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Studies on formulation development of mucoadhesive sustained release itraconazole tablet using response surface
Ashwini Madgulkar1, Shivajirao Kadam, Varsha Pokharkar
1Poona College of Pharmacy, Bharti Vidyapeeth University, Erandwane, Pune, 411038, India. ashwini.madgulkar@indiatimes.com
AAPS Pharmscitech
|September 5, 2008
Summary
Researchers developed sustained-release Itraconazole mucoadhesive tablets using solid dispersion and hydrophilic polymers. The optimized formulation demonstrated enhanced drug dissolution and favorable pharmacokinetic profiles in rabbits.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Materials Science
Background:
- Itraconazole's poor aqueous solubility limits oral bioavailability.
- Sustained-release and mucoadhesive drug delivery systems enhance therapeutic efficacy.
- Solid dispersion is a technique to improve solubility of poorly soluble drugs.
Purpose of the Study:
- To prepare and evaluate sustained-release mucoadhesive tablets of Itraconazole.
- To enhance Itraconazole's dissolution rate and oral bioavailability.
- To optimize mucoadhesive properties and drug release profiles.
Main Methods:
- Spray drying was used to prepare Itraconazole-Eudragit E100 solid dispersion.
- Mucoadhesive tablets were formulated using Carbopol 934P (CP) and Methocel K4M (HPMC).
- A 3(2) factorial design optimized polymer concentrations for mucoadhesion and dissolution; pharmacokinetic studies were conducted in albino rabbits.
Main Results:
- Solid dispersion significantly improved Itraconazole dissolution rate.
- Mucoadhesive strength increased linearly with polymer content (CP and HPMC).
- Drug release followed Peppas model (n=0.61–1.18), with optimized formulations showing good agreement between predicted and experimental results.
Conclusions:
- Sustained-release mucoadhesive Itraconazole tablets were successfully prepared.
- The optimized formulation exhibited enhanced dissolution, adequate bioadhesion, and a regulated release profile.
- Pharmacokinetic evaluation in rabbits showed a Cmax of 1898 ± 75.23 ng/ml, Tmax of 2 h, and AUC of 28604.9 ng·h/ml.
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