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BENGAL SCHOOL OF TECHNOLOGY

(A College of Pharmacy)
TOPIC-SUSTEN RELEASE & CONTROLLED RELEASE DOSAGE
FORM CONCEPTS AND APPROACHES

PRESENTED BY,
NAME –INDRANATH SANTRA
ROLL N0-19320323006
MASTER OF PHARMACY(PHARMACEUTICS)
1st YEAR, 1st SEMESTER
SUBJECT NAME– DRUG DELIVERYSYSTEM (MPT1062)
INTRODUCTION

WHAT IS DRUG DELEVERY SYSTEM?


The term "drug delivery systems" refers to technology utilized to present the drug to the
desired body site for drug release and absorption.
WHAT IS SUSTAINED RELEASE FORMULATIONS?
SRF Is describes the slow release of a drug substances from a dosage form to maintain
the therapeutic responses for extended period that is for about 8-12 hours of time.
WHAT IS CONTROLLED RELEASE FORMULATIONS?
These are the formulations which delivers the drug at a predetermined rate, for locally or
systematically, for a specified period of time.

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DIFFERENCE BETWEEN CONTROLLED
RELEASE AND SUSTAINED RELEASE
FORMULATIONS
Sustained release formulations Controlled release formulations
1. Constitutes dosage form that provides medication 1. Constitutes dosage form that maintains constant
over a extended period of time. drug levels in blood or tissue.

2.SRF'S generally do not follows zero order kinetic 2. Maintains constant drug levels in the blood in the
pattern. target tissue usually by releasing the drug in a zero
order kinetic pattern.

3. Usually do not contain mechanisms to promote 3. It contains methods to promote localization of the
localization of the drug at active site. drug at active site.

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CONCEPT OF SUSTAINED RELEASE
FORMULATIONS
The of concept of sustained release formulation can be divided into two considerations
i.e.,
a. Release rate
b. Dose consideration
RELEASE RATE:
Here, K₁= Drug release, Ka= Drug absorption
Ke= Drug elimination.

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concentration-time profile from conventional multiple dosing and single
doses of sustained release delivery formulations.

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ADVANTAGES

1. Reduction in dosing frequency.


2.Enhanced patient convenience and compliance due to less frequent drug
administration.
3. Reduction in adverse effects (both systematic and local) of potent drugs in patients.
4. Reduction in health care costs.
5. Improved efficiency of treatment.
6. Reduces nursing and hospitalizing time.
7.Reduction in blood level fluctuations of the drug,thus the better management of
disease.
8. Maximum bioavailability with minimum dose.
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DISADVANTAGES

1. Possibility of dose dumping due to food, physiologic or formulation variables or


grinding of oral formulations by patients and thus increased risk of toxicity.
2. Reduced potential for dose adjustment of drugs normally administered in varying
strengths.
3. Cost of single unit dosage form is higher than that of conventional dosage form.
4. Increase potential for first pass metabolism.
5. Requirement of additional patient education for proper medication.
6. Poor in vitro and in vivo correlation.

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FACTORS INFLUENCING SUSTAINED OR
CONTROLLED RELEASED FORMULATIONS
There are mainly six factors influences the performances of sr or cr formulations those
are as follows:
1. Drug properties
2. Route of drug delivery
3. Target sites
4. Acute or chronic therapy
5. The disease
6. Patients

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1. Drug properties :
The physiochemical properties of a drug, Including stability, solubility, partitioning
characteristics, charge, and protein binding propensity, play a dominant role in the
design and performance of controlled release systems.
2. Route of drug delivery:
The area of the body in which drugs will be applied or administered can be restrictive on
the basis of technological achievement of a suitable controlled release mechanism or
device.
At times, the drug delivery system, in certain routes of administration, can exert a
negative influence on drug efficacy, particularly during chronic administration, and
hence other routes of administration should be considered.

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3. Target sites:
In order to minimize unwanted side effects, it is desirable to maximize the fraction of
applied dose reaching the target organ or tissue. This can be partially achieved by local
administration or by the use of carriers.
However, the absorptive surfaces of most routes are impermeable to macromolecules or
other targeted delivery systems, thereby necessitating either intravascular or intra
arterial administration.
4. Acute or chronic therapy:
Consideration of whether one expects to achieve cure or control of a condition and the
expected length of drug therapy are important factors in designing controlled release
systems.

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PHYSICOCHEMICAL APPROACHES FOR THE
SR/CR RELEASE FORMULATIONS
AQUEOUS SOLUBILITY AND PKA

PARTITION COREFFICIENT AND MOLECULAR SIZE

DRUG STABILITY

BINDING

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PHARMACEUTICAL APPROACHES FOR SR/CR
RELEASE FORMULATIONS
Reservoir Devices :
Reservoir Devices are those in which a core
of drug is surrounded by polymeric membrane.

The nature of membrane determines the rate of


release of drug from system.The process of
diffusion is generally described by a series of
equations governed by Fick’s first law of diffusion.

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Matrix devices:
A matrix device, as the name implies, consists
of drug dispersed homogenously throughout a
polymer.

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Ions Exchange Based SR/CR Formulations:
Ion-exchange systems generally use resins composed
of water insoluble cross-linked polymers. These polymers
contain salt-forming functional groups in repeating
positions on the polymer chain.
The drug is bound to the resin and released by
exchanging with appropriately charged ions in
contact with the ion-exchange groups.

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REFERENCES

1. Robinson, J. R., Lee V. H. L, Controlled Drug Delivery Systems, Marcel Dekker, Inc.,
New York, 1992.

2. Biopharmaceutics and pharmacokinetics a treatise by D.M. BRAHMANKAR,


SUNIL.B. JAISWAL.

3.Korsemeyer R.W., Gumy R., Doelker E., Buri P., Peppas N.A. Mechanisms of solute
release from porous hydrophilic polymers. Int. J. Pharm. 1983;15:1249–1253.

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Thank You

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