Abstract

Amorphization of drug has been considered as an attractive approach in improving drug solubility and bioavailability. Unlike their crystalline counterparts, amorphous materials lack the long-range order of molecular packing and present the highest energy state of a solid material. Co-amorphous systems (CAM) are an innovative formulation technique by where the amorphous drugs are stabilized via powerful intermolecular interactions by means of a low molecular co-former.
 This review highlights the different approaches in the preparation of co-amorphous drug delivery system, the proper selection of the co-formers. In addition, the recent advances in characterization, Industrial scale and formulation will be discussed.

Highlights

  • A growing number of new active pharmaceutical ingredients (APIs) have been revealed as a result of high-throughput screening technology progress [1, 2]

  • In the biopharmaceutics classification system (BCS), these drugs are off the record as class II and class VI, respectively [3].The low water solubility of such drugs will decrease the drug bioavailability seriously and may prevent further development of new chemical entities if it remains without satisfactory solution [4]

  • The improvement in the apparent solubility and dissolution profile in amorphous materials might be attributed to the low energy barrier necessary for molecules to go into solution Yet, the amorphous systems potential application is limited, owing to thermodynamic instability causing recrystallization throughout processing, when they get in contact with the fluids of biological system or during storage [9]

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Summary

Introduction

A growing number of new active pharmaceutical ingredients (APIs) have been revealed as a result of high-throughput screening technology progress [1, 2]. The first drug-drug CAM was developed by combining naproxen with cimetidine, by Yamamura et al The solubility and dissolution rate enhancement were attributed to amorphous form stabilization of both drugs throughout intermolecular hydrogen bonding [16].

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