Herbal formulations

Challenges in herbal formulation
Steps in herbal drug formulation
Types of conventional herbal formulations
Liquid herbal dosage forms
Solid herbal dosage forms
Other herbal dosage forms
Novel dosage form

1. HERBAL FORMULATIONS Presented By: Mahewash Sana A. Pathan

2. CONTENTS: Challenges in herbal formulation Steps in herbal drug formulation Types of conventional herbal formulations Liquid herbal dosage forms Solid herbal dosage forms Other herbal dosage forms Novel dosage form 2

3. CHALLENGES IN HERBAL FORMULATION According to WHO, herbal dosage forms are the physical form like liquid, solid, semi-solid products produced from herbs, with or without excipients, in a particular formulation (such as decoctions, tablets, ointment, etc .) The toxicological, epidemiological & other data available regarding herbal formulation is confusing. Authentication of herbal materials is difficult. Pharmacological, toxicological & clinical documentation is tedious task. It is difficult to follow pharmacovigilance guidelines in case of herbal formulations. There is need to study herb-drug interactions. Standardization, safety & efficacy are a big challenge. There is various hurdles in conduction of clinical trials of herbal formulations. 3

4. STEPS IN HERBAL DRUG FORMULATION 4

5. TYPES OF CONVENTIONAL HERBAL FORMULATIONS 5

6. Liquid Herbal dosage forms 1. DECOCTIONS: Dosage: 3-4 times a day upto 500 ml per day. Example: Sijunzi decoction (chinese herbal remedy, mixture of Panax Ginseng, Poriacocos, Atractylodes macrocephala & Glycyrrhiza auralensis ) 6

7. 2. INFUSIONS: These are made by using cold or hot water for herbal extraction are dilute solutions. Should be stored in cold & dry place Shelf life is upto 24 hrs. Dosage: 3-4 times a day upto 500 ml per day. Example: Tea, coffee, lemon infusions. 7

8. 3. TINCTURE It is an alcoholic or hydroalcoholic extract of herbal materials, by using 1 part of herb & 5-10 parts of ethanol. Can be stored in cool, dry & dark place for 2 yrs. Dosage: 5ml diluted to 25 ml, 2-3 times a day. Example: Tincture of iodine, Benzoin tincture, cannabis tincture. 8

9. 4. SYRUP :- Syrups are viscous liquids containing high amount of sugars or other sweetening agents. May or may not contain medicine & flavoring agents. Due to high sugar content, they are susceptible to microbial contamination so they contain preservatives. EVALUATION: Organoleptic characters pH Specific gravity Total solid content Viscosity Stability Preparation: Dosage: 1-2 teaspoonful thrice a day. Example: Hempushpa syrup, Brahmi syrup, Cough syrup, Heart tonic syrup. 9

10. 5. ORAL EMULSIONS : These are liquid dosage forms consisting of two immiscible phases which are stabilized by addition of emulsifying agent. One liquid can be uniformly dispersed in another immiscible liquid in the form of small droplets using emulsification equipment such as agitators, homogenizers, colloid mills & ultrasonic devices. Example: Intralipid ® Perikabiven® 10

11. 6. AROMATIC WATERS: These are water based formulations saturated with essential oils. These are prepared by mixing distilled water with one part of essential oil & ten parts of talcum powder. It is shaken well & then kept aside for 12 hrs, & then filtered & volume is adjusted. It should be made in small quantities to protect it from decomposition. Example: cardamom water, peppermint water, camphor water. 11

12. 7. HERBAL GLYCERITES : These are tincture like dosage forms which are prepared by extracting herbal drugs with 50-60% of glycerine as extraction medium. The shelf life of glycerites is about 6 months to 2 years. This form is suitable for preparation of pediatric medicines. Glycerin cannot be used for herbs containing gums or resins. Examples: Goldenseal extract, Echinacea herbal extract, Rhodiola extract. 12

13. 8. OXYMELS : These are sweet & sour formulations containing honey & small amount of vinegar as carrier. Example: Garlic, Cayenne, lobelia oxymels. 13

14. SOLID HERBAL DOSAGE FORMS 1. HERBAL TEA BAGS: Herbal materials i.e. dried roots or leaves or flowers are packed into paper or cloth bags. Bags should be free from bleach, gluten & dioxin. The boiling should be poured on bags for making infusion. 2. DRIED POWDER: Herbs are dried & pulverized to make coarse or fine powder. It can be administered directly by mixing with warm water & can be available as capsule or sachet form. 14

