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Mrdds

The document discusses the physicochemical factors influencing sustained and controlled drug delivery systems, highlighting their advantages such as improved patient compliance and reduced side effects, as well as disadvantages like dose dumping and difficulty in dose adjustment. Key physicochemical factors include aqueous solubility, partition coefficient, drug stability, dose size, drug pKa, molecular size/weight, and protein binding. The document serves as a comprehensive overview for understanding the complexities of modern drug delivery systems.

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Sharini Y S
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12 views14 pages

Mrdds

The document discusses the physicochemical factors influencing sustained and controlled drug delivery systems, highlighting their advantages such as improved patient compliance and reduced side effects, as well as disadvantages like dose dumping and difficulty in dose adjustment. Key physicochemical factors include aqueous solubility, partition coefficient, drug stability, dose size, drug pKa, molecular size/weight, and protein binding. The document serves as a comprehensive overview for understanding the complexities of modern drug delivery systems.

Uploaded by

Sharini Y S
Copyright
© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
Available Formats
Download as PPTX, PDF, TXT or read online on Scribd
You are on page 1/ 14

PHYSICOCHEMICAL FACTORS INFLUENCING SUSTAINED AND

CONTROLLED DRUG DELIVERY SYSTEM


SUBJECT: MODERN DRUG DELIVERY SYSTEM

SUBMITTED BY,
MONIKA S PATEL
1 SEM M. PHARM
ST

DEPARTMENT OF PHARMACEUTICS

SUBMITTED TO,
Dr. A . GEETHALAKSHMI
HOD and PROFESSOR
DEPARTMENT OF PHARMACEUTICS
HARSHA COLLEGE OF PHARMCY

03/04/2025 Department of pharmaceutics 1


CONTENTS

 Introduction

 Advantages

 Disadvantages

 Physicochemical factros

03/04/2025 Department of pharmaceutics 2


SUSTAINED RELEAS DRUGS
The sustained release formulation is designed to slowly release a drug in the
body over an extended period of time especially to sustain therapeutic levels is
known as sustained drugs.

CONTROLLED RELEASE DRUGS

The controlled release formulation is designed to the drug delivery system in


which a constant level of a drug is maintained in blood and tissue for an extended
period.

03/04/2025 Department of pharmaceutics 3


ADVANTAGES OF SUSTAINED AND CONTROLLED DRUG DELIVERY

 Reduction in frequency of drug administration.


 Improvement of patient compliance.
 Reduction of drug level fluctuation in blood.
 Reduced local and systermic side effects.
 Maximum utilization of drug.
 Better control of disease condition.
 Reduction in health care cost.

03/04/2025 Department of pharmaceutics 4


DISADVANTAGES OF SR AND CDDS

 Dose dumping.
 Poor in vitro-in vivo correlation.
 Increased instability.
 Patient education is required for successful therapy.
 Retrieval of drug is difficult in case of toxicity, poisoning or hypersensitivity
reactions.
 Difficulty in dose adjustment.

03/04/2025 Department of pharmaceutics 5


PHYSICOCHEMICAL FACTRORS INFLUENCING SR AND CDDS

1. Aqueous solubility

2. Partition coefficient

3. Drug stability

4. Dose size

5. Drug pka

6. Protein binding

7. Molecular size/weight and diffusivity

03/04/2025 Department of pharmaceutics 6


1. AQUEOUS SOLUBILITY

 Most of the drugs are weak acid or weak basic.


 The drugs with low water solubility will be difficult to incorporate into SR mechanism.
 The drugs with high water solubility and rapid dissolution rate, it is often quite difficult to retard its
dissolution rate.
 The drug with high solubility can dissolve in water or GI fluid readily and tends to release its dosage
from in a burst .
 Solubility of the drugs is depends On the pH which varies through out the GIT and leads to uneven
absorption.
 Some antibiotics which shows good aqueous Solubility with slow dissolution rate are better candidates
for oral SR/ CR release matrix type System.

03/04/2025 Department of pharmaceutics 7


2. PARTITION COEFFICIENT

• Partition coefficient is generally defined as the ratio of the fraction of drug in an oil phase to that of an
adjacent aqueous phase.
• It is common to consider that these membranes are lipidic therefore, the partition coefficient of oil-
soluble drugs becomes important in determining the effectiveness of membrane barrier penetration.
K=Co/Cw
Where, Co = Equilibrium concentration of all forms of the drug in an organic phase at equilibrium
Cw = Equilibrium concentration of all forms in an aqueous phase .
• High Partition Co efficient or High Lipophilicity of the drug readily penetrate the membrane but
unable to proceed further such drugs have increase tendency to cross even the more selective barriers
like BBB.
• Low Partition co efficient or High aqueous solubility of the drug cannot penetrate through membrane.

03/04/2025 Department of pharmaceutics 8


3.DRUG SOLUBILITY

• Drugs undergo both basic /acidic hydrolysis and enzymatic degradation when administered oral route.

• Drugs showing stability problem in any particular area of GI tract are less suitable for controlled release

system that release its contents over a length of GI tract.

• The delivery system which is localized in a particular area of GI tract (Bio adhesive systems )act as

reservoir for drug release are much more suitable for these kind of drugs.

• CDDS is also suitable for drugs getting destroyed by enzymatic degradation via protection of drug by

incorporation into polymeric matrix.

03/04/2025 Department of pharmaceutics 9


4.DOSE SIZE

• A very practical problem in construction of a sustained release dosage forms is the volume of the

drug that must be administered.

• For orally administered systems, there is an upper limit to the bulk size of the dose to be

administered.

• In general, a single dose of 0.5±1.0 g is considered maximal for a conventional dosage form.

• This also holds for sustained-release dosage forms. Those compounds that require large dosing

size can sometimes be given in multiple amounts or formulated into liquid system

03/04/2025 Department of pharmaceutics 10


5. DRUG Pka

o pKa states that the uncharged form of a drug will be preferentially absorbed through many body

tissues.

o Drugs existing largely in an ionized form are poor candidates for oral SR DDS. --the absorption rate of

the ionized drug is 3-4 times less than that of the unionized drug.

03/04/2025 Department of pharmaceutics 11


6. Molecular size/weight and Diffusivity :
 Diffusivity is defined as the ability of a drug to diffuse through the membrane.
 Diffusivity depends on size and shape of the cavities of the membrane. Molecular size or weight is inversely
proportional to the diffusibility.
 Drugs with larger molecular size are a poor candidate for oral SR system.
 But 95% of drugs are absorbed by passive diffusion.
 The molecular size threshold is 150 Daltons for spherical compound and 400 Daltons for linear compound.
 Lower the molecular weight or size , faster and complete the absorption .
It can be expressed as :
logD = -Sv logV + Kv
= -Sm logM +Km
Where , D=diffusivity , V = molecular volume M= molecular weight or mass
Sv , Sm , Kv , Km =constant

03/04/2025 Department of pharmaceutics 12


7. PROTEIN BINDING

• Protein binding characteristics of drug play a significant role in therapeutic effect regardless of

the type of dosage form.

• The drug Protein complex serve as reservoir for controlled release of drugs to extra vascular

tissues.

• Extensive Protein binding will be evidenced by long half life for elimination and such drugs do

not require controlled release dosage form

03/04/2025 Department of pharmaceutics 13


03/04/2025 Department of pharmaceutics 14

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