WHMF121 Session Six Pills, Tablets & Capsules

Transcription

1 WHMF121 Session Six Pills, Tablets & Capsules Endeavour College of Natural Health endeavour.edu.au 1

2 Today s Topic o Understanding what is meant by Drug: Herb ratio o Pills and tablets Advantages and disadvantages Commercial considerations Herbs to consider o Capsules Advantages and disadvantages Commercial considerations Herbs to consider o Make herbal pills and capsules in tutorial Endeavour College of Natural Health endeavour.edu.au 2

3 Drug Extract Ratio (DER) o It is important that everyone is comfortable with the concept of the weight to volume ratio, aka the Drug Extract Ratio (DER) or the product ratio. o DER is used for: To compare doses and ensure proper dosing of patients. To convert between liquid extract quantities and dry herb amounts as well as dry herb quantity and liquid extract amount. The DER also expresses the weight of the original starting dried herbal material to the weight of the finished product Endeavour College of Natural Health endeavour.edu.au 3

4 Drug Extract Ratio The most commonly used dosage standard globally is weight of dry herb material. This is seen in both traditional and contemporary texts, eg., 1-2g of dried leaf or equivalent, twice a day. Equivalent is another preparation form or extract made from the same herb that contains that original amount of herb (Breakspear, 2014) For example, a dried herb equivalent of 1g could be: 2mL of a 1:2 (1g:2mL Liquid Extract) 1mL of a 1:1 (1g:1mL Liquid Extract) 250mg of 4:1 (1g:0.25g = 250mg Soft Extract) Extractions change the chemical profile of the original dry herb. Endeavour College of Natural Health endeavour.edu.au 4

5 Other measures of a dried herb equivalent of 1g could be 5mL of a 1:5 (1g:5mL tincture) Drug Extract Ratio 200mg of a 5:1 (1g:0.2g = 200mg spray dried herb) 20mg of a 50:1 (i.e. 20mg x 50=1000mg dried herb) Standardised (Std) Extract Pro Extract powder this is the DER used for EGb 761 (a Ginkgo biloba extract) Plant specimen taken by Johann Goethe ( ) of Ginkgo biloba ( he_ginkgo_biloba.jpg) Endeavour College of Natural Health endeavour.edu.au 5

6 Drug Extract Ratio o Extracted Herbal medicines are expressed by their ratio of herbal material to solvent o These liquid herbs can be used as Galenicals or further processed into other products. o There are multiple factors that determine the final chemical make up of the processed herb. o The ratios are like fractions Herbal material: solvent 1:2 = ½ strength 1:3 = 1/3 strength 1:1 = full strength 5:1 = 5 times the strength 18C portrait of Galen by G.P. Busch. Endeavour College of Natural Health endeavour.edu.au 6

7 o Galenicals Drug Extract Ratio Named after Claudius Galenus, a Greek physician, surgeon and philosopher in the 2 nd century. He was an avid researcher that set the ground work for the medicinal sciences. A Galenical extract (aka full-spectrum extract) is one that most closely represents the chemical complexity of the dry plant material. Each herb has a specific preparation method that has been determined to be the best way to extract the required active constituents. The result is a herbal medicine aka phytomedicine. Endeavour College of Natural Health endeavour.edu.au 7

8 Extract Pro Extract - EPE A method of percolating & re-percolating a herb, extracting very high concentrates of the herb, used in tablet making and therefore reducing the extract to almost a resin. AKA Semi-solid extract. For example all the fluid extracts of Glycyrrhiza glabra are all EPE s. Glycyrrhiza g. does not look black if it is just chopped roots extracted with H2O & EtOH. The black sweet tar we call a FE of Glycyrrhiza glabra is a reconstituted EPE (which is solid like a block of black toffee). In reality it is likely to be 4:1 extract. 1/4 part EPE is equivalent to 1 part dried herb. 250gms of EPE when dissolved in 1lt of menstruum = 1:1 All EPE s can be reconstituted to FE with 25% EtOH [ethanol] which is sufficient to give them bacteriological stability. When you see 25% EtOH in FE s you can pretty much guess it started life as an EPE - Angelica archangelica is another example. Endeavour College of Natural Health endeavour.edu.au 8

9 Drug Extract Ratio - Calculations o Multiple dosage forms are now common in herbal medicine, it is therefore essential that clinicians can convert between extract and dry herb equivalency, and vice-versa. o This process is very simple, and it is essential that all herbal students and clinicians can do these conversions quickly and accurately. o For instance, need to be able to interconvert between an Echinacea tablet stated to contain 200mg of a 4:1 extract, with a dose of 1 tablet three times daily an Echinacea purpurea radix liquid extract stated to be a 1:2 a textbook recommended dose for Echinacea purpurea radix of 1-2g three times daily So how do the calculations work? (Breakspear, 2014) Endeavour College of Natural Health endeavour.edu.au 9

