The document discusses the preparation and characterization of an inclusion complex of glaucocalyxin-A (GLA) with sulfobutylether-β-cyclodextrin (SBE-B-CD) to improve its water solubility. A 1:1 molar ratio complex was formed using co-evaporation. Solubility of GLA increased 76-fold in the complex. Analysis showed effective encapsulation of GLA in SBE-B-CD. A pharmacokinetic study in rats found the complex had a 3-fold higher AUC and significantly prolonged half-life compared to free GLA, indicating longer retention in the body. The complex is an effective way to improve the solubility and
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Drug stability:Stabilization of medicinal agents against common reactions like hydrolysis & oxidation. Accelerated stability testing in expiration dating of pharmaceutical dosage forms. Photolytic degradation and its prevention.
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Decomposition and stabilization of pharmaceutical productsArshad Khan
Drug stability:Stabilization of medicinal agents against common reactions like hydrolysis & oxidation. Accelerated stability testing in expiration dating of pharmaceutical dosage forms. Photolytic degradation and its prevention.
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Polymers Used in Pharmaceutical SciencesOyshe Ahmed
INTRODUCTION
CLASSIFICATION AND CHARACTERISTICS OF POLYMERS
MECHANISM OF DRUG RELEASE FROM POLYMER
BIO DEGRADATION OF POLYMERS
SYNTHESIS OF POLYMERS
POLYMERS USED IN FORMULATION OF DIFFERENT DRUG DELIVERY SYSTEM.
APPLICATION OF POLYMERS
An excipient is generally a pharmacologically inactive substance used as a carrier for the active ingredients of a medication
EXCIPIENTS USED IN LIQUID DOSAGE FORMS:
Solvents/co-solvents ,
Buffering agents,
Preservatives,
Anti-oxidants,
Humectants,
Wetting agents,
Anti-foaming agents,
Thickening agents,
Sweetening agents,
Flavouring agents,
EXCIPIENTS USED IN TABLETS:
Binders
Coatings
Disintegrants
Fillers
Flavours
Colours
Lubricants
Glidants
Preservatives
Sweeteners
It is a Complexaing agent.
Synonym: cavitron, cycloamyloses, cycloglucan, cyclic oligosaccharide
It is a important for increasing the solubility of poorly water soluble drugs.
Cyclodextrines are produced from starch by means of enzymatic conversion.
They are used in food, pharmaceutical, drug delivery, and chemical industries, as well as agriculture and environmental engineering.
Cyclodextrines are composed of 5 or more α-D glucopyranoside units linked 1->4, as in amylose linkage.
Cyclodextrines contains 32 1,4-anhydroglucopyranoside units, while as a poorly characterized mixture, at least 150-membered cyclic oligosaccharides are also known. Typical cyclodextrins contain a number of glucose monomers ranging from six to eight units in a ring.
CDs, with lipophilic inner cavities & hydrophilic outer surfaces, are interacting with a guest molecule to form non covalent inclusion complexes.
Today CDs are only synthesized either by fermentation or enzymatically.
Many CGTases from different microorganisms are known, cloned, sequenced, characterized and used for production of CDs.
Polymers Used in Pharmaceutical SciencesOyshe Ahmed
INTRODUCTION
CLASSIFICATION AND CHARACTERISTICS OF POLYMERS
MECHANISM OF DRUG RELEASE FROM POLYMER
BIO DEGRADATION OF POLYMERS
SYNTHESIS OF POLYMERS
POLYMERS USED IN FORMULATION OF DIFFERENT DRUG DELIVERY SYSTEM.
APPLICATION OF POLYMERS
An excipient is generally a pharmacologically inactive substance used as a carrier for the active ingredients of a medication
EXCIPIENTS USED IN LIQUID DOSAGE FORMS:
Solvents/co-solvents ,
Buffering agents,
Preservatives,
Anti-oxidants,
Humectants,
Wetting agents,
Anti-foaming agents,
Thickening agents,
Sweetening agents,
Flavouring agents,
EXCIPIENTS USED IN TABLETS:
Binders
Coatings
Disintegrants
Fillers
Flavours
Colours
Lubricants
Glidants
Preservatives
Sweeteners
It is a Complexaing agent.
