Supersaturable self-microemulsifying drug delivery system enhances dissolution and bioavailability of telmisartan
- Authors
- Park, Sun Young; Jin, Chang Hwa; Goo, Yoon Tae; Chae, Bo Ram; Yoon, Ho Yub; Kim, Chang Hyun; Song, Seh Hyon; Han, Sang Beom; Choi, Young Wook
- Issue Date
- Jan-2021
- Publisher
- TAYLOR & FRANCIS LTD
- Keywords
- Telmisartan; supersaturable self-microemulsifying drug delivery system (SuSMEDDS); precipitation inhibitor; Soluplus; dissolution; bioavailability
- Citation
- PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY, v.26, no.1, pp 60 - 68
- Pages
- 9
- Journal Title
- PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY
- Volume
- 26
- Number
- 1
- Start Page
- 60
- End Page
- 68
- URI
- https://scholarworks.bwise.kr/cau/handle/2019.sw.cau/47708
- DOI
- 10.1080/10837450.2020.1834580
- ISSN
- 1083-7450
1097-9867
- Abstract
- To enhance the dissolution and oral bioavailability of telmisartan (TMS), a poorly water-soluble anti-hypertensive drug, a supersaturable self-microemulsifying drug delivery system (SuSMEDDS) was developed. Amorphous alkalinized TMS (AAT) was formulated into a SMEDDS, composed of Capmul (R) MCM (oil), Cremophor(R)RH40 (surfactant), and tetraglycol (co-surfactant). Although the SMEDDS was rapidly dissolved (>80% within 5 min) in a limited condition (500 mL, pH 6.8), drug precipitation was observed over time, resulting in a decrease in dissolution levels. The precipitation was due to drug recrystallization, as determined by differential scanning calorimetry and powder X-ray diffraction analyses. Several polymers, including Soluplus(R)(SOL), were screened as precipitation inhibitors; ultimately, SuSMEDDS-SOL was prepared by admixing SOL and the SMEDDS at a 5:100 (w/w) ratio. SuSMEDDS-SOL was superior in terms of dissolution efficiency (>90% over 2 h) and dissolution-retaining time (no precipitation over 2 h). Anin vivopharmacokinetic study in rats revealed that the oral bioavailability of SuSMEDDS-SOL was 4.8-, 1.3-, and 1.2-fold greater than those of the TMS suspension, AAT solution, and SMEDDS, respectively. Therefore, SuSMEDDS-SOL is a promising candidate to enhance the dissolution and oral bioavailability of TMS.
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Collections - College of Pharmacy > School of Pharmacy > 1. Journal Articles
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