Sustained-release injection preparation containing donepezil and preparation method thereof
A technology of donepezil and sustained release, applied in the directions of medical preparations containing active ingredients, pharmaceutical formulations, organic active ingredients, etc., to achieve the effect of excellent injectability
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[0037] In one embodiment of the present invention, the preparation method of donepezil sustained-release microspheres is characterized by comprising:
[0038] (a) dissolving donepezil and polylactide polymer in an organic solvent to prepare a donepezil-polylactide solution (dispersed phase);
[0039] (b) adding the donepezil-polylactide solution prepared in step (a) to an aqueous phase (continuous phase) containing a surfactant to prepare an emulsion;
[0040] (c) extracting and evaporating an organic solvent from the dispersed phase in the form of an emulsion prepared in step (b) into a continuous phase to form microparticles; and
[0041] (d) recovering microparticles from the continuous phase containing microparticles of step (c) to obtain donepezil microparticles.
[0042] In step (a), the polylactide has an intrinsic viscosity of 0.10 to 1.3 dL / g, preferably 0.16 to 0.75 dL / g.
[0043] The method for uniformly mixing the donepezil-polylactide solution and the continuous...
Embodiment 1
[0056] Example 1: Preparation of microspheres using PDL04 as polymer for the dispersed phase
[0057] By mixing 3.75 g of biocompatible polymer Purasorb PDL 04 (manufacturer: Corbion, Netherlands) and 1.25 g of donepezil base (manufacturer: Neuland Laboratories, India) with 15 g of dichloromethane (manufacturer: JT Baker, USA) Prepare the dispersed phase. The dispersed phase is fully dissolved by stirring for 30 minutes or more, and then used. For the continuous phase, an aqueous solution of 1% polyvinyl alcohol (viscosity: 4.8-5.8 mPa.s) was used. A container containing 1500 mL of the continuous phase was connected to an emulsification device equipped with a membrane having pores of a diameter of 40 μm, while injecting the prepared dispersed phase into the device to prepare a microsphere suspension. The microsphere suspension was then placed in a preparation vessel and stirred at 200 rpm.
[0058] The temperature of the membrane emulsification equipment and preparation v...
Embodiment 2
[0064] Example 2: Preparation of microspheres using R202H as the polymer for the dispersed phase
[0065] By mixing 3.75 g of biocompatible polymer Resomer R202H (manufacturer: Evonik, Germany) and 1.25 g of donepezil base (manufacturer: Neuland Laboratories, India) with 9.4 g of dichloromethane (manufacturer: JT Baker, USA) Prepare the dispersed phase. The dispersed phase is fully dissolved by stirring for 30 minutes or more, and then used. For the continuous phase, an aqueous solution of 1% polyvinyl alcohol (viscosity: 4.8-5.8 mPa.s) was used. A container containing 940 mL of the continuous phase was connected to an emulsification device equipped with a membrane having pores of 40 μm in diameter, and the prepared dispersed phase was injected into the device to prepare a microsphere suspension. The microsphere suspension was then placed in a preparation vessel and stirred at 180 rpm.
[0066] The temperature of the membrane emulsification equipment and preparation vesse...
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