Impact of Luminal Fluid Volume on the Drug Absorption After Oral Administration: Analysis Based on In Vivo Drug Concentration–Time Profile in the Gastrointestinal Tract

2015 ◽  
Vol 104 (9) ◽  
pp. 3120-3127 ◽  
Author(s):  
Yusuke Tanaka ◽  
Takanori Goto ◽  
Makoto Kataoka ◽  
Shinji Sakuma ◽  
Shinji Yamashita
Keyword(s):  
Gastrointestinal Tract ◽  
Oral Administration ◽  
Drug Concentration ◽  
Drug Absorption ◽  
Time Profile ◽  
Fluid Volume ◽  
Concentration Time

A Comparative Pharmacokinetic Profile of Trahydropalmatine After Oral Administration of its Monomer, Rhizoma Corydalis Alkaloid Extracts and Tong-Bi-Si-Wei-Fang to Rats

2019 ◽  
Vol 15 (4) ◽  
pp. 338-345
Author(s):  
Lijun Ni ◽  
Lu Ding ◽  
Liguo Zhang ◽  
Shaorong Luan
Keyword(s):  
Oral Administration ◽  
Panax Notoginseng ◽  
Pharmacokinetic Profile ◽  
Apparent Volume ◽  
Bone Diseases ◽  
Glycyrrhiza Uralensis ◽  
Pharmacokinetic Property ◽  
Time Curve ◽  
Concentration Time

Background: Tong-Bi-Si-Wei-Fang (TBSWF) is a candidate formula of Traditional Chinese Medicine (TCM) for treating rheumatoid bone diseases, which is composed of rhizoma corydalis alkaloids, saponins of glycyrrhiza uralensis and panax notoginseng, flavonoids of rhizoma drynariae and glycyrrhiza uralensis. </P><P> Objective: Trahydropalmatine (THP), the main active ingredient of rhizoma corydalis alkaloids, was selected to study in vivo pharmacokinetics and druggability of TBSWF. Methods: The plasma concentration-time (C-T) profiles of THP and the pharmacokinetic property parameters after oral administration of THP monomer, extract of corydalis alkaloids (ECA) and TBSWF to rats, respectively were compared by a fully-validated HPLC method. Results: Compared to the THP monomer, the THP in TBSWF is absorbed faster, resides in the plasma longer and has a similar apparent volume of distribution Vz/F (10~20 L/kg). Compared to THP monomer and THP in TBSWF, the area under the concentration-time curve AUC 0-t of THP in ECA decreases two-third; Vz/F of THP in ECA (85.02 L/kg) is significantly higher than that of THP in TBSWF(p <0.05). Unlike THP monomer and THP in ECA, double peaks are observed in the C-T profile of THP after oral administration of TBSWF. THP in TBSWF exhibits slow release to a certain degree. Conclusion: The interactions among the ingredients of TBSWF promote the adsorption and prolong the residence time of THP in vivo, and provide an explanation for the advantages of TBSWF from the point of pharmacokinetics.

scholarly journals Mucoadhesive Microspheres Containing Amoxicillin for Clearance of Helicobacter pylori

1998 ◽  
Vol 42 (10) ◽  
pp. 2492-2494 ◽  
Author(s):  
Naoki Nagahara ◽  
Yohko Akiyama ◽  
Masafumi Nakao ◽  
Mayumi Tada ◽  
Megumi Kitano ◽  
...  
Keyword(s):  
Helicobacter Pylori ◽  
Gastrointestinal Tract ◽  
Oral Administration ◽  
Antimicrobial Agent ◽  
Extended Period ◽  
Mongolian Gerbils ◽  
Polymer Powder ◽  
Hydrogenated Castor Oil ◽  
H Pylori

ABSTRACT In an effort to augment the anti-Helicobacter pylorieffect of amoxicillin, mucoadhesive microspheres, which have the ability to reside in the gastrointestinal tract for an extended period, were prepared. The microspheres contained the antimicrobial agent and an adhesive polymer (carboxyvinyl polymer) powder dispersed in waxy hydrogenated castor oil. The percentage of amoxicillin remaining in the stomach both 2 and 4 h after oral administration of the mucoadhesive microspheres to Mongolian gerbils under fed conditions was about three times higher than that after administration in the form of a 0.5% methylcellulose suspension. The in vivo clearance ofH. pylori following oral administration of the mucoadhesive microspheres and the 0.5% methylcellulose suspension to infected Mongolian gerbils was examined under fed conditions. The mucoadhesive microspheres and the 0.5% methylcellulose suspension both showed anti-H. pylori effects in this experimental model of infection, but the required dose of amoxicillin was effectively reduced by a factor of 10 when the mucoadhesive microspheres were used. In conclusion, the mucoadhesive microspheres more effectively cleared H. pylori from the gastrointestinal tract than the 0.5% methylcellulose suspension due to the prolonged gastrointestinal residence time resulting from mucoadhesion. A dosage form consisting of mucoadhesive microspheres containing an appropriate antimicrobial agent should be useful for the eradication of H. pylori.

