Dyphylline - CAS 479-18-5
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Not Intended for Therapeutic Use. For research use only.
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Adenosine Receptor
Dyphylline is a xanthine derivative with bronchodilator and vasodilator effects.It is used in the treatment of respiratory disorders like asthma, cardiac dyspnea, and bronchitis. It acts as an adenosine receptor antagonist and phosphodiesterase inhibitor.
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1.Impact of molecular flexibility on double polymorphism, solid solutions and chiral discrimination during crystallization of diprophylline enantiomers.
Brandel C1, Amharar Y, Rollinger JM, Griesser UJ, Cartigny Y, Petit S, Coquerel G. Mol Pharm. 2013 Oct 7;10(10):3850-61. doi: 10.1021/mp400308u. Epub 2013 Sep 13.
The polymorphic behavior of racemic and enantiopure diprophylline (DPL), a chiral derivative of theophylline marketed as a racemic solid, has been investigated by combining differential scanning calorimetry, powder X-ray diffraction, hot-stage microscopy and single-crystal X-ray experiments. The pure enantiomers were obtained by a chemical synthesis route, and additionally an enantioselective crystallization procedure was developed. The binary phase diagram between the DPL enantiomers was constructed and revealed a double polymorphism (i.e., polymorphism both of the racemic mixture and of the pure enantiomer). The study of the various equilibria in this highly unusual phase diagram revealed a complex situation since mixtures of DPL enantiomers can crystallize either as a stable racemic compound, a metastable conglomerate, or two distinct metastable solid solutions. Crystal structure analysis revealed that the DPL molecules adopt different conformations in the crystal forms suggesting that the conformational degrees of freedom of the substituent that carries the only two H-bond donor groups might be related to the versatile crystallization behavior of DPL.
2.Thermoplastic polyurethanes for the manufacturing of highly dosed oral sustained release matrices via hot melt extrusion and injection molding.
Claeys B1, Vervaeck A1, Hillewaere XK2, Possemiers S3, Hansen L4, De Beer T4, Remon JP1, Vervaet C5. Eur J Pharm Biopharm. 2015 Feb;90:44-52. doi: 10.1016/j.ejpb.2014.11.003. Epub 2014 Nov 15.
This study evaluated thermoplastic polyurethanes (TPUR) as matrix excipients for the production of oral solid dosage forms via hot melt extrusion (HME) in combination with injection molding (IM). We demonstrated that TPURs enable the production of solid dispersions - crystalline API in a crystalline carrier - at an extrusion temperature below the drug melting temperature (Tm) with a drug content up to 65% (wt.%). The release of metoprolol tartrate was controlled over 24h, whereas a complete release of diprophylline was only possible in combination with a drug release modifier: polyethylene glycol 4000 (PEG 4000) or Tween 80. No burst release nor a change in tablet size and geometry was detected for any of the formulations after dissolution testing. The total matrix porosity increased gradually upon drug release. Oral administration of TPUR did not affect the GI ecosystem (pH, bacterial count, short chain fatty acids), monitored via the Simulator of the Human Intestinal Microbial Ecosystem (SHIME).
3.Application of artificial neural networks (ANNs) and genetic programming (GP) for prediction of drug release from solid lipid matrices.
Güres S1, Mendyk A, Jachowicz R, Dorożyński P, Kleinebudde P. Int J Pharm. 2012 Oct 15;436(1-2):877-9. doi: 10.1016/j.ijpharm.2012.05.021. Epub 2012 Jun 21.
The aim of the present study was to develop a semi-empirical mathematical model, which is able to predict the release profiles of solid lipid extrudates of different dimensions. The development of the model was based on the application of ANNs and GP. ANNs' abilities to deal with multidimensional data were exploited. GP programming was used to determine the constants of the model function, a modified Weibull equation. Differently dimensioned extrudates consisting of diprophylline, tristearin and polyethylene glycol were produced by the use of a twin-screw extruder and their dissolution behaviour was studied. Experimentally obtained dissolution curves were compared to the calculated release profiles, derived from the semi-empirical mathematical model.
4.The effect of polymer properties on direct compression and drug release from water-insoluble controlled release matrix tablets.
Grund J1, Koerber M2, Walther M1, Bodmeier R1. Int J Pharm. 2014 Jul 20;469(1):94-101. doi: 10.1016/j.ijpharm.2014.04.033. Epub 2014 Apr 16.
The objective of this study was to identify and evaluate key polymer properties affecting direct compression and drug release from water-insoluble matrices. Commonly used polymers, such as Kollidon(®) SR, Eudragit(®) RS and ethyl cellulose, were characterized, formulated into tablets and compared with regard to their properties in dry and wet state. A similar site percolation threshold of 65% v/v was found for all polymers in dry state. Key parameters influencing polymer compactibility were the surface properties and the glass transition temperature (T(g)), affecting polymer elasticity and particle size-dependent binding. The important properties observed in dry state also governed matrix characteristics and therefore drug release in wet state. A low T(g) (Kollidon(®) SR<Eudragit(®) RS) decreased the percolation threshold, particle size effect and tortuosity, but increased permeability and sensitivity to heat/humidity treatment. Hence, lower permeability and higher stability are benefits of a high-T(g) polymer (ethyl cellulose).
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CAS 479-18-5 Dyphylline

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