W E L C O M E

Credit Seminar On

Phytopharmaceuticals And Their Pharmacodynamic Basis

Presented by: Rahul Kumar M.Tech (DT)

INTRODUCTION
Phytopharmaceuticals,
or phytotherapeutics Synonymous to herbal medicinal products, herbal remedies or phytomedicines

Marketed as standardized preparations in the form of

liquid, solid or viscous preparations

WHO defines herbal drugs which contain plant parts or

plant materials as active ingredients in the crude or processed state plus certain excipients

Prepared by maceration, percolation or distillation

Some Terminologies.
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PHYTOCHEMICAL : refers to every naturally occurring chemical presents in plants

NUTRACEUTICAL : can be any substance that may be considered a food or part of a food that provide medical and health benefits, including the prevention and treatment of disease.

COSMECEUTICAL : term used to describe cosmetic containing ingredients that are bioactive, exerting effects on people. It is a blend of cosmetic and pharmaceutical. Examples are antiwrinkles creams, baldness treatments, moisturizers and sunscreens

Characteristics of Phytomedicine
 Do not possess an immediate or strong pharmacological action.  Wide therapeutic use  Great acceptance by the population  Frequently used to treat chronic diseases  Cost less than synthetic drugs  Occurrence of undesirable side effects seems to be less frequent with herbal medicines  Perceived to be healthier than synthetic drugs

Contd.. Contd..

 Mixtures of many constituents  Active constituents are not well established  Standardization, stability and quality control testing are time consuming, tedious and highly priced  Genuine raw materials not easily found  Chemical and/or natural variability of plant material  Influence of harvest, drying, and storage conditions

Status of Phytopharmaceutical Industry

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Global market ~$60 billion with 15-20% annual growth rate Major share -China and Korea, India sharing 0.35-3.0%. Herbal medicines are distributed under 6 basic therapeutic categories: cardiovascular, 27.0%; respiratory, 15.3%; digestive, 14.4%; tonic, 14.4%; sedative, 9.3%; topical, 7.4%; others, 12.0%

Increased use globally @ 15% against 3% for modern pharmaceuticals

The number of people using herbal products in US rose by 50% last year

In India, 60-70% population use herbal drugs

Contd Contd
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There is no differentiation between pharmaceuticals and phytopharmaceuticals in Germany

Annual expenditure on herbal medicines AU $ 621 million in Australia

In Korea, herbal medicine output over US $ 500 million which account for 12% of the total drug output.

Japan has 147 herbal medicines are eligible by national health insurance scheme

In Singapore,12% of the daily outpatients visit traditional medicine practitioners

Methods of Extraction
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Cold extraction: plant material is extracted in solvent of differing polarity at room temperature.

Hot percolation: the plant is heated in the solvent . This extraction method allows for the extraction of a large number of metabolites

Supercritical fluid extraction: some gases behave as though they are liquids with solvating properties, under pressure.they can be blown away from the extractant after the extraction is over

Contd

Soxhlet extraction: most widely and commonly used extraction technique for natural product . Although some components may be destroyed in the process, it is still the best method or extraction used in natural product chemistry

Forms of herbal medicines

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Mixtures contain 2 or more active plants ingredients Teas or Infusions prepared by steeping herbs in boiling water.

Decoction a preparation that is made by adding cold water to the required amount of the drug and then boiled and allowed to simmer for 510 min.

Maceration refers to a preparation made by adding cold water to the required amount of the drug, which is allowed to soak at room temperature for 68 h before it is strained

Juice is prepared by crushing the freshly harvested plant parts and then expressing the juice.

