ABSTRACT
With the advent of 21st century, researchers worldwide have extensively reviewed herbs and botanicals for their marked clinical efficacy. It has been estimated that most of the newly discovered compounds offer poor bioavailability due to their low aqueous solubility. Phospholipid complexation of the drug often helps to improve its water solubility and enhance the bioavailability. This study includes optimization of resveratrol-phospholipid complexes using a 3-factor, 3-level box-behnken design (15 batches). Three independent variables i.e. phospholipid-resveratrol ratio, refluxing temperature and reflux time were optimized for two dependent variables, i.e. yield and entrapment efficiency (EE). Complexes were prepared by refluxing stoichiometric ratio of Phospholipon 90G and resveratrol in dichloromethane and retrieved by precipitation with n-hexane. Complexation was confirmed by Fourier Transform Infra-Red (FTIR) spectroscopy. The data was suitably used to explore quadratic response surfaces and construct second order polynomial models with Design Expert®. Formulation with highest desirability (D=0.994) was selected as optimum and prepared using 1.5:1 Phospholipon 90G-resveratrol ratio (X1) at 59.4°C temperature (X2) and 4 h time (X3) to give maximum yield and entrapment efficiency. Analysis of variance (ANOVA) was also found to be significant for both the responses. Complexes were optimised for good yield and EE. The partition coefficient was lowered to 2.25 hypothesizing good passive absorption.
ABSTRACT
With the advent of 21st century, researchers worldwide have extensively reviewed herbs and botanicals for their marked clinical efficacy. It has been estimated that most of the newly discovered compounds offer poor bioavailability due to their low aqueous solubility. Phospholipid complexation of the drug often helps to improve its water solubility and enhance the bioavailability. This study includes optimization of resveratrol-phospholipid complexes using a 3-factor, 3-level box-behnken design (15 batches). Three independent variables i.e. phospholipid-resveratrol ratio, refluxing temperature and reflux time were optimized for two dependent variables, i.e. yield and entrapment efficiency (EE). Complexes were prepared by refluxing stoichiometric ratio of Phospholipon 90G and resveratrol in dichloromethane and retrieved by precipitation with n-hexane. Complexation was confirmed by Fourier Transform Infra-Red (FTIR) spectroscopy. The data was suitably used to explore quadratic response surfaces and construct second order polynomial models with Design Expert®. Formulation with highest desirability (D=0.994) was selected as optimum and prepared using 1.5:1 Phospholipon 90G-resveratrol ratio (X1) at 59.4°C temperature (X2) and 4 h time (X3) to give maximum yield and entrapment efficiency. Analysis of variance (ANOVA) was also found to be significant for both the responses. Complexes were optimised for good yield and EE. The partition coefficient was lowered to 2.25 hypothesizing good passive absorption.
ABSTRACT
Background: Strychnos nux-vomica, commonly known as kuchla, contains strychnine and brucine as main constituents. Minor alkaloids present in the seeds are protostrychnine, vomicine, n-oxystrychnine, pseudostrychnine, isostrychnine, chlorogenic acid, and a glycoside. Seeds are used traditionally to treat diabetes, asthma, aphrodisiac and to improve appetite. Objective: The present study was aimed to evaluate the various pharmacognostical characters and antidiabetic activity of S. nux-vomica seed. Materials and Methods: Pharmacognostical characters were performed as per the WHO guideline. Extraction was carried out in petroleum ether, chloroform, alcohol, hydroalcoholic, aqueous, and phytochemical constituents present in extracts were detected by different chemical tests. Among these extracts hydroalcoholic, aqueous extracts were evaluated for antidiabetic activity on the basis of extractive yield and phytoconstituents, in alloxan-induced diabetic rats using gliclazide as standard. Results: Various analytical values of S. nux-vomica extract were established. Phytoconstituents present in S. nux-vomica extracts were detected. Conclusion: S. nux-vomica extracts show antihyperglycemic activity in experimental animals.
ABSTRACT
Micronized piroxicam was mixed with lactose, mannitol, sorbitol, maltitol and sodium chloride to produce ordered mixture in a glass vial by manual hand shaking method. The effect of excipients, surfactant, superdisintegrant, drug concentration and carrier particle size on dissolution rate was investigated. Dissolution rate studies of the prepared ordered mixtures revealed that all water soluble excipients increased the dissolution rate of piroxicam when compared to the dissolution rate of piroxicam or its suspension. Ordered mixture formulation PLF4, consisting of lactose as water soluble excipient, SSG [8% w/s] and SLS [1% w/w], released piroxcam at a very fast rate so much so that about 90% of the composition had passed into solution within 2 min. The order of the dissolution rate enhancement for ordered mixtures of various water soluble excipients was: lactose > mannitol > maltitol > sorbitol > sodium chloride. Carrier granules of size 355-710 micro m were most effective in increasing the dissolution rate of drug from ordered mixtures. Decreasing the carrier particle size reduced drug dissolution from ordered mixtures. The dissolution rate of ordered mixtures consisisting of 1-5% w/w piroxicam was superior to dissolution rate of piroxicam suspension. The dissolution data fitting and the resulting regression parameters indicated Hixson Crowell, cube root law, as the best fit to drug release data of ordered mixtures