Method for preparing an amlodipine microsphere

A technology of amlodipine and microspheres, which is applied to medical preparations containing non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, etc. It can solve the problem of patients with large blood pressure fluctuations and increased incidence of cardiovascular events, etc. problems, to achieve the effect of solving missed doses, reducing the incidence rate, and rounding the shape

Inactive Publication Date: 2009-09-16
XIAN LIBANG PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, it is also common to not take medicine on time every day, which will lead to large fluctuations in blood pressure of patients, thereby increasing the incidence of cardiovascular events

Method used

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  • Method for preparing an amlodipine microsphere
  • Method for preparing an amlodipine microsphere
  • Method for preparing an amlodipine microsphere

Examples

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preparation example Construction

[0018] The preparation method of amlodipine microspheres of the present invention selects polylactic acid (PLA), polylactic acid-polyglycolic acid copolymer (PLGA), or polylactic acid-polyethylene glycol block copolymer (PLA-mPEG) as carrier The material encapsulates the drug amlodipine, and the relative molecular weight of the carrier material is 5×10 3 ~1.5×10 5 , the ratio to the drug is 50:1-3:1, the concentration of the carrier material in the oil phase is 1%-50% (g / ml); the carrier material and the drug are dissolved in an organic solvent to make an oil phase, and the oil phase The organic solvent in is dichloromethane, or the mixed solution of dichloromethane and ethanol, or the mixed solution of dichloromethane and ethyl acetate;

[0019] Add the oil phase to the water phase, and make the volume ratio of the oil phase to the water phase 1:300~1:5; fully emulsify through mechanical stirring or high-speed shearing to obtain an O / W emulsion, and then use the emulsion sol...

Embodiment 1

[0028] prescription:

[0029]

[0030] Preparation method:

[0031] Weigh PLGA and amlodipine according to the prescription amount, add 5ml of dichloromethane to dissolve, add to the water phase under the condition of stirring at 500rpm, continue to stir for 1 hour, then slowly raise the temperature to 40°C, and stir for 2 hours; Filter through a 125 μm sieve to collect the filtrate, then filter through a 1 μm sieve to collect the microspheres, wash the microspheres with an appropriate amount of water several times, filter out the water, and dry at 40°C to obtain the product.

Embodiment 2

[0033] prescription:

[0034]

[0035] Preparation method:

[0036] Weigh PLGA and levamlodipine according to the prescription amount, add 8ml of dichloromethane to dissolve, slowly add to the water phase under 300rpm stirring condition, continue to stir for 0.5 hours, then slowly heat up to 40°C, stir for 3 hours, Then filter through a 125 μm sieve to collect the filtrate, then filter through a 1 μm sieve to collect the microspheres, wash the microspheres with an appropriate amount of water several times, filter out the water, and dry under reduced pressure at 40°C to obtain the product.

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Abstract

The method discloses a method for preparing an amlodipine microsphere. Medicament wrapped by the prepared amlodipine microsphere is amlodipine and organic acid salts of the amlodipine; a carrier material of the microsphere is polylactic acid (PLA), a polylactic acid-glycolic acid copolymer (PLGA), a polylactic acid-glycol block copolymer (PLA-mPEG) or other biodegradable materials; a surfactant solution, a monosaccharide or amylose solution, a polyalcohol solution, a cellulose solution and a colloid solution are used as a dispersion medium; and through an emulsion solvent evaporation method, the amlodipine microsphere is prepared under the mechanical stirring or high-speed shearing action. The microsphere has a round shape and even distribution of grain diameter; the grain diameter is within the range between 1 and 125 mu m; the medicine loading capacity can reach more than 1.5 percent; and the encapsulating rate is more than 70 percent.

Description

technical field [0001] The present invention relates to a preparation method of drug-loaded microspheres, particularly amlodipine and its organic acid salt microspheres. The method uses polylactic acid (PLA), polylactic acid-polyglycolic acid copolymer (PLGA), Polylactic acid-polyethylene glycol block copolymer (PLA-mPEG) is used as the carrier material, and the drug-loaded microspheres are prepared by drying in liquid. The drug-loaded microspheres can be used for subcutaneous injection, and the concentration of the drug in the body is maintained at a stable level for a long time (2 weeks to 3 months). Compared with ordinary tablets, it avoids the blood drug concentration caused by frequent oral administration. The change reduces the occurrence of toxic and side effects and improves the safety of medication for patients. Background technique [0002] Hypertension is the most common cardiovascular disease. With the improvement of modern living standards, excess meat and pro...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/4422A61K47/34A61P9/12
CPCA61K9/1647A61K47/34A61P9/12
Inventor 胡忍乐王九成梁华丁多浩焦亚奇
Owner XIAN LIBANG PHARMA TECH
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