FORMULATION AND EVALUATION OF DRY SYRUP CONTAINING LINEZOLID

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ABOUT AUTHORS:
Akash M Patel*, Viren N Sisodiya
* Faculty of Pharmacy,
Dharmsinh Desai University, Nadiad-387001, Gujarat
aku.pharmacy@gmail.com

ABSTRACT
Taste is an important factor in the development of dosage form. The problem of bitter and obnoxious taste of drug in pediatric patient can create a bad psychological effect on mind. The purpose of this research was to mask the intensely bitter taste of Linezolid using ion exchange resin and to formulate the dry syrup of the taste masked drug. When suspension is swallowed the bitter taste of the drug may not be felt as ion exchange resin does not release the drug at salivary pH. When it comes in contact with acidic environment of stomach, the complex will be broken down releasing the drug which may then absorbed. Batch method was used for formation of drug resin complex. Various ion exchange resin like different grade of kyron and indion 214 were used for masking the bitter taste. Optimization of drug loading was carried out. Indion 214 was selected as a optimized resin with 84.47 % drug loading. Dry syrup was made using suspending agent like gellan gum, guar gum and CMC and evaluated for various parameters like colour, odour, taste, viscosity, sedimentation volume, redispersibility, % drug content, drug release. By evaluating all the parameter the batch formulation contained guar gum 3 % was the best one amongst all the other formulations.

REFERENCE ID: PHARMATUTOR-ART-2331

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

Volume 3, Issue 5

Received On: 16/12/2014; Accepted On: 19/02/2015; Published On: 01/05/2015

How to cite this article: AM Patel, VN Sisodiya; Formulation and Evaluation of Dry Syrup Containing Linezolid; PharmaTutor; 2015; 3(5); 42-48

INTRODUCTION
A number of patients, especially pediatric and geriatric, have difficulty in swallowing solid dosage forms hence liquid dosage forms are needed. Linezolid is slightly soluble in water hence formulation of a suspension will be most suitable but product may not be physically and chemically stable. In the present work, attention is paid to develop a reconstitutable suspension dosage form of linezolid and to study the stability and palatability of the same.(1)

Dry Syrups: (3,4,2)
Dry Syrups are commercial dry mixtures that require the addition of water at the time of dispensing. A number of official and commercial preparations are available as dry powder mixtures or granules that are intended to be suspended in water or some other vehicle prior to oral administration. Most of the drugs prepared as a dry suspension for oral suspension are antibiotics. The dry mixture of oral suspension is prepared commercially to contain the drug, colorants, flavors, sweeteners, stabilizing agents, suspending agents and preserving agents that may be need to enhance the stability of the formulation.

Major application - pediatric therapy: taste masking(7)
Oral Route of administration is the route of choice for administration of medicines in children. The only hurdle for dosage form designing for pediatric patients is the patient’s acceptance of the dosage form. Pediatric Patients tend to become un-cooperative during the administration of oral medication; the most common reason being the taste of the oral formulation administered among the children. Most of the drugs administered as granules for oral suspension under pediatric therapy are Antibiotics, which when administered orally as any other dosage form have a bitter taste making it unpleasant for Children to consume the medicatio.

MATERIALS AND METHODS

Table 1: List ofmaterials

Sr. No

Materials used

Manufacturer

1

Linezolid

Zydus cadila pharmaceuticals

2

Indion 214

Ion exchangePharmaceuticals

3

Gellan Gum

Chemdyes Corporation

4

GuarGum

Leben pharma, Akola

5

CarboxyMethyl Cellulose

ColorconAsiaPvt.Ltd.

6

SodiumStarch Glycollate

MapleBiotech Pvt.Ltd.,

7

SodiumBenzoate

Lesar ChemicalsLtd.

8

SodiumCitrate

Lesar ChemicalsLtd.

9

SodiumLauryl Sulphate

FinarChemicalsPvt.Ltd.

10

PotassiumBromide

FinarChemicals Pvt.Ltd.

11

Aerosil

FinarChemicalsPvt.Ltd.

12

StrawberryFlavor

Themis MedicareLtd.

13

Quinoline yellowColour

Themis MedicareLtd.

