In the present study a new co-crystal of Ticagrelor with L-Tartaric acid has been prepared with improved solubility. Ticagrelor is a class VI drug with poor solubility and permeability; hence an attempt has been made to improve its solubility by co-crystallization technology.A co-crystal is a structurally homogeneous crystalline material containing an API and the co-former in definite stoichiometric amounts. In this study the conformer selected was L-Tartaric acid based on ease of hydrogen bond formation. The co-crystal of Ticagrelor with L-Tartaric acid was prepared in different ratios (1:1, 2:1, 1:2). Ticagrelor formed stable co-crystals in the ratios 1:1and2:1. The formation of co-crystal was confirmed by FTIR, DSC and PXRD. The dynamic solubility of co-crystals in the ratios 1:1 and 2:1 was increased by approximately 2.7 and 2.6 fold respectively as compared to pure drug. The in-vitrodissolution study demonstrated a 1.5 fold increase in the solubility for selected TIC:L-TAR (1:1) as compared to its TIC active pharmaceutical ingredient and TIC physical mixture.
Co-crystal synthesis has become a field of high interest in the last decade. This category of solid forms has a variety of applications in industries such as textile, paper and electronics. For many purposes co-crystals will have superior properties in comparison to traditional salt crystals. This review article will focus on the application of co-crystals in pharmaceutical drugs. Co-crystals have opened doors to reintroduce previously poor performing bioactive ingredients in new and improved solid structures. They have also allowed for the introduction of a new range of compounds for pharmaceutical therapy. Most importantly, co-crystals can create new medicines with increased solubility and hence improve the efficiency and safety of the treatment.
Etravirine is a drug used alongside other medication in the treatment of HIV and is a non-nucleoside reverse transcriptase inhibitor. It is a BCS class IV drug, having low solubility and high permeability (Drugbank, https://www.drugbank.ca/drugs/DB06414) [1]. As a result, large doses of the drug are required for treatment. Two pills have to be taken twice a day, making it a “pill burden” (Intelence, http://www.intelence.com/hcp/dosing/administration-options) [2]. Therefore, attempts of co-crystallizing Etravirine are attractive as the solubility of the drug tends to increase in this solid form (Schultheiss and Newman, 2009) [3].In this study Etravirine co-crystals were synthesized in the molar ratios 1:1, 1:2 and 2:1 with L-tartaric acid as the co-former. Both slow evaporation and physical mixture was performed to mix the components. DSC values of final products are presented as well as FTIR spectra to observe the altered intermolecular interactions. A chemical stability test was performed after seven days using area under curve data from an HPLC instrument.
In this present study a new co-crystals of zoledronic acid with DL-tartaric acid and nicotinamide has been developed with improved solubility. Zoledronic acid is a class III drug with poor oral bioavailability due to its poor permeability and low aqueous solubility; hence an attempt has been made to improve its solubility by co-crystallization technology. Pharmaceutical cocrystals are multi-component crystals with a stoichiometric ratio of active pharmaceutical ingredients (APIs) and cocrystal coformers (CCFs) that are assembled by noncovalent interactions such as hydrogen bonds, π-π packing, and Vander Waals forces. In this study the coformers selected were DL-tartaric acid and nicotinamide based on ease of hydrogen bond formation. The co-crystal of zoledronic acid with DL-tartaric acid were prepared in three ratios (1 : 1, 1 : 2 and 2 : 1) by slow solvent evaporation method and with nicotinamide in 1 : 1 ratio by dry grinding method. The formation of co-crystal was confirmed by powder X-ray diffractometry (PXRD), differential scanning calorimetry (DSC) and Fourier transform (FT)IR. The dynamic solubility of co-crystals with DL-tartaric acid in the ratios 1 : 1, 1 : 2 and 2 : 1 increased by fold as compared to pure drug.
Alzheimer's is the typical type of dementia that affects Senior people and is an irrevocable, progressive neurodegenerative disorder. The characteristic symptoms are loss of memory, behavioral disturbances, mood and personality swing, followed by diminished cognitive performance. There is no permanent remedy for AD and the existing drugs in the treatment of disease have minimal effectiveness. Medicinal plants used Ayurveda have been found more productive source for lead development of drugs, and many advanced herbal products are being evaluated are in the developmental stage in a clinical trial. In fact, several studies have reported the use of various Ayurvedic medicinal plant extracts and their most active chemical constituents for the management of Alzheimer's disease. Although the accurate molecular mechanism is unknown. Pipali and Jyotishmati are extensively used in Ayurveda for various diseases and for the enhancement of memory. An attempt has been made in the current study to acknowledge the activity of extracts of Piper longum and Celastrus paniculatus, and marker compounds like Piperine on acetylcholinesterase inhibition by in-vitro and Rivastigmin as standard. In-silico AChE inhibition studies were carried out on various active constituents like Piperine, Paniculatine, Malkanguinine and Donepezil as standard. Both the enhanced extracts and the standard marker have promising AChE inhibitory action, indicating that they could be used to treat memory problems.
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