ABSTRACT
Sacubitril/Valsartan (SAC/VAL) is a combination drug used for the treatment of heart failure. In the present work,novel and rapid, sensitive, specific, and robust ultra high-performance liquid chromatography method was developedand validated for the simultaneous estimation of SAC/VAL in presence of their seven related impurities anddegradation products. The chromatographic separation was achieved on Accucore XL C8, (100 × 4.6) mm; 3 μmreverse phase column maintained at 30°C. The peaks were eluted using tetrahydrofuran (THF) and 0.1% perchloricacid in water (8:92, %v/v) as a mobile phase A and THF:water:acetonitrile (5:15:80, %v/v/v) as mobile phase B in agradient mode. The flow rate was set at 0.6 ml/minute and the analytes were monitored in the range of 200–400 nmusing a Photo Diode Array (PDA) detector for 21 minutes run time. The method was validated as per ICH Q2 (R1)guideline and all the validation parameters were found within the acceptance criteria. The forced degradation studyfor SAC/VAL showed that the drugs were prone to acidic, alkaline, and neutral hydrolytic as well as oxidative stressconditions. All the degradation products were separated from each other, SAC/VAL and their impurities showing thestability indicating power of the method. The newly developed method can be used for estimation of assay and relatedsubstances from bulk or their finished products with good efficiency.
ABSTRACT
Modern extraction technique was investigated for the separation of betulinic acid from the bark of Dillenia indicaLinn. Betulinic acid, a pentacyclic triterpenoid, is a potent anticancer compound and possesses other pharmacologicalactions. The objective of the present study was to investigate the optimum extraction conditions for betulinic acidusing microwave-assisted extraction by applying response surface methodology based on three factors three levelsBox–Behnken experimental design. The extraction was performed by considering three different independent variables:extraction temperature (70°C–90°C), microwave power (100 W), and extraction time (10–20 minutes) and quantifiedusing developed High-performance thin layer chromatography method. The maximum yield of betulinic acid at optimizedexperimental conditions, i.e., 90°C, 200 W, 15 minutes was found to be 0.91%w/w. Analysis of variance showed that the“p-value” was 0.0004 which indicate that the models were statistically significant (p ˂ 0.05). The value of the “coefficientof determination” (R2) for microwave-assisted extraction was 0.94 which indicate that the model shows the goodness offit. To conclude, Microwave Extraction technique along with response surface design proved to be efficient compared toconventional methods which could be applied to isolate active constituents from plant sources.
ABSTRACT
Dillenia indica Linn. and Dillenia pentagyna Roxb. plants are commonly known as ‘Karmal’ and ‘Mota Karmal’ respectively belonging to family Dilleniaceae. These plants are distributed in many Asian countries, in India from Himalaya to south India. Morphologically leaves, bark and fruit are having major differentiating characters of both species. Traditionally the different parts of these plants have curing properties like cancer, wound healing, diabetes, diarrhea, bone fracture, in cut and burns, abdominal pains etc. Based on phytochemical investigations these plants are reported to contain active constituents like betulin, betulinic acid, dillenetin, dipoloic acid, myricetin, quercetin derivatives etc. Different prepared extracts of these plants and their parts has been reported to contain wide range of flavonoids, steroids, triterpenoids, phenolics, saponins, fixed oil which may exert varied pharmacological activities like anticancer, antidiarrheal, antimicrobial, antioxidant and many more. The present review approaches for pharmacognostical description, phytochemical investigations and therapeutic importance of both the species.