The present work aims to discuss on Quality by Design based development and characterization of the sustained release mucoadhesive microspheres of quetiapine fumarate. The microspheres were prepared by non-aqueous solvent evaporation process. Factor screening study was carried out using fractional factorial design for identifying the influential factors. Systematic optimization of microspheres was accomplished by Box-Behnken design and characterized for particle size, entrapment efficiency, in vitro drug release and ex vivo mucoadhesion strength, which indicated that microspheres were consequence to be spherical and free flowing in nature. The microspheres exhibited high drug entrapment efficiency and in vitro drug release in a sustained manner, which was considered to be dependent on the concentration of rate controlling polymers. Ex vivo wash-off test on microspheres indicated good mucoadhesive property on excised goat intestinal mucosa. Out of all the accepted formulation, F6 was preferred as the optimized formulation. In vivo pharmacokinetic and brain biodistribution study revealed significant increase in the levels of drug in blood plasma and brain homogenates from the optimized formulation vis-à-vis the pure drug suspension. Overall, current study corroborated significant improvement in the biopharmaceutical attributes of quetiapine fumarate from mucoadhesive microspheres, which can be effectively used for management of depression and schizophrenia.
The concept of fast dissolving dosage form has become popular as new delivery system. This system will provide maximum therapeutic efficacy, increased bioavailability and maximum stability by reducing the frequency of dosage. It will also avoid first pass metabolism of the drugs. This system provides more rapid drug absorption from the pre gastric area which may provide quick onset of action. The present research aimed to prepare fast dissolving films (FDF) of aprepitant used in the prevention and treatment of chemotherapy-induced nausea and vomiting. The FDF was prepared using solvent casting method and optimized employing central composite design considering two independent variables film forming polymer (pullulan) and PEG 400. Disintegration time, wetting time, drug release and folding endurance were taken as dependent variables. The prepared optimized formulation showed minimum disintegration time (20 s), highest dissolution rate (88.87%) and satisfactory physicochemical properties. It is evident from the above results that the developed formulation can be an innovative dosage form to improve the drug delivery, onset of action as well as improve patient compliance.
Two methods, HPLC and TLC were presented for the determination of Oxetacaine (OXT) in the existence of its different degradation products. HPLC method was based on the separation of OXT from its degradation products using reversed phase C18 column at room temperature and isocratic elution with mobile phase mixture of acetonitrile: 5 mM sodium dihydrogen orthophosphate dihydrate, pH was adjusted to 2.4 with orthophosphoric acid (50:50 v/v). Quantitation was based on peak area at 210 nm. The second TLC-densitometric method relies on the separation and quantitation of OXT from its degradation products on TLC silica gel 60 F254 plates, using 2-propanol: triethylamine (10:0.5 v/v) as a developing system and densitometric measurement of the developed bands at 210 nm. Validation of the proposed methods was performed according to the ICH guidelines and applied to evaluate the stability of OXT under different stress conditions.
Obesity, the most prevalent metabolic disorder is associated with elevated body fat mass and body mass index. Cynara scolymus L. is famous for its hepatoprotective properties, also it seems to have good potency as anti-obese agent. In this review article, the potency of C. scolymus as anti-obese agent has been evaluated. The evidences based information were extracted from accessible international electronic databases (PubMed, Springer, Science Direct, Wiley and Google), and books (Persian or English), by key word of Cynara scolymus and artichoke plus obesity or the mechanism of anti-obese drugs. C. scolymus inhibits the digestive enzymes such as pancreas lipase, α-amylase, α-glucosidase, increases the bile secretion, inhibits of inflammation and ROS, improves liver function, gut microbiota, enhances lipolysis and lipid metabolism, and reduces blood glucose in preclinical and clinical studies. Designing large multi-center clinical trials on C. scolymus and evaluating its effects on weight loss in comparison with famous drug such as orlistate could be the subject of future studies.
