TITLE: DEVELOPMENT AND FORMULATION OF HERBAL ANALGESIC CREAM.
Introduction: Wikipedia..Any drug which is used to obtain
analgesia is known as analgesic drug/painkiller. Analgesic drugs act on both
the central and peripheral nervous systems by using various ways. Analgesics
are different from anesthetics, which impermanent affect, and in few conditions
fully eliminate consciousness .Drugs which is commonly used as analgesics include
paracetamol, the non-steroidal anti-inflammatory drugs (NSAIDs) such as the salicylates, and opioid drugs such as morphine. The choice of analgesic
agent depends on the severity and response to other medication; the World
Health Organization (WHO) pain ladder specifies mild analgesics as its first
The type of pain also play important role in choosing analgesic agent.
Traditional analgesic agents are usually less effective in the treatment of
neuropathic pain; classes of drugs that are not normally considered analgesics
are prescribed for neuropathic pain, such as anticonvulsants and tricyclic
A condition such as muscle sprains and overuse injuries, topical NSAIDs provide pain relief. Topical
preparations are preferred over oral medications because topical preparations
have fewer side effects as compared to oral medications.iii
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Paracetamol (acetaminophen): In mild to moderate pain and fever, this
medication is used. It is also
in more severe pain such as cancer pain and postoperative surgical operations
.It is a mild
agent and normally safe at prescribed doses.
Are group of drugs use to decrease pain and lower fever. When given in higher
doses NSAIDs can also reduce inflammation. In most countries NSAIDs e.g.,
aspirin, ibuprofen and naproxen are available as over the counter drugs.
inhibitors: Are drugs which are derived from NSAIDs. The cyclooxygenase enzyme
which is inhibited by NSAIDs has two types: COX1 and COX2. Advance studies
suggested most of the adverse effects of NSAIDS are due to the blockade of COX1
enzyme while the analgesic effects are due to the
4.Opioids: Morphine, codeine, oxycodone, hydrocodone, dihydromorphine all have
a similar effect on the cerebral opioid receptor system. Due to opioid toxicity
(confusion, respiratory depression, myoclonic jerks and pinpoint pupils) lower
opioid dose is recommended, higher dose can be recommended in opioid- tolerant
gate..Pain is subjective in nature and is measured by patient itself by
reporting its intensity and other subjective qualities .It has been a challenge to define pain because
it is a complex, subjective phenomenon, often caused by damaging stimuli. In medical
diagnosis, pain is considered as a sign of an underlying condition. Pain is
normally short-lived, continuing only as late as the harmful stimulus is
eliminated or the underlying injury or pathology has cured, but some painful
states, such as rheumatoid arthritis, peripheral neuropathy, cancer and
idiopathic pain, may continue for years. Pain can be classified based on its
duration, acute or chronic, as well as other characteristics such as intensity,
region of the body involved, causes etc. Pain that is minor and normally needs
treatment for not more than up to a few weeks is acute pain. Pain that lasts
for more than a one month is called chronic. Conventionally, the difference between acute and chronic pain has depend on random interval of
time from onset.
Pain is the most common cause for people to use complementary and revolutionary medicine.91 An opinion of the
13 highest quality studies of pain treatment with acupuncture,
published in January 2009, determined that there was small difference in the
effect of real, faked and no acupuncture.92 However, other
reviews have found some advantage.939495 Additionally, there
is provisional verification for a few herbal medicines.96 There has been some
interest in the relationship between vitamin
D and pain, but the
evidence so far from controlled
such a relationship, other than in osteomalacia, is uncertain.97
In health care system, plants are significant and fundamental for elimination
and restorative purposes. The use of
native herbal medicine is very old and an essential part of treatment 1.
For different healthcare products, conventional medicinal herbs have used as a
possible source of alternative medicine. Rich inheritance of former culture and
technical heritage are major sources for understanding of herbal medicines 2. According
to WHO guidelines, approximately 75-80% of world population still rely on herbal
medicines. Active components which are originated from plant sources
immediately used as therapeutic agent and medicinally active chemical constituents
are also served as lead molecule for the synthesis of many drugs 2, 3. The great number of rural and poor people is getting financial
advantages from native or herbal medicines. According to WHO guidelines, around
25% of modern medicines which are originated from plants sources are used
conventionally and nearly 75% of herbal drugs are discovered by doing research
on traditional medicinal herbal plants 3. Due to the increase in the use of
herbal medicines the field work and screening of plant has been increased
the past years, the therapeutic use of herbal medicine is getting appreciable power
in the world. Due to toxicity and side effects associated with allopathic
medicines there is abrupt increase in the use of herbal medicine. In
traditional system of medicine, herbal medicines are used as major remedy in
medical practices since many years. Because of biomedical advantages associated
with herbal medicine and its societal views in many parts of the world medical
practices continues today which made a great participation towards preserving
human health 1.
