Molecular inclusion of rofecoxib with cyclodextrin: pharmacological properties in laboratory animals.
Rofecoxib is practically insoluble in water and its prolonged use is associated with the incidence of side effects like gastrointestinal perforations, ulcerations and bleeding. Therefore, an attempt has been made to improve the aqueous solubility of the drug by making an inclusion complex using dimethyl-beta-cyclodextrin (DIMEB). The complexes were prepared by kneading and by the spray drying method. The prepared complexes showed better anti-inflammatory activity and decreased ulcerogenic potential than the pure drug.
Baboota
S
S
Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard, (Hamdard University), New Delhi, India. sbaboota@rediffmail.com
Dhaliwal
M
M
Kohli
K
K
Ali
J
J
D000818:Animals; D002351:Carrageenan; D003505:Cyclodextrins; D051546:Cyclooxygenase 2; D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors / Q000008:administration & dosage* / Q000737:chemistry* / Q000494:pharmacology; D004339:Drug Compounding; D004487:Edema / Q000139:chemically induced / Q000517:prevention & control; D005079:Excipients; D007527:Isoenzymes / Q000378:metabolism; D007783:Lactones / Q000008:administration & dosage* / Q000737:chemistry* / Q000494:pharmacology; D008297:Male; D011451:Prostaglandin-Endoperoxide Synthases / Q000378:metabolism; D051381:Rats; D017208:Rats, Wistar; D013276:Stomach Ulcer / Q000139:chemically induced / Q000473:pathology; D013450:Sulfones
D003505:Cyclodextrins; D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors; D005079:Excipients; D007527:Isoenzymes; D007783:Lactones; D013450:Sulfones; C116926:rofecoxib; D002351:Carrageenan; D051546:Cyclooxygenase 2; D011451:Prostaglandin-Endoperoxide Synthases