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Burst release-free irinotecan microsphere and preparation method thereof

A technology of irinotecan and effect, which is applied in the direction of medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas. It can solve the problems of short drug effect time, short half-life, and poor water solubility, and achieve the appearance Uniformity, extended dosing interval, pain-reducing effects

Inactive Publication Date: 2015-02-18
HEBEI UNIVERSITY OF SCIENCE AND TECHNOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, it has poor water solubility, short half-life and poor biocompatibility
At present, irinotecan is mostly administered by injection, but its short duration of drug effect and large side effects have become problems that have plagued people for a long time.

Method used

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  • Burst release-free irinotecan microsphere and preparation method thereof
  • Burst release-free irinotecan microsphere and preparation method thereof
  • Burst release-free irinotecan microsphere and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] 200mg irinotecan and 5.0g PLGA were co-dissolved in 25mL dichloromethane as the oil phase; 2.5g PVA was dissolved in 250mL distilled water as the water phase; the oil phase was slowly added to the water phase under the treatment of a high-shear dispersing emulsifier to form Milky dispersion system, the ratio of oil phase to water phase is 1:10, the speed of high shear dispersing emulsifier is 8000rpm, and the stirring time is 30s. The organic solvent was evaporated by rotary steaming at 30°C for 50 minutes, and the irinotecan microspheres were collected after washing with low-temperature high-speed centrifugation.

Embodiment 2

[0018] 200mg of irinotecan and 6.0g of PLGA were co-dissolved in 30mL of dichloromethane as the oil phase; 3.0g of PVA was dissolved in 300mL of distilled water as the water phase; the oil phase was slowly added to the water phase under the treatment of a high-shear dispersing emulsifier to form an emulsion Cloudy dispersion system, the ratio of oil phase to water phase is 1:10, the speed of high shear dispersing emulsifier is 8000rpm, and the stirring time is 30s. The organic solvent was evaporated by rotary steaming at 30°C for 50 minutes, and the irinotecan microspheres were collected after washing with low-temperature high-speed centrifugation.

Embodiment 3

[0020] 200mg irinotecan and 7.0g PLGA were co-dissolved in 35mL dichloromethane as the oil phase; 3.5gPVA was dissolved in 350mL distilled water as the water phase; the oil phase was slowly added to the water phase under the treatment of a high-shear dispersing emulsifier to form an emulsion Cloudy dispersion system, the ratio of oil phase to water phase is 1:10, the speed of high shear dispersing emulsifier is 8000rpm, and the stirring time is 30s. The organic solvent was evaporated by rotary steaming at 30°C for 50 minutes, and the irinotecan microspheres were collected after washing with low-temperature high-speed centrifugation.

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Abstract

The invention discloses a burst release-free irinotecan microsphere and a preparation method thereof. The irinotecan microsphere comprises irinotecan and a polylactic acid-glycolic acid copolymer (poly(lactic-co-glycolicacid), PLGA), wherein the weight ratio of the irinotecan to the PLGA is 1 to (10-40), and the grain size of the irinotecan microsphere is 1-5 micrometers. A long-acting burst release-free irinotecan microsphere can be prepared from the irinotecan and the PLGA at a specific ratio, and the slow release period of the irinotecan microsphere is longer than 40 days, so the medication frequency is obviously reduced, a peak and valley phenomenon of the medicine is reduced, the bioavailability of the irinotecan is improved and toxic and side effects of the medicine are reduced.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to an irinotecan microsphere without burst release effect and a preparation method thereof. Background technique [0002] Irinotecan (CPT-11) is a semi-synthetic camptothecin derivative, which is a light yellow or yellow loose substance or powder. tumor effect. Clinically, it is a commonly used broad-spectrum antineoplastic drug, and it is the first-line drug for the clinical treatment of recurrence and deterioration of colorectal cancer, and has certain curative effects on small cell and non-small cell lung cancer, breast cancer, ovarian cancer, gastric cancer, etc. However, it has poor water solubility, short half-life and poor biocompatibility. At present, irinotecan is mostly administered by injection, but its short duration of drug effect and large side effects have become a problem that has plagued people for a long time. The invention adopts PLGA as a carrier mat...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/4745A61K47/34A61P35/00
Inventor 高子彬马楠张丽男薛娇杨晓月车斌齐献利石梦谢英花孙勇军吴韶梅
Owner HEBEI UNIVERSITY OF SCIENCE AND TECHNOLOGY
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