DEVELOPMENT OF IN-VITRO PROFILE OF LANSOPRAZOLE

Mehwish ayaz(87-E-14)
PHARMACY DEPARTMENT BAHAUDDIN ZAKARIYA UNIVERSITY, MULTAN
Group No: 07 (Evening)
Assigned Drug: lansoprazole
Abstract:

Lansoprazole is an acid Proton pump inhibitor. Lansoprazole is a benzimidazole sulfoxide

derivative and produces long lasting inhibition of gastric acid secretion.The study was
aimed to develop the linearity curve. So, that concentration of drug in any sample can be
calculated from its estimated absorbance. It obeys Beer-lambert law upto 25ppm after
which it shows deviation. So calibration curve is only applicable to sample having lower
concentration of drugs. It is also use to measure the similarity index of two different brand
of lansaprazole. Slanz & inhibitol are bioequivalent as proven experimentally by using
USP dissolution apparatus –II and by applying similarity factor.

Keywords: Lansoprazole, Beer-Lambert Law, Calibration curve, Bioequivalent, Similarity factor

Introduction

Lansoprazole is a proton pump inhibitor. lt is a racemic mixture of (+)S- and (-)R-

enantiomers. lt is a slightly yellow crystalline powder. Its molecular formula is
C16H14F3N3O2S. The molecular weight is 369.363. It is slightly soluble in water at pH of
6.8.it has the following structural formula:
Peak plasma concentrations are reached 0.5 - 4 hours(2h) after oral administration.The
apparent volume of distribution is approximately 14-18L.Buffer is pH 6.8 phosphate
buffer.Absorbance maximum at 298 nm.Adult dose : 30 mg , dose to be increased only in
acute condition.
For relief of the signs and symptoms of gastric acid secretion by specific inhibition
of(H-K)ATPase enzyme at secretory zurface of gastric parital cells.It has been
characterized as gastric acid pump inhibitor .This effect is dose related & in inhibits both
basal and stimulated gastric acid secretion.

Materials and Methods:

Materials:
Chemicals required for test and evaluation of lansoprazole are Sodium Hydroxide
(NaOH),Potassium phosphate monobasic (kH₂PO₄),Distilled water,Measuring cylinder,
stirrer, beaker, weighing balance, pipette, volumetric flask, burette, PH meter, PH
strip,UV-spectrophotometer,Dissolution Apparatus-ΙΙ (peddle apparatus),Small intestine,
stomach, skin and blood plasma of rabbit.
Methods:
Linearity curve:
It is plotted by observing the dilutions made by using a single stock solution. The curve
was plotted with absorbance on Y-Axis and Concentration on X-Axis
Single point dissolution:
It was carried out by using the dissolution apparatus sampling was done only once at 30
min.The concentration was determine by finding absorbance using
UV-Spectrophotometer and referring to linearity curve plotted previously
Multiple point Dissolution:

Same method was used but sampling was done at fixed time interval of 5 mins for
30mins. The concentration was determined by finding the absorbance using the
UV-Spectrophotometer and referring to the linearity curve that was plotted previously.

Clearance of Lansoprazole by one Compartment Model: After preparing the buffer of

6.8 PH, separated it in two portions. In one portion drug was dissolved and poured it into
separating funnel while other portion was taken in burette. After setting the flow rate took
sample after regular interval, measured the absorbance and calculated the concentration
and finally clearance was calculated.

Similarity Index of different Brands: Perform dissolution test on two brands of

Lansoprazole and took sample from both after regular intervals and check the absorbance
and calculated the concentration and compare the data to find the similarity of both
brands.

Absorbance of Lansoprazole from intestine of Rabbit: Fill the drug solution in the
intestine of rabbit and held in the buffer of PH 7.4 and took the sample at different time
interval and calculated the concentration through absorbance.

Official Standards for Dissolution:

Dissolution Medium: Phosphate buffer(50ml 0.2M monobasic potassium phthalate +
22.4ml 0.2M NaOH) of pH=6.8, Volume of Medium:500ml, Dissolution time: 30 Mins
and belongs to BCS Class 2.

Results and discussion:

Table 1

Linearity curve of LANSOPRAZOLE:

Con.ppm Ug/ml mg/ml %w/v molarity Absorbance

6.25 6.25 0.00625 0.000625 0.00625 0.95

12.5 12.5 0.0125 0.00125 0.0125 1.7

25 25 0.025 0.0025 0.025 3.5

Figure I
 Time Absorbance %age conc.

0 min 0.688 100%

30 min 0.410 67.21%

60 min 0.122 33.24%

Clearance of LASOPRAZOLE by one compartment model:

b= 0.64
m=0.014
y=0.688
Clearance=47.8ml/min
Figure II

Dose Adjustment of lansoprazole:

Age of patient = 43 years, Weight = 70kg, Height =5 3 Serum creatinine = 0.9mg/dl
Creatinine clearance = 89.06ml/min
adjusted dose for Female = 11.4mg
adjusted dose for male =10.38mg
chronic renal failure patient dose is = 5.787mg.

Single point Dissolution:

Time Absorbance

30 min 1.3

y=1.3 b= 0.01, m= 0.135 %age Release = 94.2%

Multiple point Dissolution: Brand used (Reference) = lancet (30mg)

Table III

Time Absorbance Conc (ppm) mg/ml %age Release

5 min 0.10 0.666 0.000666 1.11%

10 min 0.11 0.74 0.00074 1.23%

15 min 1.002 7.34 0.00734 12.23%

30 min 1.3 9.55 0.00955 15.925%

Test Brand = slanz (30mg)

Time Absorbance Conc (ppm) mg/ml %age Release

5 min 0.4 2.88 0.00288 4.81%

10 min 1.16 8.5 0.0085 14%

15 min 1.5 11.03 0.01103 18.36%

30 min 2.11 15.55 0.01555 25.9%

Figure III
Percentage Release (Y-axis)

Time (X-axis)
Similarity Index (f2) = 30.9%

Results and Discussions

Linearity curve data shown in Table I shows that this drug obeys Beer-Lambert Law upto
25ppm after it shows deviation.
Multiple Point dissolution data showsn in Table 2 shows that lancet and Slan are similar
The results of bioequilance shows that two brands are similar
References:
1- LEON SHARGEL BIOPHARMACEUTICS AND PHARMACOKINETICS
2- Drugbank.com
3- United state pharmacopoeia (USP)
4- BNF
5- Basic Pharmacokinetics by Sunil S Jambhekar and Philip J Breen.