Loxoral Base- Ketoconazole vs MCC STudy Cards.txt

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  1. What is Loxoral?
  2. What is an Excipient?
    An excipient is an inactive substance formulated alongside the active ingredient (API) of a medication, to bulk up a formula. Bulking up a formula with an Excipient allows convenient and accurate dispensation of a drug substance when producing a dosage form.

    Explanation: Basically by adding a filler or Excipient you are allowing for a more accurate and efficacious compound. Lactose is an Excipient that is used most in drug production. Fact, 80% of the worlds population is lactose intolerant to some extent. Lactose has no positive effect or action in any way on the body. It simply takes up space in a formula. This is important to know. Loxoral has desirable properties that you can point out to a physician.
  3. What two APIs were used in the Loxoral study?
    Ketoconazole and Piroxicam
  4. What is ketoconazole?
    Anti-fungal (imidazole)
  5. What was the purpose of the Loxoral study?
    To evaluate the potential of LoxOral to enhance the dissolution properties of ketoconazole and evaluate its use in comparison microcrystalline cellulose (MCC)
  6. Poor aqueous solubility of an API is one of the most pressing problems in pharmaceutical R&D with as many as 90% of new API candidates in this category.

    True or False
    True (Lobman et al., 2013)

    Note: This is great information to disclose to a physician. What a powerful way to paint the picture of why LoxOral can be so advantageous to their patients.
  7. Dissolution rate in the gastrointestinal tract is the rate limiting factor for many drugs in oral form which may limit their bio-availability after oral administration.

    True or False
    True (Zimmerman et al ., 2009

    Explanation: Most drugs in oral form are have poor absorption. This is because the drugs do not dissolve well in the gut.
  8. Define soluble.
    Able to dissolve, especially in water
  9. LoxOral enhances the dissolution of poorly water-soluble drugs.

    True or False

    LoxOral aids in dispersibility and solubility. (PCCA LoxOral Study)
  10. Microcrystalline cellulose (MCC) is widely used as a filler for oral tablets and capsules.

    True or False
  11. Microcrystalline cellulose (MCC) has a prolonged release rate due to lack of disintegration. The outcome of this is the drug that has MCC as an excipient will have poor absorption.

    True or False
    True (Chamsai & Sriamornsac 2013)
  12. What dosage form is PCCA Loxoral designed for?
  13. When LoxOral is used in a compounded capsule, what effect does it have on the API it is formulated with?
    It improves the dissolution and solubility of all APIs and those that are poorly soluble in water.

    Explanation: Drugs used with LoxOral have better bio-availability.
  14. Define "bio availability"
    It is the fraction of unchanged drug that reaches the blood stream and is systemically circulated throughout the body.

    Explanation: When a drug is given intravenously (infusing a liquid directly into a vein) its bio availability is 100%. But when given orally, only a fraction of the drug in a capsule or tablet actually make it into the body to medicate optimally.
  15. LoxOral is free of what excipients that most other excipients used in pharmaceuticals contain?
    LoxOral is free of:

    • Gluten**********
    • Casein****
    • Sodium Laurel Sulfate******
    • Lactose************
    • Soy*****
    • Dye*****
    • Magnesium Stearate

    * indicates how often someone is concerned about putting this substance in their body.

    Note: In today's world of medicine doctors are looking for and considerate of patients with special dietary needs. Our environment is catching up with us and more and more people are having problems and it is due to allergies and sensitivities. Doctors recognize this. This is a huge selling point for a personalized compound medication to be considered.

    • 4years ago I never heard of gluten
    • 3 years ago I heard about it
    • 2 years ago 5 out every ten people I know have a sensitivity or are off gluten
    • This year I got of gluten and for the first time in 14 years do not suffer from debilitating heart burn, severe heart palpitations or pancreatic spasm. People with celiacs disease will suffer a flare up and regress 95% from a corner of a crouton. It's a very serious matter and your physicians want to know you can supply medication without these excipients commonly used in drugs.
  16. LoxOral contains isomalt which is thought to have prebiotic effects. Does this mean Loxasperse is a prebiotic or has prebiotic properties?
    NO. Isomalt has shown potential prebiotic effects.

    Explanation: LoxOral may have prebiotic effects in the gut. But this is theory and not proven.
  17. Ketoconazole is known to be orally active in treatment of....?
    Systemic blastomycosis, candidiasis, coccidioidomycosis, histoplasmosis, para coccidioidomycosis and tinea of skin and nails.

    Explanation: Fungus, Yeast and Ringworm
  18. The dissolution profile of Ketoconazole and LoxOral was compared against what?
    Ketoconazole combined with microcrystalline cellulose
  19. What is microcrystalline cellulose (MCC) and it's use in the pharmaceutical world?
    MCC it is widely used as a filler, disintegrant and binder of oral tablets, pellets and capsules.
  20. Why is MCC, not the best choice for use in oral dosage forms such as tablets, capsules?
    Most drugs show a tendency towards prolonged release due to lack of disintegration. This inhibits bioavailability of the drug.
  21. The dissolution specification for Ketoconazole has been stated in the USP as not less than 80% of the labeled amount of the drug within 30 min in 0.1N HCI (pH 1.2). Only the LoxOral formulation was compliant with the USP specification compared to the MCC test.

    What was the percent of Ketoconazole dissolved in the LoxOral arm of the study?
    80.78 % dissolution
  22. What was the percent of Ketoconazole dissolved in the MCC arm?
    Under 70%
  23. What is the conclusion of the Ketoconazole and LoxOral study?
    It shows that Ketoconazole combined with LoxOral will potentially provide rapid bioavailability and onset of action after the drug is taken orally.

    LoxOral enhances bioavailability enhancement of BSc Class 2 drugs such as Ketoconazole.
  24. "Ketoconazole is characterized by having a low solubility and a high permeability. This has shown to cause problems with drug release and there have been numerous efforts to resolve this issue."

    Why is knowing this important to you?
    • Doctor... Can I ask you a question?
    • Sure
    • Your a podiatrist or dermatologist or family practitioner so you probably prescribe a fair amount of ketoconazole, would you agree?
    • Yah, I write for it a fair amount

    Well doctor I just read that ketoconazole has a very poor solubility. In fact so much so that there have been numerous efforts to solve the issue. YTD they have not. Do you have any patients that require multiple rounds of oral anti fungal therapy?


    It is those patients that bring me to your office today. Doctor we have a new excipient that has been studied with the API ketoconazole. It has shown to increase solubility and dispersibility in the gut, therefore increasing bio-availability.

    Now Nizoral has MCC in it which only hinders the bioavailability even more, by prolonging the release of the drug.

    Our new compound base LoxOral not only aids in the dispersion and solubility of the Ketoconazole in the gut, but it is the only Ketoconazole oral preparation that complies with USP dissolution specification. It states in the USP "the dissolution specification for Ketoconazole is not to be less than 80% of the labeled amount of the drug"

    Our compounded formulation is 80.78%

    • So doctor. Would you be willing to try this on a few patients to see if we can optimize their outcome?
    • -------------------------------

    Role play with your boss, your techs whatever. This is what drug reps do and like it or not those drug reps are entering the world of compounding. They are professionally trained sales people. So everyone is going to have to up their game. If you can answer every question in this test correctly you will be able to have the conversation above off the cuff. Also it will bleed over into other areas.
  25. Who sponsored this study?
    PCCA is the full sponsor of this study.

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Loxoral Base- Ketoconazole vs MCC STudy Cards.txt
2013-11-22 22:12:16
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