Long-acting preparation for tatin medicine
A drug and statin technology, applied in the field of transdermal drug delivery system and subcutaneous implantation drug delivery system of statins, can solve the problems of forgetting to take, affecting the treatment effect, side effects and the like
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Embodiment 1
[0063] Example 1: Preparation of Transdermal Drug Delivery System or Subcutaneous Implanted Drug Delivery System
[0064] 1. Under nitrogen protection, 430 grams of ethanol and 215 grams of ethyl acetate are added to 1960 grams of polyacrylic polymer material (Durotak 387-2287, 1004 grams of solids) solution, stirred at room temperature until well mixed.
[0065] 2. According to the ratio shown in Table 1, add statins, substances used to prevent statins from crystallizing in the storage drug depot, and antioxidants. If it is used in a transdermal drug delivery system, a viscosity enhancer and a skin penetration accelerator are additionally added. If it is used for subcutaneous implantation of drug delivery system, some hydrogel can be added. The resulting mixture was stirred evenly and then put into a closed barrel for use to prevent the solvent from volatilizing.
[0066]
ingredients
transdermal administration
subcutaneous implant
Samp...
Embodiment 2
[0074] Example 2 In vitro drug permeability test
[0075] In vitro drug permeability tests were performed using human skin. The skin was clamped onto a diffusion cell (Franz cell). A single-layer simple adhesive patch (4.8 cm2, 1.0 mm thick storage drug storehouse, simvastatin) was pasted on the skin, and the drug penetration was measured at 37 ° C. The drug receiving medium was 1.0% sodium chloride aqueous solution. Methods Determination of cumulative permeation dose. The results are shown in Table 2:
[0076] time (hours)
Embodiment 3
[0077] Synthesis of simvastatin derivatives of embodiment 3 formula (2)
[0078]Under nitrogen protection, 16.0 g of dried simvastatin was suspended in 300 ml of dichloromethane. The white solid disappeared quickly and dissolved to give a clear solution. After cooling to 5-10°C, 0.5 molar equivalents of lithium bromide, 1.3 molar equivalents of triethylammonia, and 1.4 molar equivalents of 2,2-dimethyl-butyryl chloride were added. After the reaction mixture was stirred under nitrogen for 0.5 to one hour, the reaction was stirred at room temperature. After the reaction was completed, 100 ml of water was added, and the organic layer was separated after stirring for 30 minutes. The organic layer was washed once with saturated brine (100 ml), washed four times with saturated aqueous sodium bicarbonate solution (100 ml each time), washed twice with saturated brine (100 ml each time), dried with sodium sulfate, and filtered to evaporate the solvent Finally, the simvastatin deriva...
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