Transcript Tablets and Suppositories

TABLETS AND SUPPOSITORIES
Dr. Basavaraj K. Nanjwade
M. Pharm., Ph. D
Department of Pharmaceutics
Faculty of Pharmacy
Omer Al-Mukhtar University
Tobruk, Libya.
E-mail: [email protected]
2014/06/17
Faculty of Pharmacy, Omer Al-Mukhtar University,
Tobrum, Libya.
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CONTENTS
Tablets
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Introduction (properties of tablet granulation)
Tablet additives and components
Disintegrant
Colorant
Flavor and sweeteners
Preparation of components for compression
Forms of compressed tablets
Processing problems
Evaluation of tablets
Tablet coating (sugar coat, film coat)
2014/06/17
Faculty of Pharmacy, Omer Al-Mukhtar University,
Tobrum, Libya.
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Introduction
(Properties of Tablet Granulation)
• Granulation is the process in which primary powder
particles are made to adhere to form larger multiparticle entities called granules.
• Granulation normally commences after initial dry
mixing of the necessary powdered ingredients so that
a uniform distribution of each ingredient through the
mix is achieved.
• After granulation, the granules will either be packed
(when used as a dosage form) or they may be mixed
with other excipients prior to tablet compaction.
2014/06/17
Faculty of Pharmacy, Omer Al-Mukhtar University,
Tobrum, Libya.
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Tablet additives and components
• A study of the physical properties of drug molecules
is a prerequisite for product formulation and leads to
a better understanding of the relationship between a
drug’s molecular and physicochemcial properties and
its structure and action.
• These properties come from the molecular bonding
order of the atoms in the molecule and may be though
of as either additive or constitutive (dependent on the
structural arrangement of the atoms within the
molecule).
2014/06/17
Faculty of Pharmacy, Omer Al-Mukhtar University,
Tobrum, Libya.
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Disintegrant
• The substance which are added in the tablet formulation to
ensure disintegration of the tablets into smaller particles when
swallowed are called Disintegrant or Disintegrating Agents.
• These are added into the formulation of or oral tablets or
sublingual tablets.
• When the medicament is insoluble in water a disintegrating
agent is needed.
• Disintegrating agents act in three ways:
1. By swelling e.g. potato starch, maize starch, wheat starch.
2. By producing effervescence e.g. sodium bicarbonate
3. They melt at body temperature e.g. cocabutter
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Faculty of Pharmacy, Omer Al-Mukhtar University,
Tobrum, Libya.
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Colorant
• Colours of aproved certified F. D. and C, dyes are
used.
• The colours are used to improve the elegance of the
tablet.
• The colours are added to the solution of the
granulating agent or these are mixed with other
ingredients before granulation.
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Tobrum, Libya.
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Flavours
• Flavours are included in lozenges, effervescent tablets
and chewable tablets.
• Flavours are volatile oils and hence they are added
into the granules just before compression of tablets.
• Flavouring agent is dissolved in organic solvent and
the solution is sprayed on the granules.
2014/06/17
Faculty of Pharmacy, Omer Al-Mukhtar University,
Tobrum, Libya.
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Sweeteners
• Sweeteners are agents are used to improve the taste of
tablets.
• These are used in lozenges and chewable tablets.
• Artificial sweetening agents like saccharin and
cyclamates, are not used nowadays.
• Sucrose, lactose and mannitol are some of the
commonly used sweetening agents.
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Faculty of Pharmacy, Omer Al-Mukhtar University,
Tobrum, Libya.
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Preparation of components for
compression
1. Weighing of the ingredients
2. Mixing the powdered ingredients and excipients
3. Converting the mixed ingredients into granules
4. Diluents
5. Granulating agents
6. Binding agents
7. Disintegrating agents
8. Lubricants
9. Adsorbents
10. Colouring agents, Flavouring agents and Sweetening agents.
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Faculty of Pharmacy, Omer Al-Mukhtar University,
Tobrum, Libya.
