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Updated: May 4, 2026
05:44
Formation of Dispersible Taohong Siwu Tablets
Published on: February 3, 2023
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Development of novel fast-dissolving tacrolimus solid dispersion-loaded prolonged release tablet.
Jung Hyun Cho1, Yong-Il Kim2, Dong-Wuk Kim3
1College of Pharmacy, Yeungnam University, 214-1, Dae-Dong, Gyongsan 712-749, South Korea.
Summary
Researchers developed a novel tacrolimus tablet with enhanced solubility and dissolution. This new prolonged-release tablet proved bioequivalent to the commercial capsule in beagle dogs.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
Background:
- Tacrolimus is an immunosuppressant with a narrow therapeutic index, requiring precise dose control.
- Existing sustained-release formulations aim to optimize tacrolimus pharmacokinetics, but novel approaches are needed for improved bioequivalence and patient compliance.
Purpose of the Study:
- To develop a novel prolonged-release tacrolimus tablet bioequivalent to a commercial sustained-release capsule.
- To enhance the solubility and dissolution properties of tacrolimus using fast-dissolving solid dispersions.
- To optimize tablet formulation for comparable pharmacokinetic profiles to the commercial product.
Main Methods:
- Preparation of tacrolimus-loaded fast-dissolving solid dispersions using spray drying with DOSS and HP-β-CD.
- Evaluation of solubility, dissolution, and pharmacokinetics in rats.
- Formulation of prolonged-release tablets using the optimized solid dispersion with varying ratios of HPMC and ethylcellulose.
- In vivo pharmacokinetic studies in beagle dogs comparing the developed tablet with a commercial capsule.
Main Results:
- DOSS significantly increased tacrolimus solubility and dissolution in solid dispersions.
- The optimized solid dispersion (tacrolimus/HP-β-CD/DOSS, 5:40:4) showed a 700-fold increase in solubility and a 30-fold increase in dissolution compared to drug powder.
- A specific tablet formulation (20:66:112:2 tacrolimus solid dispersion:HPMC:ethylcellulose:talc) demonstrated a similar dissolution profile to the commercial capsule.
- Pharmacokinetic studies in beagle dogs revealed no significant differences in AUC, Cmax, Tmax, and MRT between the developed tablet and the commercial capsule.
Conclusions:
- The developed tacrolimus-loaded prolonged-release tablet, utilizing a fast-dissolving solid dispersion, is a promising alternative to commercial sustained-release capsules.
- The formulation achieved bioequivalence, suggesting improved drug delivery and potentially better therapeutic outcomes.
- This novel tablet formulation offers a viable option for tacrolimus delivery, potentially enhancing patient adherence and treatment efficacy.
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