Hydroxyitraconazole, Formed During Intestinal First-Pass Metabolism of Itraconazole, Controls the Time Course of Hepatic CYP3A Inhibition and the Bioavailability of Itraconazole in Rats

2008 ◽  
Vol 36 (6) ◽  
pp. 1097-1101 ◽  
Author(s):  
Sara K. Quinney ◽  
Raymond E. Galinsky ◽  
Vanida A. Jiyamapa-Serna ◽  
Yong Chen ◽  
Mitchell A. Hamman ◽  
...  
Keyword(s):  
Time Course ◽  
First Pass Metabolism ◽  
First Pass ◽  
Pass Metabolism

Identification of a Cranberry Juice Product Capable of Inhibiting Enteric CYP3A-Mediated First-Pass Metabolism in Humans

Planta Medica ◽  
2008 ◽  
Vol 74 (03) ◽  
Author(s):  
N Ngo ◽  
Z Yan ◽  
TN Graf ◽  
DR Carrizosa ◽  
EC Dees ◽  
...  
Keyword(s):  
Cranberry Juice ◽  
First Pass Metabolism ◽  
First Pass ◽  
Pass Metabolism

Development, Characterization and Optimization of Mucoadhesive Tablet for Buccal Delivery of Domperidone

2019 ◽  
Vol 9 (1) ◽  
pp. 37-49
Author(s):  
Jagdale Sachin ◽  
Panbude Aishwarya ◽  
Navasare Priya
Keyword(s):  
Drug Release ◽  
Factorial Design ◽  
Research Work ◽  
Wet Granulation ◽  
Buccal Delivery ◽  
Scanning Calorimetry ◽  
Mucoadhesive Polymers ◽  
First Pass Metabolism ◽  
First Pass ◽  
Pass Metabolism

Background and Objective: Upon oral administration domeperidone is rapidly absorbed, but subjected to the first pass effect which lowers systemic bioavailability to 15%. Mucoadhesive tablet can remain attached to buccal mucosa and becomes capable of bypassing hepatic first-pass metabolism to improve absorption directly into systemic circulation. The present research work was carried with an aim to develop, evaluate and optimize mucoadhesive tablet containing domperidone (DOME) for buccal delivery using different bio-adhesive polymeric combinations. </P><P> Methods: The buccal tablets were formulated by wet granulation method using isopropyl alcohol. The preliminary formulations were prepared using combinations of HPMC K4, HPMC K15, HPMC K100, HPMC E5 as mucoadhesive polymers. 32 full factorial design was applied to determine the effect of independent variables like concentration of mucoadhesive polymers (HPMC K15 and HPMC K100) over dependent variables like mucoadhesive properties (swelling index, bioadhesive strength and in vitro drug release). The prepared mucoadhesive tablets were evaluated for their tablet properties and mucoadhesive properties. The interactions between drug and polymers were studied by Fourier Transform Infrared Spectroscopy (FTIR) and Differential Scanning Calorimetry (DSC). </P><P> Results: All formulations of factorial design showed satisfactory physicochemical, mechanical and bioadhesive characteristics. The formulation F9 exhibited maximum cumulative drug release, mucoadhesive strength and swelling index. Conclusion: The developed buccal tablet of domperidone might prove alternative to bypass the hepatic first pass metabolism and to avoid degradation which in turn may result in reducing the frequency of administration. Thus, mucoadhesive tablet of domeperidone may become viable alternative overcoming the side effects; achieving greater therapeutic effectiveness and improving the patient compliance.

scholarly journals Effect of oral pretreatment with indomethacin on the intestinal first-pass metabolism of salicylamide in rabbits.

1988 ◽  
Vol 11 (9) ◽  
pp. 620-624 ◽  
Author(s):  
Junzo NAKAMURA ◽  
Nobuaki SEKI ◽  
Hitoshi SASAKI ◽  
Juichiro SHIBASAKI
Keyword(s):  
First Pass Metabolism ◽  
First Pass ◽  
Pass Metabolism

Bergamottin can be used to assess CYP3A-mediated intestinal first-pass metabolism without affecting P-glycoprotein-mediated efflux in rats

Xenobiotica ◽  
2019 ◽  
Vol 50 (4) ◽  
pp. 401-407 ◽  
Author(s):  
Kei Suzuki ◽  
Kazuhiro Taniyama ◽  
Takao Aoyama ◽  
Yoshiaki Watanabe
Keyword(s):  
P Glycoprotein ◽  
First Pass Metabolism ◽  
First Pass ◽  
Pass Metabolism

Prediction of the Intestinal First-Pass Metabolism of CYP3A Substrates in Humans Using Cynomolgus Monkeys

2010 ◽  
Vol 38 (11) ◽  
pp. 1967-1975 ◽  
Author(s):  
Haruka Nishimuta ◽  
Kimihiko Sato ◽  
Yasuyuki Mizuki ◽  
Masashi Yabuki ◽  
Setsuko Komuro
Keyword(s):  
Cynomolgus Monkeys ◽  
First Pass Metabolism ◽  
First Pass ◽  
Pass Metabolism

Intestinal first-pass metabolism of phenacetin, acetaminophen, ethenzamide and salicylamide in rabbits pretreated with 3,4-benzo[a]pyrene

