The whole plant of bhringaraj (Eclipta alba) was dried and pulverized. The phytoconstituents of the pulverized plant material were extracted separately with two different solvents namely petroleum ether (hot percolation) and methanol (cold maceration) to carry out a comparative extraction efficiency of the above two solvents. β-sitosterol reported to have antiandrogenic, anticancer, antiinflammatory, antiprostatitic, antitumor, etc. activity, was selected as the active biomarker for quantification of the aforementioned plant material.HPTLC was carried out for quantification of the biomarker and obtained data was compared with HPLC data. Petroleum ether was found to be an effective extracting solvent for β sitosterol from E. alba as compared to methanol. The percentage content of β-sitosterol in E. alba methanolic and petroleum ether extract was found to be 0.10% and 4.65% w/w respectively by HPTLC whereas the percentage content of β-sitosterol in Eclipta alba petroleum ether extract was found to be 4.67 % w/w by HPLC. AAS data revealed the presence of the metals (ppm ± SEM) are within safety limits, copper (1.151 ± 0.031), chromium (0.528 ± 0.012), cadmium (0.021 ± 0.035), lead (0.860 ± 0.009), arsenic (0.081 ± 0.007), mercury (0.036 ± 0.010).

Objective: The present study was aimed to develop topical gel containing β-sitosterol using carbopol 940 as a gelling agent and to investigate 5 alpha reductase (5α-reductase) inhibitory activity of suitable gel formulation and compare it with a commercial product used topically for alopecia. Methods: Three different batches of β-sitosterol hair gel formulation were manufactured and evaluated. Additionally, the 5α-reductase inhibitory activity of the prepared formulation, finasteride as a positive control, was evaluated and compared to the commercial herbal formulation used. Results: According to the analytical findings of three different batches, the gel formulation is good in appearance, homogeneous, and easily spreadable. Based on findings from HPLC and HPTLC, the amount of β-sitosterol in those formulations complies with the label claim. By checking different critical parameters of those batches, we established the manufacturing process method validation and the process reproducibility. In vitro results showed the good 5α-reductase inhibitory potential of prepared gel formulation and then commercial product. The IC50 value of the prepared formulation was 118.960±0.634 (µg/ml) and standard beta-sitosterol 88.854±0.70 (µg/ml), whereas Finasteride (positive control) 224.372±3.103 (ng/ml). Conclusion: Thus, β-sitosterol formulation utilises a straightforward, low-cost production, less time-consuming process with minimal facility and equipment requirements. The formulation may be a promising candidate for future investigation into their antiandrogenic activities.

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Modern drug discovery has led to the development of drug molecules that exhibit high lipophilicity and poor water solubility, which leads to problematic bioavailability. Approaches have thus been made to enhance dissolution of poorly water soluble drugs through modifications and creation of specific formulations. Metaclopramide is an antiemetic and gastroprokinetic agent, commonly used to treat nausea and vomiting. It is absorbed well after oral administration but a significant first pass effect in some human patients may reduce systemic bioavailability to 30%.The Metaclopramide base is thus modified from Metaclopramide hydrochloride to enhance solubility .This has been achieved by the formulating in solid dispersion since Metaclopramide is poorly water soluble. Though it is absorbed well after oral administration, a significant first pass effect in some patients reduces systemic bioavailability, which can cause adverse side effects. This solid dispersion has then been used through transdermal drug delivery. Enhancement of solubility of poorly water soluble drug by solid dispersion may be attributed to particles modified characters such as particle size reduction, improved wettability, higher porosity, decreased lattice energy, amorphous state. The main objective thus includes modification of drug Metaclopramide  hydrochloride to Metaclopramide base, preparation of solid dispersion of modified Metaclopramide  base drug which has poor water solubility, experimental analysis of Metaclopramide base drug and solid dispersion products with carriers. Keywords: solubility, Metaclopramide, solid dispersion, carriers, HPβCD, PVP K-30

Aims & Objectives: The present work deals with the modification of controlled release dosage form of poorly water soluble drug (Metoclopramide hydrochloride) in order to improve the bioavailability and to control drug release for a longer period of time by the aid of solid dispersion. Methods: Various binary combination of MET-solid dispersion was prepared with different carriers such as HPβCD, PVP K30 and PLX-188 by solvent evaporation technique and then the aqueous solubility, dissolution study and phase solubility study was performed. DSC analysis is performed to carry out for metoclopramide loaded solid dispersion, physical mixture & also for pure drug to analyze the crystalline and amorphous nature of compounds. Results and Discussion:  The saturation solubility of Metoclopramide with various carriers at different pH was performed and found that in pH 5.5 (solubility is 5553.2µg/ml), pH 6.8 (3363.3µ/ml), pH 7.4 (1367.3µg/ml) at 37oC. In dissolution study of solid dispersion (5:1) of different carriers in DDW, the Cumulative % dissolution is found in the order of PVP K30>PLX-Met>HPβCD-Met & in pH 7.4, in the order of PLX-Met>PVP K30>HPβCD-Met. DSC thermogram of Metoclopramide base showed a sharp endothermic peak at its melting point (147oC) which exhibits in crystalline form complying with that of Metoclopramide hydrochloride form, melting point was found to be 850C.  In the ex-vivo study of several transdermal patches, patch C [SD of MET: HPβCD (1:5)] showed the controlled release and permeation of drug. Conclusion: Poor solubility of new chemical entities being a well known problem for past few decades despite the imbalance between significant research efforts & few successful marketed formulations, the solid dispersion proves to hold a key position among all the various formulation strategies to enhance the aqueous solubility & dissolution rate and thereby the bioavailability of  poorly aqueous solubility of drug. Keywords: Bioavailability,DSC, Metoclopramide hydrochloride, solid dispersion, HPβCD,