Quantitative Microscopy: Particle Size/Shape Characterization, Addressing Common Errors Using 'Analytics Continuum' Approach.

Particle size/shape characterization of active pharmaceutical ingredient (API) is integral to successful product development. It is more of a correlative property than a decision-making measure. Though microscopy is the only technique that provides a direct measure of particle properties, it is neglected for reasons like non-repeatability and non-reproducibility which is often attributed to a) fundamental error, b) segregation error, c) human error, d) sample randomness, e) sample representativeness etc. Using the "Sucrose" as model sample, we propose "analytics continuum" approach that integrates optical microscope PSD measurements complimented by NIR spectroscopy-based trending analysis as a prescreening tool to demonstrate sample randomness and representativeness. Furthermore, plethora of statistical tests are utilized to infer population statistics. Subsequently, an attribute-based control chart and bootstrap-based confidence interval was developed to monitor product performance. A flowchart to serve as an elementary guideline is developed, which is then extended to handle more complex situations involving API crystallized from two different solvent systems. The results show that the developed methodology can be utilized as a quantitative procedure to assess the suitability of API/excipients from different batches or from alternate vendors and can significantly help in understanding the differences between material even on a minor scale.

HPTLC analysis and in-vitro antioxidant, anti-inflammatory and anti-diabetic activities of ethanol extract of leaves of Actinodaphne madraspatana Bedd.

The aim of the present study was to develop the HPTLC fingerprint and to evaluate the in-vitro antioxidant, anti-inflammatory and anti-diabetic activities of ethanol extract of leaves of Actinodaphne madraspatana Bedd (A. madraspatana). HPTLC fingerprint analysis of ethanol extract was investigated by win CATS planar chromatography. The antioxidant activity was evaluated by the various antioxidant assays, such as total antioxidant, reducing power, DPPH radical scavenging, hydrogen peroxide scavenging and hydroxyl radical scavenging. The antioxidant activity was compared to standard drug ascorbic acid. In-vitro anti-inflammatory activity was evaluated by inhibition of albumin denaturation assay using aspirin as a standard drug. In-vitro anti-diabetic activity was evaluated by α-amylase inhibition assay using acarbose as a standard drug. The HPTLC fingerprint of ethanol extract has shown six peaks, which indicate the presence of six different phytocomponents. The in-vitro antioxidant, anti-inflammatory and anti-diabetic activities of ethanol extract of plant leaves increased with the increasing of concentration. The result revealed that extract in all the concentration showed the in-vitro antioxidant, anti-inflammatory and anti-diabetic activities compared to standard drugs. The ethanol extract of leaves of A. madraspatana has a potential effect as an antioxidant, anti-inflammatory and anti-diabetic in all the tested in-vitro methods.

An update on prodrugs from natural products.

A natural prodrug is a chemical compound or substance obtained from plants, microorganism, animal and marine sources. Natural products are small molecule source for Food and Drug Administration approved drugs and major sources for drug discovery. Most of the drugs for different ailment diseases undergo first pass metabolism, resulting in drug inactivation and the generation of toxic metabolites in body. Enormous numbers of prodrugs naturally present in plants, microorganism, animal and marine sources and those prodrugs undergoes chemical reaction to form non-toxic compounds. This review summarizes the list of prodrugs naturally present in the natural product.