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A novel pH-enzyme-dependent mesalamine colon-specific delivery system.

Jin L, Ding YC, Zhang Y, Xu XQ, Cao Q - Drug Des Devel Ther (2016)

Bottom Line: In vitro, a small amount of mesalamine was released in HCl at a pH of 1.2 and PBS medium at a pH of 7.4 for 5 hours, and 71% of the entrapped mesalamine was further released during the subsequent 20 hours of incubation.The AUC0-t of the coated microparticles in colon was 2.63-fold higher compared to the suspensions (P<0.05).Hence, mesalamine-coated microparticles are considered to maintain the drug concentration within target ranges for a long period of time.

View Article: PubMed Central - PubMed

Affiliation: Department of Gastroenterology, Putuo Hospital, Shanghai University of Traditional Chinese Medicine, Shanghai, People's Republic of China.

ABSTRACT
The aim of the present study was to design a new pH-enzyme double-dependent mesalamine colon-specific delivery system. The drug release behaviors in vitro and pharmacokinetics and biodistribution in vivo were further evaluated. The mean particle diameters of mesalamine-coated microparticles were 312.2 µm. In vitro, a small amount of mesalamine was released in HCl at a pH of 1.2 and PBS medium at a pH of 7.4 for 5 hours, and 71% of the entrapped mesalamine was further released during the subsequent 20 hours of incubation. A greater area under the plasma concentration-time curve (AUC)0-t was obtained for the coated microparticles (1.9-fold) compared to the suspensions group, which indicated that the encapsulated mesalamine had mostly been absorbed in rats over the period of 12 hours. The AUC0-t of the coated microparticles in colon was 2.63-fold higher compared to the suspensions (P<0.05). Hence, mesalamine-coated microparticles are considered to maintain the drug concentration within target ranges for a long period of time.

No MeSH data available.


Related in: MedlinePlus

Distribution of drugs in tissues of mice following intragastric administration of a single 10 mg/kg dose of mesalamine-coated microparticles and mesalamine suspensions.Notes: Each point represents mean ± SD of six rats. The solid lines indicate mesalamine-coated microparticles and the dotted lines indicate mesalamine suspensions.Abbreviation: SD, standard deviation.
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f4-dddt-10-2021: Distribution of drugs in tissues of mice following intragastric administration of a single 10 mg/kg dose of mesalamine-coated microparticles and mesalamine suspensions.Notes: Each point represents mean ± SD of six rats. The solid lines indicate mesalamine-coated microparticles and the dotted lines indicate mesalamine suspensions.Abbreviation: SD, standard deviation.

Mentions: Both mesalamine-coated microparticles and mesalamine suspensions were taken up by the stomach, small intestine, and colon of mice. Figure 4 reflects the tissue distribution results in samples taken 1, 4, 8, 12, and 24 hours after intragastric administration of single mesalamine preparations to mice. The total amount of drug accumulated in each organ within 24 hours (AUC0–t) was calculated, and the results are shown in Table 2. The results showed that the maximum concentration of mesalamine (9.6 µg/M) was observed in small intestine after 8 hours of intragastric administration of suspensions, and a small amount reached the colon (Figure 4). Only a 3.1 µg/mL concentration of drug was measured in colon after 24 hours.


A novel pH-enzyme-dependent mesalamine colon-specific delivery system.

Jin L, Ding YC, Zhang Y, Xu XQ, Cao Q - Drug Des Devel Ther (2016)

Distribution of drugs in tissues of mice following intragastric administration of a single 10 mg/kg dose of mesalamine-coated microparticles and mesalamine suspensions.Notes: Each point represents mean ± SD of six rats. The solid lines indicate mesalamine-coated microparticles and the dotted lines indicate mesalamine suspensions.Abbreviation: SD, standard deviation.
© Copyright Policy
Related In: Results  -  Collection

License 1 - License 2
Show All Figures
getmorefigures.php?uid=PMC4920224&req=5

f4-dddt-10-2021: Distribution of drugs in tissues of mice following intragastric administration of a single 10 mg/kg dose of mesalamine-coated microparticles and mesalamine suspensions.Notes: Each point represents mean ± SD of six rats. The solid lines indicate mesalamine-coated microparticles and the dotted lines indicate mesalamine suspensions.Abbreviation: SD, standard deviation.
Mentions: Both mesalamine-coated microparticles and mesalamine suspensions were taken up by the stomach, small intestine, and colon of mice. Figure 4 reflects the tissue distribution results in samples taken 1, 4, 8, 12, and 24 hours after intragastric administration of single mesalamine preparations to mice. The total amount of drug accumulated in each organ within 24 hours (AUC0–t) was calculated, and the results are shown in Table 2. The results showed that the maximum concentration of mesalamine (9.6 µg/M) was observed in small intestine after 8 hours of intragastric administration of suspensions, and a small amount reached the colon (Figure 4). Only a 3.1 µg/mL concentration of drug was measured in colon after 24 hours.

Bottom Line: In vitro, a small amount of mesalamine was released in HCl at a pH of 1.2 and PBS medium at a pH of 7.4 for 5 hours, and 71% of the entrapped mesalamine was further released during the subsequent 20 hours of incubation.The AUC0-t of the coated microparticles in colon was 2.63-fold higher compared to the suspensions (P<0.05).Hence, mesalamine-coated microparticles are considered to maintain the drug concentration within target ranges for a long period of time.

View Article: PubMed Central - PubMed

Affiliation: Department of Gastroenterology, Putuo Hospital, Shanghai University of Traditional Chinese Medicine, Shanghai, People's Republic of China.

ABSTRACT
The aim of the present study was to design a new pH-enzyme double-dependent mesalamine colon-specific delivery system. The drug release behaviors in vitro and pharmacokinetics and biodistribution in vivo were further evaluated. The mean particle diameters of mesalamine-coated microparticles were 312.2 µm. In vitro, a small amount of mesalamine was released in HCl at a pH of 1.2 and PBS medium at a pH of 7.4 for 5 hours, and 71% of the entrapped mesalamine was further released during the subsequent 20 hours of incubation. A greater area under the plasma concentration-time curve (AUC)0-t was obtained for the coated microparticles (1.9-fold) compared to the suspensions group, which indicated that the encapsulated mesalamine had mostly been absorbed in rats over the period of 12 hours. The AUC0-t of the coated microparticles in colon was 2.63-fold higher compared to the suspensions (P<0.05). Hence, mesalamine-coated microparticles are considered to maintain the drug concentration within target ranges for a long period of time.

No MeSH data available.


Related in: MedlinePlus