Biomaterial Database

Formulation and optimization of rifampicin microparticles by Box-Behnken statistical design. 2012

D P Maurya, and Yasmin Sultana, and Mohd Aqil, and A Ali

Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard, New Delhi, India.

The objective of the present study was to optimize and evaluate in vitro gastroretentive performance of rifampicin microparticles. Formulations were optimized using design of experiments by employing a 4-factor, 3-level Box-Behnken statistical design. Independent variables studied were the ratio of polymers (Eudragit RSPO: ethyl cellulose), inert drug dispersing agent (talc), surfactant (sodium dodecyl sulfate) and stirring speed. The dependent variables were particle size and entrapment efficiency. Response surface plots were drawn, statistical validity of the polynomials was validated and the optimized formulation was characterized by Fourier Transform-InfraRed spectroscopy (FT-IR) and differential scanning calorimetry (DSC). Entrapment efficiency and particle size were determined. The designed microparticles have average particle size from 14.10 μm to 45.63 μm and entrapment efficiency from 38.14% to 94.81%. Optimized microparticles showed particle size and drug entrapment, 51.53 μm and 83.43%, respectively with sustained drug release behavior up to 12 h. In the present study, rifampicin microspheres were successfully prepared by a quasi-emulsion solvent diffusion technique for prolonged drug release. FT-IR and DSC studies did not reveal any significant drug interactions. The drug release was found to be controlled for more than 12 h by following zero order release pattern.

UI	MeSH Term	Description	Entries
D008863	Microspheres	Small uniformly-sized spherical particles, of micrometer dimensions, frequently labeled with radioisotopes or various reagents acting as tags or markers.	Latex Beads,Latex Particles,Latex Spheres,Microbeads,Bead, Latex,Beads, Latex,Latex Bead,Latex Particle,Latex Sphere,Microbead,Microsphere,Particle, Latex,Particles, Latex,Sphere, Latex,Spheres, Latex
D010316	Particle Size	Relating to the size of solids.	Particle Sizes,Size, Particle,Sizes, Particle
D011108	Polymers	Compounds formed by the joining of smaller, usually repeating, units linked by covalent bonds. These compounds often form large macromolecules (e.g., BIOPOLYMERS; PLASTICS).	Polymer
D011109	Polymethacrylic Acids	Poly-2-methylpropenoic acids. Used in the manufacture of methacrylate resins and plastics in the form of pellets and granules, as absorbent for biological materials and as filters; also as biological membranes and as hydrogens. Synonyms: methylacrylate polymer; poly(methylacrylate); acrylic acid methyl ester polymer.	Methacrylic Acid Polymers,Acid Polymers, Methacrylic,Acids, Polymethacrylic,Polymers, Methacrylic Acid
D002482	Cellulose	A polysaccharide with glucose units linked as in CELLOBIOSE. It is the chief constituent of plant fibers, cotton being the purest natural form of the substance. As a raw material, it forms the basis for many derivatives used in chromatography, ion exchange materials, explosives manufacturing, and pharmaceutical preparations.	Alphacel,Avicel,Heweten,Polyanhydroglucuronic Acid,Rayophane,Sulfite Cellulose,alpha-Cellulose,Acid, Polyanhydroglucuronic,alpha Cellulose
D002626	Chemistry, Pharmaceutical	Chemistry dealing with the composition and preparation of agents having PHARMACOLOGIC ACTIONS or diagnostic use.	Medicinal Chemistry,Chemistry, Pharmaceutic,Pharmaceutic Chemistry,Pharmaceutical Chemistry,Chemistry, Medicinal
D003692	Delayed-Action Preparations	Dosage forms of a drug that act over a period of time by controlled-release processes or technology.	Controlled Release Formulation,Controlled-Release Formulation,Controlled-Release Preparation,Delayed-Action Preparation,Depot Preparation,Depot Preparations,Extended Release Formulation,Extended Release Preparation,Prolonged-Action Preparation,Prolonged-Action Preparations,Sustained Release Formulation,Sustained-Release Preparation,Sustained-Release Preparations,Timed-Release Preparation,Timed-Release Preparations,Controlled-Release Formulations,Controlled-Release Preparations,Extended Release Formulations,Extended Release Preparations,Slow Release Formulation,Sustained Release Formulations,Controlled Release Formulations,Controlled Release Preparation,Controlled Release Preparations,Delayed Action Preparation,Delayed Action Preparations,Formulation, Controlled Release,Formulations, Controlled Release,Prolonged Action Preparation,Release Formulation, Controlled,Release Formulations, Controlled,Sustained Release Preparation,Timed Release Preparation,Timed Release Preparations
D004337	Drug Carriers	Forms to which substances are incorporated to improve the delivery and the effectiveness of drugs. Drug carriers are used in drug-delivery systems such as the controlled-release technology to prolong in vivo drug actions, decrease drug metabolism, and reduce drug toxicity. Carriers are also used in designs to increase the effectiveness of drug delivery to the target sites of pharmacological actions. Liposomes, albumin microspheres, soluble synthetic polymers, DNA complexes, protein-drug conjugates, and carrier erythrocytes among others have been employed as biodegradable drug carriers.	Drug Carrier
D004655	Emulsions	Colloids formed by the combination of two immiscible liquids such as oil and water. Lipid-in-water emulsions are usually liquid, like milk or lotion. Water-in-lipid emulsions tend to be creams. The formation of emulsions may be aided by amphiphatic molecules that surround one component of the system to form MICELLES.	Emulsion
D005079	Excipients	Usually inert substances added to a prescription in order to provide suitable consistency to the dosage form. These include binders, matrix, base or diluent in pills, tablets, creams, salves, etc.	Excipient,Stabilizing Agent,Stabilizing Agents,Suspending Agent,Suspending Agents,Agent, Stabilizing,Agent, Suspending,Agents, Stabilizing,Agents, Suspending