Table 2: List ofBatchcode of formulation

Ingredients

(%w/v)

Batchcode

F1

F2

F3

F4

F5

F6

F7

F8

F9

Linezolid+indion

214

3.86

3.86

3.86

3.86

3.86

3.86

3.86

3.86

3.86

Gellangum

1

2

3

-

-

-

-

-

-

Guargum

-

-

-

1

2

3

-

-

-

CMC

-

-

-

-

-

-

1

2

3

SSG

1

1

1

1

1

1

1

1

1

Sodiumbenzoate

0.2

0.2

0.2

0.2

0.2

0.2

0.2

0.2

0.2

Sodiumcitrate

0.2

0.2

0.2

0.2

0.2

0.2

0.2

0.2

0.2

Sucrose

23.13

23.13

23.13

23.13

23.13

23.13

23.13

23.13

23.13

SLS

0.1

0.1

0.1

0.1

0.1

0.1

0.1

0.1

0.1

KBr

0.006

0.006

0.006

0.006

0.006

0.006

0.006

0.006

0.006

Aerosil

0.5

0.5

0.5

0.5

0.5

0.5

0.5

0.5

0.5

            Flavor

q.s

q.s

q.s

q.s

q.s

q.s

q.s

q.s

q.s

    Qunoline yellow

q.s

q.s

q.s

q.s

q.s

q.s

q.s

q.s

q.s

Total(gm)

10gm

10gm

10gm

10gm

10gm

10gm

10gm

10gm

10gm

Reconstitute with water up to 30ml

EXPERIMENTAL METHOD(5,8,9)

PREPARATION OF DRY SYRUP OF LINEZOLID
• The dose of dry syrup was selected 100 mg/5 ml as syrup was meant to be prepared for pediatric patient. For pediatric patient the dose will be calculated on the basis of the weight of the patient. For Linezolid the pediatric dose is 8 mg/kg/day.
• So total 30 ml of dry syrup was prepared which contained total amount of 600 mg of Linezolid.
• Dry syrup of Linezolid (100 mg/5ml) was prepared using suspending agents, wetting agent, preservative, flocculating agent, superdisintegrant, buffer, anticaking agent, sweetener, flavours by granulation technique.
• All ingredients were passed through 200# before mixing.
• The complex of drug and resin equivalent to 600 mg Linezolid was blended with the other ingredients by geometric mixing.
• The solid ingredients were blended and massed using water.
• Granulation was carried out by means of wet granulation using water as granulating fluid.
• The wet mass was formed into granules using 30 mesh sieve. The formed granules were dried in the oven and passed through 32 mesh after drying.
• 10 gm of final Linezolid dry syrup formulation were diluted upto 30 ml for final formulation.
• Dose of granulations: 1.66gm of the granulations diluted upto was 5ml equivalent to 100 mg of Linezolid.

EVALUATION PARAMETER OF DRY SYRUP
a) Colour, odour and appearance(6)

All the developed batches of syrup were evaluated for organoleptic properties such as colour, odour and appearance.

b) Drug content(11)
Dry syrup equivalent to 100 mg of linezolid was taken in 100 ml volumetric flask and dissolved in 10 ml methanol and volume was made up to 100 ml by adding sufficient 0.1 N HCl. The solution was analyzed at 243.6 nm to found out drug content

Bulk density:
The powder (2 gm) filled in measuring cylinder called as bulk volume of powder and measure mass of that powder. Bulk density is ratio of mass of powder to bulk volume of powder. It is a measure used to describe a packing of powder. The equation for determining bulk density is

ρb = m/ vb-
Where, ρb= Bulk density m = Mass of powder vb= Volume of powder

Tapped density:
The pre-weighed powder (2gm) was filled in measuring cylinder. Then it was tapped in bulk density test apparatus. After 50 taps the volume is measured and the tapped density was measured using following formula.

ρt = m/ vt-
Where, ρt= Tapped density m = Mass of powder vt= Tapped volume

ii. Carr’s index (CI):(9,10)
Compressibility is indirectly related to the relative flow rate, cohesiveness and particle size distribution of the powder. Powders with compressibility values lesser than about 20%, has been found to exhibit good flow properties. Tapped (ρt) and Apparent (ρb) Bulk density measurements can be used to estimate the compressibility of a material.

Carr’s index (%) = (ρt - ρb) / ρt * 100 --

Where, ρb= Bulk density ρt= Tapped density

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