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Oral solid formulation containing irinotecan and method of preparing the same

a solid formulation and oral technology, applied in the field of oral solid formulations containing irinotecan, can solve the problems of severe diarrhea, extreme suppression of the immune system, adverse effects of irinotecan, etc., and achieve the effects of improving bioavailability, high stability with time, and increasing the dissolution rate of active ingredients

Inactive Publication Date: 2021-10-28
HANMI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The present invention is about an oral solid formulation containing irinotecan which has improved absorption and stability. This is achieved by adding an acidifying agent which increases the dissolution rate of the active ingredient. The formulation has reduced side effects and is effective through oral administration.

Problems solved by technology

Irinotecan has adverse effects such as severe diarrhea and extreme suppression of the immune system.

Method used

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  • Oral solid formulation containing irinotecan and method of preparing the same
  • Oral solid formulation containing irinotecan and method of preparing the same
  • Oral solid formulation containing irinotecan and method of preparing the same

Examples

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Comparison scheme
Effect test

examples 1 to 3

Tablets Including Acidifying Agent (1)

[0056]Irinotecan hydrochloride trihydrate (Dongwoo Fine-Chem, Korea), lactose, and microcrystalline cellulose were mixed together (pre-mixing) according to the compositions of Table 1, followed by adding a binding solution which was acidified by adding and dissolving citric acid, lactic acid, or acetic acid added as an acidifying agent in a binding solution of povidone dissolved in a mixture of ethanol and water (7:3) to the mixture, granulating, drying, and sieving with a 20-mesh sieve, to thereby prepare irinotecan wet granules.

[0057]Croscarmellose sodium was then added to the obtained irinotecan wet granules and mixed (mixing) together, followed by adding magnesium stearate to the mixture, mixing the mixture together (final mixing), and tableting the final mixture with a rotary tablet press (GRC-18, available from Sejong Pharmatech Co., Ltd., Korea) to form tablets having a hardness of about 5 to about 12 kp.

TABLE 1Amount (mg)IngredientExampl...

examples 4 to 6

ts Including Different Amounts of Acidifying Agent

[0058]Tablets of Examples 4 to 6 were prepared in the same manner as in Example 1, according to the compositions of Table 2, except that different amounts of citric acid were used as an acidifying agent.

TABLE 2Amount (mg)IngredientExample 4Example 5Example 6Pre-Irinotecan21.7321.7321.73mixinghydrochloridetrihydrateLactose42.0042.0042.00Microcrystalline104.20109.20114.20celluloseBindingPovidone6.006.006.00solutionCitric acid15.0010.005.00Ethanol / water(40.00)(40.00)(40.00)MixingCroscarmellose10.0010.0010.00sodiumFinalMagnesium2.002.002.00mixingstearateTotal weight200.93200.93200.93

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PUM

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Abstract

An oral solid formulation includes irinotecan or a pharmaceutically acceptable salt thereof as an active ingredient, and an acidifying agent. A method of preparing an oral solid formulation includes forming granules containing irinotecan or a pharmaceutically acceptable salt thereof, a diluent, and a binder, mixing the granules with a disintegrant and a lubricant to obtain a mixture, and includes adding an acidifying agent in step of forming granules and / or mixing the granules.

Description

CROSS REFERENCE TO RELATED APPLICATIONS[0001]This application is a Continuation of U.S. application Ser. No. 15 / 735,313 filed Dec. 11, 2017 (allowed), which is National Stage of International Application No. PCT / KR2016 / 006513 filed Jun. 20, 2016, claiming priority based on Korean Patent Application No. 10-2015-0093413 filed Jun. 30, 2015, the contents of all of which are incorporated herein by reference in their entirety.TECHNICAL FIELD[0002]The present disclosure relates to an oral solid formulation containing irinotecan and a method of preparing the same, and more particularly, to an oral solid formulation containing irinotecan with improved bioavailability and stability, and a method of preparing the same.BACKGROUND ART[0003]Irinotecan, a semisynthetic analog of camptothecin, is used as a cancer chemotherapeutic agent mainly against metastatic colorectal cancers. Irinotecan with the chemical name of (5)-4,11-diethyl-3,4,12,14-tetrahydro-4-hydroxy-3,14-dioxo-1H-pyrano[3′,4′:6,7]-i...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/4745A61K9/20A61P35/00A61K9/16A61K47/12A61K47/20
CPCA61K31/4745A61K9/2013A61K9/2054A61K9/2018A61K9/2027A61K9/4858A61K9/1617A61K9/1682A61K47/12A61K47/20A61P35/00A61K9/16A61K9/20A61K9/48A61K2300/00
Inventor PARK, CALEB HYUNG MINJUNG, MYEONG KIKIM, JIN CHEULKIM, YONG ILPARK, JAE HYUNWOO, JONG SOO
Owner HANMI PHARMA
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