oils (castor oil, o...
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PMID: 21485710
PDF is available here.
PDF is available here.
Abstract
The spray drying technique was used to obtain the roxithromycin containing microcapsules with high taste masking efficiency. Eudragit L30D-55 was chosen as a barrier coating. The taste was evaluated by an electronic tongue, and taste-masking effect in water lasted at least several dozen hours.
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PMID: 21796943
PDF is available here.
PDF is available here.
Abstract
Abstract
In the present study, the possible interactions between celecoxib and some excipients (colloidal silicon dioxide (Aerosil), microcrystalline cellulose (Avicel PH 102), lactose anhydrous, magnesium stearate, cross-povidone and talc) were evaluated by examining the pure drug or drug-excipient powder mi...
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PMID: 21648198
PDF is available here.
PDF is available here.