Multicomponent Amorphous Solid Forms of Telmisartan: Insights into Mechanochemical Activation and Physicochemical Attributes.

The present work aims to explore the new solid forms of telmisartan (TEL) with alpha-ketoglutaric acid (KGA) and glutamic acid (GA) as potential coformers using mechanochemical approach and their role in augmentation in physicochemical parameters over pure crystalline TEL. Mechanochemical synthesis was performed using 1:1 stoichiometric ratio of TEL and the selected coformers in the presence of catalytic amount of ethanol for 1 h. The ground product was characterized by PXRD, DSC, and FTIR.

Anti-glycating and anti-cytotoxic effect of silibinin on albumin at early glycation: A physiochemical study.

During persistent hyperglycaemia, albumin, one of the major blood proteins, can undergo fast glycation. It can be expected that timely inhibition of protein glycation might be add quality years to diabetic patients' life. Therefore, this study was designed to analyse the role of silibinin to reduced or delay amadori adduct formation at early glycation and its beneficial effect to improve the glycated albumin structure and conformation.

Liquid chromatographic methods for the analysis of canagliflozin: concise overview and greener assessment.

There is a pressing need for the development of greener liquid chromatographic bioanalytical methods for antidiabetic drugs for plasma monitoring and revisiting patients' dosage regimens. Besides, analytical methods are also needed for the quality assurance of finished drug products and regulatory approval. Therefore, the present review focuses on the reported liquid chromatographic methods (LC and LC-MS/MS) that are applied for quality control, forced degradation, and pharmacokinetic studies of a newer antidiabetic agent, canagliflozin (CNG).

Mitigating Drug Stability Challenges Through Cocrystallization.

Drug stability plays a significant role in the pharmaceutical industry from early-phase drug discovery to product registration as well as the entire life cycle of a product. Various formulation approaches have been employed to overcome drug stability issues. These approaches are sometimes time-consuming which ultimately affect the timeline of the product launch and may further require formulation optimization steps, affecting the overall cost.

Preparation, Characterization, and Evaluation of Curcumin-Graphene Oxide Complex-Loaded Liposomes against in Topical Disease.

This study describes the development and characterization of curcumin with graphene oxide complex (CUR + GO) loaded into liposomes for treating skin disease. The developed complex was characterized by X-ray diffraction and showed a broad halo pattern, confirming the amorphous nature of the resulting complex. Furthermore, scanning electron microscopy revealed the irregular porous morphology of the complex-highlighting loss of the crystallinity and the emergence of the amorphous phase.

Investigation of a Minocycline-Loaded Nanoemulgel for the Treatment of Acne Rosacea.

In the present investigation, a nanoemulgel of minocycline was formulated and optimized for an improved drug delivery and longer retention time in the targeted area. Combining eucalyptus oil, Tween 20, and Transcutol HP, different o/w nanoemulsions were formulated by the oil phase titration method and optimized by pseudo-ternary phase diagrams. The morphology, droplet size, viscosity, and refractive index of the thermodynamically stable nanoemulsion were determined.

Emerging Multi-Drug Eutectics: Opportunities and Challenges.

Complexity and heterogeneous nature of most diseases have posed greater challenges in the modern healthcare system. Fixed-dose combination can offer an ideal way to improve patient compliance and higher therapeutic efficacy. However, biopharmaceutical issues associated with the drug combinations remain unaddressed.

Development of L-Lysine Amino Acid-Based Co-Crystal of Telmisartan Using Crystal Engineering Approach to Improve Solubility, Dissolution, and Micrometric Properties.

Aim: To develop a co-crytsal of Telmisartan for enhancing its solubility in water.

Background: Intermolecular interaction happens in crystal packing; it utilizes and helps to understand the design of new solid with their respective chemical and physical properties called crystal engineering. It is a blueprint of molecular solids with specific chemical and physical properties through an understanding and handling of intermolecular interaction for increasing the solubility, in case of poor water-soluble drugs.

Implication of Coformer Structural Diversity on Cocrystallization Outcomes of Telmisartan with Improved Biopharmaceutical Performance.

