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The dripping pill (micropellet) preparation of dammarane sapogenins PPD & PPT

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Dammarane sapogenins (protopanaxadiol / PPD and protopanaxatriol / PPT) are well recognized for their therapeutical efficacy in cancers and other chronic health conditions. However, PPD and PPT are highly hydrophobic (in other words, they are lipophilic), meaning they are not water-soluble; therefore, PPD and PPT in traditional formulations such as tablets, powder and capsules are not well absorbed by the body as they will precipitate in the GI tract, and clinical efficacy of PPD and PPT is largely compromised.

In addition, the drug particle size is another determining factor of drug dissolution and absorption. In traditional preparations, herbal drugs exist in coarse particles and are difficult for GI absorption.

The creative dripping pill preparation takes advantage of solid dispersion and cosolvency technologies, and successfully solves these bottle-necks. In the dripping pill preparation, water-miscible matrices (e.g., PEG (PEG4000,PEG6000), PVP, Poloxamer, etc) are used in which PPD or PPT has a good solubility. After completely dissolved in matrices, PPD or PPT is enbedded in the matrices in a molecular form during condensation process (solid dispersion). Along with the dissolution of water-soluble matrices under the tongue or in GI tract, PPD or PPT will release rapidly and dissolve in an aqueous environment. The dissolved PPD or PPT can come in contact with oral mucosal or GI epithelia and is absorbed quickly.

Compared to other traditional preparations, dammarane sapogenin dripping pill takes into effect 2 and 4.5-fold faster than softgel and powder tablet, respectively, with a peak concentration 1.8 and 18.2-fold higher as well.

The dripping pills of dammarane sapogenins feature rapid release, better absorption and higher clinical efficacy. Besides dammarane sapogenins, some precious herb drugs like Fufang Danseng and Gegen also take advantage of dripping pill preparation to increase their therapeutical effects. For example, the dripping pill of Dansen has a large surface area, faster drug dissolution, quick absorption by oral mucosa and rapid response in 3 minutes, and can be used as first-aid drug for angina. The Gegen dripping pill has a 2 times clinical efficacy as its tablet form.

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