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PROGRESS REPORT
ON
PREPARATION AND EVALUATION OF SOLID DISPERSION OF
SIMVASTATIN
PRESENTED BY:-
M.PHARM 2nd YEAR
PHARMACEUTICS
GUIDED BY:-
VANDANA ARORA SETHI
ASSOCIATE PROFESSOR
LLOYD INSTITUTE OF MANAGEMENT AND
TECHNOLOGY
GREATER NOIDA
SOLID DISPERSION
The term solid dispersion refers to group of solid products consisting of at least two different components,
generally a hydrophilic matrix and hydrophobic drugs .
Solid dispersion technology is the science of dispersing one or more active ingredients in an inert matrix in
the solid stage in order to achieve increased dissolution rate, sustained release of drugs, altered solid state
properties, enhance release of drugs from ointment and suppository bases, and improved solubility and
stability.
Solid dispersion can be prepared by various methods such as solvent evaporation and melting method. Solid
dispersion technique has been extensively used to increase the solubility of a poorly water-soluble drug.
According to this method, a drug is thoroughly dispersed in a water-soluble carrier by suitable method of
preparation. The mechanism by which the solubility and the dissolution rate of the drug are increased
includes: reduction of the particle size of drug to submicron size or to molecular size in the case where solid
solution is obtained. The particle size reduction generally increases the rate of dissolution; secondly, the drug
is changed from amorphous to crystalline form, the high energetic state which is highly soluble; finally, the
wetting ability of the drug particle is improved by the hydrophilic carrier.
HYPERLIPIDEMIA
The term Hyperlipidemia is used generally to describe the increased level of lipids, lipoproteins,
Tryglycerides, cholesterol etc. in the blood.
At the erlier stages of research scientists found that the endothelium normally influences the behavior of
arterial smooth muscle cells by providing a barrier to the passage of plasma proteins, and that the major effect
of hemodynamic or other factors that injure the endothelium is to reduce the effectiveness of the barrier. But
now we know that higher lipids level, especially cholesterol and triglycerides leads to hyperlipidemia which
ultimately speeds up the process of atherosclerosis and disease associated with it. Arteries are normally
smooth and unobstructed on the inside, but in case of increased lipid level, a sticky substance called plaque is
formed inside the walls of arteries. This leads to reduced blood flow, leading to stiffening and narrowing of the
arteries.
It has been proved that elevated plasma levels of cholesterol and of LDL are responsible for atherosclerosis in
man, and epidemiological data suggests that elevated plasma levels of HDL have a protective effect.
OBJECTIVES
The main objectives of carrying this study are as follows:-
• To study about the Solid Dispersion.
• To improve the solubility of drug by formulating solid dispersion.
• To determine the preparation of solid dispersion of simvastatin.
• To determine the evaluation of solid dispersion of simvastatin.
PREFORMULATION STUDIES
ORGANOLEPTIC PROPERTIES OF DRUG:-
• Colour : White
• Odour : Odourless
• Taste : Bitter
MELTING POINT:-
• Melting point of drug was found to be 1120C to 1250C.
SOLUBILITY STUDIES:-
• Methanol : Soluble
• Water : Insoluble
• Chloroform: Freely Soluble
• Acetone : Sparingly Soluble
DETERMINATION OF ƛmax:-
• From the prepared stock solution of Simvastatin the scanning was performed on UV-VIS Spectrophotometer
to find out ƛmax at200-400nm and ƛmax was found to be 238nm.
CONTINUATION …
CALIBRATION CURVE OF SIMVASTATIN IN CHLOROFORM:-
The samples of concentration 1-9µg/ml prepared from stock solution were analyzed on ƛmax 238nm
against chloroform as blank (reference) and absorbance found in process.
Each value represents absorbance at Λ max 238nm and each sample concentration were
1µg/ml, 2µg/ml, 3µg/ml, 4 µg/ml, 5µg/ml,6 µg/ml, 7µg/ml, 8µg/ml,9µg/ml. these samples were
analyzed at UV-Spectrophotometer against chloroform as blank. The calibration curve is plotted
by using following data of absorbance.
