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In situ and in vivo study of nasal absorption of paeonol in rats.

Chen X, Lu Y, Du S, Xu B, Wang S, Zhai Y, Song X, Li P - Int J Mol Sci (2010)

Bottom Line: In vivo studies of paeonol absorption were carried out in rats and the pharmacokinetics parameters of intranasal (i.n.) and intragastric (i.g.) administration were compared with intravenous (i.v.) administration.MRT (Mean Residence Time) were 23.19 ± 6.46 min, 41.49 ± 2.96 min and 23.09 ± 5.88 min for i.n., i.g. and i.v. methods, respectively.The results demonstrate that paeonol could be absorbed promptly and thoroughly by i.n. administration in rats.

View Article: PubMed Central - PubMed

Affiliation: School of Chinese Materia Medica, Beijing University of Chinese Medicine, No.6, Zhonghuan South Road, Wangjing, Chaoyang district, Beijing 100102, China; E-Mails: chenxiaolan76@126.com (X.C.); landocean88126.com (Y.L.); dushouying@263.net (S.D.).

ABSTRACT
The objective of this work was to study the in situ and in vivo nasal absorption of paeonol. A novel single pass in situ nasal perfusion technique was applied to examine the rate and extent of nasal absorption of paeonol by rats. Various experimental conditions, such as perfusion rate, pH, osmotic pressure and drug concentration, were investigated. The in situ experiments showed that the nasal absorption of paeonol was not dependent on drug concentration, and fitted a first order process. The absorption rate constant, Ka, increased with an increase in perfusion speed. Paeonol was better absorbed in acidic solutions than in neutral or alkaline solutions. The value of Ka was higher in a hypertonic environment than under isotonic or hypotonic conditions. In vivo studies of paeonol absorption were carried out in rats and the pharmacokinetics parameters of intranasal (i.n.) and intragastric (i.g.) administration were compared with intravenous (i.v.) administration. The bioavailabilities of paeonol were 52.37% and 15.81% for i.n. and i.g, respectively, while T(max) values were 3.05 ± 1.46 min and 6.30 ± 0.70 min. MRT (Mean Residence Time) were 23.19 ± 6.46 min, 41.49 ± 2.96 min and 23.09 ± 5.88 min for i.n., i.g. and i.v. methods, respectively. The results demonstrate that paeonol could be absorbed promptly and thoroughly by i.n. administration in rats.

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Concentration of paeonol in plasma (n = 6, mean ± S.D.) following a single i.v. (♦), i.n. (▪), or i.g. (▴) administration; calculated dosage of 4 mg·kg−1 of paeonol in rats.
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f1-ijms-11-04882: Concentration of paeonol in plasma (n = 6, mean ± S.D.) following a single i.v. (♦), i.n. (▪), or i.g. (▴) administration; calculated dosage of 4 mg·kg−1 of paeonol in rats.

Mentions: The concentration-time curves resulting from administration of a single dose of paeonol by i.v., i.n. and i.g. in rats is shown in Figure 1. The i.v. as well as i.n. curve best fitted a two compartment open model. After i.v administration, the paeonol in plasma was eliminated rapidly. The plasma concentrations of paeonol decreased from 9.0 μg/mL to 0.9 μg/mL within 30 minutes. In the case of i.n. administration, the drug was absorbed rapidly. The Cmax of paeonol reached about 4.0 μg/mL and decreased rapidly from 4.0 μg/mL to 0.5 μg/mL within 30 minutes. In the case of i.g. administration, the Cmax of paeonol had reached approximately 0.4 μg/mL at the point of 6 min, and then decreased rapidly from 0.4 μg/mL to 0.05 μg/mL within 30 minutes. The main pharmacokinetic parameters of the plasma after i.v., i.n. and i.g. administration are shown in Table 5. The Kel values were 0.082 min−1, 0.14 min−1 and 0.054 min−1 for i.v., i.n. and p.o., respectively. MRT for injection, nasal and oral solutions were 23.09, 23.19 and 41.49 min, respectively while AUC (Area Under the Concentration-Time Curve) values were 111.62, 58.45 and 17.65 μg/mL·min. Our present results demonstrated that after the i.n. administration, paeonol could be absorbed rapidly and the bioavailability of paeonol was relatively high.


In situ and in vivo study of nasal absorption of paeonol in rats.