Prediction of Concentration–Time Profile and its Inter-Individual Variability following the Dermal Drug Absorption

2012 ◽  
Vol 101 (7) ◽  
pp. 2584-2595 ◽  
Author(s):  
Sebastian Polak ◽  
Cyrus Ghobadi ◽  
Himanshu Mishra ◽  
Malidi Ahamadi ◽  
Nikunjkumar Patel ◽  
...  
Keyword(s):  
Drug Absorption ◽  
Time Profile ◽  
Individual Variability ◽  
Concentration Time ◽  
Dermal Drug Absorption

The effect of ferrous sulfate and pH on L-dopa absorption

1990 ◽  
Vol 68 (5) ◽  
pp. 603-607 ◽  
Author(s):  
Roderick R. A. Campbell ◽  
Brian Hasinoff ◽  
Gary Chernenko ◽  
James Barrowman ◽  
Norman R. C. Campbell
Keyword(s):  
Gastrointestinal Tract ◽  
Complex Formation ◽  
Rat Model ◽  
Drug Absorption ◽  
Ferrous Sulfate ◽  
Iron Binding ◽  
Percent Reduction ◽  
Experimental Animals ◽  
Jejunal Segment

Ferrous sulfate decreases L-dopa bioavailability in humans probably as a result of binding of L-dopa by iron in the gastrointestinal tract. This study was conducted to determine if iron by binding L-dopa decreases L-dopa absorption and to investigate the effect of different pH buffers on intestinal absorption of L-dopa in the presence and absence of ferrous sulfate. A rat model developed to examine drug absorption was used. Control animals had buffered [14C]L-dopa solutions injected into two in vivo closed segments of intestine; a 5-cm duodenal and a 5-cm proximal jejunal segment. These studies were conducted using solutions buffered at pH 5.5, 6.5, 7.5, and 8.5. An identical procedure was followed for experimental animals except ferrous sulfate was injected with the buffered L-dopa solutions. Ferrous sulfate resulted in a reduction in L-dopa absorption in the buffers at all pHs in both the duodenum and jejunum. The average reduction in L-dopa absorption in the presence of iron was 22.6% in the duodenum and 23.9% in the jejunum. There was a tendency for ferrous sulfate to cause a greater reduction in L-dopa absorption as the buffer pH increased. There was also a decrease in L-dopa absorption in the higher pH buffers in the absence of iron. Despite this latter result, in the jejunum there was an increase in the percent reduction in L-dopa absorption associated with ferrous sulfate as pH increased. Although this tendency was not as consistent in the duodenum as the jejunum, the combined results are compatible with the chemical model of increased L-dopa–iron binding as pH increases.Key words: L-dopa, ferrous sulfate, complex formation, chelation, drug absorption.

Control of drug concentration-time profiles in vivo by zero-order transdermal delivery systems

1987 ◽  
Vol 6 (1) ◽  
pp. 99-106 ◽  
Author(s):  
T. Okano ◽  
M. Miyajima ◽  
F. Komada ◽  
G. Imanidis ◽  
S. Nishiyama ◽  
...  
Keyword(s):  
Drug Concentration ◽  
Transdermal Delivery ◽  
Delivery Systems ◽  
Zero Order ◽  
Time Profiles ◽  
Concentration Time

COMPARISON OF THE METABOLISM OF TESTOSTERONE UNDECANOATE AND TESTOSTERONE IN THE GASTROINTESTINAL WALL OF THE RAT IN VITRO AND IN VIVO

1977 ◽  
Vol 86 (1) ◽  
pp. 216-224 ◽  
Author(s):  
J. Geelen ◽  
A. Coert ◽  
R. Meijer ◽  
J. van der Vies
Keyword(s):  
Small Intestine ◽  
Gastrointestinal Tract ◽  
Portal Vein ◽  
Oral Administration ◽  
Small Extent ◽  
Great Similarity ◽  
Testosterone Undecanoate ◽  
Different Parts

ABSTRACT The metabolism of testosterone undecanoate (TU) and testosterone (T) is studied in the gastrointestinal wall of the rat in vitro. A comparison is made with the in vivo metabolism of these compounds in the rat. The major metabolite first appearing during incubation of TU with the small intestine is T. Incubation of TU or T with the small intestine reveals a great similarity between the metabolite patterns obtained. This is also the case with the patterns derived from portal vein plasma upon oral administration of TU and T. Incubation of different parts of the gastrointestinal tract with TU or T shows that the greatest metabolic activity is located in the wall of the small intestine. Unlike T, TU is metabolized only to a small extent in the wall of the stomach and the large intestine.

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