The key points of herbal biopharmaceutical are:
1.. Choice of the active ingredients most noble, the most investigated and documented, standardized and titrated, obtained using procedures with acceptable solvents, microbiologically and chemically comply with ministerial regulations, formulated so that the active fractions are stable over time.
2.Study of the limits of the active ingredients that cause their poor oral bioavailability and overcome these problems through the use of phytosomes, nanoemulsions, P-glycoprotein inhibitors and enzyme inhibitors.
The Phytosome is a complex formed by 1/3 of vegetable derived and 2/3 of the phospholipid matrix, which increases the absorption, the plasma concentration and the effectiveness ofherbal highly hydrophilic agent.
The nanoemulsion O/A is an oil/water microemulsion that increases the bioavailability of highly lipophilic active substances which, due to the high degree of lipophilicity, are not able to approach the enterocytal membrane. The nanoemulsion improves the chemical affinity of actives with the membrane.
The P-glycoprotein inhibitors are substances capable of increasing the absorption and bioavailability of active ingredients that would normally be extruded from enterocytes due to the phenomenon of the Multi Drug Resistance (MDR).
The inhibitors of phase II enzymes are substances which reduce the phenomena of hepatic metabolism of active substances which are rapidly degraded by the liver and rendered inactive before they can reach the systemic circulation.
3.Choice of pharmaceutical forms that can modulate the releases based on the variables time and pH.
Controlled pH-dependent release formulations
They are formulations with modified release, coated with gastro- and small intestine- resistant substances that make the drug insoluble at acidic pH (stomach) or higher (small intestine).
Tablets or capsules enteric coated
– Protect the assets from the dissolution at acidic pH
– Limit the gastro-oesophageal reflux
Tablets or capsules with colon-specific coating
– Release the active substances in the colon
– Enhance the action of the active substances
– Solve the problem of reflux caused by the essential oils
Controlled time-dependent release formulations
They are modified release formulations that contain excipients that control the release of the active ingredient after oral administration. The control can affect the rate of release or the start time of issue.
The time-release formulations allow to:
– Plan the disposal of assets and reduce the dispersion
– Optimize the dosing
– Improve the efficiency of the drug
Examples of modified release are:
Fast release
Slow release
Delayed or planned release