To evaluate the antioxidant properties of different extracts (chloroform, ethyl acetate, n-butanol and methanol extracts) of fungus C. cupreum SS02. The antioxidant properties were evaluated by using five antioxidant methods, metal chelating assay, 2,2-azino-bis (3-ethylbenzthiazoline-6-sulphonic acid (ABTS), hydroxyl radical (HO
) scavenging assay, superoxide anion (O2
) radical scavenging assay, and nitric oxide (NO
) scavenging assay. Methanol extract of C. cupreum showed highest metal chelating activity (63.61 ± 0.07 mg EDTAE/g DW), followed by chloroform extract (57.25 ± 0.12 mg E DTAE/g DW) and n-butanol extract (27.33 ± 0.07 mg E DTAE/g DW) whereas ethyl acetate extract showed least metal chelating activity (18.35 ± 0.07 mg E DTAE/g DW) at 50 µg/ml. In ABTS assay, n-butanol extract showed highest ABTS inhibition activity (19.91 ± 0.14 μmol RE/g DW), followed by ethyl acetate extract (13.07 ± 0.59 μmol RE/g DW) and chloroform extract (13.07 ± 0.82 μmol RE/g DW) whereas methanol extract showed the lowest activity (11.65 ± 0.16 μmol RE/g DW at 50 µg/ml). In hydroxyl radical scavenging assay, n-butanol extract showed highest scavenging activity (31.95 ± 0.21 mg RE/g DW), followed by ethyl acetate extract (28.19 ± 0.21 mg RE/g DW), methanol extract (22.93 ± 0.37 mg RE/g DW) and chloroform extract (18.04 ± 0.21 mg RE/g DW) at 50 µg/ml. In superoxide anion scavenging assay, chloroform extract showed highest scavenging activity (56.44 ± 0.03 mg RE/g DW) followed by ethyl acetate extract (49.88 ± 0.09 mg RE/g DW), n-butanol extract (19.49 ± 0.09 mg RE/g DW) and methanol extract (7.75 ± 0.06 mg RE/g DW) at 50 µg/ml. The highest inhibition of nitric oxide radical was observed in chloroform extract of C. cupreum (11.23 ± 0.11%) followed by ethyl acetate extract (7.62 ± 0.06%), n-butanol extract (4.72 ± 0.90%) and methanol extract (3.20 ± 0.06%) at 50 µg/ml. The results showed that different extracts of C. cupreum have significant antioxidant activity due to the presence of different phytochemicals. Thus, it is suggested that C. cupreum extracts should be further studied for their antioxidant properties for food and pharmaceutical applications.
Physicians’ perception of the role of the clinical pharmacist role plays a cornerstone in accepting interventions suggested by pharmacists to correct DRPs and in complying with guidelines of a pharmacist-led Antibiotic stewardship program (ASP). This study aimed at evaluating the acceptance of physicians’ to pharmacists interventions to antibiotic prescribing and the change in antibiotic consumption in Al-Haram general hospital Intensive care unit (ICU).
This study was performed in Al-Haram general hospital ICU from July 2014 till December 2015. Medication review of antibiotics started in Al-Haram hospital ICU in July 2014 by responsible clinical pharmacists. An on-job physician education program about antibiotics started in June 2015. Implementation of ASP started in July 2015. The antibiotic related interventions and response of physicians to interventions were recorded all along the study period. The pattern of physicians’ acceptance along with antibiotic consumption (in Daily define dose per 1000 patient-days) were reported.
The number of accepted interventions had increased along the study. The overall antibiotic consumption increased after implementation of ASP, however the individual pattern of antibiotic prescribing changed.
The physicians in Al-Haram hospital appeared to accept the role of clinical pharmacist in correcting antibiotic-related DRPs as well as in implementing ASP.
Specific, accurate and precise electrochemical method was developed and validated for the determination of sulfacetamide sodium in presence of its co-formulated drug (prednisolone acetate) and its pharmacopoeial impurities. The method was based on fabrication of membrane sensor. The characteristics of electrochemical response were estimated, and the proposed sensor displayed excellent characteristics for the determination of sulfacetamide sodium in bulk powder, laboratory prepared mixtures, dosage forms and in spiked biological fluid (Rabbit aqueous humor). The sensor was constructed through the use of tetradodecylammonium bromide (TDB) as an anion exchanger and 2-nitrophenyl octyl ether (NPOE) as a plasticizer in polyvinyl chloride (PVC) matrix. The performance characteristics, sensitivity and selectivity were evaluated according to IUPAC guidelines. Linearity was achieved over the concentration range of 1 × 10−4.5–1 × 10−2 M with Nernstian slope of 51.086 mV/decade over the pH range of 5–7. The sensor showed a rapid response (10–15 s) and good stability (up to 4 weeks). The obtained results were statistically compared with the official methods and no significant difference was found regarding accuracy and precision.
Mucopolysaccharidosis (MPS) and oligosaccharidosis are lysosomal storage disorders (LSDs) that share many clinical features. The present study aimed to establish a protocol for the biochemical diagnosis of these disorders and their subtypes in affected Egyptian children as well as in pregnant females, in order to prepare children or fetus for enzyme replacement therapy. Urine, plasma and leukocyte samples were collected from 280 children with symptoms suggestive of LSDs. Fourteen amniotic fluid samples were collected from pregnant females having positive family history or having one affected sibling. Assessment of urinary glycosaminoglycans (GAGs) followed by two dimensional electrophoresis (2-DEP), thin layer chromatographic (TLC) for separation of oligosaccharides and plasma or leukocyte enzyme activity were performed. Six of pregnancies were diagnosed to have affected fetuses. 84 children had abnormal 2-DEP and classified as 26 MPS I, 10 MPS II, 24 MPS III and 24 MPS VI. Two were diagnosed as α-mannosidosis and 2 as GM1 gangliosidosis. In conclusion; MPS should be excluded before suspecting oligosaccharidosis. 2-DEP and TLC alone cannot rule out the diagnosis of either MPS or oligosaccharidosis and confirmation must be done by specific lysosomal enzymatic assay. Analysis of GAGs by 2-DEP in amniotic fluid can be promising method for prenatal diagnosis of MPS.
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