I develop the water soluble powder dosage form of veterinary medicine, but the raw materials A and B (the Active Pharmaceutical Ingredients) are practically insoluble in water.
I've added some wetting agents, surfactants, and also initiate the salt-forming by adding sodium chloride to become "A-sodium" and "B-HCl" which are soluble in water (I found the solubility data on USP and BP monograph, that the "A-sodium" and "B-HCl" is very soluble in water).
Thanks... :'D
Dear Yulia,
Are you not able to get (buy) the sodium salt of A and the B hydrochloride?
Did you add NaCl to the mixture of A and B expecting to obtain them?
Have you tried to add HCl to B (which I guess is an amine) and NaOH to A (a week acid)? Follow with the common crystallization/purification steps.
Hope it helped.
Kind regards, Luis
Thanks for replying Mr. Luis.... :'D
I suggested my R&D GM to replaced that insoluble-raw material with salt form... but unfortunately, he ask me to develop more... :')
Actually, my formula of dosage form (water soluble powder) may dissolve in water, but there were some (little) particles which insoluble...
Maybe I'll follow your suggestion to add HCl and NaOH, but my final 'finished product' are powder (dry)... :'D
Sincerely yours...
In solid dosage form, you can use a cyclodextrin for complexation and solid dispersion to enhance its solubility, or you must know the material behavior of your API e.g. crystal form and you can modify it
Solubility of substance may by particle size reduction, and increasing surface area of substance and also increase with heating so that solubility of partially insoluble substance increases upon heating.
other technique are: Co-crystallisation, co-solvency solubilizing agents, molecular encapsulation with cyclodextrins, crystal engineering, salt formation, solid dispersion, use of surfactant, complexation
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3399483/
http://www.ijplsjournal.com/issues%20PDF%20files/feb_2012/10.pdf
Dear Yulia, If you are (as I guess) in a regulated medicines environment and trying to develop a drug product that needs to be approved by Regulatory Agencies prior to marketing, I advise you to keep it as simple as possible.
This is not "rocket science" and don't try to reinvent the wheel.
Buy the drug as water soluble salts (from approved, cGMP compliant API manufacturers) - your company will save money in the pharmaceutical development, in the control of excipients and API's, in the validation of the manufacturing process etc, etc, and eventually this will facilitate the drug approval process.
Take my word, I'm a Regulatory assessor for veterinary as well as for human medicines.
Kind regards, Luis
@Kapil: solubility of a substance is not dependent on its particle size! However if you want to speed up the dissolution process thenyou should reduce the particle size. These are two different things.
Solubility enhancement of poorly soluble drugs in aqueous solutions could be by using surfactants or a blend of surfactants (refer to HLB values), or using co-solvents such as Glycerin, Propylene Glycol, Alcohol, etc, or complexation with CB-yclodextrin. Also, by determining the proper pH of solubility either by using buffer system or buffering agents. While in case of solid dosage forms, by particle size reduction, salt formation, solid dispersion technique, cyclodextrin complexion, or by co-solvency.
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