Crystal engineering approach was utilized for the development of different multicomponent solid forms of telmisartan (TEL) to improve its oral bioavailability. In this context, two cocrystals, gentisic acid (GA) and maleic acid (MA), while two eutectic mixtures, para-aminobenzoic acid (PABA) and adipic acid (AA), were successfully prepared and characterized by different analytical tools. Both the cocrystals exhibited characteristic heterosynthons, viz.

Implication of Differential Surface Anisotropy on Biopharmaceutical Performance of Polymorphic Forms of Ambrisentan.

The aim of the present study was to compare the dissolution rate and in vivo biopharmaceutical performance of 2 polymorphic forms (form I and II) of ambrisentan and correlate with their surface molecular environment. Dominance of various functionalities on the surface of specific crystal facets of both forms was predicted by Bravais-Friedel-Donnay-Harker method. Hirshfeld surface analysis maps and 2D fingerprint plots indicate a difference in shape index, curvedness, and relative percentage contribution of various contacts in both forms.

Novel polymorph of ambrisentan: Characterization and stability.

The present work highlights a novel polymorph (form II) of ambrisentan (AMT), a selective endothelin type A (ETA) receptor antagonist used in the treatment of pulmonary arterial hypertension (PAH). Form II was isolated by solution crystallization and characterised by differential scanning calorimetry, powder X-ray diffraction, solution calorimetry and aqueous solubility. The single crystal X-ray diffraction shows that it crystallizes in monoclinic system with space group P21/c different from the form I (commercial form).

Antioxidant-Based Eutectics of Irbesartan: Viable Multicomponent Forms for the Management of Hypertension.

The present research work highlights the development of multicomponent solid form of the antihypertensive drug irbesartan (IRB) to improve its biopharmaceutical attributes. Mechanochemical synthesis of a new solid form of IRB with coformers having antioxidant properties (syringic acid, nicotinic acid, and ascorbic acid) resulted into three eutectic mixtures (EMs). Formation of eutectic was ascertained by differential scanning calorimetry whereas exact stoichiometry (50/50% w/w) was established by phase diagram and Tamman's triangle.

Multicomponent solid forms of felodipine: preparation, characterisation, physicochemical and in-vivo studies.

Objectives: This study aimed to improve biopharmaceutical parameters of the poorly soluble antihypertensive drug, felodipine, by preparing multicomponent solid forms using three coformers, viz. imidazole, nicotinamide and malonic acid.

Methods: The multicomponent solid forms were prepared by mechanochemical synthesis and characterised by various analytical techniques.

Drug-Drug Multicomponent Solid Forms: Cocrystal, Coamorphous and Eutectic of Three Poorly Soluble Antihypertensive Drugs Using Mechanochemical Approach.

The present study deals with the application of mechanochemical approach for the preparation of drug-drug multicomponent solid forms of three poorly soluble antihypertensive drugs (telmisartan, irbesartan and hydrochlorothiazide) using atenolol as a coformer. The resultant solid forms comprise of cocrystal (telmisartan-atenolol), coamorphous (irbesartan-atenolol) and eutectic (hydrochlorothiazide-atenolol). The study emphasizes that solid-state transformation of drug molecules into new forms is a result of the change in structural patterns, diminishing of dimers and creating new facile hydrogen bonding network based on structural resemblance.

Application of LC-MS/MS for quantitative analysis of glucocorticoids and stimulants in biological fluids.

Liquid chromatography tandem mass chromatography (LC-MS/MS) is an important hyphenated technique for quantitative analysis of drugs in biological fluids. Because of high sensitivity and selectivity, LC-MS/MS has been used for pharmacokinetic studies, metabolites identification in the plasma and urine. This manuscript gives comprehensive analytical review, focusing on chromatographic separation approaches (column packing materials, column length and mobile phase) as well as different acquisition modes (SIM, MRM) for quantitative analysis of glucocorticoids and stimulants.

Analytical methods for the detection of undeclared synthetic drugs in traditional herbal medicines as adulterants.

Traditional herbal medicines (THMs) are gaining popularity worldwide as an alternative approach to prescription drugs for many reasons including a general perception that they are safe. But recently there have been number of reported studies that reveal adulteration of THMs with undeclared synthetic drugs, which may potentially cause serious toxic adverse effects. This paper reviews the various classes of synthetic drugs that were found to be adulterated in THMs worldwide.