Preparation of Meloxicam Solid Dispersion Tablets and Study of the Dissolution
10.13748/j.cnki.issn1007-7693.20223567
- VernacularTitle:美洛昔康固体分散体片的制备及其溶出度研究
- Author:
Jiawei BI
1
;
Yumeng ZHAO
1
;
Tong ZHANG
1
;
Yanhua LIU
1
Author Information
1. College of Pharmacy, Ningxia Medical University, Yinchuan 750004, China
- Publication Type:Journal Article
- Keywords:
meloxicam;
solid dispersion;
dissolution;
preparation procedure;
tablets
- From:
Chinese Journal of Modern Applied Pharmacy
2024;41(1):33-41
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVE
To prepare meloxicam solid dispersions tablets, and to investigate their dissolution in vitro.
METHODS
Crystal inhibition experiments were carried out to screen the carrier materials, and the solid dispersion was characterized by X-ray diffraction(XRD) amd differential scanning calorimeter(DCS). The improved bioavailability of solid dispersions was evaluated through in vivo pharmacokinetic studies. The optimum preparation process of meloxicam solid dispersion tablets was investigated, and the in vitro dissolution curve similarity factor f2 was used as the main evaluation index to screen and optimize the dosage of pH regulator, filler, disintegrator, lubricant, flow aid and the mixing time in the prescription.
RESULTS
The solid dispersion prepared with Kollidon@VA64 as carrier effectively maintained the supersaturated state of the drug in solution. The results of XRD and DSC showed that the crystal state of meloxicam in the solid dispersion was completely transformed into amorphous state. Compared with meloxicam, solid dispersions significantly increased the solubility, and its peak blood concentration(Cmax) and relative bioavailability were increased by 208.09% and 241.78%, respectively. The optimal formulation and process of meloxicam solid dispersion tablets prepared by direct powder pressing method were meloxicam solid dispersion 35.2%, lactose∶microcrystalline cellulose =1∶1.5, sodium citrate 9.8%, crosslinked povidone 8%, magnesium stearate 0.75%, silica 0.8%, and mixing time 5 min. The dissolution similarity factor f2 of the prepared meloxicam solid dispersion tablets and the original reference preparation in different pH medium was above 50.
CONCLUSION
Meloxicam solid dispersible tablets are prepared by hot melt extrusion and powder pressing method. The dissolution and bioavailability of meloxicam are improved, and the dissolution behavior of meloxicam is similar to that of the original reference preparation.
