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Zalicus Inc. Message Board

  • tabecounted1 tabecounted1 Apr 15, 2013 12:08 PM Flag

    BIOAVAILABILITY ENHANCEMENT

    Who---as in experts of an oral delivery system-did Zalicus use to increase the bioavailability?
    And---what did the Zalicus science discover to increase 160's bioavailability?

    There are answers out there apparently..I'm not a chemist or scientist..
    BUT----THE ANSWERS ARE OUT THERE-AND PERHAPS JUSTIN WASN'T EXAGGERATING-AND THEY DID INCREASE THE ABSORPTION STRONGLY......

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    • TC1, see excerpt below from patent No. 8,409,560

      "A pharmaceutical composition in unit dosage form for oral administration comprising a solid dispersion of from about 20 mg to about 250 mg of substantially amorphous1-(4-benzhydrylpiperazine-1-yl)-3,3-diphenylpropan-1-one (i.e. Z-160) in a matrix polymer, wherein said matrix polymer comprises a member selected from the group consisting of a cellulose derivative, a polyacrylate, a polyvinyl pyrrolidone, a polyvinyl acetate, or acopolymer of a polyvinyl pyrrolidone and a polyvinyl acetate and wherein the percentage loading of said 1-(4-benzhydrylpiperazine-1-yl)-3,3-diphenylpropan-1-one (i.e. Z-160) in said solid dispersion is from about 10% to about 80% (w/w)."

      In essence, they mix Z-160 with a one of a host of other compounds know as " solid dispersion compounds" which help dissolution and therefore bioavailability. I assume that Z-160 in and of itself is rather insoluble in water. Solid dispersion was introduced in the 1970s so I do not think it is rocket science, but a well established approach to enhancing bioavailability for otherwise insoluble compounds. It is essentially a multicomponent system having a drug dispersed in and around a hydrophilic carrier. The whole thing is based on enhancing the surface area of the drug by mixing it with these solid dispersion compounds ( there are many different types) which change the physical status of the incorporated drug. It is akin to using soap to dissolve grease. The soap actually encapsulates the grease in "bubbles" called micelles which have hydrophobic regions on the inside which bind the grease, and hydrophilic regions on the outside which helps solubilize the grease in water.

      Zing

    • It all seemed to start with a positive comment on bioavailability. lol---I'm gonna shut up next time..

    • Slow death,looking sad,going out to watch grass grow.

 
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