How
Our System Works (Details)
Most
pharmaceutical companies involved in transdermal product line are focused
on contraception, hormone replacement therapy and smoking cessation. However
our company, through extensive literature study, dedicated effort and
long experience in herbal remedies realized the importance of the skin
as important organ for herbal remedy application in many of the common
diseases that constitute sever health problems to people and often lead
to chronic overwhelming illness.
Topically applied remedies provide controlled release of herbs directly
into the bloodstream through intact skin. It provide a number of advantages
over conventional methods of herbal administration, including:
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Enhanced efficacy. |
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Increased safety. |
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Greater convenience |
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By delivering a steady flow
of herbs into the bloodstream over an extended period
of time, transdermal systems can avoid the "peak and
valley" effect of a oral therapy and can enable more
controlled, effective treatment. |
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By avoiding first pass metabolism
through the gastrointestinal tract and the liver, the therapeutically
equivalent dosage for the transdermal delivery of certain
compounds can be significantly less than the corresponding
oral dosage, potentially reducing dosage related side-effects. |
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Easy to terminate dosing if
adverse reaction occurs. |
Delivery System:
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The concentration and solubility
of the active ingredients: high concentration or solubility
penetrate better (high concentration gradient) |
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Vehicle viscosity: viscosity
reduces diffusion coefficient. |
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Vehicle composition: non-aqueous
solvents increase penetration. |
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Penetration enhancers: disrupt
skin surface causing faster penetration. |
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Area for absorption: increased
area causes increased absorption. |
Physiological conditions in skin:
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Dead cells and lipid accumulation
in the stratum corneum decreases initial transport. |
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Sebum-pH, amount and composition
alter passage. |
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Hydration of the skin ( differ
according to the person's age and skin location): increased
hydration usually increases penetration rate. |
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Thickness of the skin: Thin
skin causes increased penetration rate e.g. the skin behind
the ear is very thin while that of palm of hand is very thick. |
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Injury- open cuts and grazes
increase penetration rate. |
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Temperature: Theoretically,
a positive relation is expected between skin temperature and
the percutaneous penetration of topically applied substances.
Studies showed that temperature effect with the highest penetration
is at 38.2 degrees C (4). |
Skin Permeation Enhancers
One literature review found more than 275 chemical compounds cited as
skin penetration enhancers (5).
Most of those compounds were generally recognized as safe (GRAS) ingredients
that would often be considered inert by a formulator. Complete texts concerning
pharmaceutical skin penetration enhancement are available and they provide
excellent descriptions and critical reviews of this subject (6,7,8).
Although there are many strategies to enhance skin permeation, some of
them include the use of chemical skin penetration enhancers. We use natural
additives that:
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Alter the solubility of the
active ingredient in the formulation (including supersaturation),
to increase its delivery through the skin |
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Optimize the ionization state
of the active ingredients in the topical remedies (using buffered
gel with the proper pH). |
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Enhance the skin permeation
(adding natural skin permeation enhancers). |
Topical products often contain many components that are considered inert
excipients with respect to the pharmacology:
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Solvents and cosolvents are
used to alter drug solubility or ease of processing. |
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Emulsifiers and gelling agents
provide the consistency and properties expected of creams,
lotions, and gels. |
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Antioxidants and preservatives
are provided to extend shelf life or ensure quality. |
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Skin permeation enhancers are
added to the topical remedies to increase skin permeability
by reversibly altering the physiochemical nature of the stratum
corneum to reduce its diffusional resistance (8). |
We use the natural skin enhancers which include:
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Iontophoresis: uses electrical
potential to carry drug through the skin, by using active
ingredients in buffered gel. |
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Linoleic acid and alpha-linolenic:
It has been found that polyunsaturated fatty acids PUFA--Linoleic
(LA), alpha-linolenic (ALA) and arachidonic acids-enhance
skin permeation stronger than monounsaturated fatty acids.
