New solid-state chemistry technologies to bring better drugs to market: knowledge-based decision making

Abstract

Modern drug development demands constant deployment of more effective technologies to mitigate the high cost of bringing new drugs to market. In addition to cost savings, new technologies can improve all aspects of pharmaceutical development. New technologies developed at SSCI, Inc. include solid form development of an active pharmaceutical ingredients. (APIs) are PatternMatch software and capillary-based crystallisation techniques that not only allow for fast and effective solid form screening, but also extract maximum property information from the routine screening data that is generally available. These new technologies offer knowledge-based decision making during solid form development of APIs and result in more developable API solid forms.

Polymorphism, phase transformation and energetic properties of 3-nitro-1,2,4-triazole

“…Crystal polymorphism, the ability of a compound to exist in different crystalline forms that have different arrangements and/or conformations of molecules in the solid state, is a widespread phenomenon that has gained much interest in both academic and industrial research. 1 In particular, the polymorphs of energetic materials have an important influence on energetic properties (insensitivity, higher density, higher energy).…”

Polymorphism and Phase Transformation Behavior of Solid Forms of 4-Amino-3,5-dinitrobenzamide

“…Crystal polymorphism, the ability of a compound to exist in different crystalline forms that have different arrangements and/or conformations of molecules in the solid state, is a widespread phenomenon that has gained much interest in both academic and industrial research . Polymorphic forms display different physicochemical properties − and are important in connection with bioavailability and ease of manufacturing of active pharmaceutical ingredients (APIs), resulting in patenting and financial profits of pharmaceutical companies. , The area of polymorphism, both in terms of experimental and theoretical studies, has advanced significantly in the past two decades, and developments in this area continue to look promising. , We have initiated our investigations on the amide class of compounds, as the amide group is an important functionality found in both natural and synthetic compounds, such as peptides, proteins, synthetic polymers, APIs, etc.…”

Highly Crystalline Forms of Valsartan with Superior Physicochemical Stability

“…The solid APIs used in the formulation could exist in distinctive solid modifications, such as polymorphs, solvates, hydrates, salts, cocrystals, and amorphous state. Among the various solid forms, polymorphs (alternative arrangements of the same molecular entity in the crystal lattice) and solvates, especially hydrates, are universal phenomena existing in the organic small molecular-based APIs and have drawn special attention from both academic and industrial researchers. − It is well-documented that new crystal modifications may present pronounced differences in pharmaceutically relevant properties, such as hygroscopicity, stability, solubility, dissolution rates, bioavailability, and sometimes biological activities. − In addition, new polymorphs are patentable and, hence, possess economic impact in terms of intellectual property protection . In order to achieve a reasonable shelf life and to prevent form transformation in the future manufacture processes, solid APIs are generally produced and stored under a desired solid form (e.g., in most cases) under the most thermodynamically stable and highly crystalline form.…”