ABSTRACT
The study aimed at investigating an inclusion complexation technique to improve solubility and dissolution characteristics of carvedilol by successful complexation with β-cyclodextrin. Inclusion complexes (ICs) of drug and β-cyclodextrin were prepared by kneading method in four different ratios. Physical mixtures were also prepared in identical ratios to compare the efficacy of prepared ICs. The preparations were subjected to rheological studies, drug loading, in vitro release study, FT-IR spectroscopy, thermal events analysis by DSC, X-ray diffraction, scanning electron microscopy (SEM) and accelerated stability study. IC granules were free flowing and compressible. FT-IR study denoted to absence of any chemical interactions between drug and carrier. DSC and X-ray diffraction suggested the presence of crystalline drug in the complexes. Dissolution of ICs revealed significant enhancement of release rate and extent compared to untreated drug. MDT, %DE and T25%, T50% and T80% indicated marked improvement in release rate from complexes. Kinetic modeling suggested that fickian diffusion was the predominant mechanism of drug release from solid complexes. Stability samples showed no significant alterations in DSC and FT-IR studies that referred to the stability of ICs. ICs were compatible, effective and stable over time. Further studies can be planned to investigate their therapeutic efficacy.
ABSTRACT
In this experiment the effect of mode of incorporation of some superdisintegrants such as sodium starch glycolate, croscarmellose sodium, crospovidone (kollidon CL), ludiflash and Xanthan gum (XG) on dissolution profile and disintegration time of carbamazepine (CBZ), apoorly water soluble drug was studied. The superdisintegrants were incorporated by extragranularly, intragranularly and in direct compression method. Different amount of superdisintegrants (1%, 3% and 6%) was incorporated in different formulations whereas all the other excipients as well as the active drug remained same. The results indicated that sodium starch glycolate, when incorporated extragranularly in wet granulation method significantly enhanced the release profile of CBZ. Kollidon CL was the most effective superdisintegrant in decreasing disintegration time of different tablet formulations (1.95 minutes when extragranularly incorporated). On the other hand, tablets prepared with SSG were found most effective in % drug release irrespective of its mode of incorporation (99.99% when extragranularly incorporated and 99.75 when intragranularly incorporated within one hour). Tablets prepared by direct compression method also showed similar drug release with other methods but tablet hardness was found lower. So addition of superdisintegrants in tablet formulation may be an effective technique to comply compendial drug release.
ABSTRACT
This attempt is made to address the phytoconstituents, free radical scavenging activity and brine shrimp lethality bioassay of five different extracts of Asparagus racemosus roots. Preliminary phytochemical examination of the crude extracts of Asparagus racemosus root disclosed the existence of different sort of chemical groups such as flavonoids, tannin, saponin, alkaloids, carbohydrate. The root displayed significant DPPH free radical scavenging activity with highest IC50 value showed by ethanol extract with a value of 78.15 μg/ml followed by methanol and petroleum ether having value of 106.44 μg/ml and 273.31 μg/ml respectively as opposed to that of the scavenging effects of ascorbic acid and BHT of 5.698 μg/ml and 8.816 μg/ml respectively. The highest reducing power was showed by ethanol extract followed by methanol and petroleum ether as opposed to that of the reducing potential of ascorbic acid and BHT. The fractions represented good cupric reducing capacity with increasing concentration taking ethanol extract in the top position. The ethanol extract yielded 108.78±2.77 mg/gm gallic acid equivalent phenolic content and methanol sub-fraction yielded 164.77±1.73 mg/gm quercetin equivalent flavonoid content that was highest among five extracts. Ethanol extract of Asparagus racemosus was found to possess the highest total antioxidant capacity (639.925±64.78) mg/gm followed by methanol (616.92±53.88) mg/gm and petroleum ether (469.17±52.95) mg/gm ascorbic acid equivalent respectively. In brine shrimp lethality bioassay, LC50 values for ethanol, methanol, petroleum ether, n-hexane and chloroform were found to be 0.674 μg/ml, 0.719 μg/ml, 0.984 μg/ml, 2.157μg/ml and 1.514 μg/ml respectively. N-hexane and chloroform extract showed least activity in all the measures. The results suggest that Asparagus racemosus is a valuable source of antioxidant and has significant cytotoxic activity hence could eliminate many diseases related to free radical.
ABSTRACT
The purpose of this study was to judge the antioxidant activity and brine shrimp lethality bioassay followed by phytochemical screening of five different extracts of Moringa oleifera leaves. Preliminary Phytochemical screening of the crude extracts of Moringa oleifera leaf revealed the presence of different kind of chemical groups such as Flavonoids, tannin, Saponin, alkaloids, glycosides, carbohydrate and Triterpenoids. The leaf exhibited significant DPPH free radical scavenging activity with highest IC50 value showed by chloroform extract with a value of 47.481 μg/ml followed by ethanol and methanol having value of 62.09 and 68.321 respectively as opposed to that of the scavenging effects of ascorbic acid and BHT of 5.698 and 8.816 respectively. Dried leaf of Moringa oleifera were subjected to brine shrimp lethality bioassay and the LC50 values of methanol, ethanol, petroleum ether, n-hexane and chloroform were found to be 0.747μg/ml, 0.712 μg/ml, 1.632 μg/ml, 2.163 μg/ml and 0.633 μg/ml respectively. The data obtained in the present study suggests that the extracts of Moringa oleifera leaves have potent antioxidant activity against free radicals and significant cytotoxic activity that can be used in disease prevention.