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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.


Plasma concentration–time profiles of mesalamine in rats after oral administration of mesalamine-coated microparticles and mesalamine suspensions (n=6).
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f3-dddt-10-2021: Plasma concentration–time profiles of mesalamine in rats after oral administration of mesalamine-coated microparticles and mesalamine suspensions (n=6).

Mentions: Plasma concentration–time profiles of mesalamine after oral administration of mesalamine-coated microparticles and mesalamine suspensions are shown in Figure 3. Pharmacokinetic parameters are shown in Table 1. As shown in Figure 3, drug plasma concentration reached a higher level (more than 12 µg/mL) in the initial 2 hours after oral administration of mesalamine suspensions. The half-life of the suspensions (2.8 hours) was shorter than that of the coated microparticles (16.2 hours), suggesting that the suspensions were taken up by other tissues more rapidly than coated microparticles. A greater AUC0–t was obtained for the coated microparticles (1.9-fold) compared to the suspensions, which indicated that the encapsulated mesalamine had mostly been absorbed over the period of 12 hours. The clearance of coated microparticles was 5.1 L/h, smaller than that (21.3 L/h) of the suspensions.


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)

Plasma concentration–time profiles of mesalamine in rats after oral administration of mesalamine-coated microparticles and mesalamine suspensions (n=6).
© Copyright Policy
Related In: Results  -  Collection

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

f3-dddt-10-2021: Plasma concentration–time profiles of mesalamine in rats after oral administration of mesalamine-coated microparticles and mesalamine suspensions (n=6).
Mentions: Plasma concentration–time profiles of mesalamine after oral administration of mesalamine-coated microparticles and mesalamine suspensions are shown in Figure 3. Pharmacokinetic parameters are shown in Table 1. As shown in Figure 3, drug plasma concentration reached a higher level (more than 12 µg/mL) in the initial 2 hours after oral administration of mesalamine suspensions. The half-life of the suspensions (2.8 hours) was shorter than that of the coated microparticles (16.2 hours), suggesting that the suspensions were taken up by other tissues more rapidly than coated microparticles. A greater AUC0–t was obtained for the coated microparticles (1.9-fold) compared to the suspensions, which indicated that the encapsulated mesalamine had mostly been absorbed over the period of 12 hours. The clearance of coated microparticles was 5.1 L/h, smaller than that (21.3 L/h) of the suspensions.

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.