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Felodipine slow-release microspheres and preparation method thereof

A felodipine and gentle technology, applied in the direction of medical preparations with non-active ingredients, pharmaceutical formulas, medical preparations containing active ingredients, etc., can solve the problems of incomplete drug release and achieve increased blood drug concentration and oral biological Utilization, the effect of improving drug bioavailability

Active Publication Date: 2012-07-18
ZHEJIANG UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The continuous phase of the O / W method is water, and the post-treatment of the microspheres is simple, but when the method is loaded with insoluble drugs, the drug release is not complete

Method used

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  • Felodipine slow-release microspheres and preparation method thereof
  • Felodipine slow-release microspheres and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Embodiment 1 O / W method prepares felodipine sustained-release microspheres

[0027] Table 1

[0028]

[0029] Preparation: Dissolve felodipine and EC in 100ml of dichloromethane according to the prescription in Table 1 as the organic phase (O). Then 5g of PVA emulsifier was dissolved in 500mL of water as the water phase (W). The organic phase is added into the water phase under high-speed stirring to homogeneously form an emulsion, and then the emulsion is poured into a large amount of water, the organic solvent is removed, the solid phase is separated by centrifugation, and the solid phase is dried to obtain the felodipine slow-release microspheres. The microsphere encapsulation efficiency is above 80%, and the particle size is 5-50 μm.

[0030]According to the quality standard of the United States Pharmacopoeia (USP35) felodipine sustained-release tablets, with PBS (pH6.5) containing 1% SDS as the release medium, the in vitro drug release assay was carried out, a...

Embodiment 2

[0031] Embodiment 2 W / O / W method prepares felodipine sustained-release microspheres

[0032] Table 2

[0033] prescription

I

II

III

IV

V

VI

VII

Felodipine

0.5g

0.5g

0.5g

0.5g

0.5g

0.5g

0.5g

EC45

2.5g

2.5g

2.5g

2.5g

2.5g

2.5g

2.5g

water

sucrose

0.1g

Mannitol

0.1g

lactose

0.1g

Glycine

0.1g

Sodium chloride

0.1g

PEG400

0.1g

Q1h(%)

25.3±0.7

24.4±1.3

34.8±6.4

25.4±1.3

27.9±1.5

39.9±2.6

23.3±2.2

Q24h(%)

89.3±2.7

86.1±0..7

86.3±5.6

83.3±5.0

82.8±1.6

89.4±2.0

93.4±0.7

[0034] Preparation: Dissolve sucrose, mannitol, lactose, glycine, sodium...

Embodiment 3

[0036] Embodiment 3: The pharmacokinetic comparison of felodipine microspheres prepared by W / O / W method and O / W method and felodipine suspension

[0037] 180 ICR mice, half male and half female, weighing 18-20 g, were randomly divided into 30 groups, 6 mice in each group. Felodipine microspheres (prescription IX in embodiment 1) prepared by O / W method, felodipine microspheres (prescription VII in embodiment 2) prepared by W / O / W method, and felodipine bulk drug are mixed with A suspension containing felodipine at a concentration of 1 mg / ml. Mouse fasting 12h, the felodipine microsphere (prescription IX in the embodiment 1) that the O / W method of 150mg / kg of felodipine dosage is prepared by intragastric administration respectively, the felodipine microsphere prepared by W / O / W method Ball (prescription VII in embodiment 2), and felodipine suspension, after administration 15min, 30min, 1h, 2h, 3h, 4h, 5h, 6h, 8h, 12h and 24h, orbital blood is taken in sodium heparin In the treat...

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Abstract

The invention discloses felodipine slow-release microspheres which consist of felodipine, ethylene cellulose and a drug release regulator and are prepared by adopting a W1 / O / W2 emulsification method, and the mass percentages of the felodipine, the ethylene cellulose and the drug release regulator are respectively 1-50, 36-99 and 0-44. The felodipine slow-release microspheres prepared in the invention adopt an in-vitro release condition of felodipine slow-release tablets in the United States Pharmacopeia (USP) and can slowly release drugs in 24 hours in vitro drug release, and compared with a felodipine dug suspension and felodipine slow-release microspheres prepared by an O / W method, the blood concentration and the oral bioavailability in vivo by adopting the felodipine slow-release microspheres prepared in the invention released are improved.

Description

(1) Technical field [0001] The invention relates to a felodipine slow-release microsphere and a preparation method thereof. (2) Background technology [0002] Felodipine is the second-generation dihydropyridine calcium antagonist developed by Astra for the company. It has high vascular selectivity and is an efficient, safe and well-tolerated antihypertensive drug. Felodipine is poorly soluble in water, and has a large first-pass effect in the liver after oral administration, and its bioavailability is only 15% to 20%. Currently commercially available preparations include felodipine common tablets and capsules, and sustained-release tablets. [0003] For poorly soluble drugs, dissolution is the prerequisite for drug absorption and the key to improving bioavailability. For improving the dissolution rate of felodipine, existing felodipine solid dispersion both at home and abroad [document 1: Rumondor AC, Taylor LS.Effect of polymer hygroscopicity on the phase behavior of amor...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/4422A61K47/38A61P9/12
Inventor 熊素彬舒丹丹尹小东
Owner ZHEJIANG UNIV OF TECH
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