EXTRUSION & SPHERIZATION-

IN NOVEL DRUG DELIVERY

SYSTEMS

PRESENTED BY: JAVERIA AJAZ

TEHREEM ANWAR
SHAISTA GULL
KAINAT NADEEM
AMINA MUZAFFFAR
AMINA MUZAFFAR
INTRODUCTION

Extrusion spheronization is a multiple process of wet mass

extrusion followed by spheronization to produce uniform
size spherical particles, called as spheroids, pellets, beads
or matrix pellets depending upon the material as well as
process used for extrusion spheronization .
Extrusion spheronization process has gained world wide
attention because it is a simple and fast processing
technology .
Any pharmaceutical products utilize pellets or beads as a
drug delivery system can be effectively produced by the
extrusion spheronization process
HOT MELT EXTRUSION [HME]
HOT MELT EXTRUSION [HME]

• Researchers have investigated a new modified method for

preparing matrix pellets for controlled release drug
delivery system to overcome the disadvantages associated
with wet mass extrusion and spheronization process.
• Hot Melt Extrusion (HME) is a method where a thermal
agent softens or gets melted during the process to obtain
matrix pellets .
The HME offers following advantage over a wet mass extrusion and
spheronization method, and are as follows, ·
It is a simple, efficient, continuous process that requires fewer
processing stages. ·
HME is continuous process as it does not require a lengthy drying
stage since it does not involve addition of water or other solvent. ·
The absence of water may prevent drug degradation as many drugs
are unstable in presence of water. ·
It produces a spherical shape pellets with narrow range particle size
distribution. ·
Reduce the loss of coating material during the coating process
associated with wet mass extrusion process.
It is a convenient technology for preparation of solid dispersion
and solid solution for delivery of poorly soluble drug as it offers
a advantage of solvent free formulation of solid dispersion.

Pellet formation by this technique produces more spherical

pellets and offers more advantages than other pelletization
process. In addition, hot melt extrusion method has provided a
new platform to produce spherical particles of drugs which are
not stable or having compatibility problem in presence of
solvents

Extrusion Spheronization –A Review Shyamala Bhaskaran1 * and Lakshmi.P.K.2 1Dept. of Pharmaceutics,Agnihotri

College of Pharmacy, Wardha,Maharashtra, India 2Department of Pharmaceutics,G.Pulla Reddy College of
Pharmacy,Mehdipatnam,Hyderabad, AP,India
• It helps to mask the bitter taste of the active ingredient. ·
SHAISTA GULL
HME process is divided in four sections that are
• Feeding of extruder
• Conveying of mass[mixing and reduction of particle size].
• Flow through the die
• Exit from the die and down stream processing
PRODUCT CHARACTERISTICS OF THE
PELLETS:

• Round pellets.
• Good flow behavior.
• Easy to dose.
• Good dispensability.
• Compact structure.
• High bulk density and
• Dense surface.
FORMULATION 

•Active pharmaceutical ingredients

•Binder
•Granulating fluid
•Spheronizing enhancer
•Filler
•Plasticizer
•Lubricant
•Separating agent
•Surfactants
•pH enhancer
•Release modifiers
•Flavoring agents
TEHREEM ANWAR
APPLICATIONS:

• Pellets have varied applications in a number of industries and an innovative

use of it’s could achieve maximum profitability.
 Taste masking:
• Pellets are ideal for products where perfect abatement of taste is required. The
pelletization technique solves difficult taste masking problem while maintaining a
high degree of bioavailability due to their high surface area, especially for oral
products.
• Furthermore, because of the special design of the manufacturing process, dust
fractions that representing an uncoated fragments which could cause taste
problems are absent in pellets. Many products, such as antibiotics
(clarithromycin, roxithromycin and cephelexin) and anti-inflammatory drugs with
a bitter taste, can now be formulated in products with high patient compliance,
thus increasing the sales potentially in the pharmaceutical markets for the
product
• 2. Immediate release:
• Administering drugs in pellet form leads to an increased surface area as
compared to traditional compressed tablets and capsules which would
considerably reduce the disintegration time and have the potential for use in
rapidly dispersible tablets.
• Sustained release:
• The pellet form provides a smoother absorption profile from the
gastrointestinal tract as the beads pass gradually through the stomach into the
small intestine at a steady rate. Pellets are being increasingly used in the
manufacture of sustained release dosage form of drugs. The advantages of the
dosage form is well known
 Chemically Incompatible Products:
• At times such ingredients are required to be delivered in a single dose. In the
compressed tablet dosage form separate tablets would have to be
administered, but the pellets can be administered in a single capsule.
• Varying dosage without reformulation:
• Pellets have excellent flow properties, due to this, they can be conveniently
used for filling capsules and the manufacturer can vary the dosage by varying
the capsule size without reformulating the product
• The process of wet extrusion, followed by extrusion-spheronization, is used to
produce a wide variety of engineered, controlled release drugs. These solid
dosage forms are mostly in the form of tablets or capsules containing high
levels of an Active Pharmaceutical Ingredient (API).
• Ram extruders are preferred during formulation development because they
are designed to allow for measurement of the rheological properties of
formulations.
• The twin-screw extrusion used for the continuous production of solid dosage
forms, i.e., useful for the wet granulation of alpha-lactose monohydrate or
microcrystalline cellulose and produces high shear granulation.
• Pharmaceutical Applications for Extruders and Spheronizers
• Controlled release pellets for encapsulation
• Delayed release enteric coated pellets
• Sustained release pellets
• Multi-particulate systems
• Multi-unit erosion matrix pellets
• Pellets for special tabletting applications
• Immediate release pellets for sachets
• References
•  
• PelletizationTechniques,Josephine Lay Peng Soh Novartis Singapore
Pharmaceutical Manufacturing Pte Ltd., Singapore,Srimanta Sarkar Paul Wan
SiaHeng Celine Valeria Liew GEA-NUS Pharmaceutical Processing Research
Laboratory, Department of Pharmacy, National University of Singapore,
Singapore
• http://ijpsr.com/bft-article/pelletization-technology-a-quick-review/?view=fullt
ext
• https://www.capsugel.com/biopharmaceutical-technologies/extrusion-sphero
nization
• http://dx.doi.org/10.13040/IJPSR.0975-8232.2(6).1337-55
JAVERIA AJAZ
SELF EMULSIFYING DRUG DELIVERY
SYSTEM: A NOVEL APPROACH
• SEDDS are isotropic mixtures of drug, oil/lipid, surfactant,
and/ or cosurfactant, which form fine emulsion/lipid
droplets, ranging in size from approximately 100 nm
(SEDDS) to less than 50 nm for self-microemulsifying drug
delivery systems (SEDDS), on dilution with physiological
fluid.
• The drug, therefore, remains in solution in the gut,
avoiding the dissolution step that frequently limits the
absorption rate of hydrophobic drugs from the crystalline
state .
• Potential advantages of these systems include;
• Reduction in dose due to enhanced oral bioavailability,
• More consistent temporal profiles of drug absorption,
• Selective targeting of drug(s) toward specific absorption window in GIT,
• Protection of drug(s) from the hostile environment in gut.
• Control of delivery profiles.
• Reduced variability including food effects. 7. Protective of sensitive drug
substances.
• Increased drug loading capacity.
• Liquid or solid dosage forms.
• https://www.researchgate.net/profile/Dr_Lalit_Singh2/publication/258026600
_Self_Emulsifying_Drug_Delivery_System_A_novel_approach/links/02e7e526
a3ea8b17e1000000.pdf
MULTIPARTICULATES DRUG DELIVERY
SYSTEMS: A REVIEW

