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Shilajit: An Ancient Panacea
Article in International Journal of Current Pharmaceutical Review and Research · May 2010
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            Mohd. Aamir Mirza                                                                                     Dr. Gulam Mustafa
            Jamia Hamdard University                                                                              Shaqra University
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     International Journal of Current Pharmaceutical Review and Research
                Volume 1, Issue 1, May 2010 – July 2010, Page 2-11
                                 Review Article
                      Shilajit: An Ancient Panacea
            Mohd. Aamir Mirza1*, Mohd. Naushad Alam1, Mohd. Faiyazuddin1,
                 Danish Mahmood2, Ranjan Bairwa3 and Gulam Mustafa11*.
        1. Research scholar, Dept of Pharmaceutics, Jamia Hamdard, New Delhi.
        2. Research scholar, Dept of Pharmacology, Jamia Hamdard, New Delhi.
             3. Lecturer, School of Pharmaceutical Sciences, J.N.U., Jaipur
ABSTRACT
Shilajit is a pale-brown to blackish–brown exudates obtained from layer of rocks in
many mountain ranges (especially the Himalayan ranges of the Indian subcontinent) of
the world. Its curative potentials were found documented in ancient books and were
used to treat many ailments since antiquity days. Major portion of Shilajit was found to
consist of humic substances. A number of preclinical trials have shown many of its
pharmacological properties. Use of its constituent in modern agriculture is a common
practice nowadays. Several researches have been carried out that explored its curative
potential and this miraculous gift of God is finally made available to pharmaceutical
industry.
Key words: Shilajit, Indigenous system, Fulvic acid, Humic acid
1. INTRODUCTION
Herbal dietary supplements are big business even in the countries like United States.
More than 40% of adult Americans use some form of alternative medicine, including
herbals, massage, chiropractic, and hypnosis, and spent $5.1 billion out of pocket for
herbal therapies in 1997. Herbal use increased by 380% and megavitamin use by
130% from 1990-1997. More than 60% of people worldwide do not disclose their use
of complementary medicine to physicians [1]. Some herbal products like Echinacea,
Authors for Correspondance:
E mail: aamir_pharma@yahoo.com , gulampharma@gmail.com
Phone: +91-9213378765, +91-9891074727
                   Gulam Mustafa et.al. / Shilajit: An ancient panacea
ginseng and St. John's wort, are now sold in supermarkets, pharmacies and discount
stores.
          Attributed with many remedial and curative properties, Shilajit is a potent
rejuvenator and anti aging compound. It is used as a panacea for many illnesses in
oriental medicine, across Himalayan regions bordering India, China, Tibet and parts
of central Asia where it occurs in the form of rock. Early ayurvedic writings from the
Caraka Samhita and Susruta Samhita describe shilajit as a cure for all disease as well
as a rasayana (rejuvenative) able to increasing longevity from 100 to 1000 years of
age. It is composed of humus and organic plant material that has been compressed by
layers of rock mixed with microbial metabolites. It contains more than 85 minerals in
Ionic form and humic substances (mainly fulvic and humic acid). The clinical studies
on shilajit, conducted have so far; have been conducted on animals only. In the light
of below mentioned facts Shilajit should be extensively studied and may be made
available as a general tonic.
                                 Table 1: Synonyms of Shilajit
Language                        Name                                           Reference
Sanskrit                        Silajit, Shilajit , Silaras                    12
Hindi ,Gujarati and Marathi     Silajita                                       12
Hindi                           Ral -yahudi                                    23
Bengali                          Silajatu                                      12
Tamil                           Uerangyum, Perangyum, Uerangyum                12
Arabic                          Hajar-ul-musa                                  12
Persian                          Momiai Faqurual Yahud                         23
Russian                          Mummio, Mumie                                 24
English                         Asphalt, Mineral Pitch , Jew’s pitch,          12, 24
                                Vegetable Asphalt
Latin                           Asphaltum                                      25
Botanical description           Bitumen mineral                                26
Origin of Shilajit
There are a number of hypotheses about the origin of shilajit [2]. Early scientific work
carried out on shilajit showed that it is mainly composed of humus – the characteristic
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                   Gulam Mustafa et.al. / Shilajit: An ancient panacea
constituents of soil – together with other organic constituents. Latex bearing plants,
namely Euphorbia royleana Boiss and Trifoleum repens which occur in the vicinity of
the shilajit bearing rocks are thought to be the most likely source of Shilajit [4, 5].
