Influence of the Liquid Phase Coexisting in Fatty Suppository Bases on the Polymorphic Transition Rate

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The influence of the liquid phase on the A-to-B transition of semisynthetic fatty suppository vehicles during storage was investigated. The addition of a liquid having a high affinity, such as isopropyl myristate, fatty oil, lauryl alcohol, etc., remarkably accelerated the transition, whereas that of a low affinity liquid had little effect. The transition rate evaluated from the time course of transition degree (k_T) increased linearly with the weight fraction ratio of liquid phase (f_L) to solid phase (1-f_L). The case where liquid phase was produced only from molten vehicle containing no liquid additive was also examined. The relation between k_T and f_L/(1-f_L) was investigated 1) for the transition of Witepsol H-15 in the temperature range from 26 to 32℃, and 2) for several commercial vehicles at 30℃. Linear relations also appeared to hold for both cases. Here, the weight fraction of liquid phase at a given temperature was determined by means of differential scanning calorimetry (DSC). The activation energy of transition (E^〓) was compared in the presence and absence of liquid additives. E^〓 values of Witepsol H-15 containing 10 and 25% fatty oil were about 40 kcal, less than one-half of that of Witepsol H-15 not containing any liquid additives. The transition mechanism was considered to involve dissolution of the solid A-form in the intervening liquid phase followed by crystallization as solid B-form.
社団法人日本薬学会の論文
1982-08-25

Influence of the Liquid Phase Coexisting in Fatty Suppository Bases on the Polymorphic Transition Rate

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