Quantification Assay of Methoxsalen from Bulk Dosage Form by UVSpectrometry Method
Manisha B. Parhad
Sch Acad J Pharm | 83-86
DOI : 10.36347/sajp
Abstract
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Rapid, specific and economic UV spectrophotometric method has been developed to determine the
methoxsalen content in bulk and pharmaceutical dosage formulations. At a pre-determined λ max of 247nm,it was
proved linear in the range of 1.0–12.0 mg/mL, and exhibited good correlation coefficient (R2-0.999 .This method was
successfully applied to the determination of methoxsalen content in marketed brand(Melanocyl R2-0.982, Meladerm R2-
0.971) and the results were in good agreement with the label claims. Methoxsalen is a photosensitizing agent which has
a chemical structure susceptible to degradation. The obtained results proved that the method can be employed for the
routine analysis of methoxsalen in bulks as well as in the commercial formulations.
Degradation Rate of Ebastine in an Aqueous Solution at pH 1.2 and the Effects of Cyclodextrins
Seiji Matsuyama, Takuro Kurita, Tadakazu Tokumura
Sch Acad J Pharm | 87-91
DOI : 10.36347/sajp
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Ebastine (EBA), 4'-tert-butyl-4-(4-(diphenyl methoxy) piperidino) butyrophenone, is a second generation H1-
antihistamine. The solubility of EBA is poor in aqueous solutions, but increases in acidic conditions. EBA is degraded in
aqueous solutions. There are no reports about the degradation rate of EBA in acidic solutions. The aim of this study was
to determine the degradation rate of EBA in an acidic solution and to stabilize EBA in the solution. The stability of EBA
in a buffer solution at pH 1.2 with 1% methanol at 37, 50 and 60°C was examined. EBA in solution was determined by
HPLC. α-, β- and γ-cyclodextrins (CDs) as stabilizers as well as the stability of the CDs in solution were examined. The
degradation of EBA was considered to be a pseudo-first-order reaction. The apparent first-order rate constant of EBA in
the pH 1.2 buffer solutions at 37°C was 14.9×10-3 hour-1. When α-, β- and γ- CDs were added, the rate constant decreased
to 12.2×10-3, 0.83×10-3 and 7.20×10-3 hour-1 for α-, β- and γ- CDs, respectively. β- CD was found to have the strongest
stabilizing effect. The activation energy for the degradation of EBA under this condition was 106.9 kJ/ mol. The addition
of CDs increased the value, and CDs were slowly degraded in the pH 1.2 solution
Anti inflammatory activity of Methanolic stem extract of Tephrosia purpurea.
Atul Kumar Gangwar, Ashoke K. Ghosh
Sch Acad J Pharm | 92-94
DOI : 10.36347/sajp
Abstract
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Tephrosia purpurea L. plant is used in the indigenous system of medicine, belonging to the Family Fabaceae.
To study the anti-inflammatory activity of methanolic stem extract of T. purpurea by using Carrageenan induced model.
Anti-inflammatory activity of methanolic stem extract of T. purpurea was studied, in which inflammation was induced
by injecting 0.1ml of 1 per cent Carrageenan in to the sub plantar side of the left hind paw. Test drugs were administered
in a dose of 10, 20 and 40 mg/kg (body weight) one hour before commencing the experiment. The anti-inflammatory
activity was assessed by determining and comparing the paw volume (ml) in the test drug group with that of the vehicle
control group. Diclofenac sodium 5 mg/kg (body weight) was used as a reference drug. Inflammation in the methanolic
stem extract of T. purpurea treated animals was found to be significantly less compared to vehicles control animals.
Diclofenac sodium (5 mg/kg body weight) produces significant reduction in inflammation when compared to control
group. Methanolic stem extract of T. purpurea (M.S.E.T.) produced significant anti-inflammatory activity. Our results
suggest that all the Methanolic stem extract of T. purpurea (M.S.E.T.) possess significant anti-inflammatory activity.
Among the three doses of T. purpurea 40 mg/kg body weight showed maximum activity.
Protective effect of multiple administration of alpha – lipoic acid in lipopolysaccharide – induced model of inflammation in rats
Nina Doncheva, Lilia Vasileva, Maria Ivanovska, Atanaska Petrova, Mariana Murdjeva, Damianka Getova
Sch Acad J Pharm | 95-99
DOI : 10.36347/sajp
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Alpha-lipoic acid is well known antioxidant and has anti-inflammatory effects. It is used to treat diabetic
neurovascular and metabolic problems. The aim of our study was to evaluate the anti-inflammatory effect of alpha- lipoic
acid (ALA) in lipopolysaccharide (LPS) - induced model of inflammation in rats. Forty male Wistar rats were divided in
five groups (n=8): control, model group and three experimental groups treated with 30, 60 and 90 mg/kg alpha – lipoic
acid for 14 days. The inflammation was induced by a single dose administration of LPS from Escherichia coli 055: B in
dose 250 μg/kg i.p. After four hours the animals were sacrificed and blood samples were collected. The levels of two proinflammatory factors including tumor necrosis factor- alpha (TNF-alpha) and interleukin -6 (IL-6) were measured by
Enzyme-Linked Immuno Sorbent Assay (ELISA). Intraperitoneal administration of LPS increased the level of both TNFalpha and IL-6 in the model group compared to the control group. In all ALA treated groups the level of TNF-alpha was
significantly decreased (p<0, 05) compared to the model group. In contrast, IL-6 release in the group treated with 30
mg/kg ALA was significantly (p<0, 05) higher than the model group. There was no significant reduction (p<0, 05) in the
level of IL-6 in all experimental groups. Our present study demonstrates that chronic ALA administration significantly
protects against lipopolysaccharide-induced inflammation in rats.
Synthesis, Characterization and Pharmacological Evaluation of Novel Mannich bases of Thienopyrimidine Derivatives
D. Rajendra, Syed Asma, K Vijaya, G Kalyani
Sch Acad J Pharm | 100-111
DOI : 10.36347/sajp
Abstract
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Thienopyrimidines has received considerable attention as they are endowed with variety of biological
activities and have wide range of therapeutic properties. Thienopyrimidines, the structural analogues of biogenic purine
class, has high significant in field of pharmaceutical and biotechnological sciences, with wide spectrum of biological
activities. A series thienopyrimidines can be easily synthesized by Gewald reaction. The first step of this multicomponent
reaction is the Knoevenagel-Cope condensation of carbonyl compound (ketone or aldehyde) with an activated nitrile (α-
cyanoester), yielding an α,β– unsaturated nitrile. This intermediate is then thiolated at the methylene group by elemental
sulfur, followed by an intramolecular cyclization yielding a polysubstituted-2-aminothiophene. The structure of
compounds were characterized by 1H-NMR, IR and mass spectral analysis, and evaluated for their anti-inflammatory
activity by carrageen induced paw oedema method and standard drug used for anti-inflammatory activity is Diclofenac
Sodium.