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    Developing The Formulation: 18 Lacap, Dixie Mae N

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    Biyaya San Pedro
    This document discusses the development and production of capsules. It outlines key considerations for formulating capsules including ensuring accurate dosage, good bioavailability, ease of production and stability. The document discusses techniques for blending ingredients uniformly and achieving homogenous mixtures. It also covers selecting appropriate capsule sizes, filling capsules, sealing capsules, and cleaning and polishing capsules. The overall goal is to prepare capsules that deliver the intended dosage accurately and effectively.

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    © All Rights Reserved
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    Developing The Formulation: 18 Lacap, Dixie Mae N

    Uploaded by

    Biyaya San Pedro
    8 views38 pages
    This document discusses the development and production of capsules. It outlines key considerations for formulating capsules including ensuring accurate dosage, good bioavailability, ease of production and stability. The document discusses techniques for blending ingredients uniformly and achieving homogenous mixtures. It also covers selecting appropriate capsule sizes, filling capsules, sealing capsules, and cleaning and polishing capsules. The overall goal is to prepare capsules that deliver the intended dosage accurately and effectively.

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    This document discusses the development and production of capsules. It outlines key considerations for formulating capsules including ensuring accurate dosage, good bioavailability, ease of production and stability. The document discusses techniques for blending ingredients uniformly and achieving homogenous mixtures. It also covers selecting appropriate capsule sizes, filling capsules, sealing capsules, and cleaning and polishing capsules. The overall goal is to prepare capsules that deliver the intended dosage accurately and effectively.

    Copyright:

    © All Rights Reserved
    Download as PDF, TXT or read online from Scribd
    Download as pdf or txt
    8 views38 pages

    Developing The Formulation: 18 Lacap, Dixie Mae N

    Uploaded by

    Biyaya San Pedro
    This document discusses the development and production of capsules. It outlines key considerations for formulating capsules including ensuring accurate dosage, good bioavailability, ease of production and stability. The document discusses techniques for blending ingredients uniformly and achieving homogenous mixtures. It also covers selecting appropriate capsule sizes, filling capsules, sealing capsules, and cleaning and polishing capsules. The overall goal is to prepare capsules that deliver the intended dosage accurately and effectively.

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    © All Rights Reserved
    Download as PDF, TXT or read online from Scribd
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    DEVELOPING THE

    FORMULATION
    18 LACAP, DIXIE MAE N.
    What is
    the GOAL?

    To prepare a capsule with:
    > Accurate dosage
    > Good bioavailability
    > Ease of filling &
    production stability
    > Elegance



    DRY FORMULATIONS
    - active and inactive components must be blended
    thoroughly to ensure a uniform powder mix for the fill.

    LOW-DOSE DRUGS
    Care in blending
    Lack of homogeneity in blending may result in
    significant therapeutic consequences.
    PRE-FORMULATION STUDIES
    To determine:
    if all the formulations bulk powders may be
    effectively blended together.
    require reduction of particle size
    any other processing to achieve homogeneity
    DILUENT/FILLER

    added to the
    formulation to
    produce the proper
    capsule fill
    volume
    provides bulk and
    cohesion to the
    powder
    beneficial in
    transferring
    powder blends into
    capsule shells
    DISINTEGRANTS
    > Assist the breakup and distribution of the
    capsule

    s content in the stomach



    HOW TO ACHIEVE UNIFORM DRUG
    DISTRIBUTION?
    *Density and particle of the drug and nondrug components
    must be similar

    Particle size
    may be reduced
    by:
    MILLING
    MICRONIZATION
    MILLED POWDER
    Milling process
    particles ranging from
    50 to 1000 micrometer
    blended effectively for
    uniform distribution
    throughout a powder mix
    ONLY IF the DRUG DOSAGE
    is 10 mg or GREATER
    MICRONIZED
    POWDER
    Micronization Process
    DRUG DOSAGE:less than 10 mg
    PARTICLE SIZE:1-20 um(mcm)
    for lower dose or smaller
    particles
    HIGH SPEED AUTOMATED
    EQUIPMENT
    LUBRICANT/GLIDANT
    enhances flow properties of powder
    mix
    aids in high-speed automated
    equipment (industrial scale
    production)
    Magnesium Stearate
    (lubricant) for it

    s waterproofing
    characteristics
    can

    t be penetrated by the
    gastrointestinal fluids
    delays drug dissolution & absorption
    useful for modied release capsule
    SODIUM LAURYL
    SULFATE
    surface active
    agent
    facilitates
    wetting by the GI
    fluids
    is added to aid
    drug dissolution
    and absorption
    delay
    DISINTEGRATION
    AGENTS
    facilitates breakup and
    distribution of the
    capsule