Synonym: cavitron, cycloamyloses, cycloglucan, cyclic oligosaccharide
It is a important for increasing the solubility of poorly water soluble drugs.
Cyclodextrines are produced from starch by means of enzymatic conversion.
They are used in food, pharmaceutical, drug delivery, and chemical industries, as well as agriculture and environmental engineering.
Cyclodextrines are composed of 5 or more α-D glucopyranoside units linked 1->4, as in amylose linkage.
Cyclodextrines contains 32 1,4-anhydroglucopyranoside units, while as a poorly characterized mixture, at least 150-membered cyclic oligosaccharides are also known. Typical cyclodextrins contain a number of glucose monomers ranging from six to eight units in a ring.
CDs, with lipophilic inner cavities & hydrophilic outer surfaces, are interacting with a guest molecule to form non covalent inclusion complexes.
Today CDs are only synthesized either by fermentation or enzymatically.
Many CGTases from different microorganisms are known, cloned, sequenced, characterized and used for production of CDs.
Cyclodextrins merupakan senyawa polisiklik kompleks yang terbentuk dari 6 sampai 8 molekul glukosa yang diikat oleh ikatan glikosida. Senyawa ini berbentuk seperti tabung tanpa tutup dengan rongga ditengahnya. Berdasarkan struktur kimianya, pada bagian dalam rongga bersifat hydrophobic dan bersifat hydrophylic pada permukaan luar rongganya.
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Preparation and Characterization of Cyclodextrin Inclusion Complexes for Impr...Jing Zang
Nimesulide (4'-nitro-2'-phenoxy methane sulfonanilide) is a selective cyclooxygenase-2 inhibitor and one of the potent non steroidal anti-inflammatory drugs (NSAIDs). It is practically insoluble in water and hence has a low bioavailability. To improve solubility and dissolution of nimesulide, its β-cyclodextrin complex were prepared.
Nimesulide was complexed with β-cyclodextrin in 1:1, 1:2 and 1:3 molar ratios using solvent evaporation method with the addition of freeze drying. The prepared inclusion complexes were evaluated for solubility, scanning electron microscopy (SEM), differential scanning calorimetry (DSC), X ray powder diffraction (XRPD) and in vitro dissolution study. All the complexes showed about up to 12 fold increase in solubility. The complex prepared in 1:3 ratios showed the greatest improvement in solubility (from 9.67 to 108.60 μg/ml). In SEM, the complexes showed irregular disc shaped non-porous surface. XRPD data indicated that maximum amorphization was induced in the complex prepared with 1:2 ratio. The DSC data confirmed the formation of inclusion complex. The dissolution of the drug in the complexes was also found to be improved. Complex prepared by solvent evaporation method in 1:2 molar ratio showed a marked improvement in dissolution profile (complete release in just 30 minutes) than that of pure drug which showed just 60.02 % drug release at the end of 3 hour. It was concluded that the β-cyclodextrin complex made in 1:2 molar ratio showed good solubility and the dissolution profile as compared to the complex made in 1:1 and 1:3 molar ratio. It was concluded that the complex prepared by solvent evaporation method with 1:2 molar ratio showed the best performance with respect to great improvement in solubility, the best amorphization and the best in vitro dissolution profile as compared to other complexes.
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RESEARCH ARTICLE ON INCLUSION COMPLEX WITH SBE-B-CD
1. Preparation, characteristic and pharmacology study on inclusion
complex of sulfobutylether-b-cyclodextrin witH glaucocalyxin-A
2. INTRODUCTION
The objective of this study was to improve the water
solubility and solubility of glaucocalyxin-A by
producing its complex with SBE-B-CD.