Concentration (µg/ml) Absorbance
1 0.034
2 0.110
3 0.173
4 0.243
5 0.302
6 0.373
7 0.452
8 0.534
Table for Calibration Curve
CONTINUATION …
0.034
0.106
0.173
0.238
0.297
0.37
0.45
0.53
0.62
0
0.1
0.2
0.3
0.4
0.5
0.6
0.7
0 1 2 3 4 5 6 7 8 9 10
Absorbance
Concentration (microgram/ml)
Calibration curve graph
METHODS OF PREPARATION
There are several methods which are being used for preparation of solid dispersion worldwide, like
Melting method, Melt agglomeration method, Solvent evaporation method, hot melt extrusion method, etc.
selection of appropriate method is done according to the pre-formulation study data.
MELTING METHOD:-
Also known as Fusion method or Physical mixing process is the simplest and the oldest way of preparing
solid dispersion. In this method physical mixture of solid drug and carrier are taken and melted, followed
by the rapid cooling action (solidification) either by using ice bath or some other cooling techniques.
Continuous mixing or stirring is given throughout the process and the solidified mass is then removed from
beaker and crushed properly and sieved.
FORMULA TABLE:-
Polymer-drug ratio for developing solid dispersion were taken according the formula table.
S No. Formulation code Drug (Simvastatin) mg Polymer
(PEG6000) mg
Drug-Polymer
ratio
1 F1 100 2000 1:20
2 F2 100 2500 1:25
3 F3 100 3350 1:33.5
4 F4 100 5000 1:50
5 F5 100 10000 1:100
WORK REMAINING
• IR-Spectrophotometry.
• Final formulation development.
• Evaluation of formulation.
1. Bulk Density
2. Tapped Density
3. Hausner’s Ratio
4. Percentage Yield
5. Drug Content
6. In-Vitro Drug Release Study
• Result and Discussion.
• Summary and Conclusion.
THAT’S ALL FOR THE DAY
THANK YOU

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Progress Report M.Pharm

  • 1. PROGRESS REPORT ON PREPARATION AND EVALUATION OF SOLID DISPERSION OF SIMVASTATIN PRESENTED BY:- M.PHARM 2nd YEAR PHARMACEUTICS GUIDED BY:- VANDANA ARORA SETHI ASSOCIATE PROFESSOR LLOYD INSTITUTE OF MANAGEMENT AND TECHNOLOGY GREATER NOIDA
  • 2. SOLID DISPERSION The term solid dispersion refers to group of solid products consisting of at least two different components, generally a hydrophilic matrix and hydrophobic drugs . Solid dispersion technology is the science of dispersing one or more active ingredients in an inert matrix in the solid stage in order to achieve increased dissolution rate, sustained release of drugs, altered solid state properties, enhance release of drugs from ointment and suppository bases, and improved solubility and stability. Solid dispersion can be prepared by various methods such as solvent evaporation and melting method. Solid dispersion technique has been extensively used to increase the solubility of a poorly water-soluble drug. According to this method, a drug is thoroughly dispersed in a water-soluble carrier by suitable method of preparation. The mechanism by which the solubility and the dissolution rate of the drug are increased includes: reduction of the particle size of drug to submicron size or to molecular size in the case where solid solution is obtained. The particle size reduction generally increases the rate of dissolution; secondly, the drug is changed from amorphous to crystalline form, the high energetic state which is highly soluble; finally, the wetting ability of the drug particle is improved by the hydrophilic carrier.
