ANDROVIR HB by

Eleonor
HIGHLY BIOACCESSIBLE
Andrographolide (Andrographis
paniculate) for an optimal &
reinforced assimilation and efficacy
• For fast relief of fever, headache and other ARTIs
symptoms
• To prevent and/or to fight against common
respiratory infections (sore throat, cold, flu,
pharyngitis…)
• To boost your natural resistance and your immune
system
• Food grade product
• A PATENT PENDING product
 share of more than 35% in 2017. The segment is estimated to be valued at
more than US$ 5,000 Mn by 2017 end and is expected to reach a value of
more than US$ 8,900 Mn by the end of 2025, creating an absolute $
opportunity of close to US$ 370 Mn in 2017 over 2016, and an incremental
GLOBAL IMMUNE $ opportunity of nearly US$ 3,600 Mn between 2017 and 2025.
HEALTH SUPPLEMENTS
MARKET

• Immunity = deseases
prevention (lifestyle)
• > 25 Billions $ in 2025
• Demand increases due to
aging of population,
pollution, other external
aggressions (virus)...
• In 2017, products sales
revenues to reinforce
immunity reached 14 billions Gain More Insights about this Report
$ (more than 5 billions for (https://www.persistencemarketresearch.com/samples/5852)
vitamins) Growing demand for immune health supplements across the
world is likely to boost the global immune health supplements
CONFIDENTIEL - ELEONOR srpl
market
 ACTIVE COMPONENTS OF
ANDROGRAPHIS PANICULATA.

• Diterpenoids (andrographolide-like
molecules)
• Main acJve = ANDROGRAPHOLIDE
• AnJpyreJc effect
• AnJ-infecJve effects (virus,
bacteria,…)
• Immunomodulatory effects
• AnJ inflammatory acJviJes

CONFIDENTIEL - ELEONOR srpl

 360 A. Panossian et al.
500
Intensive elimination of Andrographolide began 3-4

ANDROGRAPHOLIDE
E hours after drug administration and at the eighth hour,
400 Dose of AND
1 mglkg could not be detected in the blood. In some cases it
g 300 happened 4 hours after dr ug administration.
5io 200
<:
BIOACCESSIBILITY /
It might be suggested that high individual var iability
in the pharmacokinetics of andrographolide, especially

BIOAVAILIBILITY
8 100 in the phase of distribution, is due to different extents
of binding with blood proteins.
2 3 4 5 6 7 8 In addition, intensive metabolism of andro-
time. hours grapholide, was shown in rats . Because in pharmacoki-
Fig. 6. Plasma concentration of Andrographolide (AND) vs. netics human subjects are commonly divided into
time after oral administration of Kan lang (four tablets, 20 "slowly" and "fast" drug-metabolizing subjects, it may
mg AND) to humans
of an drographolide from Andrographis (mearie SEM,
paniculata 361 n=16) be assumed that individual var iables in distribution
and elimination •rates is a consequence
Weak of var ious
Bioaccessibility andme-Bioavailibility of
1500
Andrographolide (high lipophilicity,
tabolizing rates of andrographolide. On the cont rary, low aqueous
Andro grapholide is abso rbed quickly into the blood when drug metabolism solubility, rapid metabolisa>on)
and binding with blood pro -
after ora l administration of Kan jang, abso rption half- teins are not intensive, the absorption of drug does not
E
1000
life T JI2abs is abo ut 25 min. The maxim al concentra- vary substantially • inSolubility
individuals.maxTh e :absorption
betweenrate 15 & 25 mg/L whatever
"l3l
r:::: tion of AND in the+ • Css
- was
blood found at 1.36 hours af- andrographolide dose
constant and T max in 13 subjects were approximately
500 ter administering Kan Jang.. In four volunteers, distrib- the same. • Tmax : 1,36 hours (rapid assimila>on)
ution of andrographolide Cmin in tissues occured compara- Thus, the pharmacokinetics of Andrographolide are
tively quickly and the data fit a one-compartment mod- characterized by• high Cmax : 400 ng/ml
absorption from the (1mg/kg
gastroin-AND. oral)
el nicely using the TOPFIT program. In the other 12 testinal tract into• the It thenredistribu>on
blood.body
Whole binds intensively(throught proteins
6 12 18 24 30 36 42 48 54 60 66 with blood proteins bounds)
subjects, the drug distributed slowly in body organs within the
and is redistributed 1-2 blood
between hours
hourstissues, mainly in 1.5-3 hours after adm inistra-
and and tissues within 1-2 hours. Elimination half time is
tion. of
Fig. 7. Steady-state simulation T heANDpharmacokinetics
plasma concentration of andrograp holide for in the range of 2-7• Metabolites
hours. The main(mainly
route of SULFONATES)
elimina - are ac;ve
after oral administrationthose
of Kancases
l ang,is4 very well-described
tab lets, 20 mg/70 kg, by the two -compart- tion is intensive metabolism.
• Dose response effect
using the single-dose data.
ment model (Tables 11 and 12).