The enhancement effects of fatty acids on penetration through
the stratum corneum are structure-dependent, associated with
the existence of a balance between the permeability of pure
fatty acids across stratum corneum and the interaction of
the acids to skin lipids (9). |
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Oleic acid: Oleic acid has
been studied as a skin penetration enhancer for topically
applied medications, primarily via its action mainly on the
stratum corneum lipid structure. It has been found to increase
the epidermal permeability through a mechanism involving the
stratum corneum lipid membrane. It is incorporated into skin
lipid, disrupt molecular packing and alter the level of hydration
and allow drug penetrates faster (10). |
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Cod-liver-oil The enhancing
effect of the marine products could generally be associated
with their content of free unsaturated fatty acids (11). |
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Menthol derivatives as potential
skin penetration enhancers Studies showed that the permeation
enhancing effect of l-menthol is significantly high with short
lag time (12). The promoting activity of the ethyl ether derivative
of Menthol is the greatest of all menthol derivatives. Studies
showed that it is the most promising compound which has the
greatest action and relatively low skin irritancy (13,14).
A study has been made to elucidate the mechanism of skin permeation
enhancement and it was concluded that the increase in skin
flux, to eight times the base line, could be attributed to
the effect of menthol on the skin barrier properties (15).
The mechanism of permeation enhancement of menthol has been
studied by some other investigators and they concluded that
it could involve its distribution preferentially into the
intercellular spaces of stratum corneum and the possible reversible
disruption of the intercellular lipid domain. They suggested
the use of menthol as effective penetration enhancer (16). |
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Squalene: Squalene was found
to be a very effective skin permeation enhancer. 12% of the
human sebum is composed of Squalene to which is attributed
the natural moisturizing effect of the sebum. Studies also
showed the skin soothing effect of Squalene (17). |
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Glycerol derivatives: Studies
concluded that glycerol monoethers derived from linear saturated
fatty alcohols are very effective permeation enhancers (18). |
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Herbal ingredients: have the
ability to penetrate the skin fast. In vivo skin penetration
studies of the Chamomile flavones apigenin, luteolin and apigenin
7-O-beta-glucoside were carried out with nine healthy, female
volunteers. During seven hours the decline of flavonoid concentration
in a saturated aqueous alcoholic solution filled in application
chambers were repeatedly measured by spectrophotometry at
fixed time periods. It was concluded, that the flavonoids
are not only adsorbed at the skin surface, but penetrate into
deeper skin layers. This is important for their topical use
as antiphlogistic agents (19).
Another study has been done to investigate the permeability
of natural herbal compounds of different range of lipophilicity
through hairless mouse skin and the effect of certain herbal
extract called Senkyu(Ligustici Chuanxiong Rhizome )ether
extract (SEE) as permeability enhancer. It has been found
that (Senkyu) ether extract (SEE) enhanced the permeability
of the herbal ingredient that have moderate permeability rate.
The effect of SEE in vivo was similar to that obtained in
the in vitro experiment. It was concluded that the natural
compounds having high lipophilicity sufficiently permeated
into the hairless mouse skin owing to their accumulative property,
and the Senkyu ether extract enhanced the permeability of
the moderately lipophilic compounds into the skin (20). |
By using combination of buffered gel and skin permeation enhancer in addition
to the easily permeable herbal ingredients, extracted by natural solvents,
further increases the flux through the epidermis. It has been concluded
after several studies that Iontophoresis in combination with enhancers
(e.g. linolenic acid ) transformed the highly compact cells of the Stratum
corneum into a looser network of filaments, disrupted the keratin pattern,
and resulted in swelling of Stratum corneum cell layers of human epidermis,
thus increases the flux of medication through human epidermis (21).
Our scientists are and will always be appreciating the trust of their
customers all over the world. They will always make use of their unique
creative feature in developing the best of the topical herbal remedies
to protect their customers from the side effect of the long term use of
pharmacological drugs.
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