• Pharmaceutical research and development are increasingly focusing on delivery

systems which enhance desirable therapeutic objectives while minimising side
effects. Recent trends indicate that multiparticulate drug delivery systems are
especially suitable for achieving controlled and delayed release oral formulations
with low risk of dose dumping. These oral multiparticulate drug delivery systems
offer biopharmaceutical advantages with respect to predictable and even
distribution and transportation in the gastro-intestinal tract. Pelletization is novel
drug delivery system that converts fine powder particles into pellets and it is
usefull in order to develop a site-specific drug delivery system. There are different
techniques in the preparation of pellets. Consequently, multiparticulate drug
delivery systems provide tremendous opportunities for designing new controlled
and delayed release oral formulations, thus extending the frontier of future
pharmaceutical development.
KAINAT NADEEM
• ADVANTAGES OF MULTIPARTICULATES (PELLETS)
• Avoidance of the dose dumping
• Gastric emptying is faster.
• Performance is less dependent on nutritional state as multiparticulates are
sufficiently small and can be evacuated through pylorus during digestive
phase.
• Shows improved reproducibility of transit time and high degree of dispersion
in digestive tract.
• Better distributed and less likely to cause local irritation.
• Improved stability, patient comfort and compliance.
• Achieve unique release pattern.
• Extend patent protection, globalize product and overcome competition
• https://pdfs.semanticscholar.org/c71f/f881eb14256f3311c4d976a7644056404
528.pdf
ORAL CONTROLLED-RELEASE DOSAGE
FORMS

• The use of pellets as a vehicle for drug delivery at a controlled rate has
recently received significant attention. Applications are found not only in the
pharmaceutical industry but also in the agribusiness (such as in fertilizer and
fish food) and in the polymer industry. There are numerous advantages
offered by multiple unit dosage forms.
• Pellets disperse freely in the gastrointestinal (GI) tract, and so they invariably maximize
drug absorption, reduce peak plasma fluctuation, and minimize potential side effects
without appreciably lowering drug bioavailability10.
• •Pellets also reduce variations in gastric emptying rates and overall transit times. Thus
inter- and intra-subject variability of plasma profiles, which is common with single unit
regimens, is minimized11.
• •High local concentration of bioactive agents, which may inherently be irritative or
anesthetic, can be avoided12.
• •When formulated as modified-release dosage forms, pellets are less susceptible to
dose dumping than the reservoir-type, single unit formulations12.
• •Better flow properties, narrow particle size distribution, less friable dosage form and
uniform packing13, 14.
• The pellets offer advantages to the manufacturer because they provide an
ideal shape [low surface area to volume ratio] for the application of film
coating. They can also be made attractive because of the various shades of
colour that can be easily imparted to them during the manufacturing process,
thus enhancing the product elegance and organoleptic properties 12.
• •Pellets also offer the advantage of flexibility for further modifications, such as
compression to form tablets or coating to achieve the desired dosage-form
characteristics15.
• Pellet-forming mechanism according to: (a) Rowe36 – I. Cylinder; II. Cylinder with
rounded edges; III. Dumb-bell; IV. Ellipse; V. Sphere. (b) Baert – I. Cylinder; II. Rope; III.
Dumb-bell; IV. Sphere with a cavity outside; V. Sphere.
• https://www.sciencedirect.com/science/article/pii/S1461534799001364