In-vivo evaluation of clindamycin release from glyceryl monooleate-alginate microspheres by NIR spectroscopy.
The purpose of this study was to use near-infrared (NIR) transmission spectroscopic technique to determine clindamycin plasma concentration after oral administration of clindamycin loaded GMO-alginate microspheres using rabbits as animal models. Lyophilized clindamycin-plasma standard samples at a concentration range of 0.001-10 μg/ml were prepared and analyzed by NIR and HPLC as a reference method. NIR calibration model was developed with partial least square (PLS) regression analysis. Then, a single dose in-vivo evaluation was carried out and clindamycin-plasma concentration was estimated by NIR. Over 24 h time period, the pharmacokinetic parameters of clindamycin were calculated for the clindamycin loaded GMO-alginate microspheres (F3) and alginate microspheres (F2), and compared with the plain drug (F1). PLS calibration model with 7-principal components (PC), and 8000-9200 cm(-1) spectral range shows a good correlation between HPLC and NIR values with root mean square error of cross validation (RMSECV), root mean square error of prediction (RMSEP), and calibration coefficient (R(2)) values of 0.245, 1.164, and 0.9753, respectively, which suggests that NIR transmission technique can be used for drug-plasma analysis without any extraction procedure. F3 microspheres exhibited controlled and prolonged absorption Tmax of 4.0 vs. 1.0 and 0.5 h; Cmax of 2.37±0.3 vs. 3.81±0.8 and 5.43±0.7 μg/ml for F2 and F1, respectively. These results suggest that the combination of GMO and alginate (1:4 w/w) could be successfully employed for once daily clindamycin microspheres formulation which confirmed by low Cmax and high Tmax values.
Military Medical Academy, Cairo, Egypt. Electronic address: miroami@gmail.com.
Amir Ibrahim
AI
Mohamed
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi Arabia.
Osama A A
OA
Ahmed
Medical services Department, Cairo, Egypt.
Suzan
S
Amin
Faculty of Pharmacy, Cairo University, Egypt.
Omar Anwar
OA
Elkadi
Department of Pharmaceutics, Faculty of Pharmacy, Cairo University, Cairo, Egypt.
Mohamed A
MA
Kassem
D000464:Alginates / Q000737:chemistry*; D000818:Animals; D002138:Calibration; D002851:Chromatography, High Pressure Liquid / Q000379:methods; D002981:Clindamycin / Q000737:chemistry*; D020723:Glucuronic Acid / Q000737:chemistry; D005989:Glycerides / Q000737:chemistry*; D006603:Hexuronic Acids / Q000737:chemistry; D016018:Least-Squares Analysis; D008297:Male; D008863:Microspheres; D008962:Models, Theoretical; D004364:Pharmaceutical Preparations / Q000737:chemistry*; D011817:Rabbits; D019265:Spectroscopy, Near-Infrared / Q000379:methods
D000464:Alginates; D005989:Glycerides; D006603:Hexuronic Acids; D004364:Pharmaceutical Preparations; D002981:Clindamycin; D020723:Glucuronic Acid; C005953:monoolein
Ca-alginate; Clindamycin HCl; Clindamycin Hcl (PubChem CID: 16051951); Glyceryl mono-oleate (GMO); Glyceryl monooleate (PubChem CID: 5283468); Near-infrared spectroscopy (NIR); Partial least squares regression (PLS); Sodium calcium alginate (PubChem CID: 6850754); Sustained release microspheres