10 DER - Calculations Converting from dry herb to extract Example; (DIVIDE) You have a 1:3 extract and need to give 1.5g of dry herb equivalent. What dose of the 1:3 extract should you use? X (dry herb quantity) = 1.5g Y (extract quantity) = unknown Extract ratio: 1:3 (or 1/3) Rule: Divide the dry weight by the extract ratio 1.5g divided by 1/3 = 4.5mL Therefore the answer is 4.5mL (Breakspear, 2014) Endeavour College of Natural Health endeavour.edu.au 10

11 DER Calculations Converting from extract to dry herb Example: (MULTIPLY) You have 2mL of 1:3 extract, what is the equivalent quantity of dry herb? X (dry herb quantity) = unknown Y (extract quantity) = 2mL Extract ratio: 1:3 (or 1/3) Rule: Multiply the extract quantity by the extract ratio 2mL multiplied by 1/3 = 0.66g Therefore the answer is 0.66g (Breakspear, 2014) Endeavour College of Natural Health endeavour.edu.au 11

12 DER Calculations Don t Get Your Units Messed Up! It is essential that you keep your units correct throughout your calculations. Example: 1:2 extract is said to be 1kg : 2L. This is the same as: 1000g : 2000mL (because there are 1000g in 1kg and 1000mL in 1L) 1g : 2mL 1000mg : 2mL 500mg : 1mL (Breakspear, 2014) Endeavour College of Natural Health endeavour.edu.au 12

13 History of Pills and Tablets It is not exactly known where the use of tablets as a hard dosage form originated from, albeit, it seems to come from both TCM and ancient Greek paradigms of medicine. There are documented historical records of pills being used therapeutically. Traditionally powdered crude herb was literally bound with excipients such as honey, tragacanth gum or marshmallow to facilitate ease of shaping. Hippocrates ( Endeavour College of Natural Health endeavour.edu.au 13

14 History of Pills and Tablets o It became a very popular way to take medicines, obviously due to the lack of poor taste that is often associated with many of the various herbal liquid dosage forms... o A popularity that still exists today. o With the advent of tablet manufacture, so began the specialisation of herbal manufacturing, and thus, centuries of refinement later, the birth of pharmacy as we know it. Endeavour College of Natural Health endeavour.edu.au 14

15 Pills, Tablets and Capsules o A Pill is an old term to describe a tablet o It is a dosage form that incorporates the blending of various dry materials together and then moulding/compressing them into a solid form and shape conducive to swallowing ( ategory:pill_textures) o Whilst it is comprised of the active ingredient, it also contains various excipients (non-active material). Endeavour College of Natural Health endeavour.edu.au 15

16 Excipients in Pills, Tablets and Capsules Some examples of excipients are listed below: Various coatings to aid stability (reduces the uptake of moisture etc) Various coatings to aid absorption (enteric coatings) Binders (holds the ingredients in a tablet together, such as microcrystalline cellulose) Anti-adherents (reduce the adhesion of the tablet powder to the punch moulds of a pharmaceutical press machine) AKA lubricants Endeavour College of Natural Health endeavour.edu.au 16

17 Excipients in Pills, Tablets and Capsules Disintegrants (cause the tablet to break apart when in the GIT to increase dissolution/ absorption) Fillers or diluents (add bulk to a formulation, so it may meet the required size) Flavours and colours (to appeal to various people, children etc) Glidants (increase the flowability of the powder, especially in tablet machines) Preservatives (to aid stability) Endeavour College of Natural Health endeavour.edu.au 17

18 Advantages: Pills, Tablets and Capsules - o They are a potent way of administering large doses of herbs, especially if EPE s (extract pro extracts with high DER powders such as 50:1) are utilised o Tablets are convenient and portable, whilst also storing well o Tablets bypass bitterness of other unpleasant tastes (if coated) o Devoid of alcohol (< 3%), so appropriate where this solvent should be avoided. o Can be manipulated via various coatings to assist in absorption (i.e. enteric coating / delayed release) (Adams & Tan, 2012) Endeavour College of Natural Health endeavour.edu.au 18

