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Nebivolol Hydrochloride

Nebivolol Hydrochloride IDENTIFICATION Name : Nebivolol hydrochloride Chemical Name : ( 1RS,1′RS) - 1,1′ - [(2RS,2′SR)β receptor blocker with nitric oxide - potentiating vasodilatory effect used in treatment of hypertension and also for left ventricular failure It is highly cardioselective under certain circumstances. β1 Selectivity Beta blockers help patients with cardiovascular disease by blocking β1 receptors, while many of the side-effects of these medications are caused by their bl ockade of β2 receptors For this reason, beta blockers that selectively block β1 receptors (termed cardioselective or β1 -selective beta blockers) produce fewer adverse effects (for instance, bronchoconstriction) than those drugs that non-selectively block b oth β1 and β2 receptors. Nebilovol has been marketed by Micro Labs " id="pdf-obj-0-4" src="pdf-obj-0-4.jpg">

IDENTIFICATION

Name

:

Nebivolol hydrochloride

Chemical Name

: (1RS,1′RS)-1,1′-[(2RS,2′SR)-bis(6-fluoro-3,4-dihydro-2H-1- benzopyran-2-yl)] )]- 2,2′-iminodiethanol hydrochloride

Molecular Formula Molecular Weight

Boiling Point (°C) Melting Point (°C)

Appearance

: C 22 H 25 F 2 NO 4 . HCl

441.90

:

:

600.5 °C at 760 mmHg

:

220-222 °C

: White to off-white powder

Nebivolol is a β 1 receptor blocker with nitric oxide-potentiating vasodilatory effect used in treatment of hypertension and also for left ventricular failure It is highly cardioselective under certain circumstances.

β1 Selectivity

Beta blockers help patients with cardiovascular disease by blocking β1 receptors, while many of the side-effects of these medications are caused by their blockade of β2 receptors For this reason, beta blockers that selectively block β1 receptors (termed cardioselective or β1-selective beta blockers) produce fewer adverse effects (for instance, bronchoconstriction) than those drugs that non-selectively block both β1 and β2 receptors. Nebilovol has been marketed by Micro Labs

under the brand name Nebilong; by Forest Laboratories under the name Bystolic; and by Menarini under the names Hypoloc, Lobivon, Nebilet, Nebilox, Nobiten, and Temerit. Micro Labs further ventured into providing a combination with diuretic (hydrochlorothiazide) marketed under the trade name Nebilong-H. In a laboratory experiment conducted on biopsied heart tissue, nebivolol proved to be the most β1-selective of the β-blockers tested, being approximately 3.5 times more β1-selective than bisoprolol .The drug is highly cardioselective at 5 mg However, at doses above 10 mg, nebivolol loses its cardioselectivity and blocks both β1 and β2 receptors.

THERAPEUTIC USES:

Vasodilator action

Nebivolol is unique as a beta-blocker. Unlike carvedilol, it has a nitric oxide (NO)-potentiating, vasodilatory effect. Along with labetalol, celiprolol and carvedilol, it is one of four beta blockers to cause dilation of blood vessels in addition to effects on the heart.

Antihypertensive effect

Nebivolol lowers blood pressure (BP) by reducing peripheral vascular resistance, and significantly increases stroke volume with preservation of cardiac output. The net hemodynamic effect of nebivolol is the result of a balance between the depressant effects of beta-blockade and an action that maintains cardiac output.

Cardiac Arrhythmias

They control ventricular rate in atrial fibrillation and flutter

Congestive heart failure

Although β blockers can acutely worsen heart failure survey studies have reported beneficial haemodynamic effects β1 blockers.

Glaucoma

Ocular β blocker are widely used for chronic simple glaucoma

Myocardial infarction

It has been used for two purpose

  • a. Second prophylaxis of MI i) By preventing reinfarction ii) By preventing sudden ventricular fibrillation at the second attack

  • b. Myocardial salvage during evolution of MI i) By preventing arrthythmias including ventricular fibrillation ii) May boundary infarct size by reducing O2 consumption

Side-effects

Several studies have suggested that nebivolol has reduced typical beta-blocker-related side effects, such as fatigue, clinical depression, bradycardia, or impotence.

