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Related Concept Videos

Transdermal Drug Delivery Systems01:18

Transdermal Drug Delivery Systems

Transdermal drug delivery systems (TDDS) enable the controlled release of drugs across the skin into systemic circulation. They are particularly advantageous for drugs with short half-lives or narrow therapeutic indices, as they maintain consistent plasma concentrations and reduce the risk of subtherapeutic or toxic levels.TDDS are categorized into monolithic, reservoir, and mixed systems. Monolithic systems embed the drug in a polymer matrix, where diffusion governs release. Reservoir systems...
Intrauterine Drug Delivery Systems01:21

Intrauterine Drug Delivery Systems

Controlled-release systems for intravaginal and intrauterine drug delivery have been developed primarily for the administration of contraceptive steroid hormones. These delivery routes circumvent first-pass hepatic metabolism, thereby enhancing bioavailability and allowing for reduced systemic dosages compared to oral administration. Such approaches contribute to improved therapeutic efficacy and patient compliance, particularly in long-term contraceptive regimens.Intravaginal Drug Delivery...
Crystal Growth: Principles of Crystallization01:25

Crystal Growth: Principles of Crystallization

Crystallization is a phase transformation process in which crystals are precipitated from a supersaturated solution or formed from other sources. During crystallization, atoms or molecules arrange themselves into a well-defined, rigid crystal lattice to minimize energy.
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Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism01:21

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Polymorphism refers to the existence of a drug substance in multiple crystalline forms, known as polymorphs. Recently, this term has been expanded to include solvates (forms containing a solvent), amorphous forms (non-crystalline forms), and desolvated solvates (forms from which the solvent has been removed).
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Clinically Relevant Drug Product Specifications: Methods of Establishment01:29

Clinically Relevant Drug Product Specifications: Methods of Establishment

Product specifications define the acceptable quality of a pharmaceutical product by ensuring identity, purity, potency, and strength. These specifications serve as benchmarks during development, manufacturing, and post-approval quality control. Clinically relevant specifications are particularly important because they directly relate to a drug's safety and efficacy in clinical use.Dissolution studies are critical biopharmaceutic tools that link in vitro behavior to in vivo performance. They...
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Recrystallization: Solid–Solution Equilibria

Recrystallization is a purification technique used to separate impurities from solid compounds. In this technique, no chemical reactions occur. Instead, it exploits physical properties only, specifically, the solubility differences between the desired compound and impurities, either at a single temperature or at different temperatures, and under other selected conditions. The solid-solution equilibrium (solubility equilibrium) of each component in the solution represents a binary phase...

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Formulation and optimization of desogestrel transdermal contraceptive patch using crystallization studies.

Vishal Sachdeva1, Yun Bai, Agis Kydonieus

  • 1Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, Mercer University, Atlanta, GA 30341, USA.

International Journal of Pharmaceutics
|December 25, 2012
PubMed
Summary

This study explores desogestrel for transdermal contraception, finding it more permeable than levonorgestrel. Optimized patches show potential for a 7-day contraceptive delivery system.

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Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery Systems
  • Dermatology

Background:

  • Levonorgestrel (LNG) is the standard progestin for contraception.
  • Transdermal drug delivery offers an alternative contraceptive route.
  • Desogestrel's potential for transdermal application requires investigation.

Purpose of the Study:

  • To evaluate desogestrel as an alternative progestin for transdermal contraceptive patches.
  • To optimize formulation and adhesive selection for effective desogestrel delivery.
  • To assess the feasibility of a 7-day transdermal contraceptive patch.

Main Methods:

  • Saturation solubility studies of desogestrel in acrylate and polyisobutylene (PIB) adhesives.
  • Formulation development using copovidone and mineral oil to enhance drug loading in PIB.
  • Physical characterization including in vitro release, content uniformity, adhesion, and skin permeation studies.
  • Comparison of desogestrel permeability against levonorgestrel.

Main Results:

  • Desogestrel exhibited significantly higher permeability compared to LNG (p<0.05).
  • Acrylate adhesives showed higher desogestrel saturation solubility than PIB.
  • Optimized PIB formulations with mineral oil and copovidone improved drug loading and cosmetic properties.
  • In vitro studies demonstrated potential for a uniform and reproducible 7-day patch.

Conclusions:

  • Desogestrel is a promising candidate for transdermal contraceptive patches due to its enhanced permeability.
  • Formulation strategies involving specific excipients and adhesives can overcome challenges in drug loading and delivery.
  • The developed formulation shows potential for a novel, long-acting transdermal contraceptive system.