  • 3. HYPERLIPIDEMIA The term Hyperlipidemia is used generally to describe the increased level of lipids, lipoproteins, Tryglycerides, cholesterol etc. in the blood. At the erlier stages of research scientists found that the endothelium normally influences the behavior of arterial smooth muscle cells by providing a barrier to the passage of plasma proteins, and that the major effect of hemodynamic or other factors that injure the endothelium is to reduce the effectiveness of the barrier. But now we know that higher lipids level, especially cholesterol and triglycerides leads to hyperlipidemia which ultimately speeds up the process of atherosclerosis and disease associated with it. Arteries are normally smooth and unobstructed on the inside, but in case of increased lipid level, a sticky substance called plaque is formed inside the walls of arteries. This leads to reduced blood flow, leading to stiffening and narrowing of the arteries. It has been proved that elevated plasma levels of cholesterol and of LDL are responsible for atherosclerosis in man, and epidemiological data suggests that elevated plasma levels of HDL have a protective effect.
  • 4. OBJECTIVES The main objectives of carrying this study are as follows:- • To study about the Solid Dispersion. • To improve the solubility of drug by formulating solid dispersion. • To determine the preparation of solid dispersion of simvastatin. • To determine the evaluation of solid dispersion of simvastatin.
  • 5. PREFORMULATION STUDIES ORGANOLEPTIC PROPERTIES OF DRUG:- • Colour : White • Odour : Odourless • Taste : Bitter MELTING POINT:- • Melting point of drug was found to be 1120C to 1250C. SOLUBILITY STUDIES:- • Methanol : Soluble • Water : Insoluble • Chloroform: Freely Soluble • Acetone : Sparingly Soluble DETERMINATION OF ƛmax:- • From the prepared stock solution of Simvastatin the scanning was performed on UV-VIS Spectrophotometer to find out ƛmax at200-400nm and ƛmax was found to be 238nm.
  • 6. CONTINUATION … CALIBRATION CURVE OF SIMVASTATIN IN CHLOROFORM:- The samples of concentration 1-9µg/ml prepared from stock solution were analyzed on ƛmax 238nm against chloroform as blank (reference) and absorbance found in process. Each value represents absorbance at Λ max 238nm and each sample concentration were 1µg/ml, 2µg/ml, 3µg/ml, 4 µg/ml, 5µg/ml,6 µg/ml, 7µg/ml, 8µg/ml,9µg/ml. these samples were analyzed at UV-Spectrophotometer against chloroform as blank. The calibration curve is plotted by using following data of absorbance. Concentration (µg/ml) Absorbance 1 0.034 2 0.110 3 0.173 4 0.243 5 0.302 6 0.373 7 0.452 8 0.534 Table for Calibration Curve
  • 7. CONTINUATION … 0.034 0.106 0.173 0.238 0.297 0.37 0.45 0.53 0.62 0 0.1 0.2 0.3 0.4 0.5 0.6 0.7 0 1 2 3 4 5 6 7 8 9 10 Absorbance Concentration (microgram/ml) Calibration curve graph
  • 8. METHODS OF PREPARATION There are several methods which are being used for preparation of solid dispersion worldwide, like Melting method, Melt agglomeration method, Solvent evaporation method, hot melt extrusion method, etc. selection of appropriate method is done according to the pre-formulation study data. MELTING METHOD:- Also known as Fusion method or Physical mixing process is the simplest and the oldest way of preparing solid dispersion. In this method physical mixture of solid drug and carrier are taken and melted, followed by the rapid cooling action (solidification) either by using ice bath or some other cooling techniques. Continuous mixing or stirring is given throughout the process and the solidified mass is then removed from beaker and crushed properly and sieved. FORMULA TABLE:- Polymer-drug ratio for developing solid dispersion were taken according the formula table. S No. Formulation code Drug (Simvastatin) mg Polymer (PEG6000) mg Drug-Polymer ratio 1 F1 100 2000 1:20 2 F2 100 2500 1:25 3 F3 100 3350 1:33.5 4 F4 100 5000 1:50 5 F5 100 10000 1:100
  • 9. WORK REMAINING • IR-Spectrophotometry. • Final formulation development. • Evaluation of formulation. 1. Bulk Density 2. Tapped Density 3. Hausner’s Ratio 4. Percentage Yield 5. Drug Content 6. In-Vitro Drug Release Study • Result and Discussion. • Summary and Conclusion.
  • 10. THAT’S ALL FOR THE DAY THANK YOU