Chen X, Lu Y, Du S, Xu B, Wang S, Zhai Y, Song X, Li P - Int J Mol Sci (2010)

Concentration of paeonol in plasma (n = 6, mean ± S.D.) following a single i.v. (♦), i.n. (▪), or i.g. (▴) administration; calculated dosage of 4 mg·kg−1 of paeonol in rats.
© Copyright Policy - open-access
Related In: Results  -  Collection

License 1 - License 2
Show All Figures
getmorefigures.php?uid=PMC3100845&req=5

f1-ijms-11-04882: Concentration of paeonol in plasma (n = 6, mean ± S.D.) following a single i.v. (♦), i.n. (▪), or i.g. (▴) administration; calculated dosage of 4 mg·kg−1 of paeonol in rats.
Mentions: The concentration-time curves resulting from administration of a single dose of paeonol by i.v., i.n. and i.g. in rats is shown in Figure 1. The i.v. as well as i.n. curve best fitted a two compartment open model. After i.v administration, the paeonol in plasma was eliminated rapidly. The plasma concentrations of paeonol decreased from 9.0 μg/mL to 0.9 μg/mL within 30 minutes. In the case of i.n. administration, the drug was absorbed rapidly. The Cmax of paeonol reached about 4.0 μg/mL and decreased rapidly from 4.0 μg/mL to 0.5 μg/mL within 30 minutes. In the case of i.g. administration, the Cmax of paeonol had reached approximately 0.4 μg/mL at the point of 6 min, and then decreased rapidly from 0.4 μg/mL to 0.05 μg/mL within 30 minutes. The main pharmacokinetic parameters of the plasma after i.v., i.n. and i.g. administration are shown in Table 5. The Kel values were 0.082 min−1, 0.14 min−1 and 0.054 min−1 for i.v., i.n. and p.o., respectively. MRT for injection, nasal and oral solutions were 23.09, 23.19 and 41.49 min, respectively while AUC (Area Under the Concentration-Time Curve) values were 111.62, 58.45 and 17.65 μg/mL·min. Our present results demonstrated that after the i.n. administration, paeonol could be absorbed rapidly and the bioavailability of paeonol was relatively high.

Bottom Line: In vivo studies of paeonol absorption were carried out in rats and the pharmacokinetics parameters of intranasal (i.n.) and intragastric (i.g.) administration were compared with intravenous (i.v.) administration.MRT (Mean Residence Time) were 23.19 ± 6.46 min, 41.49 ± 2.96 min and 23.09 ± 5.88 min for i.n., i.g. and i.v. methods, respectively.The results demonstrate that paeonol could be absorbed promptly and thoroughly by i.n. administration in rats.

View Article: PubMed Central - PubMed

Affiliation: School of Chinese Materia Medica, Beijing University of Chinese Medicine, No.6, Zhonghuan South Road, Wangjing, Chaoyang district, Beijing 100102, China; E-Mails: chenxiaolan76@126.com (X.C.); landocean88126.com (Y.L.); dushouying@263.net (S.D.).

ABSTRACT
The objective of this work was to study the in situ and in vivo nasal absorption of paeonol. A novel single pass in situ nasal perfusion technique was applied to examine the rate and extent of nasal absorption of paeonol by rats. Various experimental conditions, such as perfusion rate, pH, osmotic pressure and drug concentration, were investigated. The in situ experiments showed that the nasal absorption of paeonol was not dependent on drug concentration, and fitted a first order process. The absorption rate constant, Ka, increased with an increase in perfusion speed. Paeonol was better absorbed in acidic solutions than in neutral or alkaline solutions. The value of Ka was higher in a hypertonic environment than under isotonic or hypotonic conditions. In vivo studies of paeonol absorption were carried out in rats and the pharmacokinetics parameters of intranasal (i.n.) and intragastric (i.g.) administration were compared with intravenous (i.v.) administration. The bioavailabilities of paeonol were 52.37% and 15.81% for i.n. and i.g, respectively, while T(max) values were 3.05 ± 1.46 min and 6.30 ± 0.70 min. MRT (Mean Residence Time) were 23.19 ± 6.46 min, 41.49 ± 2.96 min and 23.09 ± 5.88 min for i.n., i.g. and i.v. methods, respectively. The results demonstrate that paeonol could be absorbed promptly and thoroughly by i.n. administration in rats.

Show MeSH
Related in: MedlinePlus