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Salt formation to DECREASE the
solubility of a drug – A case study
on a commercially available
formulation
Presented by: D...
Reasons to decrease solubility
Controlled release and/or BA
Depot formulations
Ease of processing
 Ca, Mg salts of org...
Model drug studied
Hydroxyzine
Hydroxyzine HCl
Hydroxyzine Pamoate
Ref: Hydroxyzine - A Medical Dictionary, Bibliograph...
 Hydroxizine
Dihydrochloride
 Hydroxizine Pamoate
Comparison
Hydroxizine Dihydrochloride Hydroxizine Pamoate
Solubility Very soluble in water. Very slightly soluble in
cold...
Comparison
Hydroxizine Dihydrochloride Hydroxizine Pamoate
Solubility Very soluble in water. Very slightly soluble in
cold...
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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

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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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