In situ amorphization of active pharmaceutical ingredients using microwave irradiation

Result code in IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F60461373%3A22340%2F17%3A43914048" target="_blank" >RIV/60461373:22340/17:43914048 - isvavai.cz</a>

Result on the web

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DOI - Digital Object Identifier

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Result language

angličtina

Original language name

In situ amorphization of active pharmaceutical ingredients using microwave irradiation

Original language description

One of the common issue in the pharmaceutical industry is poor solubility of active substances (APIs, from ?Active Pharmaceutical Ingredients?). The solubility might be significantly enhanced by changing the crystalline state of the API to its amorphous one. The amorphous state is characterized by lower stability and thus better dissolution properties leading in better bioavailability. The amorphous API in a dosage form (such as tablets) must remain stable for at least shelf life of the drug product (usually 2 - 3 years). Wet and dry granulation or direct tableting can be used to create tablets containing crystalline form of API. The amorphous form can be created in situ ?on demand? by the end user using microwave radiation (MW). Proof of concept of tablets and powder composed from an Ibuprofen as a model drug and (i) Poly(ethylene glycol) 6000 (PEG 6000), (ii) PEG 3000 or (iii) silica nano-particles as excipients was experimentally investigated. The in situ amorphization of ibuprofen was investigated in a commercial microwave oven. The heating properties of the oven, i.e. spatial distribution of microwave heating were characterized. The microwave power input and composition of the tablets (excipient/Ibuprofen content) were tested with respect to the melting of the Ibuprofen. The change of crystalline structure due to the MW heating was analyzed by x-ray diffraction (XRD) and differential scanning calorimetry (DSC). Dissolution profiles of both MW untreated and treated tablets were evaluated by time-dependent UV/vis spectrophotometry. Infrared spectroscopy was used for characterization of tablets structure stability.

Czech name

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Czech description

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Type

D - Article in proceedings

CEP classification

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OECD FORD branch

20401 - Chemical engineering (plants, products)

Project

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Continuities

S - Specificky vyzkum na vysokych skolach

Publication year

2017

Confidentiality

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Article name in the collection

PROCEEDINGS 44th International Conference of the Slovak Society of Chemical Engineering

ISBN

978-80-89597-58-1

ISSN

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e-ISSN

neuvedeno

Number of pages

1

Pages from-to

877

Publisher name

Slovak Society of Chemical Engineering

Place of publication

Bratislava

Event location

Demänovská dolina

Event date

May 22, 2017

Type of event by nationality

WRD - Celosvětová akce

UT code for WoS article

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