Other recent research claims that the mosses of species such as Barbula, Fissidenc,
Minium, Thuidium and species of Liverworts like Asterella, Dumortiera, Marchantia,
Pellia, Plagiochasma and Stephenrencella-Anthoceros were present in the vicinity of
shilajit-exuding rocks and these bryophytes are responsible for the formation of
shilajit [2]. The bryophytes reveal the occurrence of minerals and metals in their
tissues such as copper, silver, zinc, iron, lead etc, which are similar to the elements
present in shilajit.
Research work with Shilajit
Indigenous system of Nepal uses it for the cure of various neuropsychiatrical
disorders and physical debilities, generally termed as a general tonic. Some of the
most interesting studies confirm shilajit’s uses as an anxiolytic (anti-anxiety) agent
and its nootropic (enhancer of learning acquisition and memory retrieval) activity.
Shilajit is generally considered safe in moderate doses and is readily available in the
United States both as a stand-alone product and in the traditional Ayurvedic formula
Chandraprabha.         One proprietary drug contains shilajit, along with Terminalia
bacteria, Phyllanthus emblica, T.chebula, Eclipta alba and cow milk. In a book,
Chopra [5] elaborated various constituents of shilajit and shown the presence of
benzoic acid, hippuric acid, fatty acid, resin, wax gums, albuminoids, vegetable
matter and sand particles in it.
        Kong et al in his study [6] revealed that major portion of hydroacloholic
fraction of Shilajit is calcium benzoate, which imparts antiseptic effect against
microbial gastro-intestinal infection and it was confirmed that benzoic acid (BA) in it
confers anti bacterial activity probably by interfering with respiratory system of
bacteria. Moreover BA does not accumulate inside the body as it forms hippuric acid
after combining with glycine and excreted out.
        Volatile components of shilajit have exhibited significant behavioral and
neurochemical manifestation in laboratory animals that clearly indicate its future use
in aroma therapy. In another study on rodents, shilajit and its active constituents
significantly enhanced the learning acquisition and memory retrieval [7]. It might
prove to be a good nootropic agent while higher doses (25-50mg/kg) have shown
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antianxiety effect [8]. Apart from its many beneficial effects, it has also been reported
to have anti-inflammatory and anti ulcerogenic activities [9]. It has been invariably
effective in all the three phases of inflammation i.e. acute, sub-acute and chronic. The
U-shaped dose responses are reminiscent of drugs that improve cognitive functions.
It has been used in rheumatism in Indian system of medicine and has significantly
raised total carbohydrate to protein ratio in gastric juice and reported to be quite safe
up to a dose of 3g/kg in mice.
       Animal studies on mice have shown to alleviate stress and have also reduced
immobility in forced swimming induced immobility [10]. In Streptozotocin (STZ)
induced diabetes mellitus, it has lowered blood glucose level [11].            STZ cause
selective destruction of ß islet cell through generation of free radicals while shilajit
has antioxidant property and this explain its antidiabetic action by protecting ß cell
destruction. Literature is replete with studies on shilajit showing its use in the cure of
various diseases. Thus shilajit may be used in various health care products but its use
is limited by its higher chance of getting contaminated by mycotoxin which requires
its isolation and purification. This synergistic effect of shilajit with herbal remedies
was studied by Chopra et al in 1958 [12]. Their findings help reduce the anti diabetic
doses of herbal drugs.
Varieties of Shilajit
There are four different varieties of shilajit which have been described in charka
samhita, namely savrana, rajat, tamra and lauha shilajit. Savrana shilajit is gold
Shilajit and is red in colour. Tamra is a copper shilajit and is blue in colour. Rajat is a
silver shilajit and is white in colour while the lauha shilajit is an iron-containing
shilajit and is brownish-black in colour. Tamra and savrana shilajit are not found
commonly but the last variety, i.e. lauha shilajit is commonly found in Himalayan
ranges and is supposed to be most effective according to the therapeutic point of view
[13, 14, 15].
