Partial Solubility Parametes of Lactose, Mannitol and Saccharose Using the Modified Extended Hansen Method and Evaporation Light Scattering Detection

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概要

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• The modified extended Hansen method was tested for the first time to determine partial solubility parameters of non-polymeric pharmaceutical excipients. The method was formerly tested with drug molecules, and is based upon a regression analysis of the logarithm of the mole fraction solubility of the solute against the partial solubility parameters of a series of solvents of different chemical classes. Two monosaccharides and one disaccharide (lactose mononydrate, saccharose and mannitol) were chosen. The solubility of these compounds was de-termined in a series of solvents ranging from nonolar to polar and covering a wide range of the solubility parameter scale. Sugars do not absorb at the UV-vis region, and the saturated solutions were assayed with a recent chromatographic technique coupled to an evaporatiev light scattering detector. This technique was suitable to determine the concentration dissolved in most solvents. The modified extended Hansen method provided better results than the original approach.The best model was the four parameter equation, which includes the dispersion δ_d, dipolar δ_p, acidic δ_a and basic δ_b partial solubility parameters. The partial solubility parameters obtained, expressed as MPa^<1/2>, were δ_d=17.6,δ_p=28.7,δ_h=19,δ_b=14.5,δ_b=12.4,δ_T=32.8 for lactose, δ_d=16.2,δ_p=24.5,δ_h=14.6,δ_a=8.7,δ_b=12.2,δ_T=32.8 for mannitol and δ_d=17.1,δ_P=18.5,δ_h=13,δ_a=11.3,δ_b=7.6,δ_T=28.4 for saccharose. The high total solubility total solubility parameters δ_T obtained agree with the polar nature of the sugars. The dispersion parametes δ_d are quite similar for the three sugars indicating that the polar δ_p and hydrogen bonding parameters (δ_h, δ_a, δ_b) are responsible for the variation in the total solubility parameters δ_T obtained, as also found for drugs. The results suggest that the method could be extended to determine the partial solubility parameters of other non-polymeric pharmaceutical excipients.

• 公益社団法人日本薬学会の論文
• 2000-02-01

著者

• Bustamante Pilar

  Departamento de Farmacia y Tecnología Farmacéutica, Facultad de Farmacia, Universidad de Alcalá

• Barra Jerome

  School Of Pharmacy Department Of Pharmaceutical Technology University Of Geneva

• Daali Youssef

  School Of Pharmacy Laboratory Of Pharmaceutical Analytical Chemistry University Of Geneva

• PENA M.

  Department of Farmacia y Tecnologia Farmaceutica, Facultad de Farmacia, Universidad de Alcala

• Pena M.

  Department Of Farmacia Y Tecnologia Farmaceutica Facultad De Farmacia Universidad De Alcala

• Bustamante Pilar

  Departamento de Farmacia y Tecnología Farmacéutica, Facultad de Farmacia, Universidad de Alcalá

• Pena M.Angeles

  Department of Farmacia y Tecnologia Farmaceutica, Facultad de Farmacia, Universidad de Alcala

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• Multiple Solubility Maxima of Oxolinic Acid in Mixed Solvents and a New Extension of Hilderand Solubility Approach
• The Behavior of Paracetamol in Mixtures of Amphirotic and Amphiprotic-Aprotic Solvents. Relationship of Solubility Curves to Specific and Nonspecific Interactions
• Partial Solubility Parametes of Lactose, Mannitol and Saccharose Using the Modified Extended Hansen Method and Evaporation Light Scattering Detection

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