19 Disadvantages: Pills, Tablets and Capsules o Loss of constituents due to processing, such as spray-drying, powdering etc. o Not as easily or efficiently absorbed as liquid dosage forms (currently a matter of vigorous debate) o Excipients are ingested, which may prove detrimental (allergies etc) o Relatively low dose (unless EPE s are used) o Fixed formulation results in a lack of flexibility in prescribing for individual patients. o Don t assist in treating localised problems, such as sore throats etc. (Adams & Tan, 2012) Endeavour College of Natural Health endeavour.edu.au 19

20 Tablets o Manufacturing techniques revolving around tablet manufacturing has changed somewhat over the years. o Tablet machines can now produce around 1 million tablets per shift, all of considerable similarity. o In contrast, herbal tablets manufactured by hand cannot achieve such volume or consistency. Fully automated tablet compression machine Pill moulds Semi automated tablet machine Endeavour College of Natural Health endeavour.edu.au 20

21 Commercial Manufacturing As far as commercial manufacturing is concerned, according to GMP and QA procedures, tablets and capsules produced from specific machines and available for sale to the general public are required to conform to many different guidelines: o Friability: How tough the tablet is. It is put in a special machine that subjects the tablet to blunt gravity based impact. o Dissolution: Measuring the rate of drug release. Eg., Folate (B9) is a nutrient that requires dissolution testing to meet TGA requirements Endeavour College of Natural Health endeavour.edu.au 21

22 Commercial Manufacturing o Disintegration: A tablet/capsule must disintegrate when placed in a 37.7 degree liquid agitator within a specified time limit. o Thickness and measurements are within specified limits o Tablet/capsule weight is within specified limits. o No metal filings are trapped in the tablet from machinery Endeavour College of Natural Health endeavour.edu.au 22

23 Capsules o There a 2 main types of capsule: 1) Soft Gel based for liquids 2) Hard Capsules for dried herbs A common form of gelatine based capsule, which is a favourite dosage form for oil based preparations like fish and krill oil preparations. ( File:Codliveroilcapsules.jpg) Capsules can contain bitter tasting materials for easy ingestion. ( Endeavour College of Natural Health endeavour.edu.au 23

24 Soft Capsules o One piece gelatinous capsules are generally only able to be manufactured commercially, due to the expensive and specialised equipment required. o The substance being encapsulated is generally liquid or semi-liquid, in contrast to the dry material used in hard capsules. o The shell of soft-caps are based mainly upon gelatine, glycerol and water. o The liquid active ingredients are generally suspended in a fill material that helps in stabilising the product, such as soya oil or Macrogol 400. Endeavour College of Natural Health endeavour.edu.au 24

25 Hard Capsules o Hard capsules are generally two piece in manufacture and made from either gelatin or cellulose. o The latter being known as a VegeCaps are good for people who dislike animal based gelatinous products. o Hard caps generally encapsulate dry powdered material. o They are quite easy to manufacture at home, albeit can be quite time consuming. Endeavour College of Natural Health endeavour.edu.au 25

26 Advantages of Capsules o Capsules are a potent way of administering large doses of herbs, especially if EPE s (extract pro extracts with high DER powders such as 50:1) are utilised. o Capsules are convenient and portable, whilst also storing well. o Capsules bypass bitterness of other unpleasant tastes. o Devoid of alcohol, so appropriate where this solvent should be avoided. o Herbs such as capsicum or turmeric can be irritating to the mouth, so capsules and tablets are a good way of avoiding this occurring. Endeavour College of Natural Health endeavour.edu.au 26

27 Disadvantages of Capsules o Potential &/or real loss of constituents due to processing, such as spray-drying, powdering etc. o Contents are not as easily or efficiently absorbed as Liquid dosage forms o Excipients are ingested, which may prove detrimental (allergies etc also depends on manufacturer) o Relatively low dose of herb/liquid and fixed formulation results in a lack of flexibility in prescribing for individual patients. o Don t assist in treating localised problems, such as sore throats etc. Endeavour College of Natural Health endeavour.edu.au 27

28 Hard Capsule Formulation Ingredients: o Any dried herbal powder can be used Procedure: o o o o o Disinfect work area, equipment, hands Determine recipe / formula Weigh out powder to get allocated dosage, Use mortar & pestle or an electric coffee grinder if required to grind into a finer powder. If you have a capsule making kit the process is simplified and it enables you to make 50 capsules within a short period of time Syrian wooden herb crush/grind device (n.d.) Science Museum, London. qc2h47 Endeavour College of Natural Health endeavour.edu.au 28

