Related Experiment Video
Updated: Feb 12, 2026
10:10
Transport Properties of Ibuprofen Encapsulated in Cyclodextrin Nanosponge Hydrogels: A Proton HR-MAS NMR Spectroscopy Study
Published on: August 15, 2016
10.8K
The hydroxypropyl-β-cyclodextrin complexation of toltrazuril for enhancing bioavailability.
Li Zhang1,2, Mengxi Liu1, Chaocheng Lu1
1Department of Pharmacy, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu, Sichuan, China.
Drug Design, Development and Therapy
|March 30, 2018
Summary
Toltrazuril-hydroxypropyl-β-cyclodextrin inclusion complex significantly enhances toltrazuril oral bioavailability in rabbits. This novel formulation improves drug absorption, offering a more effective treatment for coccidiosis.
Area of Science:
- Pharmacokinetics and Drug Delivery
- Veterinary Pharmacology
Background:
- Toltrazuril (Tol) is crucial for coccidiosis prevention and treatment.
- Poor aqueous solubility and oral bioavailability limit Toltrazuril's clinical efficacy.
Purpose of the Study:
- To enhance Toltrazuril's oral bioavailability and solubility.
- To develop a novel toltrazuril-hydroxypropyl-β-cyclodextrin (Tol-HP-β-CD) inclusion complex.
Main Methods:
- Tol-HP-β-CD complex prepared using the solution-stirring method.
- Complex formation verified by TLC, FTIR, and 1H NMR spectroscopy.
- Plasma disposition kinetics analyzed in rabbits via HPLC after oral administration.
Main Results:
- Tol-HP-β-CD exhibited a shorter Tmax (12 h) compared to Tol (24 h).
- Cmax and AUC0-∞ were significantly higher for Tol-HP-β-CD (19.92 μg/mL, 1176.86 mg/L h) versus Tol (8.02 μg/mL, 514.03 mg/L h).
Conclusions:
- Tol-HP-β-CD inclusion complex successfully increased Toltrazuril's aqueous solubility.
- Complexation with HP-β-CD significantly enhanced Toltrazuril's oral bioavailability in rabbits.
- This approach offers a viable strategy for developing improved oral Toltrazuril formulations.
Related Concept Videos
01:16Bioavailability Enhancement: Drug Solubility Enhancement
273
Body:Bioavailability is a critical factor in determining a drug's effectiveness. It refers to the proportion of a drug that enters the circulation when introduced into the body and is, as a result, able to have an active effect. Enhancing bioavailability is essential for drugs with poor solubility, as it can significantly impact their therapeutic efficacy. Various methods are employed to increase the solubility of drugs, thereby enhancing their bioavailability.Micronization and nanonization are...
273
01:27Bioavailability Enhancement: Drug Permeability Enhancement
213
Body:After oral administration, poor permeability often limits the rate at which drugs are absorbed through the intestinal epithelium. Enhancing drug permeability is crucial for effective therapy, and several strategies have been developed to overcome this challenge.One effective strategy involves the use of lipid-based formulations. These formulations enhance dissolution and solubility, targeting physiological mechanisms to increase drug absorption. This includes stimulating bile salt...
213
01:22Bioavailability Enhancement: Determination and Conceptual Approaches in Overcoming Bioavailability Problems
214
Body:Bioavailability is a critical pharmacological concept that measures the extent and rate at which an active drug ingredient or therapeutic moiety enters the systemic circulation, remaining unchanged. It's a pivotal factor in determining a drug's efficacy and safety.The Biopharmaceutics Classification System (BCS) plays an essential role in drug development by categorizing drugs into four classes based on their solubility and permeability. This classification aids in understanding drug...
214
01:05Bioavailability Enhancement: Drug Stability Enhancement and GI Retention
226
Body:Improving a drug's stability in the gastrointestinal (GI) tract is paramount for enhancing its bioavailability and therapeutic effectiveness. Various strategies are employed to protect the drug from the harsh gastric milieu and to ensure its release and absorption at the desired site within the GI tract.Polymer coatings are one such method used to shield drugs from the stomach's acidic environment. By preventing premature drug release, these coatings improve the bioavailability of unstable...
226
01:17Bioavailability: Overview
465
Bioavailability refers to the proportion of an administered drug that reaches the systemic circulation in its active, unaltered form. It is a crucial pharmacokinetic parameter that determines the effectiveness of a drug in achieving its intended therapeutic outcomes. The route of administration significantly influences bioavailability, with intravenous administration achieving 100% bioavailability as the drug directly enters the bloodstream. In contrast, oral administration often results in...
465
01:13Bioavailability: Overview
4.6K
Bioavailability refers to the proportion of an unaltered drug that, after administration, enters the systemic circulation and can be distributed to the desired action site. Factors such as gastrointestinal (GI) absorption and liver biotransformation influence the bioavailability of a drug when it is administered orally. When a drug is administered intravenously, it enters the systemic circulation directly; by definition, its bioavailability is assumed to be 100%. The bioavailability of an...
4.6K