Herbal medicines are the synthesis of corrective experiences and
practice of native systems of medicine for over hundreds of years. During the past
decades there is huge progress in medical research but still the treatment of
many dangerous diseases including pain and inflammation is troublesome. The
analgesic and anti-inflammatory drugs which we are using are found with some dangerous
side effects; for this reason there is a need to develop such analgesic and
anti-inflammatory drugs which have less side effects. When compared with
synthetic drugs it can be seen that herbal medicine have more safety, efficacy,
cultural acceptability and less side effects 27.-The number of chemical
compounds, which are found inside the
plant kingdom are supposed to have good consistency with the human body as
these are part of the physiological events of living flora 2. Different phytoconstituents
like alkaloids, flavonoids, xanthone, coumarin, sterols, withaferin-A,
andrographolide etc., are also proved efficient as analgesic and
anti-inflammatory agent 5, 6. Therefore it is the need of time to explore
herbal medicine and uses them in our daily life.
EXAMPLES OF HERBS USED AS ANALGESICS:
Vera can be used to achieve analgesia e.g., reduction in pain without losing
consciousness. During dental treatments Aloe vera can be used topically for
pain reduction. For moth ulcers, sores, burns, cuts, scrapes it can be used
effectively for treatment. For quick relief of pain after dental surgical
procedures it can be recommended. It is also used for pain healing purposes in
the treatment of piles and hemorrhoids.
For arthritic pain, Aloe Vera juice is effective and has been used for
The Arnica can be used for medicinal purposes; it is applied to the skin
for soothing muscle aches, relieving sprains, reduction in inflammation,
healing and bruising wounds. However, it can cause serious side effects when
taken orally. For diabetic eye damage and post-surgical operations the
homeopathic version of Arnica is used.
Some varieties of Basil have analgesic activity which can be used to
reduce pain on a lower level.
Piperine is a chemical present in black pepper it can be used for pain
reduction. For reduction in pain an analgesic cream can be made by mixing
piperine with other ingredients.
Advance research has shown that cardamom has gastro-protective
properties. The pain which is associated with stomach cramps and other stomach
problems can be reduced with cardamom. Painful muscle spasms in animals can be
reduced with the use of cardamom.
Capsaicin is a natural pain relieving herb which is present in super-hot
cayenne. Capsaicin reduces the amount of substance P which delivers pain
messages to the brain. Capsaicin creams and patches are used for pain
Patients with arthritis, osteoporosis and gout are treated with celery
seed extract, after few weeks it can be seen that patients reported lower pain
levels and some reported complete pain relief.
For hay fever, inflammation, muscle spasms, menstrual disorders, diaper
rash, skin infection, ulcers, wounds, Chamomile can be used because it contains
terpenoids and flavonoids which contribute to its medicinal properties.
have analgesic and antibacterial properties due to the presence of compound
eugenol and are considered as traditional remedy for toothache or mouth ulcers.
Cloves are used in many topical preparations for the purpose of pain reduction
and to reduce mouth and throat inflammation.
Coriander has analgesic properties and is used in the treatment of
hemorrhoids, toothaches and joint pain.
Studies have reported that fennel is an effective herb in menstrual
For headaches or migraine pains, ginger play important role as it can
reduce pain effectively. Advance research has shown that sumatriptan and ginger
has comparable analgesic properties. Patients of osteoarthritis also can get
benefits from the use of ginger. One advantage of using ginger is that it does
not cause any side effects like other medications.
Jamaican Allspice can be used in both ways externally and internally for
menstrual cramps, stomach pains.
Licorice root is used for various medical conditions, used in the
manufacturing of both eastern and western medicine. Patients with stomach
ulcers who had not get benefits with conventional medicines when used licorice
fluid extract get maximum benefits and after about 6 weeks of therapy ulcers
are completely removed in these patients. The itching which is associated with
eczema can be minimized with the use of topical licorice gel. The pain which is
caused by sores and mouth ulcers can stop when licorice root is gargling with
Eugenol is present in marjoram and has analgesic qualities. It is a best
home remedy for patients who have arthritis and inflammatory bowel conditions.
