Experiment #1

Generic Name and Brand Name

Generic Name:-

The established Non Proprietary or Common name of active drug in a drug product

Generic name is usually given by the pharmaceutical generic association WHO and FDA along with the consultation of scientist who knows in IUPAC (international union of applied chemistry)

Description of generic name of drug in pharmacopoeia is according to the country languages. Generic name includes structural formula. IUPAC name and CAS number.

Brand Name:-

A brand name drug is a medicine that discovered and marketed by pharmaceutical company once a drug is developed that that company file for patient to protect against other companies making copies and selling that drug .it included all the preparation i.e. tablets capsule injection

Experiment#1

S No Generic Brand Tabs Cap Syp Drug suspension

Inj drops

1 Albone-D 0.25/0.5/1mg 0.25/0.5/1mg - - - -2 Bone-One 0.25/0.5/1mg 0.25/0.5/1mg - - - -3 One -alpha 0.25/0.5/1mg 0.25/0.5/1mg - - - -4 X-Bone 0.25/0.5/1mg 0.25/0.5/1mg - - - -5 Bone-care 0.25/0.5/1mg 0.25/0.5/1mg - - - -6 Alfa-D 0.25/0.5/1mg 0.25/0.5/1mg - - - -7 Alcidol 0.25/0.5/1mg 0.25/0.5/1mg - - - -8 Bonedol 0.25/0.5/1mg 0.25/0.5/1mg - - - -9 Reboost 0.25/0.5/1mg 0.25/0.5/1mg - - - -10 Osteodol 0.25/0.5/1mg 0.25/0.5/1mg - - - -

Experiment#1

S No

Generic Brand Tabs Cap Syp Drug suspension

Inj drops

1 Omeprazole Risek - - - - -2 Omeprazole Risek - - - - -3 Telmisartan Tasmi 40mg - - - -4 Telmisartan Co-tasmi 40+12.5mg

80+12.5mg- - - -

5 Domperidone Pelton 10mg - - - -6 Domperidone

maleatePelton-v 12.72mg - - - -

7 Olanzapine Olanzia 5/7.5/10mg - - - -8 Olanzapine Olanzia - 5/7.5/10mg - - - -9 Rifampicin Lednif 150/300mg 150/300mg - - - -10 Rifampicin+INH rimacfal 150/300mg 150/300mg - - - -

Experiment#2

Pharmaceutical Equivalence and alternatives:-

Pharmaceutical equivalence:-

Drug are said to be pharmaceutical equivalent

If

They have same active ingredients. They have same dosage form. They have same route of administration. They have same strength or concentration.Pharmaceutical equivalence must meet the content uniformity, disintegration and dissociation rate.

Pharmaceutical equivalence drugs may different in characteristics such as

Shape Release mechanism Labeling Excipient

Pharmaceutical alternative :-

Those drugs products having the same active ingredients but different in term of salts, esters, complexes of active ingredient differ in strength or concentration and also differ in route of administration and dosage form i.e. diclofenac potassium

s.no Generic Brand Dosage & strength1 Cephradine Velosef Injection:250/500//1gm vial2 Ceftriaxone Cefxone Injection:250/500/1gm vial3 Ceftazidine Fortum Injection:250/500/1gm vial4 Cefotaxime cefotax Injection:250/500/1gm vial

S.no Generic Brand Dosage form & strength

1 Atrovastatin Lipiget Tab:10/20/40mg

2 Fenofibrate Fenoget Cap: 67/200mg

3 Ezitimibe Ezita Tab :10mg

4 Nicotinic acid Nicosur Tab : 250/500mg

EXPERIMENT #3

Plotting of exponential decay data on a linear graph

Theory :-

Decay is often recorded in pharmaceutical and stability studies of the drug .

The data is plotted on linear graph(rectangular or semilog graph paper )

For the representation of data .if an exponent

N=bx

Where

N = the number

b=the base which is often 10 or e (natural log=2.7183)

“x” is the exponent having th common base exponent can be added subtracted to perform multiplication or division.

e.g

1-ax/ay= ax-y

2-ax/ay=ax=y

The given data x=0.0,0.5,1.0,1.5,2.0,2.5,3.0

Calculate the value for log (10-x)

Plot the value on the linear graph versus the value of K

X 10-X e-X

0.0 1 10.5 0.316 0.61.0 0.1 0.361.5 0.03 0.222.0 0.01 0.132.5 0.003 0.8203.0 0.0001 0.497

EXPERIMENT#4

Therapeutic equivalence and therapeutic alternative drugs

Therapeutic Equivalence:-

Drug products are considered to be therapeutic equivalent only if they are pharmaceutical equivalent and if they can expect to have the same clinical effects and safety profile when administered to patient under the condition in the labeling

FDA classifies as therapeutically Equivalent those products that meet the following general criteria.