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Forms of compressed tablets
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Tablets are prepared by the compression method and are
hence called the “Compressed Tablets”
Multilayered tablets
Sustained action tablets
Enteric coated tablets
Sugar coated tablets
Film coated tablets
Chewable tablets
Buccal tablets Sublingual tablets
Lozenge tablets and traches
Dental cones
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Faculty of Pharmacy, Omer Al-Mukhtar University,
Tobrum, Libya.
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Processing problems
• The following defects may occur during the
compression of granules into tablets.
1. Capping
2. Picking and sticking
3. Mottling
4. Weight variation
5. Hardness variation
6. Double impression
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Faculty of Pharmacy, Omer Al-Mukhtar University,
Tobrum, Libya.
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Evaluation of tablets
• The following test should be carried to maintain the
quality control of tablets:
1.
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3.
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Shape of tablets
Appearance
Content of active ingredient in tablets
Uniformity of weight
Disintegration test for tablets
Dissolution test for tablets
Mechanical strength
Friability test.
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Faculty of Pharmacy, Omer Al-Mukhtar University,
Tobrum, Libya.
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Tablet coating
(Sugar coat)
• Sugar coating is done by the pan coating method.
• It is one of the oldest arts to mask the unpleasant flavours
and tastes of medicaments, but nowadays sugar coating of
tablets is done for improving its aesthetic value.
• The various stages in the sugar coating process are:
1.
2.
3.
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6.
Sieving
Sealing
Subcoating
Syrup coating
Finishing
Polishing
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Tobrum, Libya.
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Tablet coating
(Sugar coat)
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Tobrum, Libya.
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Tablet coating
(Film coat)
• In this case the tablets are coated by a single or mixture of
film forming polymers, such as, hydroxypropyl
methylcellulose,
hydroxyethyl
methyl
cellulose,
carbowax, polyethylen glycol 400 etc.
• The polymer is dissolved in some volatile organic solvent
and is sprayed over the tablets in a rotating pan.
• The process is continued till a uniform good film is
formed over the tablets.
• Film coating is also used to make the tablets water proof
before the sugar coating.
• Film coating can be enteric or non-enteric
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Faculty of Pharmacy, Omer Al-Mukhtar University,
Tobrum, Libya.
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CONTENTS
Suppositories
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Introduction
Advantages rectum physiology
Drug absorption form rectum
Factors affecting formulation of suppositories
Classification of bases
Choice of adjuvant
Suppository production
Quality control
References
2014/06/17
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Tobrum, Libya.
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Introduction
1. The patient have a problem with their gastrointestinal tract, is
nauseous or is postoperative.
2. Several categories of patients, i.e. the very young, the very
old or the mentally disturbed, may more easily use the rectal
than the oral route.
3. The drug under consideration is less suited for oral
administration.
4. The drug may be insufficiently stable at the pH of the GI
tract, or susceptible to enzymatic attack in the GI tract or
during the first passage of the liver after absorption.
5. The formulation into suppositories of certain drugs that are
candidates for abuse, as in suicide, has also been considered.
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Definition of Suppositories
• Suppositories are solid dosage form of medicament for
insertion into body cavities other than mouth. They may
be inserted into rectum, vagina or nasal cavity.
• The medicament is incorporated into the supository base
and the product is formulated in such a way that they will
either melt or dissolve in the body cavity fluid to release
the medicament.
• Suppositories are available in different shapes, sizes and
weights. Suppositories are used to produce local, systemic
and mechanical action.
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Advantages rectum physiology
• Under normal circumstances the rectum is empty;
filling provokes a defection reflex, which is under
voluntary control.
• Data comparing drug absorption from freshly
prepared and aged, more viscous suppositories
suggest that there is enough motility to provoke the
spreading even of rather viscous suppositories.
• Suppositories are inserted in to rectum to promote
evacuation of the bowel.
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Faculty of Pharmacy, Omer Al-Mukhtar University,
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Advantages of Suppositories
1. These can be easily administered to children, old
persons and to unconscious patients who cannot
swallow the drug easily.