Solubility of GLA and its complex were 2.4 x 10² and
1.82x10⁴ug/ml, respectively, and the value of
incusion complex was improved by 76 fold compared
with solubility of free GLA.
3. WHY SOLUBILITY ENHANCEMENT
Solubility the phenomenon of dissolution of solute in
solvent to give a homogeneous system
Important to achieve desired conc. Of drug to show
pharmacological response in systemic circulation.
Insufficient disso rate of the drug is limiting factor in
oral availability of poorly water soluble drug.
Any drug to be absorbed must be prsent in
aqueous form at the site of absorption.
4. COMPLEXATION
Hydrophobic molecules are incorporated in cavity of CD
by displacing water . The reaction is followed by
repulsion of the molecule by water.
Effective encapsulation of molecule occur.
5. CYCLODEXTRIN
They are cycloamyloses family of compounds
made up of sugar molecule bound together in a ring.
they are hydrophobic inside and hydrophilic outside.
hydrophilic to
impart CD
water
solubility.
less hydrophilic than aq. Solvent.
6. cyclodextrin were called cellulosine in 1891.
Schardinger identified naturallyn occuring α,β,γ
cyclodextrins-SCHARDINGER SUGAR.
WHY β-CD USED?
α-CD-6 glucopyranose units. Small cavities not capable of
accepting many molecule.
γ-CD-8 glucopyranose units. larger cavities than many
molecules to be incorporated and CD hydrophobic charges
cannot effectively interact to facilitate complexation.
β-CD- 7 glucopyranose units. cavity diameter most appropriate
site for hormones,vitamins, other compound frequently used.
Β,α,γ-CD ARE GENERALLY REGARDED AS SAFE.
7. SYNTHESIS OF CD
STARCH
enzymatic conversion
LIQUID PRODUCT
CGTase synthesise all form of CD,product of
conversion result in mix. of 3 main type of cyclic
molecule in ratio strictly dependent on enzyme used.
β-CD has v.poor water solubilty,can be retrieved through
crystallisation while α and γ purified by
chromatography.
8. CHEMICALLY MODIFIED CD
Different chemical moieties introduced into CD
molecule by reaction with OH group lining upper and
lower ridge of toroid. Ex.
Hydroxypropyl-β-CD:CH₂CHOHCH₃
Diethyl-β-CD:CH₃CH₃
Sulfobutylether-β-CD:(CH₂)₄SO₃Na
CD-3n substituents, n=no.of glucopyranose units.
Randomness of position and type of subs. cause
resultant CD pdk to be amorphous i.e.
AQUEOUS SOLUBILITY.
Maximum degree of substitution-21-for β-CD.
9. RELEASE OF DRUG MOIETY
MECHANISM of controlled degradation of such
complex based on ph, change of water solution leading
to loss of hydrogen or ionic bond between host and
guest molecule.
Alternative means-
1. by heating
2. enzymatic cleavage of α-1,4 linkage between glucose
monomer .
10. ADVANTAGES OF COMPLEXATION WITH CD
a) Imp. Comp like vitamins & hormones having low
solubility get solubilised.
b) Used as carriercaaaaaaaaaaaaaaaaaaaa carrier.
c) α & γ- food-soluble
dietary fibre –can be
found as a-CD on list of
ing.of commercial pdks.
d) β-CD-complex with caretenoid food colorant –intensify
color by increasing water solubility and improving light
stability
e) Inclusion compd CD penetrate body tissues,
f) Aq.solubility enhancement by CD diff than co-solvent
and surfectant.
Surfectant-toxicity. Co solvent-enhance solubility nonlinearly
11. SULFOBUTYLETHER-β-CD
CAPTISOL
Polyanionic variably substituted
sulfobutylether of β-CD as non
nephrotoxic.
Interact v.well with neutral drug
to facilitate solu and stability .
Polyanionic interact well with
cationic drug.
Complex disso rapidly after
parentral administration to have
no tissue-irritating effect,no
advrse effect on kidney,or other
organs following i.v.
Provide protective effect against
drug induced cytotoxicity.
