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New tablet formulation of tacrolimus with smaller interindividual variability may become a better treatment option than the conventional capsule formulation in organ transplant patients.

ABSTRACT: To evaluate the pharmacokinetic (PK) and tolerability profiles of a new tablet formulation of tacrolimus and its interindividual variability (IIV) in the systemic exposure, and to compare them with those of the conventional capsule formulation, a randomized, open-label, two-treatment, two-period, two-sequence, crossover study was performed in 47 healthy males. The capsule or tablet formulation of tacrolimus was orally administered, and serial blood samples were collected up to 96 hours after dosing. Whole-blood tacrolimus concentration was determined using liquid chromatography-tandem mass spectrometry. The maximum whole-blood tacrolimus concentration (Cmax) and the area under the whole-blood tacrolimus concentration-time curve from 0 hour to the last quantifiable concentration (AUClast) were compared between the two formulations. The similarity factor (f2) of the in vitro dissolution profiles was calculated. The geometric mean ratio (90% confidence interval) of tablet to capsule was 0.9680 (0.8873-1.0560) and 1.0322 (0.9359-1.1385) for Cmax and AUClast, respectively. The IIV of Cmax and AUClast of the tablet was smaller than the capsule. The f2 values were >50 in all media. Both formulations were well tolerated. Thus, the tablet formulation of tacrolimus has smaller IIV in the systemic exposure than capsule, while having comparable PK and tolerability profiles, which may render it as a better treatment option for organ transplant patients.

SUBMITTER: Kim YK

PROVIDER: S-EPMC5628684 | biostudies-literature | 2017

REPOSITORIES: biostudies-literature

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New tablet formulation of tacrolimus with smaller interindividual variability may become a better treatment option than the conventional capsule formulation in organ transplant patients.

Kim Yu Kyong YK Kim Anhye A Park Shin Jung SJ Lee Howard H

Drug design, development and therapy 20170928

To evaluate the pharmacokinetic (PK) and tolerability profiles of a new tablet formulation of tacrolimus and its interindividual variability (IIV) in the systemic exposure, and to compare them with those of the conventional capsule formulation, a randomized, open-label, two-treatment, two-period, two-sequence, crossover study was performed in 47 healthy males. The capsule or tablet formulation of tacrolimus was orally administered, and serial blood samples were collected up to 96 hours after dos ...[more]

PMID: 29033547

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Project description:Fast-track surgery (FTS), a multimodal rehabilitation technique, has been recommended as surgical therapy for colorectal cancer. The objective of the present study was to compare the outcomes of FTS and conventional laparoscopic surgery. This study was a blinded randomized trial. A total of 70 patients with colorectal cancer were divided into two groups and underwent laparoscopic colorectal resection. The FTS group consisted of 31 patients and the control group consisted of 39 patients. Protocols for the treatment of the FTS group included skipping pre-operative mechanical bowel preparation, early restoration of diet and early post-operative ambulation. Outcome measures, length of hospital stay, post-operative surgical stress response [C-reactive protein (CRP)] and post-operative complications were compared between the two groups. The average length of total hospital stay for the FTS and the control groups was 5.9±0.8 and 10.9±1.3 days, respectively (P<0.05), and the length of post-operative hospital stay for the FTS and control group was 4.3±0.8 and 8.0±1.1 days, respectively. (P<0.05) First flatus time for the FTS and control groups was 1.6±0.8 and 2.5±0.9 days, respectively (P<0.05). Defecation time for the FTS and control groups was 2.2±0.7 and 4.5±0.7 days, respectively (P<0.05). The time to restoration of a solid diet also showed a significant difference between the FTS and control groups (1.1±0.3 vs. 3.6±0.9 days; P<0.05). Following surgery, due to post-operative surgical stress, the two groups CRP levels increased significantly, but the levels of the FTS group were lower than those of the conventional control group (P<0.05). There was no difference in post-operative complications between the FTS and control groups. This study confirms that FTS shortens hospital stay and accelerates the recovery of bowel function without increase of post-operative complications. FTS is safe, improves post-operative recovery and is a better option than conventional laparoscopic surgery for treating colorectal cancer patients.

Dataset Information

New tablet formulation of tacrolimus with smaller interindividual variability may become a better treatment option than the conventional capsule formulation in organ transplant patients.

Publications

New tablet formulation of tacrolimus with smaller interindividual variability may become a better treatment option than the conventional capsule formulation in organ transplant patients.

Similar Datasets

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