ABSTRACT
An HPLC method for the determination of geniposide concentration in mouse plasma was developed and the pharmacokinetics after intranasal administration of Xingnaojing microemulsion (XNJ-M) and mPEG2000-PLA modified Xingnaojing microemulsion (XNJ-MM) were investigated. Eighty mice were treated by XNJ-M and XNJ-MM nasally. The plasma samples were collected at different times and the drug in samples was detected by HPLC. The pharmacokinetic parameters were calculated by the software of Kinetica. The pharmacokinetic parameters of geniposide of XNJ-M were C(max) (4.36 +/- 2.69) mg x L(-1), t(max) 1 min, MRT (29.73 +/- 4.54) min, AUC (53.63 +/- 14.03) mg x L(-1) x min. The pharmacokinetic parameters of geniposide of XNJ-MM were C(max) (9.75 +/- 4.14) mg x L(-1), t(max) 1 min, MRT(22.34 +/- 2.90) min, AUC (131.87 +/- 40.13) mg x L(-1) x min. Geniposide can be absorbed into blood in a higher degree after intranasal administration with XNJ-MM compared to XNJ-M, which maybe caused by its less irritating and more absorption.
Subject(s)
Animals , Male , Mice , Drugs, Chinese Herbal , Chemistry , Emulsions , Iridoids , Blood , Pharmacokinetics , Lactic Acid , Chemistry , Polyesters , Polyethylene Glycols , Chemistry , Polymers , ChemistryABSTRACT
In order to test the equilibrium solubility of puerarin in different solvents and solubilizer,cilia toxicity and irritation of these excipient, the balance method, toad in the ciliary body toxicity and rat nasal mucosa irritation were used respectively. Results showed that puerarin solubility was 56.44 g x L(-1) in combined solvent of 30% PEG200 and 10% Kolliphor HS 15. With normal saline solution as negative control and sodium deoxycholate as positive control, the effects of 30% PEG200, 30% PEG 400, 10% Kolliphor HS 15 and combination of 30% of PEG200 and 10% Kolliphor HS 15 on toad palate cilium were observed and cilia movement duration was recorded. The results indicated that there was no significant difference in cilia movement duration among 30% PEG200, 10% Kolliphor HS 15 and normal saline group. The rats long-term nasal mucous membrane irritation of 30% PEG 400, 10% Kolliphor HS 15, which had no cilia toxicity, was studied, with normal saline solution as negative control. There were no significant difference revealed on rat nasal mucosa epithelial thickness among 30% PEG 400, 10% Kolliphor HS 15 and normal saline. Above researches showed 30% PEG 400, 10% Kolliphor HS 15 was ideal for solubility of puerarin nasal drops and showed a lower cilia toxicity and irritation, and can be used as the solvent and solubilizer of puerarin nasal drops.
Subject(s)
Animals , Female , Male , Rats , Administration, Intranasal , Methods , Anura , Cilia , Chemistry , Isoflavones , Chemistry , Nasal Mucosa , Polyethylene Glycols , Chemistry , Rats, Sprague-Dawley , Solubility , Solvents , ChemistryABSTRACT
In order to research the pharmacokinetic characteristic of borneol in plasma and brain of stroke rats given XNJ and investigate the influence of stroke on the borneol passing through the blood-brain barrier, this study established the GC to determine the borneol in brain and blood, and made the stroke mode rats by middle carotid artery occlusion (MCAO) and set sham-operated group. After oral administration of Xingnaojing (XNJ) suspension, their blood and brain were collected at different time and detected by GC. The data was analysed by Kinetica. Results showed that in stroke group, the Cmax and AUC0-t of brain and plasma are (1.82 +/- 0.825), (1.35 +/- 0.43) mg x L(-1) and (123.39 +/- 55.82), (87.91 +/- 39.81) mg x L(-1) x min, Te (brain/blood drug ratio) was 70.93%; those pharmacokinetic values were larger than in sham-operated group. We can conclude that the pathological state of stroke can increase the amount of borneol permeating into brain.
Subject(s)
Animals , Humans , Male , Administration, Oral , Camphanes , Metabolism , Pharmacokinetics , Brain , Metabolism , Drugs, Chinese Herbal , Metabolism , Pharmacokinetics , Plasma , Chemistry , Metabolism , Stroke , Drug Therapy , MetabolismABSTRACT
Olfactory perception of myristic, palmitic, stearic and oleic acids and their corresponding methyl esters by Asian corn borer moths, Ostrinia furnacalis (Guenée) (Lepidoptera: Crambidae) was investigated. It was found that mated females with both antennae amputated, in contrast to intact females and females with one antenna removed, could not discriminate between simultaneously provided control filter papers and filters treated with a blend of oviposition-deterring fatty acids. Oviposition by mated females exhibited a very marked periodicity, with all egg masses deposited during the scotophase and most egg masses laid before midnight. According to the peak and trough period of oviposition, electroantennogram (EAG) responses from both mated females and males to the four fatty acids and four methyl esters were tested within two two-hour periods from 3 to 5 hours after the start of darkness and from 1 to 3 hours after light onset, respectively. Significant EAG responses above solvent and background were elicited by all test chemicals from females, and by most of the test compounds from males. EAG values of all test chemicals from mated females were not statistically different between the two test periods except for methyl myristate. Conversely, EAG responses from mated males to myristic acid, stearic acid and their methyl esters significantly differed between the two test periods.