Contd

Syrup is a preparation containing about 66% sucrose and generally has a viscous consistency

Tincture refers to an alcoholic solution (usually 3070% water) prepared from medicinal plant materials

Capsules are usually small but soft or hard containers normally made from gelatin

Tablets There are two types or tabletsuncoated and coated tablets

Ointments are usually semi-solid preparations aimed at external application

Modes of administration
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Oral: A decoction, infusions, tinctures, syrups and tablets are most often taken orally Nasal (Smoking, snuffing or steaming): essential oils suspended in hot liquids or powdered materials may be snuffed so that the active compounds are resorbed through the mucosa. Smoke from burning materials is inhaled and the active compounds resorbed into the lungs Topical: Lotions, oils or creams containing extracts of medicinal plants are applied directly to the skin, where the active compound is absorbed Bathing: Herbs or herbal extracts may be added to bath water Sub-cutaneous or intramuscular injections: Some phytomedicines are injected into the bloodstream

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Pharmacodynamics
Study of the actions and effects of drugs on organ, tissue, cellular, and subcellular levels
Site of action Mode of action

Pharmacodyanamics

Mechanism of action

Site of Action
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Enzyme Inhibition: Drugs act within the cell by modifying normal biochemical reactions.

Drug-Receptor Interaction: Drugs act on the cell membrane by physical and/or chemical interactions. This is usually through specific drug receptor sites known to be located on the membrane

Non-specific Interactions: Drugs act exclusively by physical means outside of cells. These sites include external surfaces of skin and gastrointestinal tract

The interaction of a drug with a specific receptor site is characterized by three factors, namely:

1. 2.

Chemical and structural specificity Stereo isomeric specificity

3. Potency: Potency is a measure of how much a drug is required in order to produce a particular effect

Plants as Medicines

Herbal Products from common plant sources

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Garlic ( Allium sativum) Allicin S-methylcysteine sulphoxide (SMCS) Inhibit both platelet aggregation and thrombus formation, and thus may be of value in the treatment of thrombotic disorders Inhibition of LDL oxidation and platelet aggregation were proposed as mechanisms of benefit against cardiovascular disease Decrease the risk of nitrosamine formation and

possible cellular damage and cancer development

2. Ginger (Zingiber officinale)

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Active constituents :gingerol, gingerdione, and shogaol

Effective for Morning sickness, nausea & vomiting and Vertigo

6-shogaol acts on serotonin receptors or 5-HT(5-hydroxytryptamine receptors) to check the nausea & appetite.

6-gingerol controls the morning sickness by increasing gastrointestinal motility.

3. Tulsi (Ocimum sanctum)

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Active component eugenol. Act as vasodilator Possess membrane stabilizing properties on synaptosomes cells which helps in management of neurological (e.g. convulsions & epilepsy) disorders

4. Green tea (Camellia sinensis)

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epicatechin (EC), epigallocatechin (EGC), epicatechin (ECG), and epigallocatechin gallet (EGCG)

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kaempferol, quercetin, and myricetin The hypocholesterolemia activity of tea catechins can be attributed to the inhibition of intestinal cholesterol absorption as well as the enhancement of cholesterol excretion through feces

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Grape seed extract Resveratrol Interfere with cancer cell growth and proliferation, as well as induce apoptosis

Reduce risk of heart disease, such as by inhibiting platelet aggregation

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Amla (Emblica officinalis) Lignans, alkaloids, and bioflavonoids Its extracts induce apoptosis Free radical scavenger

Regulatory aspects and approval of herbal drugs

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WHO has published guidelines in order to define basic criteria for evaluating the quality, safety, and efficacy of herbal medicines

WHO has prepared pharmacopeic monographs on herbal medicines and the basis of guidelines for the assessment of herbal drugs

In USA since 1994, herbal medicines have been regulated under the Dietary Supplement Health and Education Act of 1994

y Germanys Commission E (phytotherapy and herbal

substances) was established in 1978
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In India ,in 2001, the Central Drugs Standard Control Organisation of Directorate General of Health Services has issued GCP guidelines. These guidelines recommend the approach to clinical trials of herbal remedies and medicinal plants

Conclusion
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Phytomedicines have several benefits over prescription drugs, which makes the basis of their increased demand in the market

Doses and efficacy of phytomedicines or phytopharmaceuticals need to be validated

Standardisation for plant-derived ingredients in medicinal products is necessary

Close collaboration is expected between clinicals and scientists with a common aimproduction of safe, quality and efficacious phytomedicinal products

T H A N K Y O U A L L