Mustard seeds are used in various medicinal problems; the seed have
analgesic activity and can be recommended in muscular pain, ringworm and
respiratory disorders. Mustard seed poultice is known for its natural analgesic
effects and can be used in various painful conditions nd in muscle aches.
In itching and painful conditions neem can be used topically, it is a
potent analgesic agent and provides analgesia within a short duration of time.
In various medical problems like eye disorders, stomach upset, gum disease,
intestinal worms etc. Neem has been used for many years.
Nutmeg has analgesic properties and it has been used to treat various
painful conditions. It can be used topically or ingested to get pain relieving
Parsley root has analgesic properties it can relax stiff joints and
eliminate the pain associated with joints.
The pain associated with heartburn, intestinal gas, gout and headache
can be relieved with the use of rosemary. Topical preparations of rosemary are
available which can lessen the severity which is associated with toothache,
eczema and joint or muscle pain.
Sage is used in teas and gargles as an herbal remedy to eliminate the
pain associated with sore throats, mouth ulcers, gum disease, laryngitis and
coughs. For dental pain two tablespoons of dried sage and one tablespoon of sea
salt add in water , rinse your mouth with this water you can get relief from
Topical and oral preparations of slippery elm are used to relieve
toothaches, coughs, sore throats, boils, burns and skin inflammation.
Advance research has shown that thyme has excellent analgesic effects. It
can work better than ibuprofen .In menstrual pain the analgesic activity of
thyme is remarkable. In different aches and pains thyme can be recommended to
get best pain relieving effects.
Curcumin is present in turmeric which is responsible for analgesic
the treatment of painful joints and other painful conditions related with
joints, this root has been used traditionally in medicines for centuries.
Semisolid dosage forms which are made up of oil phase, aqueous phase and
emulsifying agent are known as creams. Creams has high viscosity, virgin
coconut oil is used for the preparation of
base for cream which is oil phase, distilled water is used which served
as aqueous phase and nonionic surfactant Tween 80 is used as the emulsifying
agent. A different topical preparation e.g., creams and gels combine distinct
ingredients which have analgesic activity, for a better synergistic effect. Different
complications are faced during the preparation of cream e.g., instability such
as creaming or sedimentation, flocculation, coalescence, Ostwald ripening
(disproportionation) and phase inversion etc. For the determination of
shelf life of emulsions, stability tests such as thermal stability, freeze-thaw
and centrifugation testing, optical monitoring at accelerated temperatures and
valuation such as microscopic examination, pH and viscosity are done. Glucosamine, chondroitin, celadrin, comfrey
root, capsicum, green-lipped muscle extracts are very effective natural
ingredients which are used in many topical preparations.
Preformulation tests for cream:
properties of a novel drug molecule are very important and significant, preformulation
group of studies should focus on such properties as these properties could
affect the drug presentation and the evolution of a dosage form. These studies
are very meaningful, could give significant information for formulation design
and development or support the demand for molecular adaptation. The main
purpose of preformulation studies is to create particulars helpful to the
formulation in evoluting stable and bioavailable dosage forms which can be put-together
Preformulation tests for cream include:
Organoleptic tests: In organoleptic
tests, we observe the color, physical
appearance, smell, taste, odor, melting point and solubility.
Micromeritic properties: In micromeritic
properties we determine the bulk density, tapped density, Hausner’s ratio,
angle of repose and compressibility index.
Visual solubility: The visual
solubility was determined in different solvents such as distilled water,
ethanol, phosphate buffer pH 6.8 etc., the solutions were checked visually for
Determination of pH: For the
determination of pH 0.5 g of the formulation was dispersed in 50 ml of
distilled water and the pH was determined.
SOME EXAMPLES OF HERBAL ANALGESIC CREAMS:
For the production of
synovial fluid glucosamine in topical preparations provides building blocks, oils
which mobile joints, and cartilage which cushions bones. Glucosamine in topical preparations
reduce inflammation and increase the process of tissue repair. Glucosamine which
is found in these topical treatments is in the form of n-acetyl glucosamine,
which is little to sink into skin and penetrate underlying tissues to
eliminate pain. Within four weeks topical preparations which contain
glucosamine can greatly eliminate the pain of knee osteoarthritis. One advance
research on glucosamine
cream found that 100% of those with arthritis of the shoulder gained
advantage. 75% of patients with arthritis of the ankle, wrist or elbow are
found with reduction in pain and 58% of those with knee osteoarthritis are
gained benefit with this topical preparation.
and glucosamine both are mixed together in various topical preparations.