Patents on Shilajit
USPTO has issued few patents on Shilajit, which are good repertoire of knowledge on
the said topic. Purification of shilajit is an imperative necessity to ensure its optimum
therapeutic effect. Patent number 6,440,436 issued to Ghosal (2002) which deals with
composition of purified shilajit obtained from native sources and also various
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                    Gulam Mustafa et.al. / Shilajit: An ancient panacea
formulations. It contains abundant amount of bioactive components, about 0.4-1%
(w/w) oxygenated dibenzo-.alpha.-pyrones (DBPs), and 65-70%, (w/w) of Fulvic
acids of low-to-medium molecular weight (700-2000). E4 /E6 ratio is 8-10 at λ
465/665 nm. 2% aqueous solution has a pH 7-8. Fulvic acid acts as a carrier for DBPs
which is obtained by successive extraction of native Shilajit with water and organic
solvents. Purified shilajit composition also contains about 3-12 % of benzoic acid, m-
OH benzoic acid or C16-C22 alkanol esters thereof. 0.5-1% heterocyclic aromatic
compounds containing N and S are also found. Variable amount (0.1- 60% w/w) of
this invention is used in different formulations like pharmaceutical, nutritional and
personal care. Like 0.2-10% w/w is used in personal care formulations.
                          Table 2: Traditional uses of Shilajit
Category                              Uses                                References
                                      Disorders of poor digestive         15
                                      activities
Gastrointestinal                      Enlargement of the abdomen          15
                                      Hemorrhoids                         22
                                      Rectal distula                      15
                                      Worms                               15
                                      Dysuria                             15
Urinary tract system (kidney,         Madhu-Meha (vata type diabetes       15,22
ureter, bladder)                      mellitus -type I)
                                      Gravel or stones in the bladder     22
                                      Cough                               15
Respiratory                           Scrofula (tuberculous cervical      15
                                      lymphadenitis)
                                      Loss of consciousness               15
Neurology, psychiatry                 Epilepsy                            22
                                      Insanity                            22
                                      Benign tumor                        15
Immunology and cancer                 Malignant tumor                     15
                                      Gulma (internal tumors)             22
                                      Phthisis (wasting of the body)      22
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       Purification process involves treatment of aqueous solution of exudated,
powdered shilajit with different solvents. Hot organic solvents like methanol is used
to separate out phenolic bioactive compounds, dilute NaOH is added to precipitate out
polymeric quinines and bringing the pH of the solution to 3 precipitates out humic
acid resulting in final brown acidic Fulvic acid solution. Fractionation of fulvic acid
solution over activated carbon is done to get low to medium molecular wt Fulvic acid.
Fulvic acid solution obtained at last is mixed with suitable portion of bioactive
phenolic compounds. HPLC method is used to standardize purified shilajit
composition.
       Another patent (US 6558712 B1) issued to Ghoshal (2003) describes in detail
about the use of purified shilajit as a delivery system of pharmaceutical, nutritional
and cosmetic ingredients. A purified Shilajit composition containing at least 40% by
weight Fulvic acid is used as a carrier. Active ingredient added is 0.5-40% weight of
Fulvic acid. The characteristics which attribute Fulvic acid this unique property are its
sponge like structure punctured by voids of about 200-1000 A0 and an average
molecular weight of about 700-2500. Bioactivity of water insoluble active ingredient
is increased by using this technique. Since Shilajit is not the only source of FA
comparative study of FA with other sources was also studied and Shilajit-FA was
found to be a candidate of choice. The cutting edge of Shilajit –FA is its oxygenated
dibenzo-α-pyrones as core nucleus, significantly presence of oligomeric dibenzo-α-
pyrones and acylated DBP with a lipid chain and its endogenous origin i.e produced
by animal system. On one hand well organized core structure of FA scavenges
unwanted metal ions and free radicals in vivo while on the other hand it entraps within
its network different metal ions in reduced state and help production in various co-
enzyme systems. Complexes of FA with various drugs were developed and increased
in solubility and bioavailabilities were obtained e.g. Glibenclamide, Insulin,
Pentazocin, Methotrexate etc.
