In vivo evaluation of modified gum karaya as a carrier for improving the oral bioavailability of a poorly water-soluble drug, nimodipine.
This work examines the influence of modified gum karaya (MGK) on the oral bioavailability of a poorly water-soluble drug, nimodipine (NM), in comparison with that of gum karaya (GK). A cogrinding method was selected to prepare mixtures of NM and GK or MGK in a 1:9 ratio (NM:GK/MGK). Differential scanning calorimetry (DSC), Fourier transmission infrared (FT-IR) spectroscopy, X-ray diffraction (XRD), solubility studies, and in vitro release studies were performed to characterize the properties of the cogrinding mixtures. No drug-carrier interactions were found, as confirmed by DSC and FT-IR studies. The XRD study revealed that the crystallinity of NM was identical in both the cogrinding mixtures and was decreased when compared to that of physical mixtures or pure NM. The in vitro release rate of NM from both cogrinding mixtures was significantly higher than that of physical mixtures or pure NM. The in vivo study revealed that the bioavailability of NM from pure drug was significantly lower when compared to the cogrinding mixtures. The oral bioavailability was found to be NM powder < cogrinding mixtures of NM and GK < cogrinding mixtures of NM and MGK < NM solution. It can be inferred from the above results that MGK, an economical carrier, could be used for the dissolution enhancement of NM.
Murali Mohan Babu
Gedela V
GV
Division of Industrial Pharmacy, Department of Pharmaceutical Sciences, Andhra University, Visakhapatnam-0 003 AP, India.
Kumar
Namballa R
NR
Sankar
Kasina H
KH
Ram
Battu J
BJ
Kumar
Namburu K
NK
Murthy
Kolapalli V R
KV
D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D002152:Calorimetry, Differential Scanning / Q000379:methods; D018592:Cross-Over Studies; D004337:Drug Carriers / Q000737:chemistry / Q000378:metabolism / Q000493:pharmacokinetics*; D004353:Drug Evaluation, Preclinical / Q000379:methods; D007618:Karaya Gum / Q000097:blood / Q000737:chemistry / Q000378:metabolism* / Q000493:pharmacokinetics*; D008297:Male; D009553:Nimodipine / Q000097:blood / Q000737:chemistry* / Q000378:metabolism / Q000493:pharmacokinetics*; D011817:Rabbits; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared / Q000379:methods; D013678:Technology, Pharmaceutical / Q000295:instrumentation / Q000379:methods; D014867:Water / Q000737:chemistry*; D014961:X-Ray Diffraction / Q000379:methods
D004337:Drug Carriers; D014867:Water; D009553:Nimodipine; D007618:Karaya Gum