Development and characterization of porous starch curcumin solid dispertion in aproch to inprove solubility and dissolution
1. NAME OF STUDENT
MS. NIKITA D. GIDDE
FINAL YEAR B. PHARM
NAME OF GUIDE
MR. NITIN H. SALUNKHE
(DEPARTMENT OF PHARMACEUTICS)
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2. 1. Introduction
2. Objectives
3. Need of Present investigation
4. Drug Profile
5. Polymer Profile
6. Plan of Work
7. Methodology
8. Result and Discussion
9. Conclusion
10.References
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3. Oral bioavailability of a drug depends on its solubility and dissolution rate. Therefore to
increase dissolution of drug with solubility is often needed.
There are the variety of new drug which having poorly aqueous solubility, out of that
curcumin is one of the example
Curcumin is Poorly aqueous soluble drug which consist some functional groups and
starch consist some hydrophilic groups.
Intermolecular bonding between the functional groups of curcumin and hydrophilic
groups of polymer i.e. starch is carried out by solid dispersion method for the solubility
enhancement.
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4. 1. To prepare the porous starch powder.
2. To prepare and evaluate solid dispersion of curcumin-Starch.
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5. There are variety of new drugs and their derivatives are available. But less than 40
% of lipophilic drugs candidates fail to reach market due to poor bioavailability,
even though these drugs might exhibit potential pharmacodyanamic activities
The lipophillic drug that reaches market requires a high dose to attain proper
pharmacological action.
The basic aim of the further formulation and development is to make that drug
available at proper site of action within optimum dose.
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6. 1. Curcumin is diarylheptanoid.
2. Synonyms: Indian Saffron
3. ChemicalName:1,7-bis(4-hydroxyl-3-Methoxyphenyl)-1,6-heptadiene-3,5-dion
4. Molecular Structure :
5. Molecular Formula: : C21H20O6
6. Molecular weight: 368.38g/mol
7. Melting Point : 1830C
8. Solubility : Poorly Soluble in water.
Soluble in organic solvents like benzene and methanol
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7. 1. Chemical Name : Cornstarch
2. Molecular Formula : C12H48O20
3. Molecular weight : 692.661g/mol
4. Structural Formula :
5. Melting Point : 2560-2580C
6. Density : 1.5g/cm3
7. pH : 6
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8. Plan of work
Literature surve
Experimental
work
A. Authentication of
Pure Curcumin
B. Preparation of
Porous Starch
C. Preparation of
Solid Dispersion of
Curcumin-Starch
D. Evaluation of Solid
Dispersion of
Curcumin-Porous
Starch
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9. B. Preparation of Porous Starch
10 gm starch + 40mL of distilled water at room
temperature.
60 ml distilled water was heated to its boiling point.
Starch dispersion was addedto the boiling water under
rapid stirring.
The temperature was steadily brought down to room
temperature
a translucent gel was formed. The gel was stored in excess
water at 8°C overnight
The gel was then subjected for solvent exchange by
ethanol.
The gel was equilibrated and stored in ethanol at 8°C for 48
h to maintain its porous structure.
After achieving the equilibrium state, the gel was then
dried at 30°C.
The dried material was milled and stored
Porous Starch
Authentic
ation of
Pure
Curcumin
Thermal
Analysis
by using
DSC
Crystallini
ty study
by using
XRD
Compatibi
lity study
by using
FTIR
Determinati
on of
Calibration
Curve
Melting
Point
Solubility
studies
Organolep
tic
characteri
stics
A. Authentication of Pure Curcumin
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10. METHODOLOGY
C. Preparation of Solid Dispersion of Curcumin-
Starch
Batches of solid dispersions for Curcumin were prepared
Drug: Porous Starch (1:0.5, 1:1, 1:2, and 1:3 w/w).
For preparation of ball milled SDs of Curcumin drug
with porous starch were subject to ball milling for 3 h
at 100 rpm[7].