29 Hard Capsule Formulation For manual filling: o Place herbal powder into a bowl. oget comfortable. o Scoop up herb using a pharmacy palette (or miniscule teaspoon), and pack (tamp) into the longer capsule end with a narrow chopstick o Close smaller end over larger end to seal the capsule o Place in an airtight container o Label and store correctly (Adams & Tan, 2012) 18 th century European Wooden Herb Mill Science Museum, London Endeavour College of Natural Health endeavour.edu.au 29

30 Making up Herbal - Hard Capsules oplease watch the video of making capsules o 01.mp4?dl=0 Endeavour College of Natural Health endeavour.edu.au 30

31 Using a Cap-M-Quick system 31 Endeavour College of Natural Health endeavour.edu.au 31

32 Gentle Herbal Laxative Capsules Ingredients: o Glycyrrhiza glabra powder 10 grams o Taraxacum off. (radix) powder 10 grams o Juglans nigra powder 10 grams Method: o Blend the powders together thoroughly o Set up Cap-M-Quick system and follow instructions Dose: o 2-3 capsules 3 x daily o Use as required (Caution: Avoid in pregnant or lactating women) Endeavour College of Natural Health endeavour.edu.au 32

33 Traditional Pill Manufacturing Prepare and disinfect all work areas and equipment. Ensure the herb is suitably pure and powdered as appropriate. Place the allocated amount of herbal material into a bowl and moisten with water or honey to form a sticky paste. Thicken the mixture with Slippery Elm if required to form a smooth paste much like bread dough consistency. Mould the tablets in balls or appropriate shapes. Can roll into cylinders and cut off pills or roll them into balls individually Coat with carob or slippery elm powder. Dry in the sun or very low (Gas- pilot flame) oven for several hours. Stored in an airtight container, they can last up to 12 months. 18 th century Pill Mould Brussels. Wellcome Collection Endeavour College of Natural Health endeavour.edu.au 33

34 Colic & Flatulent Pills Ingredients: o Cinnamomum verum powder o Elettaria cardomum powder o Foeniculum vulgare powder o Syzygium aromaticum powder o Zingiber officinale powder o Mentha x piperita oleum o Honey, water and Slippery Elm to make paste 10g 10g 10g 1g 1g 1-2 drops Endeavour College of Natural Health endeavour.edu.au 34

35 Colic & Flatulent Pills Procedure: o Disinfect work area and equipment o Wash hands thoroughly consider wearing gloves as this can get messy o Weigh out ingredients o Place in large SS bowl and mix thoroughly (if mixer available, use this) o Add honey & water to form a sticky paste o Add Slippery elm powder and constantly mix and knead until the consistency of dough (bread). oroll the mixture into tablet size shapes. ocoat in Carob/Slippery Elm. oweigh, and dry in an oven. oweigh again, then store in airtight container/label. Beecham s Pills England Endeavour College of Natural Health endeavour.edu.au 35

36 PILLS No 1 (Traditional Rx) Ingredients Lobelia seed 115g Cayenne 115g Valerian 115g Slippery elm 60g Dandelion extract 115g Procedure o Mix and roll in slippery elm. o Designed to relax the system gradually, so as not to produce vomiting. o Useful in all cases of constriction or fever, head-ache, liver complaint. o DOSE: From 1-4 at night, or as often as the nature of the case may require Endeavour College of Natural Health endeavour.edu.au 36

37 Tutorial Session Practical Session: o Using the recipes included in the lesson 1. Make the gentle laxative capsules 2. Make colic and flatulence pills Manufacturing Workbook: o Remember to write up your experience of the herbs and this manufacturing process. Endeavour College of Natural Health endeavour.edu.au 37

38 Preparation for next week o Read through your textbook pages in preparation for the lecture. o Read through your slides for Session 8 Endeavour College of Natural Health endeavour.edu.au 38

39 Suggested Readings British Herbal Medicine Association. (1996). British Herbal Pharmacopoeia. Bristol, UK: British Herbal Medicine Association. Fenner, B. (1888). Fenner s complete formulary and hand-book (6 th ed.). New York: B. Fenner. Retrieved from Green J. (2000). The herbal medicine-maker s handbook: A home manual NY: Crossing Press. (p ). Endeavour College of Natural Health endeavour.edu.au 39

40 References Adams, J., & Tan, E. (2006). Herbal manufacturing: How to make medicines from plants (pp.24-26). Preston, VIC: Northern Melbourne Institute of TAFE. Breakspear, I., (2014). Dosage calculations and extract equivalency in herbal medicine. Mills, S., & Bone, K. (2000). Principles and practice of phytotherapy, London, UK: Churchill Livingstone. Endeavour College of Natural Health endeavour.edu.au 40

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