FORMULATION AND EVALUATION OF FLOATING TABLET OF ECLIPTA ALBA EXTRACT FOR HEPATIC DISORDERS

Objective: The aim of the present study was to design and estimate gastro retentive floating tablet of Eclipta alba extract to increase the efficacy by extending the release of extract. Eclipta alba is reported to be useful in liver ailments and has been shown to possess hepatoprotective activity.Methods: The floating tablet extract of Eclipta alba was prepared by using kollidon SR as floating and release retarding polymer. The effect of various additive excipient was also studied and optimized using 32full factorial design to alter the floating behaviour and extract release from the floating tablet.Results: The polymeric structure of Kollidon® SR possesses appreciable porosity during the compression process. Results of multiple regression analysis show that the amount of stearic acid and lactose has significant influence on Q2, Q6 and Q10.Conclusions: From the desirability function, the levels of the optimized batch were selected as -1 for the X1 and 1 for the X2 which correspond to batch F3 of factorial design. This study can open the avenues for the In-vitro dissolution testing of herbal extracts by simple UV method for the determination of extract release in extended release formulations.Â

Anti-arthritic activity of a classical Ayurvedic formulation Vatari Guggulu in rats

In India, Vatari Guggulu has been traditionally used in the Ayurvedic system of medicine to treat rheumatoid arthritis (RA). The current study was undertaken to evaluate anti-arthritic activity of alcoholic extract of Vatari Guggulu in rats. Arthritis was induced by administration of formaldehyde (2%v/v) or Complete Freund's Adjuvant (CFA) into the sub-plantar surface of left hind paw of the animals. The extract was administered to the rats by oral gavages in different doses. Joint swelling was measured in formaldehyde induced arthritis. Various physical, biochemical and histopathological parameters were determined in CFA induced arthritis. Vatari Guggulu extract (VGE) produced significant (P < 0.05) inhibition of joint swelling in both formaldehyde and CFA induced arthritis. The treatment also brought to normalcy the increased white blood cell (WBC) count, rheumatoid factor (RF), erythrocyte sedimentation rate (ESR), cholesterol, triglycerides and LDL with an enhancement of haemoglobin (Hb) levels and red blood cell (RBC) count. These effects were found to be dose dependent. These effects were comparable with standard drug indomethacin. Histo-pathological studies of the ankles of VGE treated animals exhibited significant improvements. VGE did not show any toxic symptoms even at a dose of 2000 mg/kg in acute toxicity studies on rats. Thus, Vatari Guggulu, a classical Ayurvedic formulation of the Indian System of Medicine, exhibited significant anti-arthritic activity in formaldehyde and CFA induced arthritis in rats. This study corroborates the claims of Ayurveda on Vatari Guggulu

Anti-anaphylactic and antiasthmatic activity of Euphorbia thymifolia L. on experimental animals

In Ayurveda, Euphorbia thymifolia L. (Euphorbiaceae) prescribed in the treatment of various ailments like bronchial asthma, cough, diarrhea and bleeding piles. The present study was investigated to evaluate antianaphylactic, mast cell stabilizing and antiasthmatic activity of methanol and aqueous extract of E. thymifolia (ET) on experimental animals. Anaphylaxis was induced by administration of horse serum and triple antigen vaccine intraperitoneal (i.p.) in albino Wistar rats. Extracts of ET were administered to the rats in dose of 250 and 500 mg/kg orally for 14 days. At the end of treatment, asthma score was measured and various blood parameters like differential count (DC), total WBC count and IgE were estimated. Interleukin (IL)-4, IL-5 and TNF-α were measured by ELISA commercial kit from BALF. Histopathological changes of lungs were observed. Antiasthmatic activity of extracts of ET was also studied on histamine-induced bronchospasm in guinea pigs. In vitro mast cell stabilizing activity of extracts was evaluated on compound 48/80 challenged rat intestinal mesenteric mast cells. The treatment with extracts of ET produced significant decrease in asthma score and they also brought to normalcy the increased total WBC, DC counts, serum IgE, TNF-α, IL-4 and IL-5 in BALF. The histopathological study further supported the protective effect of ET extracts. The pretreatment with extracts of ET displayed significant reduction in degranulation of mesenteric mast cell numbers. The treatment with extracts of ET significantly increased in time of PCD. Thus, these findings concluded that E. thymifolia could be effectively used in the treatment of anaphylaxis and asthma. Keywords: Euphorbia thymifolia, IgE, TNF-α, IL-4 and IL-