15. 3. DRY EXTRACT POWDER: These can be prepared by spray drying or freeze drying of fluid extract with or without using an adsorbent, or made by drying & milling to produce a powder. It may contain excipients, stabilizers & preservatives.dry extracts can be incorporated in capsules, tablets or granules. 4. HERBAL MIXTURES: These are combination of two or more plants. Plants are dried & pulverized & mixed into specific proportions to get herbal mixtures. 15

16. 5. GRANULES: These are agglomerations of small spherical particles made from dried fluid extracts. Can be administered after reconstitution with water as solution or suspensions. Can be used to make tablets or capsules. E.g. Vasawlehachurna granules, chyavanprash granules, Gastrobeet oral dispersible granules. 6. PILLS: These are spherical dosage forms larger than granules made from herbal extracts. These are made by triturating dried powdered herbs or dry extract with excipients to form mass. E.g. Madhunashinivati , chandraprabhavati , khadiradivati , etc. 16

17. 7. CAPSULES: These are solid dosage forms containing drug & appropriate filler enclosed in a gelatin container. Advantages: Mask unpleasant taste of medicine. Provide uniformity of dosage. Release content rapidly than tablets. E.g. Fenugreek capsules, Chlorella capsules, pudinhara , moringa capsules, etc. 8. LOZENGES: These are solid dosage form which slowly release medication in mouth. Can give local or systemic action. Herbal extract is boiled with sucrose & water to make lozenges. 17

18. 9. TABLETS: Tablets are solid dosage form made up of herbal extract, granule is blended with excipients & compressed to form a defined size & shape. Preparation methods: Direct compression Wet granulation Dry granulation Coating of tablets: it is done to mask undesirable colour, odour, taste, to protect from moisture. It is carried out by using pan coating or press coating method. Evaluation: Pre-compression: Bulk density, tapped density, housner’s ratio, carr’s index, angle of repose. Post compression; Hardness, thickness, friability, weight variation, content uniformity, disintegration time, dissolution time, etc. 18

19. OTHER HERBAL DOSAGE FORMS 1. OINTMENTS: These are semi-solid greasy preparations containing anhydrous immiscible base generally used for skin, rectum or nasal mucosa. The process of making ointment involve heating of oil & aqueous phase separately & then mixing of both phases with constant stirring until the mixture get congealed. E.g. Calendula ointment, Herboheal ointment, pilex , pain care ointment. 2. HERBAL CREAMS: Creams are semisolid dosage forms containing herb in hydrophilic base. Prepared by mixing powdered drug or extract in cream base. It has relatively short shelf life as compared to ointment. E.g. herbal fairness cream, baby cream, etc. 19

20. 3. HERBAL BALMS: These dosage forms are like ointment used to relieve pain. These are made by mixing herbs with ointment base. E.g. tiger balm, herbal pain balm, lip balm. 4. INHALATIONS: These preparations intended to be used in bronchial tubes or lungs in the form of aerosols. They may be dry powder inhalation or liquid inhalation. E.g. Astha aid drops, karval plus inhalation capsules. 20

21. 5. PLASTERS & PATCHES: These are made by spreading soft or dry herbal extract on support made up of fabric or synthetic resin. Intended to use topically on the skin & deliver the active ingredient through the skin. E.g. capsicum patch, herbal medicated plasters. 6. MEDICATED OIL: These are prepared by mixing, macerating or boiling herbal drug, extract of fresh juice with suitable fixed oils. E.g. indulekha oil, tea tree oil, peppermint oil, etc. 21

22. 7. HERBAL SOAPS: These are prepared by incorporating herbal drugs having antifungal or antimicrobial properties with detergent base. E.g. neem & turmeric soap, papaya skin whitening soap. 8. HERBAL PASTES: These are similar to ointment which contain 50% of drug powder incorporated in fatty base. E.g. Dantkanti toothpaste, miswak , Aloe vera toothpaste. 22