2. These are inserted into body cavity to produce local
effect of the medicament incorporated in the base.
3. These are inserted into the rectum to exert a direct
and rapid action on the rectum.
4. These are inserted into the rectum to promote
evacuation of the bowel.
5. Suppositories are unit dosage form of drugs
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Drug absorption form rectum
• Blood supply, especially venous drainage, is
important for the understanding of drug absorption.
• Recent investigation have shown that avoiding the
first passage through the liver is possible, but the
extent of this effect cannot be generalized, as it will
depend on the actual part of the rectum through
which the drug is absorbed
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Faculty of Pharmacy, Omer Al-Mukhtar University,
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Factors affecting formulation
of suppositories
1. Drug solubility in vehicle: The drug solubility in the vehicle
is of special interest from the biopharmaceutical point of
view.
2. Surface properties: The surface properties of drug particles
are also important as these particles will be transferred from
one phase to another.
3. Particle size: The particle size of the drug is an important
parameter, both technologically and biopharmaceutically.
4. Amount of drug: A complicating factor is the amount of
drug present in a suppository. If the number of particles
increases, this would also increase the rate to form
agglomerates.
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Faculty of Pharmacy, Omer Al-Mukhtar University,
Tobrum, Libya.
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Classification of bases
• Suppository bases can be broadly classified into three
categories:1. Fatty bases eg. Theobroma oil
2. Water soluble and water miscible bases eg.
Glycero-gelatin
3. Emulsifying bases eg. Witepsol, massa estarinum,
massuppol.
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Faculty of Pharmacy, Omer Al-Mukhtar University,
Tobrum, Libya.
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Choice of adjuvant
• Colloidal silicon oxide or aluminium monostearate,
both approximately 1-2%
• The addition of lecithin is a worthy possibility when
high amounts of solid drug are used.
• Surfactans act as wetting agents
• Surfactants may also act as ‘deglomerators’ which
may prevent the formation of cake in the melting
suppository, which in turn would certainly slow down
the drug release.
2014/06/17
Faculty of Pharmacy, Omer Al-Mukhtar University,
Tobrum, Libya.
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Suppository production
• Suppositories are manufactured both on a small scale
in batches of 10-20 and on a (semi) automatic scale in
batches up to 20 000 per hour.
• Essentially the mode of manufacture is similar in both
cases, and involves melting of the vehicle, mixing the
drug and the molten vehicle, dispensing in a former
cooling to solidify and, if necessary, packing in the
final container.
• This includes a number of technological processes for
which the relevant theory should be considered.
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Tobrum, Libya.
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Suppository production
• The suppositories are prepared by any of the
following methods:1. Rolling method
2. Hot process or fusion method
3. Cold compression method
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Tobrum, Libya.
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Suppository production
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Rolling method: It is an ancient method of preparing the
suppositories. The suppository base is rolled and then desired
shape is given with the hand. The method is not used nowadays.
Hot process or fusion method: This method is commonly used
in the preparation of suppositories for dispensing purposes. The
suppository base is melted, the medicament is incorporated in it
and filled in lubricated mould. On cooling, suppositories are
formed which are removed from the suppository mould.
Cold compression method: The method is useful for
thermolabile and insoluble drugs because heating and stirring of
the base with medicament is not required.
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Faculty of Pharmacy, Omer Al-Mukhtar University,
Tobrum, Libya.
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Quality control
• A list of properties that should be controlled.
1. Appearance (odour, colour, surface condition and shape)
2. Weight
3. Disintegration
4. Melting (dissolution) behaviour
5. Mechanical strength
6. Content of active ingredient
7. Release
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Faculty of Pharmacy, Omer Al-Mukhtar University,
Tobrum, Libya.
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THANK YOU
e-mail: [email protected]
2014/06/17
Faculty of Pharmacy, Omer Al-Mukhtar University,
Tobrum, Libya.
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