In <a href=chemistry , spectrophotometry is the quantitative measurement of the reflection or transmission properties of a material as a function of wavelength. It is more specific than the general term electromagnetic spectroscopy in that spectrophotometry deals with visible light, near - ultraviolet , and near - infrared , but does not cover time-resolved spectroscopic techniques. Spectrophotometry involves the use of a spectrophotometer. A spectrophotometer is a photometer (a device for measuring light intensity) that can measure intensity as a function of the light source wavelength. Important features of spectrophotometers are spectral bandwidth and linear range of absorption or reflectance measurement. The use of spectrophotometers spans various scientific fields, such as physics , materials science , chemistry , biochemistry , and molecular biology . They are widely used in many industries including semiconductors, laser and optical manufacturing, printing and forensic examination, as well in laboratories for the study of chemical substances. Ultimately, a spectrophotometer is able to determine, depending on the control or calibration, what substances are present in a target and exactly how much through calculations of observed wavelengths. " id="pdf-obj-2-2" src="pdf-obj-2-2.jpg">

In chemistry, spectrophotometry is the quantitative measurement of the reflection or transmission properties of a material as a function of wavelength. It is more specific than the general term electromagnetic spectroscopy in that spectrophotometry deals with visible light, near-ultraviolet, and near-infrared, but does not cover time-resolved spectroscopic techniques.

Spectrophotometry involves the use of a spectrophotometer. A spectrophotometer is a photometer (a device for measuring light intensity) that can measure intensity as a function of the light source wavelength. Important features of spectrophotometers are spectral bandwidth and linear range of absorption or reflectance measurement.

The use of spectrophotometers spans various scientific fields, such as physics, materials science, chemistry, biochemistry, and molecular biology. [4] They are widely used in many industries including semiconductors, laser and optical manufacturing, printing and forensic examination, as well in laboratories for the study of chemical substances. Ultimately, a spectrophotometer is able to determine, depending on the control or calibration, what substances are present in a target and exactly how much through calculations of observed wavelengths.

There are two major classes of devices: single beam and double beam. A double beam spectrophotometer

There are two major classes of devices: single beam and double beam. A double beam spectrophotometer compares the light intensity between two light paths, one path containing a reference sample and the other the test sample. A single beam spectrophotometer measures the relative light intensity of the beam before and after a test sample is inserted. Although comparison measurements from double beam instruments are easier and more stable, single beam instruments can have a larger dynamic range and are optically simpler and more compact. Additionally, some specialized instruments, such as spectrophotometer built onto microscopes or telescopes, are single beam instruments due to practicality.

In short, the sequence of events in a modern spectrophotometer is as follows:

  • 1. The light source is imaged upon the sample

  • 2. A fraction of the light is transmitted or reflected from the sample

  • 3. The light from the sample is imaged upon the entrance slit of the monochromator

  • 4. The monochromator separates the wavelengths of light and focuses each of them onto the photodetector sequentially

EXPERIMENT INVESTIGATION OF NEBIVOLOL HYDRO CHLORIDE BY SPECTROPHOTOMETRIC DETERMINATION

About 100 mg of nebivolol Hydrochloride pure drug was accurately weighed and dissolved in water and volume made upto 100ml with water (1mg/ml).the final concentration of nebivolol Hydrochloride was made to 100mcg/ml with water by dilution. For formulation analysis, 20 tablets of nebivolol Hydrochloride each containing 5mg were accurately weighed and powdered. An amount equivalent to100mg nebivolol Hydrochloride was weighed and dilutions were made suitably.

ASSAY METHOD

Aliquots of nebivolol hydrochloride ranging from 0.2-1.0ml (1ml=100mcg) were transferred into series of 10ml volumetric flask .To each flask 0.5ml of ferric chloride,1.0ml of 1,10-phenanthroline were added and heated for 30min on water bath at 95degree,cooled to room temperature.The volumes were made upto the mark with water.the absorbance of the red colored chromogen was measured at 509nm against reagent blank. The colored species was stable for more than 4hr.The amount of nebivolol hydrochloride present in the sample was computed from calibration curve.