23. 9. HERBAL SUPPOSITORIES & PESSARIES: Made by mixing finely powdered herbs or extracts with cocoa butter base. E.g. tea tree pessaries, neem oil suppositories, herbal vaginal pessaries. 10. Herbal liniments: Used in the treatment of soreness in muscles & ligaments & pain. Should not be applied on cut or broken skin Prepared by using alcoholic extract of heat producing herbs. E.g. liniment plus, penil . 23

24. NOVEL DOSAGE FORM Novel drug delivery system (NDDS) means the approaches, formulations, technologies, & systems to transport a pharmaceutical compound in the body so that it can safely achieve its desired therapeutic effects. NDDS is nothing but combination of advanced techniques & new dosage forms in which drug is delivered by the system other than conventional drug delivery system. Advantages of NDDS: Solubility & bioavailability enhancement Enhance distribution & pharmacological activity. Drugs can be released at predetermined rate Less toxicity Improve stability Easily administered Sustained action 24

25. 1. LIPOSOMES: These are microparticulate or colloidal carriers having 0.05-0.5 micrometer diameter. Liposomes are artificial microscopic vescicles containing one or more phospholipid layers enclosing an aqueous core. They are used to convey vaccines, drugs, enzymes, or other substances to target cells or organs. Advantages: Highly biocompatible, Biodegradable, non-immunogenic, Easy to prepare, Pharmacokinetic properties can be easily modulated, Can produce sustained or controlled release. Preparation: Examples: Therapeutic efficacy of anticancer drug, ampelopsin is improved. Catechins show improved permeability in skin Uric acid liposomes show enhanced solubility. 25

26. 2. PHYTOSOMES Phyto - plant; soma - cell like. Phytosomes are NDDS of standardized plant extract or water soluble phytoconstituents which are entrapped into phospholipids to produce lipid compatible molecular complexes. Preparation: Example: silymarin phytosome showed increased bioavailability , quercetin phytosome exhibit improved hepato -protective action. 26

27. 3. NANOPARTICLES These are nano-sized particles, ranging from 10-1000 nm, containing synthetic or semisynthetic or herbal drugs. Advantages: enhance solubility, reduce doses, can deliver drug to site of action & improve absorbance. Preparation: Examples : A rtemisinin nano-capsules show sustained drug release, improved bioavailability of glycyrrhizic acid. 27

28. 4. Microsphere These are spherical micro particles having diameter of 1-1000 mm. Made up of biodegradable polymers like polylactic acid, glycolic acid, albumin dextran & firinogen . Advantages: can be ingested or injected, easy to get desired release profile, do not affect drug activity, Preparation: microspheres are prepared by various techmiques such as spray drying, solvent evaporation, single & double emulasification , phase seperation coacervation , solvent extraction & quassi - emulsion solvent diffusion. Examples: Rutin -alginate-chitosan microcapsules able to target cardiovascular or cerebrovascular region, camptothecin loaded microspheres show prolong drug action. 28

29. 5. ETHOSOMES Ethosomes are nano-vesicles made up of phospholipids & have high content of ethanol i.e. 20-45%. Advantages: Help to improve transdermal permeation of drug through skin. Can be used for drug delivery of variety of drug . As it is in semi solid ,provide improved patient compliance . Preparation: Cold method ,classic mechanical dispersion method. E . g. liquorice ethosome show anti inflammatory activity and sustained release Cannabis ethosome show improved skin permeation. 29

30. 6. TRANSFEROSOMES They are vesicular system consisting of phospholipids, 10-25% surfactant and 3-10% ethanol. Preparation: Thin film hydration , modified hand shaking , lipid film hydration E.g.. Capsicum transferosome show increased skin permeation 30

31. 7. NIOSOME This are multilamellar vesicles similar to liposomes & made up of non ionic surfactant & cholesterol. 31

32. 8. PRONIOSOME They are water soluble carrier particles coated with surfactant . Before use these are hydrated to form niosome by shaking . These are gel formulation E. g. levonorgestrel proniosome gel or patch . 32

33. 9. TRANSDERMAL DRUG DELIVERY SYSTEM (TDDS) It is NDDS in which drug is delivered in the form of patches through the skin. Preparation: Basic component are polymer or drug reservoir, drug, permeation enhancer , backing laminates, release liner & excipients. Following methods are used Polymer membrane permeation controlled TDDS Matrix diffusion controlled TDDS Micro-reservoir controlled TDDS 33

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