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전임교원이 최근 5년간 출판한 논문 중, 연도별 카테고리별 피인용 상위 1%에 달성된 논문
매월 1회 업데이트

SCIE Article

Improved Bioavailability and High Photostability of Methotrexate by Spray-Dried Surface-Attached Solid Dispersion with an Aqueous Medium

Author

[Giri, Bhupendra Raj; Kim, Dong Wuk] Kyungpook Natl Univ, FOUR Community Based Intelligent Novel Drug Disco, Vessel Organ Interact Res Ctr VOICE, Coll Pharm,Res Inst Pharmaceut Sci,MRC, Daegu 41566, South Korea; [Kim, Jung Suk; Park, Jong Hyuck; Choi, Han

Corresponding Author Info

Prof. Choi, Han Gon(약학과 최한곤 교수

Professor

E-mail

hangon@hanyang.ac.kr

Document Type

Source

PHARMACEUTICS 2021, 13, 1,

Times Cited

10(2022.2.21.)

External Information

10.3390/pharmaceutics13010111

Abstract

History]
- 7월/8월 2021부로, 이 인용 빈도가 높은 논문의 인용 횟수가 분야와 출판 연도에 대해 인용 빈도가 높은 임계값을 기반으로 Pharmacology & Toxicology Science 관련 학술 분야에서 상위 1%에 올랐습니다.

[Abstract]
Low aqueous solubility and poor bioavailability are major concerns in the development of oral solid-dosage drug forms. In this study, we fabricated surface-attached solid dispersion (SASD) to enhance the solubility, bioavailability, and photostability of methotrexate (MTX), a highly lipophilic and photo-unstable drug. Several MTX-loaded SASD formulations were developed for spray-drying using water as the solvent, and were investigated for their aqueous solubility and dissolution kinetics. An optimized ternary SASD formulation composed of MTX/ sodium carboxymethyl cellulose (Na-CMC)/sodium lauryl sulfate (SLS) at 3/0.5/0.5 (w/w) had 31.78-fold and 1.88-fold higher solubility and dissolution, respectively, than MTX powder. For SASD, the in vivo pharmacokinetic parameters AUC and C-max were 2.90- and 3.41-fold higher, respectively, than for the MTX powder. Solid-state characterizations by differential scanning calorimetry and X-ray diffraction revealed that MTX exists in its crystalline state within the spray-dried SASD. The MTX-loaded SASD formulation showed few physical changes with photostability testing. Overall, the results indicate that the spray-dried MTX-loaded SASD formulation without organic solvents enhances the solubility and oral bioavailability of MTX without a significant deterioration of its photochemical stability.

Web of Science Categories

Pharmacology & Pharmacy

Funding

National Research Foundation of Korea (NRF) - Korea government [2018R1D1A1B07050598, 2020R1A5A2017323]

Language

English

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