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Glimepiride nano-particle capsule and preparation method thereof

A technology of glimepiride and nanoparticles, applied in the field of medicine, can solve the problems of poor water solubility of glimepiride, poor effect of targeted therapy, and low bioavailability, and achieve improved bioavailability, good effect, and half-life of the drug prolonged effect

Inactive Publication Date: 2012-07-25
ZHENGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] In view of the above situation, the main purpose of the present invention is to provide a kind of glimepiride nanoparticle capsule and its preparation method, which can effectively solve the problem of poor water solubility of glimepiride, short half-life, instability, low bioavailability and targeted therapy effect. bad question

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  • Glimepiride nano-particle capsule and preparation method thereof
  • Glimepiride nano-particle capsule and preparation method thereof

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preparation example Construction

[0013] The preparation method of the glimepiride nanoparticle capsule of the present invention comprises the following steps:

[0014] (1) Preparation of primary suspension: dissolving glimepiride or the mixture of glimepiride and the surfactant in an organic solvent, the volume concentration of the organic solvent is 10-70% (v / v ), the selected organic solvent is methanol, ethanol, acetonitrile, ether, acetone, isopropanol, ethyl acetate, dichloromethane or a mixed solution of two equal volumes. When the drug cannot be completely dissolved, It can be heated and dissolved at 40-60°C, and the initial suspension can be prepared by high-speed homogenization method, magnetic stirring method, or ultrasonic method;

[0015] The high-speed homogenization method is: dissolving the surfactant in ultrapure water to make a water phase containing the surfactant, and adding the water phase containing the surfactant to the In the organic solvent of urea, use an internal cutting type homoge...

Embodiment 1

[0025] Weigh 20mg of glimepiride and 150mg of soybean lecithin, add 10ml of acetone to ultrasonically dissolve to form an organic phase; weigh 150mg of PVP-K30 and dissolve in 20ml of ultrapure water to form an aqueous phase. Heat the organic phase and the aqueous phase in a water bath at 40-60°C for 3 minutes, add the aqueous phase to the organic phase, and use an internal cutting homogenizer at 15,000 rpm to homogenize for 5 minutes to obtain an initial suspension; The suspension was rotated under reduced pressure at room temperature to remove the organic solvent, then placed on a high-pressure homogenizer, and circulated 15 times at 9k psi and 18k psi each to obtain a milky white nanosuspension; 1000mg of xylitol was dissolved in the nanomixer suspension, put it in a -80°C refrigerator for 6 hours, and then place it in a freeze dryer at a temperature and pressure of -84°C and 98×10 -3 Under the condition of Mbar, dry for 24 hours to prepare glimepiride nanoparticle freeze-...

Embodiment 2

[0028] Weigh 50 mg of glimepiride, add 10 ml of acetone to ultrasonically dissolve to form an organic phase; weigh 450 mg of PEG6000 and dissolve in 20 ml of ultrapure water to form an aqueous phase. Heat the organic phase and the aqueous phase in a water bath at 50°C for 10 minutes, add the aqueous phase to the organic phase, and homogenize with an internal cutting homogenizer at 15,000 rpm for 5 minutes to obtain a primary suspension. Then the primary suspension was rotated under reduced pressure at normal temperature to remove the organic solvent, and then placed on a high-pressure homogenizer, and circulated 18 times under 9k psi and 18k psi to obtain a milky white nano-suspension; mannitol and xylitol After mixing according to the ratio of 1:1, weigh 1500mg and dissolve it in the nano-suspension, put it in a -20 ℃ refrigerator for 12 hours, and then place it in a freeze dryer. ×10 -3 Under the condition of Mbar, dry for 12 hours to prepare glimepiride nanoparticle freeze...

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Abstract

The invention relates to a glimepiride nano-particle capsule and a preparation method thereof. The problems of poor water-solubility, short half-life period, instability, low bioavailability and poor targeted therapeutic effect of the glimepiride can be effectively solved. The technical scheme for solving the problems is that the glimepiride nano-particle capsule comprises the following components in parts by weight of 1 part of glimepiride, 1-30 parts of surfactant and 3-60 parts of freeze-drying protective agent. The preparation method comprises the steps of: dissolving the glimepiride or a mixture of the glimepiride and the surfactant into an organic solvent to prepare an initial suspension, and carrying out a high-pressure homogenization method or emulsification dispersion method to obtain a suspension with an average particle size of 300+ / -60nm; and freeze-drying and screening the nano suspension, and then filling into a capsule. Through adding the proper surfactant, the mutual attraction among anno particles is overcome, a solid preparation has excellent long-term stability, long-term storage and transportation are facilitated, half-life period of medicines is prolonged, absorption degree is increased, bioavailability is improved, and a targeted therapeutic effect is good.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a glimepiride nanoparticle capsule and a preparation method thereof. Background technique [0002] Glimepiride (GM) is the third-generation oral sulfonylurea hypoglycemic drug, which has been widely used in the treatment or adjuvant therapy of type II diabetes. Compared with other sulfonylurea hypoglycemic agents, glimepiride can not only increase the secretion and release of insulin by pancreatic β cells, but also has a significant extrapancreatic hypoglycemic effect. Its hypoglycemic mechanism is to act on receptors on the islet β cell membrane, preventing K + efflux, promoting Ca 2+ Influx, thereby stimulating the secretion and release of insulin, and can increase the number of insulin receptors and the affinity of insulin and its receptors (Mary U et al., Clin Ther, 26 (2004): 63-69 ), and at the same time, enhance liver glycogen The activity of synthetase and the function of gluco...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/48A61K31/64A61K47/38A61K47/34A61K47/32A61K47/26A61K47/24A61P3/10
Inventor 杜斌孙惠斌姚寒春王丹丹庞丽陈政
Owner ZHENGZHOU UNIV
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