Salt Formation To Decrease The Solubility Of A Drug – A Case Study On A Commercially Available Formulation

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Salt formation to DECREASE the solubility of a drug – A case study on a commercially available formulation

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Salt Formation To Decrease The Solubility Of A Drug – A Case Study On A Commercially Available Formulation

  1. 1. Salt formation to DECREASE the solubility of a drug – A case study on a commercially available formulation Presented by: Debanjan Das NOTE: Typically, salt formation is carried out to enhance solubility. Here, the reverse process was required to adjust required bioavailability
  2. 2. Reasons to decrease solubility Controlled release and/or BA Depot formulations Ease of processing  Ca, Mg salts of organic acids form soaps which can tolerate the rigors of manufacturing operations Easier to control polymorphism with a salt of less solubility
  3. 3. Model drug studied Hydroxyzine Hydroxyzine HCl Hydroxyzine Pamoate Ref: Hydroxyzine - A Medical Dictionary, Bibliography, and Annotated Research Guide, Icon Health Publications; Icon Health Publications, ISBN: 0597844569, March 2004
  4. 4.  Hydroxizine Dihydrochloride  Hydroxizine Pamoate
  5. 5. Comparison Hydroxizine Dihydrochloride Hydroxizine Pamoate Solubility Very soluble in water. Very slightly soluble in cold water. Molecular Weight Weight: 447.83 g/mole 763.29 g/mole Toxicity LD50 Oral Rat 950 mg/kg LD50 IP Mouse 122 mg/kg LD50 IP Rat 126 mg/kg LD50 IV Mouse 48.9 mg/kg LD50 IV Rat 45 mg/kg ORAL (LD50): Acute: 1740 mg/kg [Rat]. 1840 mg/kg [Mouse].
  6. 6. Comparison Hydroxizine Dihydrochloride Hydroxizine Pamoate Solubility Very soluble in water. Very slightly soluble in cold water. Molecular Weight Weight: 447.83 g/mole 763.29 g/mole Toxicity LD50 Oral Rat 950 mg/kg LD50 IP Mouse 122 mg/kg LD50 IP Rat 126 mg/kg LD50 IV Mouse 48.9 mg/kg LD50 IV Rat 45 mg/kg ORAL (LD50): Acute: 1740 mg/kg [Rat]. 1840 mg/kg [Mouse].

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