Celecoxib nanosuspension and preparation method thereof

A nano-suspension, celecoxib technology, applied in anti-inflammatory agents, pharmaceutical formulations, non-central analgesics, etc., can solve the problems of low bioavailability of celecoxib, large drug dosage, etc. The effect of increasing solubility and dissolution rate, simple formulation and process, and easy industrialization
CN105147607AInactive Publication Date: 2015-12-16CHINA PHARM UNIV
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
CHINA PHARM UNIV
Publication Date
2015-12-16
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention belongs to the field of pharmaceutical preparations and provides a Celecoxib nanosuspension and a preparation method thereof. Celecoxib is a novel non-steroidal anti-inflammatory drug, inhibits cyclooxygenase -2(COX-2) is through specificity, has anti-inflammatory and pain-easing effects and is clinically used for treating osteoarthritis and rheumatoid arthritis. However, the Celecoxib has very low solubility and in-vivo bioavailability. In order to increase the dissolution and the bioavailability of the drug, a high-speed shearing combined high-pressure homogenizing method is adopted to prepare the Celecoxib nanosuspension, the particle size and the polydispersion index PI are used as indicators for formulation technology optimization, a laser particle analyzer and a transmission electron microscope are adopted to study the particle size and form of the drug, the dissolution of the drug is evaluated through in-vitro dissolution experiments, and rat in-vivo pharmacokinetic study is conducted. Measurement results prove that the drug particle size of the nanosuspension is 50-500 nm, and the dissolution and the in-vivo bioavailability of the drug are increased obviously.
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Description

technical field

[0001] The invention relates to the field of pharmaceutical preparations, in particular to a celecoxib nanosuspension and a preparation method thereof. Background technique

[0002] Celecoxib is a nonsteroidal anti-inflammatory drug (NSAID) s ), can specifically inhibit cyclooxygenase-2 (COX-2), prevent the production of inflammatory prostaglandins, and then exert anti-inflammatory, analgesic and antipyretic effects. Clinically, it is mainly used for the treatment of osteoarthritis, rheumatoid arthritis and peripheral and central analgesia.

[0003] Celecoxib is soluble in methanol, ethanol, dimethyl sulfoxide, acetone and other organic solvents, but hardly soluble in water. The solubility in water is only 3-7μg / mL (pH7, 40℃), and it belongs to the BCSII class of biopharmaceutical classification system . The extremely low solubility of celecoxib in water directly leads to poor gastrointestinal absorption and low oral bioavailability of the drug, which grea...

Claims

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