1. they are approved as safe and effective 2. they are pharmaceutical equivalent in that condition (a) contain identical amount of same active ingredients in the same dosage form and route of

administration .(b) they meet the applicable standard of strength quality ,purity and identity

3. they are bioavailable bioequivalent in that (a) they don’t present a known bioequivalence problems ,and they meet an acceptable initial

standard 4. those are properly labeled 5. they are manufactured in compliance with current good manufacturing practice regulation.

Therapeutic alternative:-

Those drugs are considered to be therapeutic alternative if they contain different active ingredients but they are intended to be used for same clinical and therapeutic effect

Therapeutic alternative should belong to the same class.

Bioequivalence:- d drugs are said to be bioequivalent if “ the rate and extent of absorption of the test drug do not show a significant difference from the rate & extent of absorption of the reference drug when administered at the same molar dose of therapeutic ingredient under similar experimental conditions in either single or multiple doses.”

Experiment # 5

PLOTTING OF EXPONENTIAL decay data on a linear graph :-

Theory :-

Decay data is often encountered in pharmacokinetics and stability studies of the drug .the data is plotted on the linear graph paper for representation of data.

If an exponent N=bx where Nis the number and b is the base ,which is often 10 or e (e=2.7183) and x represent the exponent having the common base .

Exponent an be added or substracted to perform multiplication or divison .

e.g

ax .ay

or

ax/ay= ax-y

the given data

x=0.0.0.5,1.0,1.5,2.0,2.5,3.0

calculate the value for (log) (10-x), e-x (ln) and plot the value on linear graph versus the value of x .

X 10-X e-X

0.0 1 10.5 0.316 0.61.0 0.1 0.361.5 0.03 0.222.0 0.01 0.132.5 0.003 0.8203.0 0.0001 0.497

Exponential decay data

Experiment #6

Area under plasma drug conc: Vs time curve.

Theory:Area under curve (AUC) is the measure of total plasma exposure of the drug over a given time period.

Area under the curve is derived from the area under the plasma drug concentration to time curve and is estimated by multiple conc measurement at various time point in order to predict AUC.The AUC is determined by the administered dose and clearance of the drug.

During constant infusion or multiple dosing of drug,drug level rises until they reach steady state level in the blood and time.

CMIN:-

Minimum plasma concentration Cmin is the lowest plasma drug conc observed,also referred as a trough concentration.

CMAX:-

Maximum plasma concentration Cmax is the highest plasma drug concentration observed.

It is the time at which highest drug concentration occur following administration of an extravascular dose.

T1/2:-

T1/2 is the required for given drug concentration to decrease by 50%.T1/2is determined by clearance and volume of distribution.

CLEARANCE :-

Clearance is the measure of efficacy of removal of drug from the drug or plasma.

Removal of drug from the body Is mediated by metabolism and excretion.

Volume of distribution:-

V is the apparent volume of body fluids into which a drug distributes at equilibrium. Different drugs have different volume of distribution. Reflecting the extent of partitioning in the tissue relative to plasma .

Therapeutic window:-

The range of plasma concentration b/w the minimal effective concentration associated with the toxicity is called therapeutic window.

During clinical trials,the patients plasma drug concentration to time profile can be draw by measuring the plasma concentration at several time points .

The AUC can be estimated by knowing the bioavailabilty of the drug , the clearance of the drug may be calculated by dividing the dose absorbed by the AUC . the clearance calculated is relatively independent of the shape of conc time profile .this method gives precious information on the pharmacokinetics behavior of drug on trial .it can be used to study the change in the clearance of drug in specific clinical conditions such as any disease.

Experiment # 7

Calculate the value of natural log for x and plot the n on linear graph paper :-

Readings :-

X= 10,20,30,40,50,60,70,80,90,100

X Ln(x)10 2.320 2.930 3.440 3.650 3.960 4.070 4.280 4.390 4.4100 4.6

EXPERIMENT # 8

Estimate the area under the curve :- (AUC)

Theory :-

There are several methods used for estimating area under the concentration time curve .the area under the curve is required to estimate different pharmacokinetic parameters such that bioavailabilty volume of distribution ,clearance and so many other parameters.the most common method used for estimating area under the curve is trapezoid rule . a blood level time curve an be described by each concentration time point the area bounded by trapezoid pproximately the area under the curve greater the numder of data points ,greater will be number of approximation the area of trapezoid is equal to ½ the product of the sumof the area under the drug concentration .

This can be formulated by the following formula that is :

AUC = ½ ( C1+C2)(T2+T1)

ABSOLUTE BIOAVAILABILTY =(AUC) ORAL .DOSE ORAL /(AUC) I/V.DOSE I/V

OBSERVATION TIME PLASMA CONC.

1 0 0.0

2 1 6.6

3 2 8.5

4 3 9.5

5 4 9.4

6 5 8.7

7 8 6.6

8 12 3.7

EXPERIMENT # 9

Calculation of area under the curve using the trapezoid rule.

Time (hrs) Plasma concentration (mg/L)

0 100

1 50

2 25

3 12.5

4 6.25

5 3.13

6 1.56

RESULT :-

As graph shows the given data is of IV route .