Direct and enhanced delivery of nanoliposomes of anti schizophrenic agent to the brain through nasal route

The problem of inadequate oral bioavailability of Quetiapine Fumarate, a lipophilic drug used for schizophrenia, due to hepatic metabolism and repulsion by brain barrier was attempted in this study. Combination of two approaches, viz. Quetiapine inclusion into the liposomal carrier for better diffusion and administration through nasal route to avoid hepatic metabolism and barrier elimination was applied. Thin film hydration followed by sonication method was employed in liposome preparation and the formulation was optimized using 32 full factorial design. The number of sonication cycles (X1) of 2 min and 80% amplitude and molar ratio of constructional components such as cholesterol to egg phosphatidylcholine (X2) as independent variables and a % of entrapment efficiency (Y1) and cumulative in vitro drug release (Y2) at 6 h as dependent variables was selected. Batch F7 prepared by 2 cycles of sonication and 1:3 M ratio of cholesterol:egg phosphatidylcholine was optimized as a consequence of substantial entrapment efficiency of 75.63 ± 3.77%, and 99.92 ± 1.88% drug release and 32.33 ± 1.53% drug diffusion, which was optimum among all other batches at 6 h. Diffusion study was done for all the batches of liposomal formulation by using sheep nasal mucosa and good amount with better diffusion rate was measured which proved liposomal dispersion a virtuous delivery system for brain drug delivery through nasal route. Results of in vivo, ciliotoxicity and gamma scintigraphy studies on mice supported the above inference

Amelioration of anaphylaxis, mast cell degranulation and bronchospasm by Euphorbia hirta L. extracts in experimental animals

The current investigation was aimed to assess anti-anaphylactic, mast cell stabilizing and anti-asthmatic activity of methanol and aqueous extract of Euphorbia hirta L. (Euphorbiaceae) on experimental animals. Anaphylaxis was induced by administration of horse serum and triple antigen vaccine subcutaneously in albino Wistar rats. Extracts of E. hirta (EH) were administered to the rats in dose of 250 and 500 mg/kg b.w. orally for 14 days. At the end of treatment, asthma score was measured and various blood parameters like differential count (DC), total WBC count and IgE were estimated. Interleukin (IL)-4, IL-5 and tumour necrosis factor (TNF)-α were measured by ELISA commercial kit from Broncho alveolar lavage fluid (BALF). Histopathological changes of lungs were observed. Anti-asthmatic activity of extracts of EH was also studied on histamine-induced bronchospasm in guinea pigs. In vitro mast cell stabilizing activity of extracts was evaluated on compound 48/80 challenged rat intestinal mesenteric mast cells. The treatment with extracts of EH produced significant decrease in asthma score and they also brought to normalcy the increased total WBC, DC counts, serum IgE, TNF-α, IL-4 and IL-5 in BALF. The histopathological study further supported the protective effect of EH extracts. The pre-treatment with extracts of EH displayed significant reduction in degranulation of mesenteric mast cell numbers. The treatment with extracts of EH significantly increased in time of pre-convulsive dyspnoea (PCD). Thus, these findings concluded that E. hirta could be effectively used in the treatment of anaphylaxis and asthma

Studies in formulation and pharmacotechnical evaluation of controlled release transdermal delivery system of bupropion

The objective of the present study was to design and evaluate unilaminate transdermal adhesive matrix systems capable of diffusing bupropion base at a constant rate over an extended period of time as an alternative route of administration. Unilaminate transdermal adhesive matrices have been fabricated with different concentrations of Eudragit E as the adhesive and rate-controlling polymer. The in vitro release and epidermal flux through human cadaver skin were studied. The release of drug from the matrices obeyed zero order release kinetics (r2=0.9810 to 0.9960). The delivery rate of bupropion ranged from 10.5 mg to 31.4 mg per day from a 3.14 cm2 area of matrix. The relation between concentration of bupropion base in matrix and epidermal flux, concentration of drug in matrix, and epidermal adsorption of bupropion during diffusion follow hyperbolic fashion. Triethylcitrate (TEC) and dibutylphthalate (DBP) have no influence on the diffusion of bupropion through human cadaver skin when used as plasticizers. Incorporation of succinic acid in the adhesive matrix retarded diffusion due to the formation of rigid cross linking of the polymer, while propylene glycol and myristic acid, alone or in combination, significantly enhanced the flux of bupropion through human cadaver skin