STAMFORD UNIVERSITY

BANGLADESH

Pharmaceutics - II
Assignment
Course Code: BPH – 320
Topic: Modified Release Drug Delivery System

Submitted To:
Dr. Madhabi Lata
Assistant Professor
Pharmacy Department of
Stamford University

Submitted By:
Md Owasiul Anas
ID: BPH - 067 07430
SECTION: BPH – S - 67
Department of Pharmacy

Date of Submission: 03, May – 2021.

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Index

SL No. Content Page No.

01 Definition 02

02 Prospect Over the Dosage Forms 02 – 03

03 Classification 04

04 Release pattern from the formulation 05

05 Typical types of MRDDS 05 – 06

06 Advanced Types of MRDDS 06

07 Challenges for MRDDS 07

08 MR Tablets available in Bangladesh 07 – 09

09 Reference 10
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Modified Release Drug Delivery System

Definition:

The term “modified release” refers to both delayed and extended-release systems for oral
administration as well as other delivery systems designed specifically to modify the release of
poorly water-soluble drugs. Modified-release dosage is a mechanism that (in contrast to
immediate-release dosage) delivers a drug with a delay after its administration (delayed-
release dosage) or for a prolonged period of time (extended-release [ER, XR, XL] dosage) or
to a specific target in the body (targeted-release dosage). Modified release dosage forms are
drug delivery systems (DDS) which, by virtue of formulation and product design, provide drug
release in a modified form distinct from that of the conventional dosage forms. Drug release
can either be delayed or extended in nature. Modified release dosage forms are those that alter
the timing and/or the rate of release of drug substance.

Prospect over the dosage form:

➢ Controlled release dosage forms.

➢ Sustained release dosage form.
➢ Trans-dermal drug delivery.
➢ Inhalation and other aerosols.

The need of dosages form:

➢ AcCurate dose.
➢ Protection e.g., coated tablets, sealed ampules.
➢ Protection from gastric juice.
➢ Masking taste and odour.
➢ Placement of drugs within body tissues.
➢ Sustained release medication.
➢ Controlled release medication.
➢ Optimal drug action.
➢ Insertion of drugs into body cavities (rectal, vaginal)
➢ Use of desired vehicle for insoluble drugs.
Controlled release dosage forms:

➢ Controlled drug delivery is one which delivers the drug at a predetermined rate, for
locally or systemically, for a specified period of time.
➢ Continuous oral delivery of drugs at predictable & reproducible kinetics for
predetermined period throughout the course of GIT.

Trans-dermal drug delivery:

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➢ Transdermal dosage forms provide a safer and more convenient method of parenteral
therapy than, for example, intravenous infusions; yet they retain many advantages
associated with drug therapy through the parenteral route.
➢ These stem mainly from avoidance of the gastrointestinal tract variables (acidity,
motility, enzymatic activity, food intake, and transit time) that frequently make
absorption from the gut unpredictable. A first pass through the liver prior to reaching
the systemic circulation is also avoided, minimizing drug degradation by that organ.

Inhalation and other aerosols:

➢ Inhalation aerosols continue to be the basis for successful lung therapy for several
diseases, with therapeutic strategies and the range of technology significantly evolving
in recent years.
➢ In response, this third edition takes a new approach to reflect the close integration of
technology with its application. After briefly presenting the general considerations that
apply to aerosol inhalation, the central section of the book uses the focus on disease and
therapeutic agents to illustrate the application of specific technologies.
➢ The final integrated strategies section draws the major points from the applications for
disease targets and drug products.
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Classification:

It can be classified in more:

➢ Dissolution granules.
➢ Diffusion granules.
➢ Enteric coated granules.
➢ Reservoir.
➢ Matrix
➢ Osmotic pump.
➢ Repeat action.
➢ Microparticles.
➢ Meter release.
➢ Ion exchange resins.
➢ SODAS.
➢ Hydrodynamically balanced.
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Release pattern from the formulation:

Modified release dosage forms have been developed to deliver drug to the part of the body
where it will be absorbed, to simplify dosing schedules and to assure that concentration of drug
is maintained over an appropriate time interval. Drugs that are not inherently long lasting
require multiple daily dosing to achieve the desired therapeutic effects. Multiple daily dosing
id often inconvenient and can result in missed doses, made-up doses and patient non-compliant
with therapeutic regiment. Blood levels of drugs forms conventional immediate release dosage
forms taken more than once daily following definite schedule usually demonstrate sequential
peaks and troughs (valleys) associates with each dose. Design to release their medication in
controlled manner, at pre-determined rate, duration and location in the body to achieve and
maintained optimum therapeutic blood levels of drug.