Table No: 1: Different Ratios of Curcumin Solid
Dispersion using Porous Starch
Ratio Curcumin (mg) Porous Starch(gm)
[F1]1:0.5 500 0.250
[F2]1:1 500 0.500
[]F31:2 500 1
[F4]1:3 500 1.5
D. Evaluation of Solid Dispersion of
Curcumin-Porous Starch
1.Micromeritics study
2.Phase Solubility Study
3.Drug Dissolution Study
4.Infra-Red Spectroscopy
5.Crystallinity Study by
1. Powder X-ray
Diffraction(XRD)
2. Differential Scanning
Calorimetry (DSC)
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11. D. Calibration Curve: Straight Line Equation: y= 0.0132x+0.0134
A. Organoleptic
Properties
Color : Yellow
Odour : Earthy
Taste : Bitter
B. Melting Point
Observed value : 1820-
1840C
Reference Value :
1790-1830C
C. Solubility Study
Insoluble : cold water
Soluble : Alcohol,
Very Soluble : Ethanol
0
0.05
0.1
0.15
0.2
0.25
0.3
0.35
0.4
0.45
5 10 15 20 25 30
Absorbance
Concentration(mg/ml)
Sr. No. Concentration (ug/ml) Absorbance
1 0 5 0.081
2 10 0.145
3 15 0.212
4 20 0.277
5 25 0.337
6 30 0.415
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12. RESULT AND DISCUSSION
Batch Code
Angle of
Repose(0)
Bulk Density(gm/cc)
Tapped
Density(gm/cc)
Hausner Ratio Carr’s Index(%)
Curcumin 37.88 0.3488 0.3564 1.194 17.25
F1 32.56 0.3643 0.418 1.143 13.06
F2 33.56 0.2753 0.316 1.147 13.5
F3 34.89 0.334 0.385 1.145 13.32
F4 35.25 0.3716 0.402 1.168 35.25
E. Flow Properties
F. Saturated Solubility Study
solid dispersion increase in the saturation solubility of the drugs.
G. In vitro drug dissolution study
The dissolution profile indicates that porous starch shows better improvement in
dissolution as compared to plain drugs 12
F1 88% dissolution at the end of 120 min
F2, F3, F4 approximately 98 % dissolution at the end of 120 min
F2 ~90 % dissolution at the end of 60 min
14. RESULT AND DISCUSSION
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H. FTIR spectroscopy
The prominent peaks of curcumin exhibited at wave number, which is given in table
respectively.
Porous starch showed the prominent peaks at their respective position. A shift in the peaks
corresponding to O–H stretching of porous starch and curcumin, respectively, indicates a
strong possibility of hydrogen bonding.
O-H stretching 3504.66 cm-1
C=O stretching, ketone 1618.28 cm-1
C=C 1591.27cm-1
15. RESULT AND DISCUSSION
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I.Crystanillity Study
a. Powder X-ray diffraction
The SDs (1:1 w/w) showed a significant reduction in crystalline peaks corresponding to
curcumin, indicating that crystals were transformed to an amorphous or a
microcrystalline form. It means that solid- state interaction between curcumin and
porous starch was observed
16. RESULT AND DISCUSSION
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b. Differential scanning calorimetry (DSC)
The thermograms of curcumin clearly showed sharp endothermic peaks at 173.17 ºC –
180.62 ºC.The Sharp narrow peaks were observed from the thermograms of pure curcumin,
indicating the high crystallinity of the drugs. From the comparison of all thermograms, SDs
(1:1 w/w) showed almost complete reduction of peak area.
Thus, the results of DSC analysis confirm that curcumin is completely converted to
amorphous form and favourable interactions were taking place with porous starch.
17. The solid dispersions of curcumin were successfully prepared by using porous
starch. The developed solid dispersions were characterized with respect to
solubility study, FTIR, dissolution study and crystallinity study (XRD and DSC).
Curcumin-PS systems showed an improved performance as compared to curcumin.
Interestingly, porous starch has been improved solubiliuty of curcumin by one fold.
Thus, PS can be used as a solubility enhancer and carrier for various other drug
candidates.
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