       A novel herbal composition that includes combination of Shilajit with extracts
of Withania somnifera and Mangifera indica is discussed in patent (US 7,250,181 B
2).It is used as an antiviral and /or immuno supporting agent in pharmaceutical,
veterinary and nutritional compositions. This cost effective aniviral or immuno
supporting agent is used during the maintenance phase of the treatment following an
initial viral load reduction (also against HIV) phase in which it is used as an adjuvant
to anti viral drug therapy. It can be developed in oral, tropical or parenteral dosage
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                 Gulam Mustafa et.al. / Shilajit: An ancient panacea
form. This formulation can be used in various pharmaceutical and nutritional
formulations like, multivitamin tablets, weight loss support tablets, anti-diabetic
tablets and capsules, snack bar, beverages and blood building powders. The dose of
composition varies from 50- 5000 mg once or twice a day for a human.
       Some preparations are also developed to treat and prevent iron deficiency
anemia by Sibnath ghosal (US patent -2003/0198695). This preparation expedites the
iron absorption in blood stream without any side effect. This herbo-mineral
composition contains purified shilajit having dibenzopyrones (DBPs), optionally, but
preferably, in synergistic combination with an extract of Emblica officinalis plant
containing gallo/ellagi-tannoids (GET) and an added mineral supplement like iron,
copper or chromium. The DBPs and GETs are the bioactive constituents that maintain
the bioavailable and oxidation state of metals. The average molecular weight of DBP-
humato-ferrate complex in the preparation lies between 450-2500 daltons. A 100 ml
of syrup typically contains about 200mg of purified shilajit, 500 mg of Emblica
officinalis extract, and about 250 mg of added mineral. Resultant formulation has
pleasant taste, sweet to mildly bitter taste, pH 4.4, density 1.2g/ml and dark brown
color. Another capsule preparation (100mg) contains 25mg of purified shilajit, 50 mg
of Emblica officinalis and 10 mg of elemental iron. The preparation is found to raise
the hemoglobin level of blood 1gm/dl or more per week without side effect. On the
other hand this preparation is helpful in people who do not respond to conventional
chemical metal preparation and who has mal absorption syndrome. People suffering
from insufficient erythrocyte production and taking NSAIDs for a long period get
benefited from this combination.
       A few components of shilajit may be explored to sort out the bioavailability
problems of poorly water soluble drugs (BCS II & IV). There are also some Indian
patents on the said topic. Patent application number 814/Del/2001 by Saluja and
Agarwal claims better bioavailability of piroxicam when complexed with Humic acid
(a component extracted from Shilajit). Another patent explores completely the bio
enhancement capacity of the components of shilajit. Patent application number
531/Del/2005 explains in detail the isolation and characterization of humic acid and
fulvic acid from shilajit. These macromolecules have large hydrophobic core and
hydrophilic exterior. These can entrap and give rise to inclusion complexes. This
complexed drug molecule shows better solubility, wettability, dissolution and
permeability. There are different methods available to develop complexes [16].
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                   Gulam Mustafa et.al. / Shilajit: An ancient panacea
2. Needs of modern techniques
          Free radical causes irreversible cellular damage. Shilajit and its constituents
(Fulvic acid, Humic acid and Humin) possess variable concentration of free radicals
which increases with increasing pH of solution [17]. ESR spectrometry and N-
Vinylcarbazole polymerization show presence of significant amount of free radical in
aqueous solution of Shilajit and its constituents [18]. Also, stability of free radical
increases at higher pH (≥8.0) as they are converted into semiquinones [19] and
aqueous solution of Shilajit from different regions exhibit different pH. These free
radicals cannot be removed easily by techniques used in traditional systems of
medicines. While in modern pharmaceutical techniques this problem can be ruled out
easily.
          Fungal infection of Shilajit samples cannot be overlooked. Research works by
Ghosal [20, 21] evidenced the production of some lethal mycotoxins like 12,13-
epoxytrichothecenes and naptho-γ-pyrones.
          Abovementioned health risk is always associated with shilajit. Indigenous
systems of medicines can’t eliminate this risk potential completely. It is better to
isolate its active constituents by modern techniques and dispense in suitable dosage
form.
3. CONCLUSION
Considering these evidences shilajit or its constituents may be used as an integral
component of health care preparation and in general tonic but the use of modern
techniques        to      reduce      the      associated     risk       is    desirable.
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