Typical Types of Modified Release Drug System:

➢ Extended-release dosage forms.

1. Sustained release.
2. Controlled release.
➢ Delayed release dosage forms.
➢ Targeted release dosage forms.
➢ Repeat action dosage forms.
➢ Prolonged action dosage forms.
➢ Extended-release dosage forms:
One that allows a reduction in dosing frequency to that presented by a conventional
dosage form. Designed to release their medication in controlled manner, at pre-
determined rate, duration and location in the body to achieve and maintain optimum
therapeutic blood levels of drug. Examples-controlled release, sustained release and
long-acting drug products.

➢ Delayed release dosage forms:

These are dosage forms designed to release the drug at a time other than promptly after
administration. The delay may be time-based or based on the influence of
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environmental conditions such as GI, pH, enzyme, pressure, etc. E.G – Enteric coated
dosage forms like enteric coated aspirin, other NSAIDS, etc.

➢ Targeted release dosage forms:

Drug release that is directed towards isolating or concentrating a drug in a body region,
tissue, or site for absorption or drug action.

➢ Repeat action dosage forms:

These are dosage forms usually containing 2 single doses of medication, one for
immediate and the second for delayed release e.g., bi-layered tablets.

Advances types of modified release drug delivery systems:

➢ Bilayer tablets:

Consists of two layer-

first layer releases the drug via immediate release and second layer provides controlled
release. This can also be used to formulate dosage form containing two incompatible
APIs.

➢ Multi particulate systems:

The APIs are coated with different concentrations of polymer for individual particle of
API achieving different release paean and improving the patient compliance.

➢ Nanotechnology:

This technology is on the boom. Liposome’s, nanoparticles, SMEDS (Self Micro

Emulsifying Delivery Systems) , SEDS(Self Emulsifying Delivery Systems) are
emerging drug delivery systems for achieving modified release paean.

➢ Inserts/Bot system:

Variety of machines containing API or use of nanobots containing API can be place at
the target site and then machine will allow pulsatile drug delivery systems.

➢ Hydrogels:

These are 3D cross linked networks of water-soluble proteins. The degree of cross
linking inside the hydro gel will control the release paean for the drug.
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Challenges for modified release drug delivery system

➢ Drug solubility and permeability:

Class IV drugs having low water solubility and low permeability drugs cannot be used
as modified release systems. It’s always advised to use solubility enhancers and
permeability enhancers in given dosage form.

➢ Concentration of polymer:

When polymers are used for forming membrane controlling devices, concentration will
decide the release rate of drug into blood stream. Too much concentration of polymer
around the dosage form may not cause release of the drug since drug may become
stagnant in polymeric membrane.

➢ Integrity of the membrane:

If the membrane integrity is not proper, there are chances of dose dumping. Integrity of
depends upon the type of polymer used for the coating. For optimum integrity and
concentration of polymer, it is always to advised to use the Design of Experiment tool
to get productive results.

➢ Therapeutic index/Therapeutic window:

Smaller the therapeutic index or therapeutic window, potent is the concentration for
API. Any slight deviation from safety margin will lead to toxicity and slight deviation
from MEC will lead to undermedication. Hence the drugs having higher therapeutic
index are considered for modified release systems. Ideal therapeutic index for API
should be greater than 10 to form modified release systems.

MR Tablets Available in Bangladesh

➢ Admira MR

30 mg

Gliclazide

UniMed UniHealth

➢ Angimet MR
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35 mg

Trimetazidine Dihydrochloride

Orion Pharma Ltd.

➢ Glix MR

60 mg

Gliclazide

Navana Pharmaceutics Ltd.

➢ Kezid MR

30 mg

Gliclazide

Kemiko Pharmaceutics Ltd.

➢ Metacard MR

35 mg

Trimetazidine Dihydrochloride

Aristo pharma Ltd.

➢ Consucon MR

60 mg

Gliclazide

Incepta Pharmaceutics Ltd.

➢ Diamicron MR

30 mg

Gliclazide

Servier Bangladesh Operation

➢ Feelnor MR
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35 mg

Trimetazidine Dihydrochloride

Incepta Pharmaceutics Ltd.

➢ Gliclid MR

60 mg

Gliclazide

ACME Laboratories Ltd.

➢ Gliclazide MR

30 mg

Gliclazide

Eskayef Pharmaceutics Ltd.

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Reference

http://www.wikipedia.com

http://www.slideshare.net

http://www.sciencedirect.net

http://www.slideplayer.com