Andrographolide binding to bovine serum albumin CONFIDENTIEL - ELEONOR srpl

(BSA) and human blood plasma
Table proteins (HBPP)
11. Individual pharmacokinetic parameters of Andrographalide in every human subject, n=15*.
 cording to literature suggestions (Szejtli et al. 1994), a de- AND into the HP-b-CD cavity. Inclusion complex of the

ORIGINAL ARTICLES

Table 3: Pharmacokinetic parameters (mean " S.D.) obtained China). Me

after oral administration (25 mg kg&1) to rats (n ¼ 6) Shandong Y

Enhanced release & bioavailability AND PM IC

this experim
was prepare

of AD from ANDROVIR HB
AUC0&t mg $ L&1min&1 426.00 545.74 681.47 3.2. Anima
" 67.81 " 100.62 " 113.92 Healthy Sp
AUC0&1 mg $ L&1 min&1 482.01 623.79 751.29 were obtain
" 88.56 " 127.94 " 132.40 chuan (PR
Cmax mg $ L&1 2.07 2.66 4.10 temperature
with free ac
" 0.27 " 0.27 " 0.92
for at least
Tmax min 61.67 50.00 41.67 experiments
" 14.72 " 8.94 " 11.69 Care and U

3.3. Prepar
Fig. 7: Mean plasma concentration-time curves of (~) IC, (&) PM and AND and H

• Androvir HB delivers more than 2

Fig. 6: Dissolution profiles of (&) free AND, (~) PM and (&) IC (^) AND after oral administration to rats (n ¼ 6) Inclusion c
pared by c
518 Pharmazie 64 (2009) 8 4.28 g of H
amount of A

fold soluble AD (thus bioaccessible)

50% ethano
suspension
evaporated

compared with basic extract 40% AD

(Büchi Rota
Physical mi
weight rati
viously siev
and pestle f

• Results : Cmax & AUC are increased 3.4. Chara

(see figures on a rodents model for 3.4.1. Diffe

Approximat

the same composition than

DSC analy
used as a r
with the sca

ANDROVIR) 3.4.2. Powd

Powder X-
model PW3

• > 2*C max & > 1,5*AUC (more

matized Cu
(where theta

efficacious) Fig. 8: Schematic representation of the starting orientations of AND/HP-b-

3.5. Determ
Concentrati
tography (H
CD (1 : 1 stoichiometry) used in the molecular modeling calcula- tion module

• 33% T max reduction (faster action) tions. (A) naphthaline (two rings) in wide rim, (B) furan in wide
rim, (C) naphthaline (partial) in wide rim, (D) naphthaline (two
rings) in narrow rim, (E) furan in narrow rim and (F) naphthaline
(partial) in narrow rim
collected an
ment from
carried out
physical ch
Shimadzu
(Chiyoda-K
methanol (
drug was remarkably less crystalline and, therefore, more 0.22 mm me
soluble than the AND itself in aqueous media. In addition, tion volume
the dissolution degree and rate were greatly enhanced by 35 # C. The
inclusion process. In vivo studies showed that Cmax and
AUC were significantly different (p < 0.05) between in- 3.6. Phase
CONFIDENTIEL - ELEONOR srpl clusion complex and AND powder. Meanwhile, a lower Solubility m
Tmax was observed for the inclusion complex. the method
added to 10
The use of this multicomponent system provided a new
 ANDROVIR HB
For an op4mal & a reinforced
assimila4on & efficacy of
andrographolide
• ANDROVIR HB : 500 mg delivers 60 mg of
Andrographolide (min 35-40 mg of 100% soluble
andrographolide – unachievable by classic extracts
whatever the administrated dosages) – Most of
posiFve clinical trials on humans have been made
with 60 mg AD daily
• Posology : 500 mg daily
• EFSA Pending claims : Respiratory comfort/helps to
soJen respiratory troubles like coughs, sore throats
in a natural way, Increases the physiological
resistance of the organism in case of severe
ambiance condiFons.