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Delta-mannitol to enable continuous twin-screw granulation of a highly dosed, poorly compactable formulation
Contributor(s):: Vanhoorne, V., Almey, R., De Beer, T., Vervaet, C.
In current study, it was investigated if the moisture-mediated polymorphic transition from δ- to β-mannitol during twin screw granulation (TSG) also took place in high drug loaded formulations and if the specific granule morphology associated with the polymorphic transition could enable tableting...
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Twin-screw granulation and high-shear granulation: The influence of mannitol grade on granule and tablet properties
Contributor(s):: Megarry, Andrew, Taylor, Agnes, Gholami, Aida, Wikstrom, Hakan, Tajarobi, Pirjo
Granule structure has a key influence on tablet critical quality attributes. The ability to control this structure through excipient choice is an important part of formulation development. Mannitol is a popular diluent and the choice of input grade has been shown to impact granule properties....
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Selective preparation of elusive and alternative single component polymorphic solid forms through multi-component crystallisation routes
Contributor(s):: Thomas, LH, Wales, C, Wilson, CC
A transferable, simple, method for producing previously elusive and novel polymorphic forms of important active pharmaceutical ingredients (APIs; paracetamol (acetaminophen), piroxicam and piracetam) is demonstrated. Nitrogen heterocyclic co-molecules are employed to influence the self-assembly...
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Recent Developments in the Crystallization Process: Toward the Pharmaceutical Industry
Contributor(s):: Gao, Zhenguo, Gong, Junbo, Rohani, Sohrab, Wang, Jingkang
Crystallization is one of the oldest separation and purification unit operations, and has recently contributed to significant improvements in producing higher-value products with specific properties and in building efficient manufacturing processes. In this paper, we review recent developments in...
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Process Analytical Technology for Crystallization of Active Pharmaceutical Ingredients
Contributor(s):: Malwade, CR, Qu, HY
Background: Pharmaceutical industry is witnessing increased pressure to introduce innovative and efficient processes for manufacturing Active Pharmaceutical Ingredients (APIs) in order to be competitive as well as to meet the stringent product quality requirements set by regulatory authorities....
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Polymorphism in Solid Dispersions
Contributor(s):: Ortiz, KS, Espinell, JRHTorres, DO, Lopez-Mejias, V, Stelzer, T
Solid dispersions embed active pharmaceutical ingredients in polymeric carriers to improve their solubility. Three solid dispersion preparation techniques are typically employed: solvent evaporation, solventfusion, and fusion methods. Although these are also widely recommended as preparative...
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Improved tabletability after a polymorphic transition of delta-mannitol during twin screw granulation
Contributor(s):: Vanhoorne, V., Bekaert, B., Peeters, E., De Beer, T., Remon, J-P., Vervaet, C.
In most formulations processed via continuous twin screw granulation microcrystalline cellulose (MCC) and/or lactose are used as excipients, but mannitol is also a preferred excipient for wet granulation and tableting due to its non-hygroscopicity and inertness. Therefore, the aim of the current...
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Future Supply Chains Enabled by Continuous Processing - Opportunities and Challenges
Contributor(s):: Jagjit Singh Srai, Markus Krumme, Mauricio Futran, Clive Badman, Craig Johnston
This paper examines the opportunities and challenges facing the pharmaceutical industry in moving to a primarily “continuous processing”-based supply chain. The current predominantly “large batch” and centralized manufacturing system designed for the “blockbuster” drug has driven a slow-paced,...
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Engineering a New Access Route to Metastable Polymorphs with Electrical Confinement
Contributor(s):: Al-Ani, AJ, Herdes, CWilson, CC, Castro-Dominguez, B
Polymorphism is the ability of solid materials, including active pharmaceutical ingredients (APIs), to exist in structurally distinctive arrangements. The existence of polymorphism and the difference in molecular packing can cause crystals to have a variety of different physical properties....
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Crystallisation and physicochemical property characterisation of conformationally-locked co-crystals of fenamic acid derivatives
Contributor(s):: Wittering, KE, Agnew, LRKlapwijk, AR, Robertson, K, Cousen, AJP, Cruickshank, DL, Wilson, CC
Polymorphism in drug compounds can cause significant problems for industrial-scale production and so a method for restricting the conformational freedom of the target compound whilst retaining desired chemical properties is highly beneficial to the pharmaceutical industry. Co-crystallisation is...