PREPARATION AND CHARACTERIZATION OF ETHYL CELLULOSE BASED SALBUTAMOL SULPHATE AND THEOPHYLLINE COMBINATION MICROSPHERE

 

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ABOUT AUTHORS
*Nayak Chandan1, PadhiPriyanka1
Gayatri Institute of Science and Technology,
Gunupur Odisha, India
*nayakchandan279@gmail.com

ABSTRACT: 
The study is concerned with the development of Ethyl Cellulose microspheres by the o/w emulsification and solvent evaporation method in the presence of tween 80 as an emulsifying agent. The influence of process parameters such as solvent mixture, composition, concentration of the emulsifying agent and speed of stirring has been examined. The microspheres have been analysed for their size, drug loading capacity and drug release study. Spherical and smooth surfaced microspheres with desired encapsulation efficiencies were obtained. Slow drug release from microspheres observed up to6- 8 h. An optimization procedure was employed to investigate and identify the key parameters affecting the properties of the microspheres.

REFERENCE ID: PHARMATUTOR-ART-2512

PharmaTutor (Print-ISSN: 2394 - 6679; e-ISSN: 2347 - 7881)

Volume 6, Issue 4

Received On: 16/04/2017; Accepted On: 19/03/2018; Published On: 01/04/2018

How to cite this article: Nayak C, Padhi P; Preparation and Characterization of Ethyl Cellulose based Salbutamol Sulphate and Theophylline Combination Microsphere; PharmaTutor; 2018; 6(4); 51-69; http://dx.doi.org/10.29161/PT.v6.i4.2018.51

INTRODUCTION:
For many decades, acute diseases or a chronic illness has been treated and managed by conventional pharmaceutical dosage forms like tablet, capsules, liquids and semi-solid preparation. Microspheres are one of the multiparticulate drug delivery systems and are prepared to obtain prolonged (or) controlled drug delivery, to improve bioavailability or stability and to target drug to specific sites. Microspheres can be defined as solid, approximately spherical particles ranging from 1 to 1000µm, containing dispersed drug in either solution (or) microcrystalline form. Ethyl cellulose is non-biodegradable, bio-compatible, non-toxic natural polymer and widely used in oral and topical formulation. The microspheres can be produced by several methods utilizing emulsion system (o/w, w/o, o/w/o and w/o/w). The common emulsion system used oil-in-water (o/w), with microspheres being produced by the emulsion solvent evaporation method. This relatively simple method enables the entrapment of a wide range of hydrophobic drugs.4 The main object of present study was to investigate the possibility of obtaining sustained release aspirin microsphere by using different concentration of ethyl cellulose, different composition of solvent mixture, different concentration of emulsifying agent and different stirring rate. Some of the basic factors to be taken in an account while designing a controlled release drug delivery system includes:

* Effective therapeutic concentration of the drug
* The release kinetic and mechanism of drug release from the device
* The physico-chemical properties of the drug as well as the delivery device

MATERIALS:
Salbutamol sulphate as a model drug, Ethyl Cellulose as a polymer, Tween80 and span 80 as an Emulsifying agent, Acetone and Ethyl Acetate as a solvent were used for present investigation. All the materials were provided by G.I.S.T COLLEGE, GUNUPUR

METHODS:
Preparation of Microspheres: Microspheres were prepared based on oil-in-oil emulsion solvent evaporation technique by using the formulation.  In this method 900mg of ethyl cellulose was dissolved in 15 ml of acetone and a given amount of the drugs were dispersed in it to make different drug to polymer ratio 1:1,1:5,1:2 for salbutamol sulphate microspheres and 1:1,1:2,1:3 for combination microspheres and stirred for about 10minut .then the polymer drug dispersion was poured into 50ml of liquid paraffin(light)containing varying of dispersing agents which are dispersed and stirred for about 30 minute before the polymer –drug dispersion was added. The whole systems was then stirred for about 4hour at 900rpm.after stirring  process is over the liquid paraffin (light) was decanted off and microcapsule formed were collected and washed with cyclohexane to completely remove the reaming oil and dried at 60˚C in vacuum drier for 6 hour and collected for further studies and characterized. 

