Biopharmaceutical classification system (BCS) is an advanced tool used for classifying medicines based on dissolution, water solubility, and intestinal permeability, which affect the absorption of active pharmaceutical ingredients (API) from immediate-release solid oral forms. It is useful to the formulation researchers to develop novel dosage forms based on modernistic rather than experimental approaches. The current review focuses on the fundamentals, objectives, guidance of BCS, characteristics of BCS drugs, their importance and applications of BCS. This review explains the challenges in drug development in terms of solubility and in vivo disposition. In the current review, new strategies for improving BCS II drug solubility as well as biopharmaceutical drug disposition properties which are utilized throughout the early stages of drug development and commercialization are mainly discussed.

In this study, a novel series of pyridine-based thiadiazole derivatives (NTD1-NTD5) were synthesized as prospective anti-inflammatory agents by combining substituted carboxylic acid derivatives of 5-substituted-2-amino-1,3,4-thiadiazole with nicotinoyl isothiocyanate in the presence of acetone. The newly synthesized compounds were characterized by FTIR, ¹H NMR, ¹³C NMR, and mass spectrometry. First, the compounds underwent rigorous in vivo testing for acute toxicity and anti-inflammatory activity and the results revealed that three compounds-NTD1, NTD2, and NTD3, displayed no acute toxicity and significant anti-inflammatory activity, surpassing the efficacy of the standard drug, diclofenac. Notably, NTD3, which featured benzoic acid substitution, emerged as the most potent anti-inflammatory agent among the screened compounds. To further validate these findings, an in silico docking study was carried out against COX-2 bound to diclofenac (PDB ID: 1pxx). The computational analysis demonstrated that NTD2, and NTD3, exhibited substantial binding affinity, with the lowest binding energies (−8.5 and −8.4, kcal/mol) compared to diclofenac (−8.4 kcal/mol). This alignment between in vivo and in silico data supported the robust anti-inflammatory potential of these derivatives. Moreover, molecular dynamics simulations were conducted, extending over 100 ns, to examine the dynamic interactions between the ligands and the target protein. The results solidified NTD3's position as a leading candidate, showing potent inhibitory activity through strong and sustained interactions, including stable hydrogen bond formations. This was further confirmed by RMSD values of 2-2.5 Å and 2-3Ǻ, reinforcing NTD3's potential as a useful anti-inflammatory agent. The drug likeness analysis of NTD3 through SwissADME indicated that most of the predicted parameters including Lipinski rule were within acceptable limits. While these findings are promising, further research is necessary to elucidate the precise relationships between the chemical structures and their activity, as well as to understand the mechanisms underlying their pharmacological effects. This study lays the foundation for the development of novel anti-inflammatory therapeutics, potentially offering improved efficacy and safety profiles.

A simple, validated RP-HPLC method for the simultaneous estimation of Paracetamol and Flupirtine maleate in pharmaceutical dosage form was developed and validated. This method was developed by selecting Inertsil, C18, (250 x 4.6mm, 5μ) column as stationary phase and Methanol: O-Phosporic acid (85: 15 v/v) as mobile phase. Flow rate of mobile phase was maintained at 1 ml/min at ambient temperature throughout the experiment. Quantification was achieved with ultraviolet (DAD) detection at 239 nm. The retention times of Paracetamol and Flupirtine maleate were found as 2.78 min and 3.47 min respectively. The detector response was linear in the concentration range of 65–190 μg/ml and 20–60 μg/ml for Paracetamol and Flupirtine maleate respectively, and the regression coefficients found as 0.998 and 0.999 for Paracetamol and Flupirtine maleate respectively. From recovery studies we concluded that the recovery of Paracetamol and Flupirtine maleate has no interference with any excepients in the formulation. This method has been validated according to ICH guidelines and shown to be Specific, Sensitive, Precise, Accurate, Rugged and Robust. Hence, this method can be applied for routine quality control of Paracetamol and Flupirtine maleate in dosage forms as well as in bulk drug.

Analytical methods are required to characterize drug substance and drug product composition during all phases of pharmaceutical development. Early phase methods must support changes in synthetic routes and dosage form and elucidate the structures and levels of impurities. In later phases, goals change to the development of rapid and robust methods for release and stability evaluation. Hence we attempt to develop a simple accurate RP-HPLC method for the simultaneous estimation of Simvastatin a hypo-lipidemic drug and Sitagliptin an oral antihyperglycemic drug in pharmaceutical formulations. The quantification was carried out on Prontosil ODS C18 Column (250 x 4.6 mm and 5μm) in isocratic mode, with mobile phase consisting of Methanol: Water: Acetonitile in the ratio of 50:30:20 (v/v/v). The mobile phase was pumped at a rate of 0.80ml/min and the detection was carried out at 261nm and the linearity was found to be in the range of 2 to 12μg/ml for Simvastatin and 5–30μg/ml for Sitagliptin. The regression equation was found to be y = 25876x + 41754 (r²=0.999) for Simvastatin and y = 18801x + 12921 (r² = 0.998) for Sitagliptin. The % recovery values were found to be in the range of 98–102% for both the drugs. LOD and LOQ value was found to be 0.005μg/ml, 0.016μg/ml for Sitagliptin and 0.025μg/ml, 0.08μg/ml for Simvastatin respectively. The proposed method was validated for accuracy and precision. Statistical analysis proves that the method was found to be simple, precise, accurate, rapid and reproducible and can be used for the routine simultaneous determination of Simvastatin and Sitagliptin in bulk drug and in pharmaceutical formulations.

Objective: The objective of this work is to develop a precise, accurate and validated reverse phase ultra-performance liquid chromatographic technique for effective simultaneous determination of Emtricitabine, Tenofovir and Efavirenz in bulk and tablet formulation. Method: Separation of the selected drugs was optimized after several trials including changing mobile phase and its composition, stationary phase, flow rate, column temperature, etc. Finally the separation of drugs was achieved on BEH C18 column using a mixture of methanol and phosphate buffer having pH 3.5 in the ratio of 65:35 v/v as mobile phase with flow rate of 0.3 ml/min and the analytes were detected at a wavelength of 260 nm. Results: The developed method was validated by determining the parameters like linearity, system suitability, recovery, precision, specificity, robustness, ruggedness, LOD, and LOQ as per the International Council for Harmonization of Technical Requirements for Pharmaceuticals for Human Use (ICH) guidelines. The system suitability parameters were within the limits, retention times (Rt) for Emtricitabine, Tenofovir and Efavirenz were found to be 0.432, 0.671, and 2.772 min respectively. The method showed linearity between the concentration range of 10-50 μg/ml for Emtricitabine (r2= 0.9987), 15-75 μg/ml for Tenofovir (r2= 0.9983) and 30-150 μg/ml for Efavirenz (r2= 0.9982). The percentage recovery results at 50%, 100% and 150% of Emtricitabine, Tenofovir and Efavirenz were found to be in the range of 99.45 % - 100.15 %. Since there was no interference due to excipients and mobile phase, the method was found to be specific. The assay results of the combined tablet dosage form by the developed method were identified as in good agreement with the acceptance limit. Conclusions: The current method was proved to be effective for routine simultaneous determination of Emtricitabine, Tenofovir and Efavirenz in bulk and tablet formulation.