Preparation of a solid dispersion of felodipine using a solvent wetting method.
A straightforward solvent wetting method was used to prepare felodipine solid dispersions in the presence of various carriers. Dichloromethane is not needed when HPMC solid dispersions were produced using the solvent wetting method. The amount of ethanol used to prepare solid dispersions did not have a significant effect on the dissolution rate of felodipine. The results of X-ray diffraction and thermal analysis indicated that the drug was in the amorphous state when PVP, HPMC, and poloxamer were used as carriers. The dissolution rates of felodipine in PVP, HPMC, or poloxamer solid dispersions were much faster than those for the corresponding physical mixtures. However, dissolution profiles were found to depend on the carrier used; the dissolution rate of felodipine increased slowly for solid dispersions prepared using HPMC, whereas rapid initial dissolution rates were observed for solid dispersions prepared using PVP or poloxamer. Increases in dissolution rates were partly dependent on the ratios of felodipine to carrier. No significant changes in crystal form were observed by X-ray diffraction or thermal analysis, and no significant changes in dissolution rate were observed when sorbitol and mannitol were used as carriers.
Kim
Eun-Jung
EJ
College of Pharmacy, Chosun University, Gwangju, Republic of Korea.
Chun
Myung-Kwan
MK
Jang
Jae-Sang
JS
Lee
In-Hwa
IH
Lee
Kyeo-Re
KR
Choi
Hoo-Kyun
HK
D002121:Calcium Channel Blockers / Q000737:chemistry; D002152:Calorimetry, Differential Scanning / Q000379:methods; D003460:Crystallization; D018360:Crystallography, X-Ray / Q000379:methods; D004337:Drug Carriers / Q000737:chemistry*; D004339:Drug Compounding / Q000379:methods*; D004355:Drug Stability; D004356:Drug Storage; D000431:Ethanol / Q000737:chemistry; D015736:Felodipine / Q000737:chemistry*; D065347:Hypromellose Derivatives; D008353:Mannitol / Q000737:chemistry; D008747:Methylcellulose / Q000031:analogs & derivatives / Q000737:chemistry; D008752:Methylene Chloride / Q000737:chemistry; D020442:Poloxamer / Q000737:chemistry; D011205:Povidone / Q000737:chemistry; D033362:Powder Diffraction; D012995:Solubility; D012997:Solvents / Q000737:chemistry*; D013012:Sorbitol / Q000737:chemistry; D013997:Time Factors; D044366:Transition Temperature; D017155:Wettability
D002121:Calcium Channel Blockers; D004337:Drug Carriers; D012997:Solvents; D020442:Poloxamer; D000431:Ethanol; D065347:Hypromellose Derivatives; D008353:Mannitol; D013012:Sorbitol; D008752:Methylene Chloride; D008747:Methylcellulose; D011205:Povidone; D015736:Felodipine