RESULTS AND DISCUSSION

The optical characteristics such as absorption maxima, beer’s law limit,molar absoptivity and sandell’s

sensitivity are presented in table I.

PARAMETERS

METHOD

Lamda nm

509

Beer’s law limit(mcg/ml)

Molar absorptivity(L1/mol.1/cm)

4.425x10x10x10

Sandell’s sensitivity(mcg/ml/cm2/

0.01

absorbance unit)

regression equation(y*) Slope(b)

0.0491

Intercept(a)

0.0161

Correlation coefficient(r)

0.9986

%RSD**

1.160

Range of errors** Confidence limits with 0.05 level

0.00562

Confidence limit with 0.01 level

0.00825

Y=bC+a

Where C is the concentration of nebivolol hydrochloride in mcg/ml and Y is the absorbance at the respective lamda max, for eight measurements

TABLE II: Evaluation of nebivolol hydrochloride in pharmaceutical dosage form

Formulation

Labeled

Amount obtained

Percentage

Amount

by proposed

Recovery**

(mg/tab)

method

S.D

Tablet(Nebicard)

5

  • 4.89 99.77

 

Tablet(nebilong)

5

  • 4.95 99.81

0.043

Tablet(nebitime)

5

  • 4.92 98.79

0.035

d

The percent relative standard deviation and percent range of error(0.05 and 0.01 level of confidence

limits) calculated from the 8measurement at ¾ of the upper beer’s law limit of nebivolol hydrochloride

are shown in table I. The results shown that this method has reasonable precision. The result of analysis

of tablet formulation are done at three levels recorded in tablet II.To evaluate the validity and reproducibility of the methods, known amounts of the pure drug were added to the previously analysed by the proposed methods.Interference studies revealed that the common excipients and other additives are usually present in the tablet dosage forms and they did not interfere at their regularly added levels

The proposed method were found to be simple,sensitive,selective,accurate precise and economical and can be used for determination of nebivolol hydro chloride in bulk drug and its pharmaceutical dosage form in a routine manner Severe allergic reactions (rash; hives; itching; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue; unusual hoarseness); chest pain or tightness; fainting; mental or mood changes; numbness or tingling of the hands; persistent or severe vision changes; red, swollen, blistered, or peeling skin; severe dizziness; shortness of breath or wheezing; sudden, unusual weight gain; swelling of the hands, ankles, or feet; unusual bruising or bleeding; unusual tiredness or weakness; unusually slow or irregular heartbeat; very cold or blue fingers or toes.

s

of tablet formulation are done at three levels recorded in tablet II.To evaluate the validity andcuvette of width ℓ . The law states that there is a logarithmic dependence between the transmission (or transmissivity), T , of light through a substance and the product of the absorption coefficient of the substance, α , and the distance the light travels through the material (i.e., the path length), ℓ . The absorption coefficient can, in turn, be written as a product of " id="pdf-obj-6-8" src="pdf-obj-6-8.jpg">

beer,s lambert law in solution

An example of BeerLambert law, a green laser lighting in a solution of Rhodamine 6G, the beam beco

Diagram of BeerLambert absorption of a beam of light as it travels through a cuvette of width .

of tablet formulation are done at three levels recorded in tablet II.To evaluate the validity andcuvette of width ℓ . The law states that there is a logarithmic dependence between the transmission (or transmissivity), T , of light through a substance and the product of the absorption coefficient of the substance, α , and the distance the light travels through the material (i.e., the path length), ℓ . The absorption coefficient can, in turn, be written as a product of " id="pdf-obj-6-24" src="pdf-obj-6-24.jpg">

The law states that there is a logarithmic dependence between the transmission (or transmissivity), T, of light through a substance and the product of the absorption coefficient of the substance, α, and the distance the light travels through the material (i.e., the path length), . The absorption coefficient can, in turn, be written as a product of

either a molar absorptivity (extinction coefficient) of the absorber, ε, and the molar concentration c of absorbing species in the material, or an absorption cross section, σ, and the (number) density N' of absorbers. example of BeerLambert law: green laser light in a solution of Rhodamine 6B. The beam intensity becomes weaker as it passes through solution