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Preparation method for Itraconazole composite particles

A technology of itraconazole and composite particles, which is applied in the directions of non-active ingredients medical preparations, medical preparations containing active ingredients, and pharmaceutical formulas, can solve problems such as unfavorable production scale-up, and achieves favorable dispersion and safe formulation. Stable and effective, easy to produce and scale up

Inactive Publication Date: 2019-02-26
HAINAN HONZ PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Using methanol as a solvent requires strict control of residues, which is also not conducive to production scale-up

Method used

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  • Preparation method for Itraconazole composite particles
  • Preparation method for Itraconazole composite particles
  • Preparation method for Itraconazole composite particles

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] prescription:

[0019] Material composition

Prescription ratio (%)

Itraconazole

35

hypromellose

50

polyethylene glycol 6000

15

[0020] Preparation:

[0021] 1) Preparation of mixed solution: Accurately weigh the mixture of 1.75g ​​itraconazole, 2.50g hypromellose and 0.75g polyethylene glycol 6000 into a 500mL conical flask, add 200mL ethanol and dichloromethane Mix solvents (volume ratio 1:2) to dissolve completely;

[0022] 2) CO2 feed: such as figure 1 As shown, open the valve of the CO2 cylinder, and the liquefied CO2 is continuously introduced into the high-pressure crystallization kettle of the supercritical fluid crystallization equipment system through the two symmetrical channels of the kettle head (60° from the middle solution channel) by the high-pressure pump, and the flow rate is controlled at 50mL / min;

[0023] 3) Control temperature and pressure: by regulating figure 1 The back pressure valve shown in t...

Embodiment 2

[0028] prescription:

[0029] Material composition

Prescription ratio (%)

Itraconazole

40

hypromellose

50

polyethylene glycol 6000

10

[0030] Preparation method: 1) Preparation of mixed solution: Accurately weigh the mixture of 1.6g itraconazole, 2.0g hypromellose and 0.4g polyethylene glycol 6000 into a 500mL conical flask, add 200mL ethanol and two A mixed solvent of methyl chloride (volume ratio 1: 1) to completely dissolve;

[0031] 2) CO 2 Feed: as figure 1 shown, open the CO 2 Cylinder valve, liquefied CO 2 The high-pressure pump is continuously introduced into the high-pressure crystallization kettle of the supercritical fluid crystallization equipment system through the two symmetrical channels of the kettle head (at 45° to the intermediate solution channel), and the flow rate is controlled at 75mL / min;

[0032] 3) Control temperature and pressure: by regulating figure 1 The back pressure valve shown controls the p...

Embodiment 3

[0037] prescription:

[0038] Material composition

Prescription ratio (%)

Itraconazole

40

hypromellose

40

polyethylene glycol 6000

20

[0039]Preparation method: 1) Preparation of mixed solution: Accurately weigh the mixture of 2.0g itraconazole, 2.0g hypromellose and 1.0g polyethylene glycol 6000 into a 500mL conical flask, add 200mL ethanol and two A mixed solvent of methyl chloride (volume ratio 1: 1) to completely dissolve;

[0040] 2) CO 2 Feed: as figure 1 shown, open the CO 2 Cylinder valve, liquefied CO 2 The high-pressure pump is continuously introduced into the high-pressure crystallization kettle of the supercritical fluid crystallization equipment system through the two symmetrical channels of the kettle head (60° to the intermediate solution channel), and the flow rate is controlled at 75mL / min;

[0041] 3) Control temperature and pressure: by regulating figure 1 The back pressure valve shown controls the press...

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Abstract

The invention discloses a preparation method for Itraconazole composite particles. Itraconazole composite particles can be prepared through a supercritical fluid crystallization equipment system; andthe composite particles can be prepared from dissolving 30-60 wt% of Itraconazole, 30-60 wt% of hydroxypropyl methylcellulose and 0-20 wt% of polyethylene glycol 6000 into a mixed solvent of dichloromethane / ethanol and performing supercritical fluid crystallization. The adjuvant materials used by the preparation method are all adjuvant materials in a commercial Itraconazole preparation Spirenol formula, and has no compatibility problems with the Itraconazole through full verification, so that the composition is safe, stable and effective; and methanol is not used during preparation, so that easier production amplification can be achieved, the yield in unit time can be higher, the dispersibility of obtained products can be better, and similarity factors of the prepared Itraconazole preparation and Itraconazole capsules are greater than 50, so that the Itraconazole preparation accords with consistency evaluation requirements.

Description

technical field [0001] The invention relates to a preparation method of itraconazole composite particles. Background technique [0002] Itraconazole is a triazole antifungal drug. Itraconazole has strong lipophilicity and is extremely difficult to dissolve in water. The saturated solubility of its aqueous solution at neutral pH value is less than 1ng / mL. The saturated solubility in solution is 6 μg / mL, and its oral bioavailability is determined by the dissolution rate of the drug in the gastrointestinal tract. Because itraconazole is poorly soluble in water, its dissolution rate in the gastrointestinal tract is low, and its oral bioavailability is low. Sporanox (SPORANOX, whose main component is itraconazole) injection, oral solution and capsule are currently commercialized itraconazole preparations. Injection and oral solution increase the solubility of itraconazole by complexing itraconazole with 2-hydroxypropyl-β-cyclodextrin, but 2-hydroxypropyl-β-cyclodextrin is mainl...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/496A61K47/38A61K47/10A61P31/10
CPCA61K9/1641A61K9/1652A61K9/1694A61K31/496
Inventor 洪江游孙永达刘贵金凌日金
Owner HAINAN HONZ PHARMA
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