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Lyophilisation: difference between revisions

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Revision 16 — 16:40, 27 Oct 2024
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5| Physical requirement = Pressure below the triple point of water5| Physical requirement = Pressure below the triple point of water
6| Typical cycle length = 20–70 hours6| Typical cycle length = 20–70 hours
+7<!-- Representative process conditions -->
+8| Freezing shelf temperature = −40 to −50 °C
+9| Chamber pressure, primary drying = 5–20 Pa (roughly 40–150 mTorr)
+10| Product temperature, primary drying = −40 to −20 °C
+11| Shelf temperature, secondary drying = 20–40 °C
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13A lyophilisation cycle has three phases: freezing, primary drying in which ice is sublimed, and secondary drying in which water sorbed to the solid is desorbed. Each phase is bounded by a physical constraint. Freezing determines the ice-crystal structure and therefore the resistance the vapour must overcome later; primary drying must be conducted below the temperature at which the freeze-concentrated matrix loses rigidity; secondary drying must reach a residual moisture low enough for stability without over-drying a solid that may require a small amount of water for conformational integrity.{{r|tang2004,carpenter1997}}18A lyophilisation cycle has three phases: freezing, primary drying in which ice is sublimed, and secondary drying in which water sorbed to the solid is desorbed. Each phase is bounded by a physical constraint. Freezing determines the ice-crystal structure and therefore the resistance the vapour must overcome later; primary drying must be conducted below the temperature at which the freeze-concentrated matrix loses rigidity; secondary drying must reach a residual moisture low enough for stability without over-drying a solid that may require a small amount of water for conformational integrity.{{r|tang2004,carpenter1997}}
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+20The finished cake is characterised by appearance, residual moisture, reconstitution time and the chemical purity of the reconstituted solution. None of these is visible from a purity figure alone, which is one reason a [[certificate of analysis]] that reports only [[Area percent purity|area percent purity]] leaves the physical quality of the vial undocumented.{{r|usp1207}}
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15== Physical basis ==22== Physical basis ==
16Water can pass directly from solid to vapour only at pressures below its triple point, which lies at 611.657 Pa and 0.01 °C. Above that pressure, warming ice produces liquid; below it, warming ice produces vapour. Every lyophilisation cycle therefore operates at a chamber pressure well beneath 611 Pa, typically between 5 and 20 Pa, so that heat supplied to the product drives sublimation rather than melting.{{r|nail2002}}23Water can pass directly from solid to vapour only at pressures below its triple point, which lies at 611.657 Pa and 0.01 °C. Above that pressure, warming ice produces liquid; below it, warming ice produces vapour. Every lyophilisation cycle therefore operates at a chamber pressure well beneath 611 Pa, typically between 5 and 20 Pa, so that heat supplied to the product drives sublimation rather than melting.{{r|nail2002}}
50<ref name="chang2009">Chang LL, Pikal MJ. "Mechanisms of protein stabilization in the solid state." ''Journal of Pharmaceutical Sciences'' 98(9):2886–2908 (2009).</ref>57<ref name="chang2009">Chang LL, Pikal MJ. "Mechanisms of protein stabilization in the solid state." ''Journal of Pharmaceutical Sciences'' 98(9):2886–2908 (2009).</ref>
51<ref name="murphy2005">Murphy DM, Koop T. "Review of the vapour pressures of ice and supercooled water for atmospheric applications." ''Quarterly Journal of the Royal Meteorological Society'' 131(608):1539–1565 (2005).</ref>58<ref name="murphy2005">Murphy DM, Koop T. "Review of the vapour pressures of ice and supercooled water for atmospheric applications." ''Quarterly Journal of the Royal Meteorological Society'' 131(608):1539–1565 (2005).</ref>
+59<ref name="usp1207">United States Pharmacopeia, General Chapter <1207>, "Package Integrity Evaluation — Sterile Products". USP–NF, current revision.</ref>
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53{{DEFAULTSORT:Lyophilisation}}61{{DEFAULTSORT:Lyophilisation}}