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Related Concept Videos

Routes of Drug Administration: Parenteral01:25

Routes of Drug Administration: Parenteral

The administration of drugs via parenteral routes allows for direct drug introduction into the systemic circulation, resulting in high bioavailability because the medication bypasses the harsh conditions of the gastrointestinal tract and hepatic metabolism.
The intravenous route (IV) of drug administration can be further categorized into two types. The bolus injection administers the entire dose rapidly, while an intravenous infusion slowly delivers smaller doses steadily.
The IV route is often...
First Pass Effect01:12

First Pass Effect

Presystemic elimination, or the first-pass effect, is the metabolism of drugs that reduces their effective concentration at the site of action. Apart from the first-pass effect, the systemic bioavailability of the drug is also reduced by other factors, including incomplete absorption or chemical degradation of drugs.
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Factors Influencing Drug Absorption: Drug Dissolution01:27

Factors Influencing Drug Absorption: Drug Dissolution

The pharmacokinetic journey of drugs from solid oral dosage forms into systemic circulation is multifaceted. It begins with disintegration, a prerequisite ensuring a solid dosage form's subdivision into minute particles. Dissolution occurs next as these granulated entities solubilize in gastrointestinal fluids. This solubilization is crucial for the succeeding stage, permeation, which describes the traversal of the drug across the intestinal membrane and its subsequent entry into the blood...
Factors Influencing Drug Absorption: Presystemic Elimination01:24

Factors Influencing Drug Absorption: Presystemic Elimination

The pharmacokinetic journey of oral drugs begins with a crucial first pass through the hepatic portal system, called the first-pass effect. This first pass significantly impacts bioavailability — the proportion of a drug that enters systemic circulation and is available for therapeutic action. The primary route sees the drug absorbed by intestinal membranes and then shunted to the liver via the hepatic portal vein. Here, pre-systemic elimination occurs as drugs face metabolism or biliary...
Non-Oral Extravascular Drug Absorption Routes01:15

Non-Oral Extravascular Drug Absorption Routes

Non-oral extravascular routes, which encompass sublingual, buccal, topical, intramuscular, and inhalation methods, primarily utilize passive diffusion to transport drugs into the systemic circulation. The absorption rates and effectiveness of these routes depend on the drug's physicochemical properties, as well as the patient's anatomical and pathophysiological state.
Lipophilic drugs that are stable at salivary pH (6) and exhibit minimal binding to the oral mucosa are absorbed more effectively...
Ophthalmic Drug Delivery Systems01:23

Ophthalmic Drug Delivery Systems

Ophthalmic drug delivery faces major limitations due to poor absorption across the corneal membrane. This process is primarily driven by diffusion and is influenced by two main factors: the physicochemical properties of the drug and tear drainage. Most ophthalmic drugs, such as pilocarpine, epinephrine, atropine, and local anesthetics, are weak bases. They are typically formulated at an acidic pH to enhance chemical stability. However, this leads to high ionization, reducing their ability to...

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Related Experiment Video

Updated: Jul 28, 2026

In Vivo, Percutaneous, Needle Based, Optical Coherence Tomography of Renal Masses
09:31

In Vivo, Percutaneous, Needle Based, Optical Coherence Tomography of Renal Masses

Published on: March 30, 2015

Percutaneous absorption of Octopirox.

J G Black1, V B Kamat

  • 1Environmental Safety Laboratory, Unilever Research, Sharnbrook, Bedford, England.

Food and Chemical Toxicology : an International Journal Published for the British Industrial Biological Research Association
|January 1, 1988
PubMed
Summary

Octopirox is primarily excreted in feces, with minimal absorption through the skin. Even with direct skin contact, systemic exposure to Octopirox is very low, indicating a high safety margin for consumers.

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Visualizing and Quantifying Pharmaceutical Compounds within Skin using Coherent Raman Scattering Imaging
11:07

Visualizing and Quantifying Pharmaceutical Compounds within Skin using Coherent Raman Scattering Imaging

Published on: November 24, 2021

Area of Science:

  • Pharmacokinetics and Toxicology
  • Dermatology and Cosmetic Science

Background:

  • Octopirox is an active ingredient used in topical formulations, necessitating an understanding of its absorption and excretion profile.
  • Evaluating the potential for systemic exposure is crucial for assessing the safety of cosmetic and dermatological products.

Purpose of the Study:

  • To investigate the excretion pathways of Octopirox after oral administration in rats.
  • To determine the extent of skin penetration and systemic absorption of Octopirox following topical application.
  • To assess the safety margin of Octopirox in consumer products like shampoos.

Main Methods:

  • Rats were administered radiolabeled Octopirox via intubation or injection to track excretion in feces and urine.
  • Skin penetration studies were conducted using various concentrations and contact times of Octopirox formulations on rat skin.
  • Blood and tissue levels were measured after both oral and topical administration.
  • Safety factors were calculated based on estimated consumer exposure and toxicological data.

Main Results:

  • The majority of orally administered Octopirox was excreted in feces (65-85%), with a smaller fraction in urine (6-19%).
  • Topical application showed dose- and time-dependent skin penetration, but rinsing significantly reduced absorption.
  • Blood levels remained low after topical application, especially when the product was rinsed off, indicating minimal systemic absorption.
  • A high safety factor (29,400) was calculated for 1% Octopirox in shampoo, suggesting a remote possibility of systemic effects.

Conclusions:

  • Octopirox is predominantly eliminated via the fecal route, with limited urinary excretion.
  • Skin absorption of Octopirox is minimal, particularly when formulations are rinsed after application.
  • The extensive safety factor supports the safe use of Octopirox in consumer products at recommended concentrations.