12. GLAUCOCALYXIN-A
BIO-ACTIVE ent-kauranoid
diterpenoid.
Have v.poor water solubility
USES:
Inhibit tumour cell proliferation
Inhibit platelet aggregation
Immunosuppression
Antioxidative
DNA-protective activity.
Earlier complex of GLA with HP-β-
CD lead to increase in solubilty by
only 13 fold.
13. Rabdosia japonica
GLA isolated from leaves of
Rabdosia japonica,chinese
herb
o Family-
lamiaceae,Rabdosia.
o Perennial herb
Leaves contain
GLA,sitosterol,ursolic acid.
• USES:
• Gastric &abdominal swelling
pain
• Bites by insects &snakes
• jaundice
14. 1:1 molar ratio GLA-SBE-B-CD inclusion complex was
prepared using CO-EVAORATED METHOD.
Weighed amount of SBE-B-CD was dissolved in water
Solution of GLA in ethanol was added slowly to SBE-B-
CD Solution
Suspension stirred at RT for 24h.
Fitered through 0.22um filter
Dried under reduced pressure for 12h in vacuum
dessicator.
SOLID COMPLEX
Method is simple & economical on lab and large scale.
15. ANALYSIS OF COMPLEX
Chromatography
Solubility study
Phase solubility
UV
Thermal analysis
Fourier transform infrared spectroscopy
Powder X-ray diffraction
Proton nuclear magnetic resonance spectroscopy
Pharmocokinetic study
16. Solubility study
Excess GLA
added
10 ml of
water in
vials
Mixture
agitated at
25˚C for 24 h.
Filtered
through
0.22um
membrane
Drug conc
determind
by HPLC
17. PHASE SOLUBILITY STUDY
Purified water
+various conc
of captisol(0-
10mM)
Excess GLA
Mixture stirred
at 35˚C for
24h.
Cooled to RT&
filtered through
0.45um filter.
GLA conc
measured
using HPLC
18. DISSOLUTION STUDY
Rotation -50 rpm
Temperature 25±0.5˚C
Conc-1mg GLA
RESULTS
a) PHASE SOLU.
LINEAR PORTION-A1 TYPE C
complex.
Kc of complexes
134.9/M
25. PHARMACOKINETIC STUDY
24 male sprague rats taken
All rats assigned in 2 groups (n=12/group)
Single iv dose given
Blood samples at 5,10,15,30,45,60,90 min
withdrawn
Plasma separated by centrifugation
Plasma conc with respect to time was plotted
Maximum plasma drug conc,time to reach
it,elimination half life,mean residence
time,systemic clearance was measured.
26.
27. Plasma AUC₀₋∞ of
complex was 3 fold
greater than free GLA.
HALF LIFE of complex
was significantly
prolonged than free
GLA.
THUS FORMULATION
OF GLA-SBE-B-CD
COMPLEX WAS
RETAINED FOR A
LONGER PERIOD
COMPARED WITH
FREE GLA INJECTION
SOLUTION.
28. CAPTISOL & HP-B-CD –CLEARED safety studies & used in 6
product approved by FDA.
Vfend (iv voriconazole; captisol)
Geodon (im ziprazidone)
Abilify (im aripiprazole)
Ceremia (sc maropitant)
Sporanpox (iv & liq itraconazole ; HP-B-CD)
HP-B-CD-approved for administration in brain-OMMAYA
RESERVOIR-to treat NEIMAN-PICK-TYPE-DISEASE
29. CYCLODEXTRINS are gaining popularity day by day & many
researchers pay great emphasis on this approach.
The solubility & disso behaviour of complex was improved.
Sustain delivery of drug observed
Thermal methods are best method to characterise complexes & CD
Not much compounds have been complexed with captisol
Research can be done for inclusion complex of any other bioactive
drug having solubility problem with captisol.
Analyse the complex to check the enhancement in solubility of the
guest molecule and hence its action.
This inclusion complex aids strategies to produce more effective and
marketable drugs.