I have performed release experiment of poorly water-soluble drug from different polymer matrix. I have used simulated intestinal fluid SIF conform to USP (pH 7.4 buffer solution). As suspected the release has been close to zero. On the other side, the in-vivo experiment demonstrate the intestinal absorption of the drug. Do exist simulated intestinal fluid appropriate for poorly water-soluble drugs?
Best regards
Marco
Hello. Dear Marco
My university degree is Chemistry , your question is related to Pharmacy, on the other hand, my article is about Oil Spill. Sorry , I do not have knowledge about your question.
Kind Regards
Reza Pashaei
Dear Marco
if the release was close to zero, that meant the polymer problem rather than the drug itself. You have to select a carrier that could disintegrate at your experimental condition. on the other hand, if your drug was released but not soluble in the SIF, then you have to increase the solubility of your compound first either by chemical modification (by conjugating ester group) or by adding some surface active agent.
You may consider changing the polymer to liposome or nanoemulsion or any other suitable carrier. formulating oil-in-water emulsion could help as well.
Hope you found these answers useful
regards
Dear Marco
if the release was close to zero, that meant the polymer problem rather than the drug itself. You have to select a carrier that could disintegrate at your experimental condition. on the other hand, if your drug was released but not soluble in the SIF, then you have to increase the solubility of your compound first either by chemical modification (by conjugating ester group) or by adding some surface active agent.
You may consider changing the polymer to liposome or nanoemulsion or any other suitable carrier. formulating oil-in-water emulsion could help as well.
Hope you found these answers useful
regards
If drug is official in pharmacopoeia, use the appropriate recommended disso media. If not then you can first find out solubility of your drug in different media and select appropriate one base of drug absorption window.
Dear Marco,
from my experience I would recommend not only the change of composition of the fluid but also the method choice. In case of poorly soluble drugs, dissolution in apparatus 4 give positive effects. It give you possibility of use closed or open loop disolution.
Dear Marco,
from my experience I would recommend not only the change of composition of the fluid but also the method choice. In case of poorly soluble drugs, dissolution in apparatus 4 give positive effects. It give you possibility of use closed or open loop disolution.
Dear All,
Thanks for your answers. I guess if I the change the media (SIF) I lost the "instestinal absorption simulation". THe apparatous 4 is really ineteesting, do you know the most appropriate flow rate to simulate and intestinal release ?
Dear Marco Consumi,
Solubility can be performed in the dissolution medium in the drug product or in generic media such as simulated gastric fluid (SGF) or simulated intestinal fluid (SIF). Basically, the two media purposely simulating gastrointestinal fluids currently used in USP tests solutions.
Soluble Compositions of SGF
2g sodium chloride, 3.2 gm pepsin, 7 ml HCl, and 1000ml water for SGF.
Soluble composition of SIF
6.8 gm Monobasic potassium phosphate, 77ml NaOH, 10gm Pancreatin, q.s. 1000 mL for SIF.
The main composition difference of these media with regular buffer solutions is the addition of enzymes (pepsin and pancreatin) that can modify the behavior of drug products, in particular those in gelatin capsules. Pancreatic is poorly soluble in SIF. However, these media cannot be considered as biorelevant as they do not contain any biliary components (phospholipids, bile salts, etc.) or food components. s factors affecting the solubility of drug in various aqueous media (e.g. pH, salts and counter-ions, co-solvents, surfactants) and the typical experimental methods used to assess drug solubility.
Ashish
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