S Isomer

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Csaba Szantay - One of the best experts on this subject based on the ideXlab platform.

Laszlo Poppe - One of the best experts on this subject based on the ideXlab platform.

Martin P Redmon - One of the best experts on this subject based on the ideXlab platform.

  • preformulation StudieS on the S iSomer of oxybutynin hydrochloride an improved chemical entity ice
    Drug Development and Industrial Pharmacy, 2001
    Co-Authors: Paul E Luner, Shingai Majuru, Anjali B Joshi, Euichaul Oh, Dale Eric Wurster, Lee E Kirsch, Martin P Redmon
    Abstract:

    (S)-Oxybutynin HCl (S-OXY) iS a white cryStalline Solid powder with an acicular particle morphology. Differential Scanning calorimetry (DSC) thermogramS revealed one characteriStic endotherm at 116.2°C. On reScanning a Sample heated to 120°C, no thermal eventS were diStinguiShed in the temperature range 25°C to 150°C. Weight loSS curveS determined by thermogravimetric analySiS Showed a continuouS, gradual weight loSS of about 0.15% over the temperature range 30°C to 110°C, followed by a change in Slope and more rapid weight loSS beginning at 150°C. ObServation by hot-Stage microScopy confirmed the melting endotherm obServed by DSC. Equilibrium moiSture uptake StudieS indicated low water vapor uptake at low relative humiditieS (< 52.8%). At relative humiditieS of 75.3% and 84.3%, S-OXY firSt deliqueSced and then converted to a lower melting point cryStal form. X-ray powder diffraction (XRPD) data Supported the DSC findingS. S-OXY underwent degradation by eSter hydrolySiS at alkaline pHS. The kineticS of th...

  • preformulation StudieS on the S iSomer of oxybutynin hydrochloride an improved chemical entity ice
    Drug Development and Industrial Pharmacy, 2001
    Co-Authors: Paul E Luner, Shingai Majuru, Anjali B Joshi, Dale Eric Wurster, Lee E Kirsch, Martin P Redmon
    Abstract:

    (S)-Oxybutynin HCl (S-OXY) iS a white cryStalline Solid powder with an acicular particle morphology. Differential Scanning calorimetry (DSC) thermogramS revealed one characteriStic endotherm at 116.2 degreeS C. On reScanning a Sample heated to 120 degreeS C, no thermal eventS were diStinguiShed in the temperature range 25 degreeS C to 150 degreeS C. Weight loSS curveS determined by thermogravimetric analySiS Showed a continuouS, gradual weight loSS of about 0.15% over the temperature range 30 degreeS C to 110 degreeS C, followed by a change in Slope and more rapid weight loSS beginning at 150 degreeS C. ObServation by hot-Stage microScopy confirmed the melting endotherm obServed by DSC. Equilibrium moiSture uptake StudieS indicated low water vapor uptake at low relative humiditieS (<52.8%). At relative humiditieS of 75.3% and 84.3%, S-OXY firSt deliqueSced and then converted to a lower melting point cryStal form. X-ray powder diffraction (XRPD) data Supported the DSC findingS. S-OXY underwent degradation by eSter hydrolySiS at alkaline pHS. The kineticS of thiS reaction were Studied at 25 degreeS C in carbonate-bicarbonate bufferS. ObServed rate conStantS of 0.008 h(-1) and 0.0552 h(-1) were determined at pH 9.69 and 10.25, reSpectively. The pKa of S-OXY waS 7.75. The aqueouS Solubility of S-OXY waS deScribed aS a function of pH and the free-baSe Solubility. The mean partition coefficient log P waS 3.33 uSing 1-octanol. The Surface tenSionS of aqueouS SolutionS of S-OXY decreaSed with increaSing concentration, but no concentration-independent region waS obServed, indicating that S-OXY doeS notform micelleS in aqueouS Solution. The diSSolution rate of S-OXY from a compreSSed diSk in 0.1 N HCl waS rapid, whereaS it waS conSiderably Slower at pH 7.4. Addition of 1% hexadecyltrimethylammonium bromide (CTAB) at pH 7.4 Significantly improved the diSSolution rate. S-OXY diSplayed very poor flow propertieS when compared to Standard pharmaceutical excipientS. XRPD reSultS indicated that S-OXY exhibited a loSS in cryStallinity following ball milling. HieStand tableting indiceS indicated that S-OXY haS good bonding propertieS andformS Strong compactS, but iS likely to be SuSceptible to capping on ejection from the die. ThiS indicated the needfor a plaStically deformable excipient Such aS Avicel PH-101 in tablet formulationS.

J Devenyi - One of the best experts on this subject based on the ideXlab platform.

L Novak - One of the best experts on this subject based on the ideXlab platform.