Advance research has shown that people with osteoarthritis when apply a cream
containing both glucosamine
and chondroitin produced
significant pain reduction than a placebo cream. After 4 weeks, the active
glucosamine and chondroitin cream was 20% more potent, and after 8 weeks, it
was 80% more powerful than the placebo cream.
has an anti-inflammatory and pain relieving action. It is a mixture of waxy,
cetylated fatty acids that perforate in cell membranes to ameliorate their
pliancy and elasticity.
fatty acids are naturally found in only two sites – in sperm whale oil and in a
strain of mice distinguished for their indemnity against arthritis. The
celadrin which is used in creams for joint pain is obtained from
monounsaturated fats present in olive oil. Advance studies shows that celadrin
fatty acid cream when applied with menthol to knees there is significant
reduction in arthritis pain and this can make better the extent of mobility.
Celadrin cream is considered best in joints pain, it makes it comfortable to
climb up and down stairs. Celadrin cream cetylated fatty acids can
also decrease muscle pain which is associated with pressure on trigger points
in the neck.
Sulphur is an important constituent of connective tissues and structural proteins;
MSM (methyl-sulfonyl-methane) is an abundant source of
sulphur. It is needed for the recovery and better functions of muscles, joints
and ligaments, has wonderful antioxidant and anti-inflammatory activity.
Comfrey root has been
used to heal wounds and fractures since long. Advance studies reveal that
comfrey root has two active constituents: allontoin which helps in tissue
regeneration and rosmarinic acid which reduces pain and eliminate inflammation.
Cream which contains comfrey root is very famous and powerful remedy for joint
pain, sprains and strains. A research with 120 patients who have upper and
lower back pain when used comfrey root cream thrice a day for 4 to 6 days their
severity of pain can reduce by 95% compared with inactive placebo cream which
can reduce pain up to 38%. Researchers have reveal that comfrey cream is better
than a prescribed, NSAID e.g., diclofenac gel in treatment of ankle sprains; it
works rapidly and provides excellent pain reducing effects after an hour
Capsicum cream helps in
pain reduction by constantly provoking nerve endings in the skin at a very low
grade; this will expend nerve endings of neurotransmitter chemicals so they
become less responsive and pass on small number of pain messages to the brain.
This action can also decrease perception from underlying painful joints.
Essential oils used in topical preparations:
Eucalyptus, Camphor and Oil of Wintergreen are used in various topical preparations;
these are easily absorbed into the skin and produce a chilling or melting
sensation. Wintergreen is an abundant origin of methyl salicylate, a natural
anti-inflammatory analgesic related to aspirin.
ZIZIPHUS JUJUBA: Wikipedia
It is a
deciduous tree or shrub, small in diameter with height of about 5-12 meters.
Twigs are spiny, the leaves are shiny-green, ovate-acute, 2-7 centimeters tall
and 1-3 centimeters in width .The flowers are small, fruit is an edible ovate
plum. There is only one pretentious seed which has similarity to an olive pit.
usual distribution is unclear due to large-scale gardening, but is thought to
be in southern Asia, between Lebanon, northern India, and southern and central
China, and perhaps also southeastern Europe though more possibly started there.
Figure 1: Leaves of Ziziphus jujuba
many years Zizyphus jujuba has been used as an essential oriental folk medicine.
The fruits of Z.jujuba are consumed
in Asian countries as a food, food additive and flavoring agent due to its high
nutritional value, the ripe fruit is also used as emollient, aphrodisiac,
tonic, laxative, antiemetic, and appetizer. The seeds of Z.jujuba are used for
many medicinal purposes such as used as tonic,
tranquillizer, analgesic, anticonvulsant, aphrodisiac, astringent; and are used
to cure cough, asthma, vomiting, burning sensation, biliousness, leucorrhea,
and eye infections in traditional systems of medicine. It is extensively for the treatment of anxiety, insomnia,
dreaminess, and night sweats and hence considered as one of the most popular
traditional Chinese medicines .Recent pharmacological research reported that it
possesses anti-inflammatory, hepatoprotective, antimicrobial, anxiolytic, and
hair growth promoting effects.
Bioactive essential oil, saponins, phenolic compounds, alkaloids, and
been reported from the seeds of Z. jujuba. Different analytical
methods are used for the estimation of saponins and fatty acids.
The plant of Z.jujuba
contains Rutin, ?-sitosterol, Maslinic acid, Heptadecanoic acid, Tetracosanoic acid, D-glucose as main active
The aim of this research was to develop and formulate the
herbal cream containing petroleum ether extract of Ziziphus