[Preparation process of rutacarpine-hydroxypropyl-beta-cyclodextrin inclusion complex]

Area of Science:

• Pharmacology
• Drug Delivery
• Materials Science

Background:

• Rutaecarpine (Rut) is an indole quinazoline alkaloid with diverse pharmacological effects, including anti-hypertension and anti-inflammation.
• Rut's poor water and oil solubility significantly hinders its oral absorption and bioavailability.
• Developing strategies to improve Rut's solubility is crucial for its therapeutic application.

Purpose of the Study:

• To prepare a Rutaecarpine-hydroxypropyl-beta-cyclodextrin (Rut-HP-beta-CD) inclusion complex.
• To enhance the water solubility and bioavailability of Rutaecarpine.
• To optimize the preparation process for the Rut-HP-beta-CD inclusion complex.

Main Methods:

• The stirring-freeze-dry method was employed to prepare the Rut-HP-beta-CD inclusion complex.
• Orthogonal tests were utilized to optimize preparation parameters, including molar ratio, temperature, time, and stirring speed.
• Characterization involved apparent solubility, thin layer chromatography, microscopic identification, melting point, and dissolution studies.

Main Results:

• Optimal preparation conditions were identified as a 1:1 molar ratio of Rut to HP-beta-CD, 60°C, 4 hours, and 600 rpm.
• The optimized process yielded an inclusion rate of 91.04% for the Rut-HP-beta-CD complex.
• The inclusion complex demonstrated significantly improved solubility and dissolution compared to native Rut.

Conclusions:

• The stirring-freeze-dry method is a simple, feasible, and reproducible technique for preparing Rut-HP-beta-CD inclusion complexes.
• The optimized Rut-HP-beta-CD inclusion complex effectively enhances Rutaecarpine's solubility and bioavailability.
• This study provides a solid experimental foundation for the potential clinical application of Rutaecarpine.