Physicochemical Characterization of Microsphere
Percentage yield : The dried microspheres were weighed and percentage yield of the prepared microspheres was calculated by using the following formula, Percentage yield = {the weight of microspheres / (The weight of polymer + drug)}*100

Carr’s index
It was measure by using following formula,
Carr’s Index = {(Vb –Vt) / Vb}* 100    
Where, Vb and Vt are the bulk volume and tapped volume respectively. 

Angle of Repose
Angle of repose of the microspheres, is the maximum angle possible between the surface of the pile of microspheres and the horizontal plane, was obtained by fixed funnel method using the formula; Angle of Repose (θ) = tan−1 (h/r )   Where, h is height and d is the diameter of the microsphere pile.

Particle Size Analysis
Particle size of the microspheres was determined by optical microscopy. The eye piece micrometre was calibrated with the help of a stage micrometre. The particle diameters of more than 50 microspheres were measured randomly. The average particle size was determined by using Edmondson’s equation. D = ∑ nd / ∑ n Where, n = Number of microspheres checked; D = Mean of the size range.

FORMULATION OF SALBUTAMOL SULPHATE MICROSPHERE:
Different drug to polymer ratios as well as different concentration (%v/v in light mineral oil) of emulsifying agent was taken to study their effects on different properties of the resultant microsphere. Formulation variables are listed in details in the following tables:

Table-1

FORMULATION USING TWEEN 80:

FORMULATION CODE

DRUG:POLYMER

AMOUNT OF POLYMER(mg)

AMOUNT OF SALBUTAMOL SULPHATE(mg)

PERCENTAGE OF DISPERSING AGENT (%)

A1

1:1

900

900

0.2

A2

1:1

900

900

0.6

A3

1:1

900

900

1

B1

1:1.5

900

600

0.2

B2

1:1.5

900

600

0.6

B3

1:1.5

900

600

1

C1

1:2

900

450

0.2

C2

1:2

900

450

0.6

C3

1:2

900

450

1

Table-2
FORMULATION USING SPAN 80:

FORMULATION CODE

DRUG:POLYMER

AMOUNT OF POLYMER(mg)

AMOUNT OF SALBUTAMOL SULPHATE(mg)

PERCENTAGE OF DISPERSING AGENT (%)

D1

1:1

900

900

0.2

D2

1:1

900

900

0.6

D3

1:1

900

900

1

E1

1:1.5

900

600

0.2

E2

1:1.5

900

600

0.6

E3

1:1.5

900

600

1

F1

1:2

900

450

0.2

F2

1:2

900

450

0.6

F3

1:2

900

450

1

Table-3 FORMULATION OF COMBINATION:


SL NO


FORMULATION CODE


AMT OF POLYMER (mg)


AMT OF ANHYDROUS THEOPHYLLINE (mg)


AMT OF SALBUTAMOL SUPHATE(mg)


PERCENTAGE OF TWEEN 80(%V/V)


RPM


1


T1


1219.2


1200


19.2


1


900


2


T2


1219.2


600


9.6


1


900


3


T3


1219.2


400


6.4


1


900

PARTICLE SIZE DETERMINATION OF MICROSPHERE
The particle size of the microspheres was determined by microscopic method (72, 73).the ocular micrometre was calibrated using stage micrometre and each division of the ocularmicrometre was measured in micrometre.For each batch of the microsphere, 100 particles were counted and done in triplicate.  Calibration of ocular micro meter:  1 division of ocular micro meter =15µm.

DRUG ENTRAPEMENT EFFICIENCY:  
The amount of salbutamol sulphate present in the microsphere was determined by extraction in distilled water (48). 50 mg of the crushed and powdered microsphere was taken and extracted in 50 ml of distilled water and stirred for 15 minute at 1500rpm. The solution was filtered and after suitable dilution the content of salbutamol sulphate was determined spectrophotometric ally at 276nm. The same also applied for combination microsphere. Drug entrapment efficiency =experimental drug content /theoretical drug content ×100

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