Abstract
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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Administration, Oral
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Angiotensin I
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Angiotensin-Converting Enzyme Inhibitors / administration & dosage
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Angiotensin-Converting Enzyme Inhibitors / chemistry*
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Angiotensin-Converting Enzyme Inhibitors / pharmacology
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Animals
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Antihypertensive Agents / administration & dosage
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Antihypertensive Agents / chemistry*
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Antihypertensive Agents / pharmacology
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Blood Pressure / drug effects
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Captopril / administration & dosage
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Captopril / chemistry*
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Captopril / pharmacology
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Cellulose / analogs & derivatives*
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Cellulose / chemistry
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Chemistry, Pharmaceutical
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Crystallography, X-Ray
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Delayed-Action Preparations
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Disease Models, Animal
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Drug Compounding
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Female
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Hypertension / chemically induced
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Hypertension / drug therapy
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Hypertension / physiopathology
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Kinetics
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Methylcellulose / chemistry*
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Microscopy, Electron, Scanning
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Models, Chemical
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Povidone / chemistry
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Powder Diffraction
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Powders
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Rats
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Rats, Wistar
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Solubility
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Technology, Pharmaceutical / methods*
Substances
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Angiotensin-Converting Enzyme Inhibitors
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Antihypertensive Agents
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Delayed-Action Preparations
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Powders
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ethyl cellulose
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Cellulose
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Methylcellulose
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Angiotensin I
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Captopril
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Povidone