Altitudinal variation of berberine, total phenolics and flavonoid content in Thalictrum foliolosum and their correlation with antimicrobial and antioxidant activities.

BACKGROUND: The quality of herbal medicine is determined by its secondary metabolites, which may vary according to growth, season and altitude etc. OBJECTIVE: We studied the variation in phytochemistry and biological activities of Thalictrum foliolosum (TF) roots collected from four sites at different altitudes. MATERIAL AND METHODS: The berberine content in different extracts of T. foliolosum roots collected from various altitudes was estimated using HPTLC. Total phenolic and flavonoid contents were determined using Folin-Ciocalteau reagent and aluminum chloride method respectively. The sensitivity of microbes for the extracts was studied using disc diffusion and the MIC was estimated using broth dilution method. Antioxidant capacity of the plant was studied using ß-carotene bleaching assay, lipid peroxidation assay using goat liver, reducing power assay and DPPH free radical scavenging activity. RESULTS: Berberine content varied inversely with altitude; while phenol and flavonoid content of TF increased at higher altitudes. All the TF extracts showed moderate to high activity against Candida albicans, Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa. Extracts with high berberine content were most effective against C. albicans and S. aureus and also showed relatively significant anti-lipid peroxidation, ß-carotene bleaching and reducing power. TF extracts with higher phenol and flavonoid content showed better scavenging of DPPH free radicals. Berberine was used as a standard in all the antioxidant and antimicrobial experiments performed. CONCLUSION: Thalictrum from lower elevations can be explored as an alternate source of berberine and the plant has high antioxidant and antimicrobial properties owing to its berberine content.

Controlled release effervescent buccal discs of buspirone hydrochloride: in vitro and in vivo evaluation studies.

In the present study controlled release effervescent buccal discs of buspirone hydrochloride (BS) were designed using HPMC as rate controlling and bioadhesive polymer by direct compression method. Sodium bicarbonate and citric acid were used in varying amounts as effervescence forming agents. Carbon dioxide evolved due to reaction of sodium bicarbonate and citric acid was explored for its potential as buccal permeation enhancer. The designed buccal discs were evaluated for physical characteristics and in vitro drug release studies. Bioadhesive behavior of designed buccal discs was assessed using texture analyzer. In vivo animal studies were performed in rabbits to study bioavailability of BS in the designed buccal discs and to establish permeation enhancement ability of carbon dioxide. It was observed that effervescent buccal discs have faster drug release compared to non-effervescent buccal discs in vitro and effervescent buccal discs demonstrated significant increase in bioavailability of drug when compared to non-effervescent formulation. Hence, effervescent buccal discs can be used as an alternative to improve the drug permeation resulting in better bioavailability. However, the amount of acid and base used for generation of carbon dioxide should be selected with care as this may damage the integrity of bioadhesive dosage form.

Effect of HPMC and mannitol on drug release and bioadhesion behavior of buccal discs of buspirone hydrochloride: In-vitro and in-vivo pharmacokinetic studies.

Delivery of orally compromised therapeutic drug molecules to the systemic circulation via buccal route has gained a significant interest in recent past. Bioadhesive polymers play a major role in designing such buccal dosage forms, as they help in adhesion of designed delivery system to mucosal membrane and also prolong release of drug from delivery system. In the present study, HPMC (release retarding polymer) and mannitol (diluent and pore former) were used to prepare bioadhesive and controlled release buccal discs of buspirone hydrochloride (BS) by direct compression method. Compatibility of BS with various excipients used during the study was assessed using DSC and FTIR techniques. Effect of mannitol and HPMC on drug release and bioadhesive strength was studied using a 3(2) factorial design. The drug release rate from delivery system decreased with increasing levels of HPMC in formulations. However, bioadhesive strength of formulations increased with increasing proportion of HPMC in buccal discs. Increased levels of mannitol resulted in faster rate of drug release and rapid in vitro uptake of water due to the formation of channels in the matrix. Pharmacokinetic studies of designed bioadhesive buccal discs in rabbits demonstrated a 10-fold increase in bioavailability in comparison with oral bioavailability of buspirone reported.