Experiment #10

Determine the absolute bioavailability

Theory:-

Absolute bioavailability is the fraction of drug systemically absorbed from the dosage form .it is denoted by “F”

“F” is calculated as the ratio of the area under the curve for the dosage form given orally to the area under the curve obtains after IV administration.

The following data was obtained after IV administration and oral administration and oral administration of drug .the dose of the drug was 50mg by both routes .find the absolute bioavailability of the drug through oral administration.

Time (hr) I/V (ug/ml) PO (ug/ml)

0 0 0

0.25 20 0.8

0.5 18 1.3

0.75 15 2.0

1 12.5 2.1

1.5 9.5 2.7

2 7 3.9

3 3 4.8

4 1.5 4

6 0.5 2.5

8 0.1 0.8

Experiment #11

Determine the absolute bioavailabilty

Theory:-

Absolute bioavailability is the fraction of drug systemically absorbed dosage form is calculated is the ratio of the area under the curve for the dosage form given orally to the area under the curve obtained after the intravenous drug administration.

The following data was obtained after 10 administration and overall administration drug the dose of the drug was 50mg by both routes find the absolute bioavailability of the drug through overall administration.

Time I/V (ug/ml) PO (ug/ml)0 0 00.25 20 0.80.5 18 1.31 12.5 2.01.5 9.5 2.72.0 7 3.93 3 4.84 1.5 46 0.5 2.5

8 0.1 0.8

FORMULA :- F= [AUC]PO/[AUC]IV

Exp 12

Determine the relative bioavailabilty :-

The ory:-

Relative bioavailabilty is the systemic bioavailabilty of the standard drug from a dosage form as compared to reference drug given by the same route of administration.

Following data was obtained by overall administration of drug in tablets and capsule dosage form if the drug was 250mg in both dosage form find the relative bioavailabilty of the drug in tab for the overall administration.

FORMULA:-

Time(hr) P0 tab PO capsule0 0 00.5 0.7 0.81 1.1 1.31.5 1.6 1.752 2.0 2.1

4 1.8 2.96 1.5 1.48 1.15 0.9512 0.55 0.65

Exp# 13

Draw the intravenous bolus graph from the following data :-

Theory :-

When a drug is given in IV bolus and distributed from the blood in to tissue quickly the serum concentration often declines in a straight line when plotted on a semilog graph paper in this case one compartment model intravenous bolus equation can be used

Time (hr) Cp (mg/L)0 01 7.09

2 6.293 5.584 4.956 3.849 2.7112 1.8918 0.9224 0.44

Experiment 14

Determination of various pharmacokinetic parameters of a drug eliminated by 1 st order renal excretion and hepatic circulation:-

The ory :-

Drug clearance is the time measurement of drug elimination from the body without reference to the mechanism of action.

Clearance is defined as volume of fluid (containing drugs) which is cleared a drug per unit of time .

Clearance is equal to

Excretion rate/plasma conc

cl =Ddu/dt/cp

Procedure:- single dose of 100mg of a drug was given orally to a volunteer in systemic availability of drug was determined .the total amount of metabolite recovered in urine was 30mg in total amount of unchanged drug recovered in urine was 60mg.

Calculate the value of total body clearance and non renal clearance of drug .

DISCUSSION:-in case of renal hepatic impairment ,the elimination half life will be prolong resulting in the accumulation of drug in the body .the dosage of this drug must be lowered to prevent the accumulation of the toxic level .

Data given :-

Dose of drug =100mg

Systemic bioavailabilty =90%

Amount of drug excreted in urine = Du=60mg

Amount of drug excreted as metabolite =Dm= 30mg

Elimination of half life of a drug t ½=3.3hours

Apparent volume of distribution =Va=1000mL

Calculation:-

1) Total body clearance= ClT== KVd

= 0.693.vd/t1/2=0.693.1000/3.3

2) Renal clearance :-Cle= KeVdWhere Ke is 0.14hrs-1

=0.14*1000=140mL/hr

3) Hepatic Clearance :-Clh = CLt-CLr

= 210-140= 70mL/hr

Experiment # 15

Water soluble drugs and lipid soluble drugs :-

1) Water soluble drugs :-All inorganic compound that cannot cross the BBB or CNS but absorbed to stomach and intestine and reach to the blood circulation are known as water soluble drugs .Water solubility of drugs depends upon primarily on two factors 1) ionic character 2 hydrogen bonding capacity The presence of O2and nitrogen containing functional group usually enhance the water solubility . water solubility is required for i) Dissolution ii) Preparation of parenteral solutionsiii) Preparation of ophthalmic solution

e.g antacid ,antibiotic,antidiarrhoeal ,antimalarial

2) Lipid soluble drugs:-All the drugs that can cross the BBB and CNS are known as lipid soluble drugs . lipid solubility is enhanced by non ionizable hydrocarbon chain and ring system .Lipid solubility is required for 1) Penetration through lipid by layer in GIT 2) Penetration through BBB3) Preparation of injectibles4) Enhance pulmonary absorbtion with in the respiratory tract

5) Enhance plasma protein binding.