    s content
    aids GI fluids to
    displace the air around
    the powder for the
    penetration to occur
    and drug dispersion and
    dissolution to start
    microcrystalline cellulose
    Why do we INSERT CAPSULES/
    TABLETS inside capsules?
    to separate chemically
    incompatible agents
    to add pre-measured
    amounts of potent drug
    subs.
    rather than weighing a potent
    drug
    COATED PELLETS
    (industrial scale)
    designed for
    modified release
    drug delivery
    commonly placed in
    capsule shells
    DICLOMAX
    diclofenac
    SLOW RELEASE
    GELATIN CAPSULES
    unsustainable for
    aqueous liquids
    water softens
    gelatin, causing
    leakage
    GELATIN CAPSULES
    FIXED OR VOLATILE OIL
    do not interfere with gelatin shell
    stability
    LOCKING GELATIN CAPSULES/ Capsule
    sealed with a THIN COAT OF GELATIN
    WET MASS/PASTE
    fixed/volatile oil with INERT POWDER
    placed in caps. in usual manner
    ex POLYETHER
    EUTECTIC MIXTURES
    mixtures of agents that have a propensity
    to liquefy when admixed
    mixed with a DILUENT/ADSORBENT to
    separate interacting agent & to absorb
    any liquefied material that may form
    LARGE SCALE CAPSULE
    PRODUCTION
    liquids are placed in SOFT GELATIN
    CAPSULES that are sealed during filling &
    manufacturing
    IND. VS COMMUN.
    slight loss in fill material during
    preparation & capsule filling will not
    materially affect an industrial sized
    batch
    slight loss of powder could result in an
    inadequate quantity to fill the last
    capsule
    CP can calculate in excess of 1 or two capsules more than what is
    required to ll the capsule EXCEPT when dealing with capsules
    containing controlled subs!

    amount of drug used & called for must STRICTLY COINCIDE
    SELECTING THE
    CAPSULE SIZE
    18 LACAP, DIXIE MAE N.
    DURING PRODUCT
    DEVELOPMENT
    FORMULATION
    REQUIREMENTS
    dose of the active ingredient
    density and compaction
    characteristics
    Diluents are added when dose of the
    drug is inadequate to fill the volume
    of the capsule body
    GUIDE IN SELECTING
    CAPSULE SIZE
    density & compaction characteristics
    of a capsule

    s active & inactive


    components
    comparison to other similar materials
    prior experiences
    HARD GELATIN
    CAPSULES
    encapsulates 65 mg- 1g
    SMALLEST CAPSULE(#5)
    65 mg or more
    SELECTING THE
    CAPSULE SIZE
    (extemporaneous) best capsule size
    determined by TRIAL
    SMALLEST PROPERLY FILLED capsule
    body filled with the drug mixture,
    not the cap
    Easy Method to Select
    the Proper Capsule Size
    weigh ing. for the REQUIRED # OF
    CAPSULES
    place powder in GRADUATED
    CYLINDER(take note of volume)
    divide volume by the # of capsules
    compare the vol with the approx. on
    the table and select the caps. size
    that will accommodate the powder
    if caps is to big

    caps size(ml) x #caps = FINAL
    VOLUME

    then just add diluent to attain
    the nal volume
    TETRACYCLINE CAPSULES
    ACTIVE ING: Tetracycline
    HCl (250 mg)
    FILLER: Lactose
    LUBRICANT: Magnesium
    Stearate
    CAPS COLORANT: FD&C
    YELLOW#6
    CAPS OPAQUANT:Titanium
    dioxide
    FILLING HARD CAPSULE
    SHELLS
    18 LACAP, DIXIE MAE N.
    PUNCH METHOD
    amount of powder packed into the
    capsule depends on the degree of
    compression
    should punch each capsule in the same
    manner and weigh the product after
    capping
    NONPOTENT drug - 1st filled capsule
    is weighed
    POTENT drug - EACH CAPS is weighed
    such weighing protects
    against uneven lling of
    capsules and premature
    exhaustion or underuse of
    powder
    PUNCH METHOD
    HAND-OPERATED FILLING
    MACHINE
    24-300 caps per machine

    200-2000 caps per hour
    MACHINE DEVELOPED
    FOR INDUSTRIAL USE
    automatically separate
    th caps from the empty
    capsules
    fills the bodies
    scrapes off the excess
    powder
    replace the caps
    seals the capsiles
    cleans the outside caps
    165000 caps per hour

    ACCURACY OF DRUG DOSGE IS
    VERIFIED THROUGH

    AYTOMATED IN PROCESS
    SAMPLING & ANALYSIS

    CAPSULE SEALING
    18 LACAP, DIXIE MAE N.
    TAMPER EVIDENT CAPSULES
    KAPSEALS, PARKE-
    DAVIS
    seals with a colored
    band of gelatin
    if removed, the band
    cannot be restored
    without expert
    releasing with gelatin
    HEAT-WELDING
    PROCESS
    fuses cap to the
    body through the
    double wall
    thickness at their
    juncture
    distinctive ring
    around the capsule
    where heat welded
    TAMPER EVIDENT CAPSULES
    THERMAL COUPLING

    uses a liquid
    wetting agent that
    lowers the melting
    point in the contact
    areas of the cap and
    body, and then
    thermally bonds the
    two parts using low
    temp (40C-45C)
    CAPSULE SEALING
    INDUSTRIAL CAPSULE SEALING MACHINES
    60000 to 150000 gelatin banded, heat
    welded or thermally coupled capsules
    PER HOUR
    EXTEMPORANEOUSLY
    seal by lightly coating the inner
    surface of the cap with a warm
    gelatin soln then immediately pour to
    placement on the filled capsule body.
    CLEANING AND
    POLISHING CAPSULES
    18 LACAP, DIXIE MAE N.
    CLEANING & POLISHING CAPSULE
    MACHINE

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