Sustained-release drug delivery system
A drug and pharmacy technology, applied in the direction of drug delivery, pharmaceutical formulation, aerosol delivery, etc., can solve the problems of pain and irritation at the injection site, oil gel preparations that have not been seen, preparation application restrictions, etc., to achieve good biophase Compatibility, good drug safety and tolerability, and ease of administration
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[0102] Example 1 Solution of different types of saturated phospholipids in castor oil and each organic solvent
[0103]1g castor oil, organic solvent was added to the EP tube, and 0.1 g of saturated phospholipids (about 100 mg / g, 10% w / w), 50 ° C ultrasound, observed dissolution, and the results are shown in Table 1-1.
[0104] Table 1-1 Investigation of solubility
[0105]
[0106] Among them, ETOH represents anhydrous ethanol; BB represents benzyl benzoate; BA represents benzyl alcohol; NMP represents N-methylpyrrolidone; DMSO represents dimethyl sulfoxide.
[0107] According to the dissolution, saturated phospholipid (HSPC, DPPC, DMPC, DSPC) has better solubility in alcohol solvents (ethanol, benzyl alcohol, propylene glycol, etc.), and phosphatidylglycerol (DPPG), phosphatidyl ethanolamine (DPPE) However, phosphatidic acid (DPPA) category cannot be solved in the above solvent.
Example Embodiment
[0108] Example 2 Combination ratio studies
[0109] (1) Combination room temperature morphology test
[0110] The composition is prepared according to each of the ingredients and ingredients shown in Table 2-1 below. The solvent phospholipin, oil and solvent are mixed, and the mixture is stirred while heating the heating edge until a solution of a transparent uniform, cooling to room temperature, and investigating the physical form. At the same time, the room temperature morphology of unsaturated phospholipid composition is carried out as a comparative study.
[0111] Table 2-1 Room Temperature of Compositions under Different Metals
[0112]
[0113] This example examines a form of formulation containing 0.5 to 30% (W / W) saturated phospholipids (HSPC, DPPC, DSPC and DMPC), 0 to 50% (w / w) solvent, and the results are shown in Table 2 According to the composition of the composition room temperature of the present invention, the composition of the present invention is related t...
Example Embodiment
[0121] Example 3
[0122] (1) Effect of different types of phospholipids on the phase change of the composition
[0123] A pharmaceutical composition containing saturated phospholipid (composition 16), no phospholipid (pure castor oil group) and an unsaturated phospholipid is prepared according to Table 3-1. The methalkoxin is dissolved in N-methylpyrrolidone, and the concentrated solution of 50 mg / g is prepared, and ropivacaine, soybean phospholipid or dioplamyyl phosphatidine choline is added to liquid oil, solvent and machetin at 50 ° C. In the heating solution, the mixture is stirred while heating the heating edge until a solution of a transparent uniform is cooled to room temperature. The composition was slowly injected into water with a syringe to observe the morphological changes in the water in the water. See Picture 1-1 .
[0124] Table 3-1 Different compositions
[0125]
[0126] The above experiments respectively examined the morphological changes of a composition (...
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