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Related Concept Videos

Non-Oral Extravascular Drug Absorption Routes01:15

Non-Oral Extravascular Drug Absorption Routes

177
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...
177
Methods for Studying Drug Absorption: In vitro01:16

Methods for Studying Drug Absorption: In vitro

168
In vitro experiments are crucial for understanding the transport and absorption of drugs through biological materials. These studies employ varied methods such as the diffusion cell method, the everted sac technique, and the everted ring technique.
The diffusion cell method uses a two-compartment cell, including a donor compartment with the drug solution, which simulates the environment where the drug is applied, and a receptor compartment with a buffer solution, which simulates the environment...
168
Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry01:20

Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry

148
Orally administered drugs primarily enter the systemic circulation via passive diffusion through the intestinal membranes. The drug's absorption is influenced by drug stability in the gastrointestinal GI tract, membrane permeability, the surface area available for absorption, luminal drug concentration, and residence time in the lumen. Drug permeability can be enhanced by adjusting the lipophilicity, polarity, or molecular size of the drug, promoting its passive transport across intestinal...
148
Drug Delivery: Enteral Route01:18

Drug Delivery: Enteral Route

331
The enteral drug administration involves three primary routes: oral, sublingual, and buccal. Oral ingestion is the most prevalent, safe, economical, and convenient method for drug administration. However, it has certain drawbacks, including limited absorption due to the drug's low water solubility or poor membrane permeability, possible emesis from GI mucosa irritation, destruction of drugs by digestive enzymes or low gastric pH, and irregular absorption along with food or other drugs.
331
Methods for Studying Drug Absorption: In situ01:09

Methods for Studying Drug Absorption: In situ

175
In situ experiments, such as the Doluisio method and Single-Pass Perfusion technique, provide critical insights into drug uptake by simulating in vivo conditions for drug absorption.
The Doluisio method involves perfusing a prepared segment of a rat's small intestine with a solution of radiolabeled drug and a non-absorbable marker. This helps to differentiate between absorbed and non-absorbed drug concentrations. The intestinal segment is connected at both ends using tubing and syringes,...
175
Factors Influencing Drug Absorption: Drug Dissolution01:27

Factors Influencing Drug Absorption: Drug Dissolution

372
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...
372

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Related Experiment Video

Updated: May 10, 2025

An In Vivo Estrogen Deficiency Mouse Model for Screening Exogenous Estrogen Treatments of Cardiovascular Dysfunction After Menopause
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In Vitro Percutaneous Absorption of Permeation-Enhancing Estrogen Formulations.

Guiyun Song1, Kendice Ip1, Bruce Biundo1

  • 1Professional Compounding Centers of America (PCCA), 9901 South Wilcrest Drive, Houston, TX 77099, USA.

Pharmaceuticals (Basel, Switzerland)
|April 26, 2025
PubMed
Summary
This summary is machine-generated.

Compounded estradiol formulations offer steady skin absorption for hormone replacement therapy (HRT). These preparations provide a consistent hormone delivery, unlike commercial gels that peak and decline rapidly.

Keywords:
estradiolextemporaneously compounded formulationspermeation-enhancerssemisolid preparationsskintopicaltransdermal

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Area of Science:

  • Dermatology and Pharmaceutical Sciences
  • Endocrinology and Hormone Therapy

Background:

  • Hormone Replacement Therapy (HRT) is crucial for managing hormone deficiencies in women.
  • Oral estrogen administration (estradiol [E2] and estriol [E3]) can cause side effects.
  • Topical estrogen application offers an alternative delivery route for improved patient outcomes.

Purpose of the Study:

  • To evaluate the in vitro percutaneous absorption of compounded estradiol and bi-estrogen formulations.
  • To compare the absorption profiles of compounded topical estrogens against a commercial estradiol transdermal gel (ESTROGel®).

Main Methods:

  • Utilized a validated In Vitro Permeation Test (IVPT) to assess skin absorption.
  • Analyzed the concentration of estradiol and estriol in five test formulations using Ultra Performance Liquid Chromatography (UPLC).

Main Results:

  • ESTROGel® showed rapid initial estradiol absorption, peaking within 0.5 hours, followed by a swift decline.
  • Compounded formulations demonstrated a slower, steady increase in estradiol absorption, reaching peak flux within 6 hours.
  • All tested compounded formulations maintained steady estradiol absorption over a 16-hour period.

Conclusions:

  • Compounded bases facilitate consistent percutaneous estradiol absorption, avoiding rapid flux changes desirable in HRT.
  • Estradiol compounded formulations represent a viable option for topical hormone delivery.
  • Compounding pharmacists and healthcare providers can consider these formulations for patient hormone therapy.