Hollow Miro for Angina

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DESIGN AND CHARACTERISATION OF HOLLOW

MICROSPHERE FOR THE TREATMENT OF

ANGINA PECTORIS

Guided by Prepared By

Mr. ANANDKUMAR K. PATEL UTSAV RATHOD

ASST. PROFESSOR EN. ROLL:102070808006

M.Pharm-sem III utsav rathod 1



Index Introduction

Aim of work

Objective of the study

Drug and Polymers

Plan of work

Literature review

References 2 utsav rathod



Introduction The sustain release dosage form are design to

release the drug at predetermined rate in order tomaintained constant drug concentration for the

specific period of time with minimum side effect.

1) Rate programmed drug delivery system

2) Activation modulated drug delivery system

3) Feedback regulated drug delivery system

4) Site targeting drug delivery system

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Gastro retentive drug delivery…

Low density

High density Bio adhesion

Expansion by swelling or unfolding to large size

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hollow microsphere

Hollow microspheres are in strict sense, spherical

empty particles without core.

Floating microsphere

Size less than 200 micrometer

Low density system remain stomach for prolongperiod.

Drug released at desired rate so reduced

fluctuation in plasma concentration

Wall thickness several micron to as low as 0.1 µm

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Method of preparation

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Advantage Enhanced bioavailability

Enhanced first pass biotransformation

Reduce frequency of dosing

Reduce fluctuation of drug concentration

Improved selectivity in receptor activation

Reduce counter activity of body

Better therapeutic effect of short half-lifedrugs can be achieved

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Aim of work To design and characterization of hollow

microsphere.

They are characterized by their

micromeritic properties such asparticle size, tapped density,compressibility index, true density andflow properties.

Surface topography Drug & excipient interaction

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Rationale for selection Ca channel blocker are relatively selective

for myocardium, reduce myocardial oxygendemand and reverse coronary vasospasm,and are often used to treat Angina.

Administration of conventional tablethas been reported to exhibit fluctuations in

plasma drug level resulting either in sideeffect of reduction in drug concentration atreceptor side.

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Drug profile Diltiazem Hcl

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Pharmacokinetic parameter Bioavailability : 30-40%

Metabolism : Hepatic

Half-life : 3- 4.5 hrs

Excretion :Renal

Lactic ( in lactating females)

protein binding : 70-80%

log P: 2.8

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Mechanism of action By inhibit ion-control gating mechanisms, and

interfering with the release of calcium from thesarcoplasmic reticulum

Diltiazem inhibits the influx of calcium across both

the myocardial . The resultant inhibition of the contractile processes

of the myocardial smooth muscle cells leads todilation of the coronary and systemic arteries and

improved oxygen delivery to the myocardial tissue.

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Polymer Cellulose acetate

Eudragit

Acrycoat

Methocil

Polyacrylates

Polyvinylacetate

Carbopol

Agar

Chitosan

Polycarbonates Ethyl cellulose

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Objective To reducing dosing of selected model drug.

Site specific absorption from the upper partof the gastrointestinal tract are potential

candidate for the hollow microsphere. To formulated as floating drug delivery

systems, there by maximizing theirabsorption.

Better Patient compliance.

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Plan of Work

Literature survey

Formulation of dosageform- by solvent

evaporation

Evaluation of dosageform

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Evaluation Parameter Micromeritics property

Surface Morphology

Entrapment efficiency

Drug content

Buoyancy determination

In vitro dissolution

Stability study

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Literature Review N.J. Joseph et al. Prepared floating type

dosage form of piroxicam in hollow

polycarbonate (PC) microspherescapable of floating on simulated gastricand intestinal fluids was prepared by asolvent evaporation technique.

Basavaraj BV et al. developed hollowmicrosphere of diclofenac sodium byemulsion solvent diffusion method.

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George C. K. et al formulate NovelPEGylated pH-Sensitive Polymeric HollowMicrosphere.

H.S. Yoo et al. developed Biodegradablehollow microspheres were prepared bydouble oil and water emulsion using alipophilic surfactant.

S. Wang et al Porous hollow microspheresof crystalline ceria were synthesized via asimple carbon sphere template method.

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Y. Liu et al. prepared glyceryl monooleate-coated hollow-bioadhesive microspheresfor gastroretentive drug delivery.

Jain et al designed a controlled release

system to increase GRT without contactwith gastric mucosa. The was achievedthrough the preparation of floatingmicrospheres by emulsion solvent diffusion

technique . Y. Sato et al developed Hollow

microspheres (microballoons) weredeveloped as a floating controlled drug

delivery system. 19 utsav rathod



References Talukder, R. and Fissihi, R., Gastroretentive Delivery

Systems: A Mini review. Drug Dev. and Ind. Pharm., 30: 1019-1028. 2004.

R Garg, GD Gupta review on ” Progress in Controlled

Gastroretentive Delivery Systems” Trop J Pharm Res,

September 1055 2008; 7 (3) Gholap S. B., Banarjee S. K., Gaikwad D. D., Jadhav S. L.,

Thorat R. M. hollow microsphere: review ,Volume 1, Issue 1,March – April 2010; Article 015

Goyal M, Prajapati R, Purohit K, Mehta S.C., Floating

Drug Delievery System- REVIEW, Journal of CurrentPharmaceutical Research 2011; 5(1):7-18

Whitehead L, Fell JT, Collett JH. Development of agastroretentive dosage form. Eur. J. Pharm. Sci. 1996; 4(Suppl.): S 182.

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References Desai S,Boltan S.A floating controlled release drug delivery

system in vitro in vivo evaluation.Pharm res;1993:1321-1325

Chein, Y. W.,Oral Drug Delivery and Delivery systems. In,Novel drug delivery systems, Vol. 50, Marcel Dekker, Inc.,New York, 1992; 50: 139-17

Minami H & McCallum RW, The physiology and pathophysiology of gastric emptying in humans, Gastroenterology,86, 1984,1592-1610.

Robinson JR, Lee VH. Controlled drug delivery,fundamentals and applications. 2nd ed. New York: Marcel

Dekker Inc; 1987.

Seth PR, Tossounian J. The hydrodynamically balancedsystem, a novel drug delivery system for oral use. Drug Dev.Ind Pharm. 1984; 10: 313-339.

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Hollow Miro for Angina