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    Thread: Exemestane (Aromasin) Solubility and Thermal Degredation Info

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      Exemestane (Aromasin) Solubility and Thermal Degredation Info

      PREFACE:
      I was able to dissolve Exemestane in PEG400 @25mg/ml, only after bringing to a temp of 170 degrees.
      Prepared hot water in pan. Brought slowly to 170 degrees measured with thermometer.
      While bringing up to temp, stopped at 130F, let sit. Then 150F, then 160F.
      Most dissolved at 160F after 10 minutes. Still some settling.
      Brought to 170F, then turned off heat, checked in 5 minutes(temp will slowly fall due to removal of heat of course)...
      All dissolved except for a couple of small slivers/flakes/granules. Will most likely dissolve within a day or two.
      Some compounds begin to dissolve over time in PEG.

      FURTHER RESEARCH:
      I began research and came across this.
      Oral Bioavailability Enhancement of Exemestane from Self-Microemulsifying Drug Delivery System (SMEDDS)
      "Exemestane possess the highest solubility in Capryol 90 (88.7 mg/mL)followed by castor oil (30.4 mg/mL);"
      Here is a table of solubility:
      Exemestane Solubility.jpg

      Thermal Degredation:
      When the drug exposed to dry heat in oven at 120°C for 24 h, it was observed that there was rise in two degradation products at 3.23 and 4.59 min of retention time and also a significant change in peak area of the drug was observed. Almost 4.39% degradation was observed. The assay of the active substance in thermal degraded sample was found to be 95.61%

      Thermal Degredation PDF
      Last edited by Plate Smacker; 07-09-2018 at 12:41 PM.
      "It's a lot of hard work, it's hard work that most people don't realize. I think the consistency of the hard work, is the hardest part." Dallas McCarver

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      You should use PEG 300 for examestane since it's molar mass is close to 300.

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      Quote Originally Posted by THX View Post
      You should use PEG 300 for examestane since it's molar mass is close to 300.
      What happens when you use a higher PEG?
      Have you researched this?

      Let's say a compound has a molecular mass of 300 but you only have 400,...

      Does it offer more solvency? Does it effect solubility in a negative way?
      I have more 300 on the way.

      I updated post and title with Thermal Degredation info.
      I am willing to bet if I said that I put the bottle of Exemastane in the oven @250F for 20 minutes... some would say "you killed it bro"...

      Research is key. Alot of misinformation is passed around, bro science, without backing up. Some merely parrot information.

      There is however no real reason to blast Exemastane in the oven. If you have slivers, flakes....
      Exemastane raws should be ground to a fine powder, as they are usually supplied very course, grains a little smaller than commercially available sugar or salt.

      If you do have flakes, 25 minutes at 250F, remove, shake vigorously.... and they will dissolve.(may be a very small amount that doesn't during my tests)
      Amber Boston bottles can withstand the temp, without the lid. The rubber in the lid, can withstand the temp after removed from oven... to shake.

      Info on the melting point of Exemastane shows various temps from different sources. 155C to 188C or so.
      (311F to 377F approximately).

      Info on PEG(Polyethylene glycol)
      "Its the molecular mass of the polymer chain. The smaller the number, it will be presented in liquid form. Molecular mass arround 1000 is terrible to work with, because it has a semi-solid aspect. PEGs above 3000 are solid and can be found in small pearls or granulated."
      "200 or 400 refer to average of molecular weight of PEG. PEG 200 has a lot of diol character and is more soluble in water, while PEG 4000 has more polyether character and the solubility is due more to hydrogen bonding. Different molecular weights have different solubility, surface tension, viscosity, freezing point, and melting points."
      Last edited by Plate Smacker; 07-09-2018 at 02:00 PM.
      "It's a lot of hard work, it's hard work that most people don't realize. I think the consistency of the hard work, is the hardest part." Dallas McCarver

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      You can use water with ba or alcohol if you want. Only difference will be that it won't dissolve so the dosage of each dose won't be as accurate.

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      Update:
      30ml Aromasin 25mg/ml
      760mg (10mg extra) Exemastane Aromasin powder from PPL.
      Placed on plastic lid. Crushed with chapstick top (must be done for best results). Poured and scraped into amber bottle. I have a tiny smooth funnel with wide mouth.
      Add: Using Class A graduated cylinder.
      20ml Everclear
      9.4ml PEG 400
      Shake
      Fill 1 cup with 6oz hot water from Keurig machine(165F).
      Put bottle in water. Slightly un-twist cap for venting. Not really necessary, but whatever.
      Let sit 5 minutes. Tighten cap (DON'T FORGET). Remove and shake 1 minute.
      Place back in hot water bath for another 5 minutes.
      Done. Remove and shake vigorously.
      Should be clear.
      If not clear, it will be in an hour or two as PEG400 dissolves it.
      20190213_105501-800x600.jpg
      20190213_122410-800x600.jpg
      "It's a lot of hard work, it's hard work that most people don't realize. I think the consistency of the hard work, is the hardest part." Dallas McCarver

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      Why are you still using peg 400?

      You can make 20mg/ml with 90-95% ethanol. I'm going to try to make 25mg/ml next time.

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      Quote Originally Posted by THX View Post
      Why are you still using peg 400?

      You can make 20mg/ml with 90-95% ethanol. I'm going to try to make 25mg/ml next time.
      Never ordered PEG 300 LOL.
      Does in completely dissolve in everclear?
      Won't really matter too much if ground to micronized powder. Will matter if not ground and larger unground chunks of various size are floating around after shaking.
      "It's a lot of hard work, it's hard work that most people don't realize. I think the consistency of the hard work, is the hardest part." Dallas McCarver

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      Quote Originally Posted by Plate Smacker View Post
      Never ordered PEG 300 LOL.
      Does in completely dissolve in everclear?
      Won't really matter too much if ground to micronized powder. Will matter if not ground and larger unground chunks of various size are floating around after shaking.
      I can try it and get back to you. Found this couple of months ago
      https://www.caymanchem.com/pdfs/15008.pdf

      "Exemestane is soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide (DMF), which should be purged with an inert gas. The solubility of exemestane in ethanol is approximately 20 mg/ml and approximately 30 mg/ml in DMSO and DMF."

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