Development of controlled release captopril granules coated with ethylcellulose and methylcellulose by fluid bed dryer.
Captopril granules of controlled release with different polymers as ethylcellulose, ethyl/methylcellulose, and immediate release with polyvinylpyrrolidone (PVP) were developed by fluid bed dryer technique. The formulations were analyzed by scanning electron microscopy, X-ray powder diffraction, and dissolution profiles. To compare the formulations an in vivo setting rat blood pressure assay was performed, using angiotensin I as a vasoconstrictor agent. The scanning electron microscopy of granules showed differences in morphology, and X-ray powder diffraction technique presented some modification in crystalline structure of captopril in granules coated with PVP and ethyl/methylcellulose. The dissolution profile of granules coated with ethylcellulose showed a median time release of 4 hr whereas for granules coated with ethyl/methylcellulose, this time was 3.5 hr. The blockage of angiotensin I-induced hypertensive effect lasted 8 hr in granules coated with PVP and of more than 12 hr in the granules coated with ethylcellulose and ethyl/methylcellulose.
Stulzer
Hellen Karine
HK
Departamento de Ciências Farmacêuticas, Universidade Federal de Santa Catarina, Florianópolis, SC, Brazil. hellen.stulzer@gmail.com
Silva
Marcos Antonio Segatto
MA
Fernandes
Daniel
D
Assreuy
Jamil
J
D000284:Administration, Oral; D000803:Angiotensin I; D000806:Angiotensin-Converting Enzyme Inhibitors / Q000008:administration & dosage / Q000737:chemistry* / Q000494:pharmacology; D000818:Animals; D000959:Antihypertensive Agents / Q000008:administration & dosage / Q000737:chemistry* / Q000494:pharmacology; D001794:Blood Pressure / Q000187:drug effects; D002216:Captopril / Q000008:administration & dosage / Q000737:chemistry* / Q000494:pharmacology; D002482:Cellulose / Q000031:analogs & derivatives* / Q000737:chemistry; D002626:Chemistry, Pharmaceutical; D018360:Crystallography, X-Ray; D003692:Delayed-Action Preparations; D004195:Disease Models, Animal; D004339:Drug Compounding; D005260:Female; D006973:Hypertension / Q000139:chemically induced / Q000188:drug therapy / Q000503:physiopathology; D007700:Kinetics; D008747:Methylcellulose / Q000737:chemistry*; D008855:Microscopy, Electron, Scanning; D008956:Models, Chemical; D011205:Povidone / Q000737:chemistry; D033362:Powder Diffraction; D011208:Powders; D051381:Rats; D017208:Rats, Wistar; D012995:Solubility; D013678:Technology, Pharmaceutical / Q000379:methods*
D000806:Angiotensin-Converting Enzyme Inhibitors; D000959:Antihypertensive Agents; D003692:Delayed-Action Preparations; D011208:Powders; C013517:ethyl cellulose; D002482:Cellulose; D008747:Methylcellulose; D000803:Angiotensin I; D002216:Captopril; D011205:Povidone