Sustained-release pharmaceutical compositions comprising an immunomodulating agent and uses thereof
A technology for immunomodulators and compositions, applied in the field of sustained-release pharmaceutical compositions, can solve problems such as limiting the dose of drugs and reducing the frequency of administration of the immunomodulators
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example 1
[0048] Example 1: Preparation of fingolimod liposome formulation
[0049] Empty liposomes were prepared by the lipid film hydration-extrusion method. HSPC, cholesterol and DSPE-PEG2000 (59.5 / 39.6 / 0.9 mole percent) were dissolved in chloroform, and the organic solvent was removed under vacuum by a rotary evaporator to form a thin lipid film. The dried lipid film was hydrated with 300 mM ammonium sulfate at 60° C. for 30 minutes to form empty liposomes with an aqueous core embedded with ammonium sulfate. After six freeze-thaw cycles between liquid nitrogen and 60°C water, the empty liposomes were then squeezed 10 times through a polycarbonate filter with a pore size of 0.2 μm. Unentrapped ammonium sulfate was removed by dialysis against 9.4% sucrose solution.
[0050] A reaction mixture containing 7.8 mg / mL fingolimod hydrochloride (MedChem Express), empty liposomes with a lipid concentration of 20.7 mM, and 50 mM histidine buffer (pH 7) was reacted at 60° C. for 15 minute. ...
Embodiment 2
[0053] Embodiment 2: the preparation of Ozamod liposome formula
[0054]Empty liposomes were prepared by the lipid film hydration-extrusion method. HSPC, cholesterol and DPPG (59.5 / 39.6 / 0.9 mole percent) were dissolved in chloroform, and the organic solvent was removed under vacuum by a rotary evaporator to form a thin lipid film. The dried lipid film was hydrated with 300 mM ammonium sulfate at 60° C. for 30 minutes to form empty liposomes with an aqueous core embedded with ammonium sulfate. After six freeze-thaw cycles between liquid nitrogen and 60°C water, the empty liposomes were then squeezed 10 times through a polycarbonate filter with a pore size of 0.2 μm. Unentrapped ammonium sulfate was removed by dialysis against 9.4% sucrose solution.
[0055] A reaction mixture containing 7.2 mg / mL Ozamod (DC Chemicals), empty liposomes with a lipid concentration of 20.6 mM, and 50 mM histidine buffer (pH 6.5) was reacted at 60° C. for 15 minutes. by Sephadex TM G-50 fine ge...
Embodiment 3
[0058] Example 3: Effects of Different Capture Agents on Drug Loading Profiles
[0059] Liposome formulations with the following capture agents were prepared according to Example 1: (1) 75 mM sucrose octasulfate triethylammonium, (2) 300 mM ammonium sulfate, (3) 200 mM ammonium phosphate, and (4) 7.0 mM Dextran Sulfate. Table 1 shows the effect of different capture agents on the drug loading profile.
[0060] Table 1. Drug loading curves of different capture agents
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