A new polymorph of glipizide with enhanced properties obtained using environmentally friendly methods

Abstract

A new polymorph of glipizide was obtained through environmentally friendly approaches without using any organic solvent. This polymorph exhibits enhanced apparent solubility, dissolution rates, stability, and powder liquidity compared with the reported solid forms.

Different Dissolution Molecular Pathways of Azilsartan Crystals with Different Forms Revealed by In Situ Atomic Force Microscopy

“…Crystalline materials and their dissolution processes are very important in many fields, such as mineral dissolution for geochemical element cycling, − pathological stone dissolution for disease therapy, − and drug dissolution to allow the active ingredient to be released. − In pharmaceutics, dissolution behavior is one of the most crucial factors in the use of different drug formulations and is strongly connected to the bioavailability of drugs. Understanding how crystalline drugs dissolve has grown more and more important as the need for poorly water-soluble drugs has increased. , Traditionally, time dependence of solute concentration in the bulk solution has been used to assess drug crystal dissolution characteristics. − This approach yields the overall average dissolving rate of a population of crystals in suspensions, but it leaves unresolved the most fundamental physical chemistry aspect of dissolution, which is drawing researchers’ growing interests. − That is, what mechanistic pathway do molecules take to escape from the crystal into solution? There may be a direct detachment mechanism or a surface diffusion mechanism. ,− Moreover, polymers such as polyethylene glycol (PEG) are frequently used to enhance drug dissolution ,− and control release. , However, further research is required to determine the underlying molecular mechanisms by which polymers interact with crystals and their molecular roles in dissolution.…”

The Physico-Chemical Properties of Glipizide: New Findings

“…It crystallizes in the triclinic P-1 Space Group, Z = 2, a = 5.1578(3) Å, b = 8.9760(5) Å, c = 23.9704(13) Å, a = 83.247(2)°, b = 85.543(2)°, g = 78.987(2)°, V = 1080.01(11) Å 3 at 100 K. The crystal structure data are deposited in the Cambridge Crystallographic Data Centre (CCDC N. 1516974). In the last few years studies have been performed with the aim to identify new polymorphs of this compound [ 14 , 15 , 16 ]. This interest arises from the need to improve its dissolution profile in order to achieve a higher bioavailability [ 17 , 18 ].…”

“…The amorphous form can be obtained by grinding, but to avoid its intrinsic tendency to recrystallize, a proper selection of the process parameters is necessary [ 19 , 20 , 21 , 22 , 23 ]. K. Xu et al [ 15 , 16 ] defined the process parameters to ball-mill glipizide form I, identified by Renuka et al [ 14 ], that allow its transition to form II (amorphous form) and form III. However, also in this work, the experimental set up seems to be inappropriate, and the conclusions drawn from the experimental evidence are not convincing.…”

Different Solid Forms of Vitamin K3 and Their Effect on the Chemical Stability

“…Active pharmaceutical ingredients (APIs) may exist in a variety of solid forms, such as amorphous forms, polymorphs, hydrates, and solvates . Their different molecular conformations and crystal packing can result in different physicochemical properties, such as stability, flowability, tableting, performance, solubility, and dissolution rate, which are of vital importance in the pharmaceutical industry. − Therefore, it is crucial to understand the existence of each form of APIs and their specific crystallization conditions, not only for choosing the optimal form but also to prevent accidental transformation during the manufacture processes, which may lead to potentially harmful results. − …”