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Development and evaluation of dexibuprofen formulation with fast onset and prolonged effect.
Drug Dev Ind Pharm. 2019 Jun; 45(6):895-904.DD

Abstract

In the present study, in order to improve the solubility and bioavailability of poorly water-soluble dexibuprofen, a novel dexibuprofen-loaded solid dispersion was developed using the spray-drying technique. The controlled-release dexibuprofen formulation was developed by combining the immediate-release dispersion powder and the sustained-release formula. The solid dispersion composed of dexibuprofen/poloxamer 407/hydroxypropyl methylcellulose (HPMC) 2910 (50 cps)/sodium lauryl sulfate (SLS) (10/1/4/0.1 mg) was selected as the immediate-release formulation due to its increased solubility and dissolution rate. This immediate-release formulation showed a significantly higher initial plasma concentration, AUC, and Cmax of dexibuprofen than those of dexibuprofen powder. Based on the prolonged effect of high plasma concentration, the formulation consisting of dexibuprofen/ethylcellulose/HPMC 2910 (4000 cps)/magnesium stearate (66/16.5/16.5/1 mg) was selected as the sustained-release formulation. Finally, the controlled-release (CR) formulation was prepared by encapsulating the immediate-release and sustained-release formulations in hard gelatin capsules. The proposed CR formulation showed enhanced AUC (5.5-fold) and Cmax (3.5-fold) compared to dexibuprofen powder. The results of the present study suggest that the CR formulation containing dexibuprofen may be a potential oral dosage form for a fast onset and a prolonged effect of poorly water-soluble dexibuprofen.

Authors+Show Affiliations

a College of Pharmacy , Seoul National University , Seoul , Republic of Korea.b College of Pharmacy and Inje Institute of Pharmaceutical Sciences and Research , Inje University , Republic of Korea.a College of Pharmacy , Seoul National University , Seoul , Republic of Korea.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

30889990

Citation

Choi, Yoonho, et al. "Development and Evaluation of Dexibuprofen Formulation With Fast Onset and Prolonged Effect." Drug Development and Industrial Pharmacy, vol. 45, no. 6, 2019, pp. 895-904.
Choi Y, Min KA, Kim CK. Development and evaluation of dexibuprofen formulation with fast onset and prolonged effect. Drug Dev Ind Pharm. 2019;45(6):895-904.
Choi, Y., Min, K. A., & Kim, C. K. (2019). Development and evaluation of dexibuprofen formulation with fast onset and prolonged effect. Drug Development and Industrial Pharmacy, 45(6), 895-904. https://doi.org/10.1080/03639045.2019.1576720
Choi Y, Min KA, Kim CK. Development and Evaluation of Dexibuprofen Formulation With Fast Onset and Prolonged Effect. Drug Dev Ind Pharm. 2019;45(6):895-904. PubMed PMID: 30889990.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Development and evaluation of dexibuprofen formulation with fast onset and prolonged effect. AU - Choi,Yoonho, AU - Min,Kyoung Ah, AU - Kim,Chong-Kook, Y1 - 2019/03/19/ PY - 2019/3/21/pubmed PY - 2019/9/3/medline PY - 2019/3/21/entrez KW - HPMC KW - Pain reliever KW - controlled release KW - dexibuprofen KW - solid dispersion KW - spray drying SP - 895 EP - 904 JF - Drug development and industrial pharmacy JO - Drug Dev Ind Pharm VL - 45 IS - 6 N2 - In the present study, in order to improve the solubility and bioavailability of poorly water-soluble dexibuprofen, a novel dexibuprofen-loaded solid dispersion was developed using the spray-drying technique. The controlled-release dexibuprofen formulation was developed by combining the immediate-release dispersion powder and the sustained-release formula. The solid dispersion composed of dexibuprofen/poloxamer 407/hydroxypropyl methylcellulose (HPMC) 2910 (50 cps)/sodium lauryl sulfate (SLS) (10/1/4/0.1 mg) was selected as the immediate-release formulation due to its increased solubility and dissolution rate. This immediate-release formulation showed a significantly higher initial plasma concentration, AUC, and Cmax of dexibuprofen than those of dexibuprofen powder. Based on the prolonged effect of high plasma concentration, the formulation consisting of dexibuprofen/ethylcellulose/HPMC 2910 (4000 cps)/magnesium stearate (66/16.5/16.5/1 mg) was selected as the sustained-release formulation. Finally, the controlled-release (CR) formulation was prepared by encapsulating the immediate-release and sustained-release formulations in hard gelatin capsules. The proposed CR formulation showed enhanced AUC (5.5-fold) and Cmax (3.5-fold) compared to dexibuprofen powder. The results of the present study suggest that the CR formulation containing dexibuprofen may be a potential oral dosage form for a fast onset and a prolonged effect of poorly water-soluble dexibuprofen. SN - 1520-5762 UR - https://www.unboundmedicine.com/medline/citation/30889990/Development_and_evaluation_of_dexibuprofen_formulation_with_fast_onset_and_prolonged_effect_ DB - PRIME DP - Unbound Medicine ER -