Determination of pK(a) of felodipine using UV-Visible spectroscopy.

In the present study, for the first time, experimental pKa value of felodipine is reported. Dissociation constant, pKa, is one of the very important physicochemical properties of drugs. It is of paramount significance from the perspective of pharmaceutical analysis and dosage form design. The method used for the pKa determination of felodipine was essentially a UV-Visible spectrophotometric method. The spectrophotometric method for the pKa determination was opted by acknowledging the established fact that spectrophotometric determination of pKa produces most precise values. The pKa of felodipine was found to be 5.07. Furthermore, the ruggedness of the determined value is also validated in this study in order to produce exact pKa of the felodipine.

Interaction of calcium sulfate with xanthan gum: effect on in vitro bioadhesion and drug release behavior from xanthan gum based buccal discs of buspirone.

Bioadhesive polymers in buccal drug delivery systems play an important role in delivery of therapeutic drug molecules for local and systemic action. Xanthan gum, a GRAS listed natural polymer was used to design buccal discs of buspirone hydrochloride by direct compression method. Effect of calcium sulfate on bioadhesive and drug release behavior of xanthan gum buccal discs was studied. Varying amount of calcium sulfate (0%, 5%, 10%, 20%, 30%, 40% and 50%, w/w) in combination with xanthan gum was used to prepare buccal bioadhesive discs. Increase in calcium sulfate concentration resulted in faster drug release and decreased the bioadhesive strength of the designed discs. Further, in rheological evaluation it was observed that viscosity of xanthan gum gel reduces with increasing concentration of calcium sulfate. Compatibility of drug with various excipients was assessed using DSC and FTIR techniques.

Indian traditional ayurvedic system of medicine and nutritional supplementation.

Food is the major source for serving the nutritional needs, but with growing modernization some traditional ways are being given up. Affluence of working population with changing lifestyles and reducing affordability of sick care, in terms of time and money involved, are some of the forces that are presently driving people towards thinking about their wellness. There has been increased global interest in traditional medicine. Efforts to monitor and regulate traditional herbal medicine are underway. Ayurveda, the traditional Indian medicine, remains the most ancient yet living traditions. Although India has been successful in promoting its therapies with more research and science-based approach, it still needs more extensive research and evidence base. Increased side effects, lack of curative treatment for several chronic diseases, high cost of new drugs, microbial resistance and emerging, diseases are some reasons for renewed public interest in complementary and alternative medicines. Numerous nutraceutical combinations have entered the international market through exploration of ethnopharmacological claims made by different traditional practices. This review gives an overview of the Ayurvedic system of medicine and its role in translational medicine in order to overcome malnutrition and related disorders.

Tractor controls actuating force limits for Indian operators.

In four-wheel tractors, proper design of controls is important for comfortable and safe operation of the tractor. The design involves location and dimensions of controls as well as strength limits for operating these controls. The present study was aimed to quantify human strength for operation of tractor controls and to recommend the maximum control actuating forces for normal operation of tractors based on strength capability of 3,423 Indian male agricultural workers. The 5th percentile values of strength parameters i.e. leg strength sitting (left and right), foot strength sitting (right), torque strength (both hands) sitting, push strength (left hand and right hand) sitting and pull strength (left hand and right hand) sitting of agricultural workers collected using a strength measurement set-up were taken into consideration for the study. It was recommended that the maximum actuating forces for normal operation of frequently operated brake and clutch pedals of tractors should not exceed 260 N and 125 N based on 5th percentile values of right and left leg strength of male agricultural workers, respectively. The maximum actuating force required in steering wheel operation should not exceed 51 N based on 5th percentile value of torque strength (both hands) sitting of workers. The maximum actuating forces required for operating frequently operated levers viz. gear selection, speed selection, hydraulic control and hand throttle of Indian tractors should not exceed 46 N, 46 N, 25 N and 25 N, respectively. It may be concluded that the maximum actuating force limits as given in Bureau of Indian Standards IS 10703 are very high as compared to the findings of the study based on strength data of Indian male operators, which highlight the need to revise the standard.