Pharmaceutical emulsion compositions comprising progestogen
A composition and progesterone technology, which are used in the field of treating traumatic injury of the central nervous system and parenteral administration, and can solve the problems of inability to provide pharmaceutical compositions and the like
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[0238]A particularly preferred embodiment of the preparation method comprises the following steps:
[0239] A) Dissolving the osmotic agent in the aqueous medium and stirring;
[0240] B) adding a surfactant, preferably egg lecithin, and stirring;
[0241] C) Optionally, adding a co-surfactant and a pH adjuster and mixing;
[0242] D) dissolving progesterone in oil to form an oil phase;
[0243] E) filtering the oil phase, then adding the filtered oil phase to the water phase and mixing;
[0244] F) homogenization to form a homogeneous emulsion;
[0245] G) Optionally, adding water;
[0246] H) Optionally, add enough 1N NaOH to adjust the pH to pH 8.0-8.8;
[0247] I) Optionally, add enough aqueous medium to bring up to final volume.
[0248] In a particularly preferred embodiment, the homogenization is carried out at greater than or equal to 350 bar, preferably greater than or equal to 370 bar.
[0249] In a particularly preferred embodiment, the process for preparing ...
Embodiment 1
[0277] Example 1 - Preferred Embodiment
[0278] The formulation of Example 1 is a 6% oil emulsion composition comprising 0.2% progesterone and 1.2% egg lecithin. The phospholipids are present in an amount of 17% w / w of the oil and the ratio of progesterone to oil is 1:30 (w / w)
[0279] Table I
[0280]
[0281] The emulsions of Table I were prepared as follows. Components, mixtures and finished emulsions were maintained under nitrogen at a temperature of 55-60°C unless otherwise noted.
[0282] 180 L of water for injection (w.f.i.) was added to the first vessel, warmed to 58°C while mixing at 50 Hz, and degassed with nitrogen until a residual oxygen concentration of ≤0.1 mg / L was obtained. 9.98 kg glycerol (anhydrous glycerol, Axelis, Austria) was added to the water and mixed at 50 Hz for 5 minutes. 23.97 kg soybean oil (Fresenius Kabi, Sweden) was added to a second vessel, stirred at 50 Hz, and warmed to 58°C. Under constant stirring, 0.81 kg of progesterone (mic...
Embodiment 4
[0311] Example 4 - Effect of Phospholipids
[0312] The following examples demonstrate the effect of varying the phospholipid content of the emulsion composition on the properties of the emulsion. The 6% oil emulsions of Table IV were prepared by the procedure described below. The emulsion contained 0.2% progesterone and 1.8%, 1.5%, 0.9% or 0.6% lecithin.
[0313] Table IV
[0314]
[0315] The emulsions of Examples 4A-D were prepared by the following method. 600 g soybean oil (Fresenius Kabi, Sweden) was added to the vessel and warmed to 58°C. The oil was kept under a nitrogen atmosphere while 20 g of progesterone (micronized progesterone, Proquina, Mexico) was added to the soybean oil and dissolved by mixing with a magnetic stirrer. Put water for injection into a second container and heat to 58°C. 250 g of glycerol (anhydrous glycerol, Axelis, Austria) was added to the aqueous phase and dissolved by high shear mixing. The indicated amounts of egg lecithin (PL90,...
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