1987 ◽  
Vol 36 (7) ◽  
pp. 1171-1174 ◽  
Author(s):  
Junzo Nakamura ◽  
Tadahiro Nakamura ◽  
Samir Kumar Podder ◽  
Hitoshi Sasaki ◽  
Juichiro Shibasaki
Keyword(s):  
First Pass Metabolism ◽  
First Pass ◽  
Pass Metabolism

Development of Microneedle Devices for Drug Delivery

2021 ◽  
Author(s):  
◽  
Olivia Howells
Keyword(s):  
Drug Delivery ◽  
Stratum Corneum ◽  
Drug Formulation ◽  
Therapeutic Drug ◽  
Hydrophobic Barrier ◽  
First Pass Metabolism ◽  
First Pass ◽  
Out Of Plane ◽  
Pass Metabolism ◽  
Hollow Microneedles

There are numerous modes of therapeutic administration, of which oral delivery is the most convenient and conventional as it involves administration of therapeutics in the form of liquids or solid capsules and tablets. However, this mode encounters several challenges, such as chemical processes within the gastrointestinal track and first pass metabolism which subsequently reduce the efficacy of the therapeutic drugs. To overcome these issues, transdermal drug administration in the form of hypodermic needles, topical creams, and transdermal patches have been employed. However, the effect of transdermal administration is limited due the stratum corneum layer of the skin, which acts as a lipophilic and hydrophobic barrier preventing external molecules from entering the skin. Therefore, hypodermic needles are used due to their sharp tip facilitating penetration through the stratum corneum to deposit the drug formulation into the skin, subcutaneous fat, or muscles layers. However, these needles induce needle-phobia and reduce patient compliance due to the complexity with administration and pain associated with injection. Microneedle devices have been developed to avoid these issues and provide enhanced transdermal therapeutic drug delivery in a minimally invasive manner to eliminate the first-pass metabolism and provide a sustained release. Unlike hypodermic needles injection, they do not cause pain and related fear or phobia in individuals, thereby improving compliance to the prescribed dosage regime. Till now different types of microneedles have been fabricated. These include, solid, coated, hollow and dissolvable, where each type has its own advantages and unique properties and designs. In this thesis, two novel methods utilising silicon etching processes, for the fabrication of both out-of-plane and in-plane silicon microneedles are presented. Hollow out-of-plane microneedles are manufactured through deep reactive-ion etching (DRIE) technology. The patented three-step process flow has been developed to produce multiple arrays of sharp bevelled tipped, hollow microneedles which facilitate easy insertion and controlled fluid injection into excised skin samples. The in-plane microneedles have been fabricated from simultaneous wet KOH etching of the front and reverse of (100) orientated silicon wafers. The characteristic 54.7˚ sidewall etch angle was utilised to form a sharp six-sided microneedle tip and hexagonal shaped shaft. Employing this method allowed fabrication of both solid and hollow microneedles with different geometries i.e., widths and heights of several µm, to determine the optimal MN height and width for effective penetration and transdermal drug delivery. All microneedles fabricated during the PhD studentship tenure have been characterised through histology, fluorescent studies, and delivery into ex-vivo porcine and human skin tissue (research ethics committee reference 08/WSE03/55) to demonstrate effective microneedle based transdermal therapeutic drug delivery. The transdermal delivery of insulin and hyaluronic acid has been successfully demonstrated by employing a simple poke and patch application technique, presenting a clinical improvement over traditional application such as creams and ointments.

An Insight into delivery of drug through The Skin: Transdermal Drug Delivery system

2021 ◽  
pp. 4-12
Author(s):  
Lakshmi Usha Ayalasomayajula ◽  
M. Kusuma Kumari ◽  
Radha Rani Earle
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Transdermal Drug Delivery ◽  
Drug Delivery Systems ◽  
Dosage Forms ◽  
Transdermal Drug Delivery System ◽  
First Pass Metabolism ◽  
First Pass ◽  
Pass Metabolism

In the recent days about 75% of the drugs taken orally are does not show the desired therapeutic effect. Oral conventional dosage forms have several disadvantages such as poor bioavailability due to hepatic first pass metabolism and tendency to produce rapid blood level spikes (Both high and low). Thus, rapid drug levels in the plasma leads to a need of high and/or frequent dosing, which can be both uneconomical and inconvenient. To overcome such disadvantages transdermal drug delivery system was developed. TDDS is such a delivery system which has been explored extensively over the last two decades, with therapeutic success. Transdermal drug delivery systems (TDDS) are the drug delivery systems which involves transportation of drug to epidermal and dermal tissues of the skin for local therapeutic action while major fraction of the drug is transported into the systemic blood circulation. Topical administration of therapeutic agents offers vast advantages over conventional oral and invasive methods of drug delivery. Some of the advantages of transdermal drug delivery include limitation of hepatic first pass metabolism, enhancement of therapeutic efficiency and maintenance of steady state plasma level concentration of the drug. This study includes a brief overview of TDDS, its advantages over conventional dosage forms, drug delivery routes across human skin, permeation enhancers, and classification, formulation, methods of preparation and evaluation of transdermal patches.

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