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Dear Researchers,
I am Research fellow based at Mumbai working on Itraconazole
solubility enhancement. following are my set of questions:
1. Can anyone suggest me a suitable dissolution media for it which
could be correlated to the invivo dissolution behaviour also.
2. What are the related impurities in it and its classification ie
process impurities, api impurity.
3. Formulation strategies.
Hope to see your response soon.
regards
SHANKAR SWAMINATHAN
SENIOR RESEARCH FELLOW,
A-257, C/o Prof. P. R. Vavia,
UICT, N. P. Marg, Matunga, MUMBAI 400019
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The following message was posted to: PharmPK
Dear Shankar Swaminathan,
There are 3 commercial Itraconazole dosage form, Sporanox oral
solution, iv formulation (10mg/ml) and oral capsule (100mg). The liquid
formulations are solubilized in 40% hydroxypropyl-beta-cyclodextrin
(HPBCD) solution with the aid of hydrochloric acid and propyleneglycol.
The solubility of itraconazole is very sensitive to pH in the range
of pH 1
to 2. (see the paper of Miyake et al: Int. J. Pharm, 179 237-245, 1999).
A HPBCD complexation method for an oral formulation improvement
is published by M.E. Brewster et al in: Journal of Inclusion Phenomena
and Macrocyclyc Chemistry, Vol 44, No 1-4, 2002.
http://www.springerlink.com/content/gl21104258423238/
I suggest to check Pubmed using itraconazole-cyclodextrin keywords
to find publications for itraconazole solubilization.
Best regards, Maria Vikmon
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Itraconazole can be easily solubilized in tartaric acid (one of the
old Jensen publications), so see if this helps in developing your
dissolution media, other suggestion is to incorporating bile salts
into your dissolution medium (I doubt about its use in this
particular case), Itraconazole is insoluble like rock so you might
have to take clue from other insoluble drugs.
Best of luck
Prasad
Prasad NV Tata, Ph.D., FCP
Manager-Pharmacokinetics
Mallinckrodt, Inc.
675 McDonnell Blvd.
Saint Louis, MO 63134
Tel: (314) 654-5325
Fax: (314) 654-9325
e-mail: prasad.tata.aaa.tycohealthcare.com
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