Food Engineering Progress (산업식품공학)

Korean Society for Industrial Food Engineering (한국산업식품공학회)
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Oral Bioavailability for Sub-micron Particle Curcumin (TheracurminCR-033P) and Absorption Rate by Product Composition in Healthy Human Volunteers

서브마이크론 입자 형태 커큐민의 생체 흡수율 및 제품 조성에 따른 흡수율 동등성 연구

  • 박희정 (국민대학교 식품영양학과) ;
  • ;
  • Received : 2017.06.28
  • Accepted : 2017.08.18
  • Published : 2017.08.31
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Abstract

Curcumin have various health-beneficial properties in numerous studies. However, its bioavailability is low due to its limited intestinal uptake and rapid metabolism. This study aimed to evaluate the pharmacokinetics of newly developed sub-micron particle curcumin with increased water dispersibility (Theracurmin(R) CR-033P). Plasma curcumin levels were measured at 0, 1, 2, 4, 8 h after Theracurmin(R) CR-033P intake using high-performance liquid chromatography. For analyzing pharmacokinetics of Theracurmin(R) CR-033P, eighteen healthy subjects were recruited and received Theracurmin(R) CR-033P at a single oral dose containing curcumin 30 mg. $C_{max}$ was 28.14 ng/ml, and the area under the curve for 8 h was estimated to be 104.36 ng/ml. Based on the area under the plasma concentration (AUC), the bioavailability of sub-micron particle curcumin was higher 22-, 35-, 28-fold than native curcumin in men, women, and all subjects, respectively. For comparing by formulation, seven healthy subjects were recruited and received two type of treatment: (1) existing dosage form 300 mg (contained curcumin 30 mg) ${\times}$ 3 capsule, (2) high dosage form 300 mg (contained curcumin 90 mg) ${\times}$ 1 capsule + placebo 300 mg ${\times}$ 2 capsule. In the cross-over study, there was no significant differences in $C_{max}$ and AUC of plasma curcumin. In conclusion, submicron particle curcumin with increased water dispersibility significantly improved its oral bioavailability and women absorbed curcumin more effectively than men. Different formulation of Theracurmin(R) CR-033P has shown equivalent to the reference in terms of pharmacokinetics.

커큐민 분말은 항산화 및 항염증 등의 생리활성을 내세우며, 건강기능식품 및 일반식품의 마케팅 포인트로 광범위하게 사용되고 있다. 커큐민의 낮은 체내 흡수율은 생리적 기능성에도 영향을 미칠것으로 사료되어 리포좀 형태나 인지질 결합 형태로 커큐민의 제형 개발이 활발이 진행되고 있다. 본 연구에서는 커큐민의 체내 흡수율을 높이고, 실제 산업에의 활용도를 높이기 위해 커큐민을 서브마이크론 입자 형태의 제형으로 개발하여, 일반 커큐민 형태와의 흡수율을 비교해보고자 하였다. 본 연구 결과, 일반 커큐민 보다 서브마이크론 입자 형태 커큐민의 체내 흡수율이 남녀 평균 28배 더 높게 나타났다. 서브마이크론 입자 형태 커큐민의 체내 흡수율은 성별에 따라 다르게 나타났으며, 남성의 경우는 22배, 여성의 경우는 35배 흡수율이 높게 나타났다. 편의성을 증진시킨 농축제제와 기존 제제의 흡수율은 $C_{max}$ 값이 각각 166.0과 177.7로 통계적 유의성이 나타나지 않았다. 단회 투여 후 8시간 동안의 AUC 값 역시 약 952와 약 849로 나타나 제제의 동등성에서 유의적인 차이는 없었다. 결론적으로, 본 연구를 통해 일반 커큐민 보다 서브마이크론 입자 형태 커큐민의 체내 흡수율이 남녀 평균 약 28배 증진되는 것으로 확인되었으며, 편의성을 증진시킨 농축제제와 일반 제제의 흡수율이 거의 동일하게 나타났다.

Keywords

Acknowledgement

Supported by : (주)한독

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