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Preformulation eval...
Preformulation evaluation of AZD1305, an oxabispidine intended for oral and intravenous treatment
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- Sigfridsson, Kalle, 1964 (författare)
- Chalmers tekniska högskola,Chalmers University of Technology
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- Lundqvist, R. (författare)
- AstraZeneca AB
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- Ohlson, K. (författare)
- AstraZeneca AB
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(creator_code:org_t)
- 2011-06-27
- 2012
- Engelska.
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Ingår i: Drug Development and Industrial Pharmacy. - : Informa UK Limited. - 0363-9045 .- 1520-5762. ; 38:1, s. 19-31
- Relaterad länk:
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http://dx.doi.org/10...
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https://doi.org/10.3...
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Abstract
Ämnesord
Stäng
- Aim: AZD1305 is a novel, water-soluble investigational antiarrhythmic agent for restoration and maintenance of sinus rhythm in atrial fibrillation patients. The present studies were performed to evaluate the possibility for further development of the compound.Methods: A set of technical approaches were used, including X-ray powder diffractometry, differential scanning calorimetry, thermogravimetrical analysis, dynamic vapor sorption, scanning electron microscopy, salt screen, and liquid chromatography.Results: AZD1305 is a crystalline oxabispidine and its neutral form is a base with a pK(a) of 9.9. The substance degrades with higher temperature and lower pH. The free base of the solid substance is stable at 25 degrees C (closed container), 40 degrees C/75% relative humidity (open container), and at 50 degrees C (closed container) for at least 3 months. The free base of AZD1305 is polymorphic with two known forms. Both forms are non-hygroscopic ansolvates with melting points of approximately 90 degrees C. No salt was found with overall improved properties. The substance had a strong odor, which was reduced by increased particle size.Conclusions: The free base of AZD1305 seemed to be the most suitable agent for product development even though it has a fairly low melting point and occurred as two different crystal forms. Form B was the most stable thermodynamically in the temperature interval of interest.
Ämnesord
- NATURVETENSKAP -- Kemi (hsv//swe)
- NATURAL SCIENCES -- Chemical Sciences (hsv//eng)
Nyckelord
- smell
- salt-screen
- polymorphs
- stability
- early development
- Drug delivery
- odor
- solid-state
Publikations- och innehållstyp
- art (ämneskategori)
- ref (ämneskategori)
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