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SELF EMULSIFIED DRUG DELIVERY
SYSTEM (SEDDS)
Presented By
B. Swadeep M.pharm.,
Mobile No 9032638446
M.R. COLLEGE OF PHARMA...
CONTENTS
 INTRODUCTION
 LIPID FORMULATION
CLASSIFICATION SYSTEM
 FORMULATION DEVELOPMENT
 SOLID SELF EMULSIFYING DRUG
...
INTRODUCTION
 Poor drug solubility is a frequently encountered
problem for pharmaceutical formulation scientists,
since m...
DEFINITION
SEDDS are isotropic mixtures of drug, lipids and
surfactants, usually with one or more hydrophilic co-
solvents...
MECHANISM
According to Reiss:
self-emulsification occurs when the entropy
change that favors dispersion is greater than
th...
LIPID FORMULATION
CLASSIFICATION SYSTEM (LFCS)
TYPE 1
DRUG
+
LIPID
+
LIPOPHILIC
SURFACTANT
HLB< 12
DRUG
+
LIPID
DRUG
+
LIP...
Conducting
binary
screening
Suitable
formulation
technique
Invivo
performance
Optimizing
the
formulation
FORMULATION DEVEL...
EXCIPIENTS
LIPIDS SURFACTANTS COSOLVENTS
Solubilize
lipophilic drug
Promotes
lymphatic
transport
protection of
drugs
Eg: C...
1.Retards
gastric
emptying
2.Simulation
of bile
3.Pancreatic
secretion
4.Membrane
lipid fluidity
5.Acts on
Enterocyte
tran...
Solid dosage forms with self
emulsification properties
SOLID SELF-EMULSIFYING DRUG
DELIVERY SYSTEM (S-SEDDS)
M.R. COLLEGE ...
CAPSULES
DRY EMULSIONS
SOLID DISPERSIONS
SUPOSITORIES
SUSTAINED/CONTROL LED RELEASE
TABLETS
PELLETS
MICROSPHERES
BEADS
NAN...
SOLIDIFICATION TECHNIQUES
CAPSULE
FILLING
SPRAY
DRYING
SPRAY
COOLING
ADSORPTION
ON SOLID
CARRIERS
M.R. COLLEGE OF PHARMACY
CAPSULE
FILLING
• Liquid or semisolid self emulsifying formulations are
encapsulatedincapsulefororalroute
SPRAY
DRYING
• L...
SPRAY
COOLING
• Molten formula is sprayed in to a cooling chamber
• On contact with cooling air, the matter droplets conge...
Droplet size
Turbidity measurement
Electron microscopic studies
Emulsification time
Zeta potential measurement
Equilibrium...
M.R. COLLEGE OF PHARMACY
M.R. COLLEGE OF PHARMACY
M.R. COLLEGE OF PHARMACY
BIOPHARMACEUTICAL ISSUES
Role of
lipolysis
M.R. COLLEGE OF PHARMACY
COMPOUND
SELECTION
Compounds which are in
BCS type II drugs
When conventional
formulations approaches i.e
salt or crystall...
EFFECT OF
P-GP
Enhanced uptake of
hydrophobic drugs
formulated as SEDDS
from the GI tract is also
due to P-gp drug efflux....
RECENT ADVANCES
• Helps to reduce or prevent drug
precipitation upon GI fluid dilution.
•Cellulose polymer, hydroxy propyl...
LITERATURE UPDATES ON BIOAVAILABILITY
ENHANCEMENT USING SELF EMULSIFYING
FORMULATIONS
DRUG ENHANCEMENT DOSAGE FORM SPECIES...
Drug name Compound Dosage form Company
Neoral Cyclosporin Soft gelatin
capsules
Novartis
Norvir Ritonavir Soft gelatin
cap...
REFERENCES
1 Kanchan Kohli, Sunny Chopra, Deepika Dhar, Saurabh Arora and Roop K.
Khar. Self emulsifying drug delivery sys...
6 C.W. Pouton. Lipid formulations for oral administration of drugs: non-
emulsifying, self-emulsifying and ‘self-microemul...
12 Christopher J.H. Porter, Colin W. Pouton, Jean F. Cuine, William N. Charman.
Enhancing intestinal drug solubilisation u...
M.R. COLLEGE OF PHARMACY
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  1. 1. SELF EMULSIFIED DRUG DELIVERY SYSTEM (SEDDS) Presented By B. Swadeep M.pharm., Mobile No 9032638446 M.R. COLLEGE OF PHARMACY
  2. 2. CONTENTS  INTRODUCTION  LIPID FORMULATION CLASSIFICATION SYSTEM  FORMULATION DEVELOPMENT  SOLID SELF EMULSIFYING DRUG DELIVERY SYSTEM  CHARACTERIZATION  BIOPHARMACEUTICAL ISSUES M.R. COLLEGE OF PHARMACY
  3. 3. INTRODUCTION  Poor drug solubility is a frequently encountered problem for pharmaceutical formulation scientists, since most of the new chemical entities synthesized are hydrophobic.  Lipid based systems are a promising choice for the delivery of hydrophobic drug substances. These systems avoid the dissolution step upon oral administration and bypass first pass effect. M.R. COLLEGE OF PHARMACY
  4. 4. DEFINITION SEDDS are isotropic mixtures of drug, lipids and surfactants, usually with one or more hydrophilic co- solvents or co-emulsifiers. Upon mild agitation followed by dilution with aqueous media, these systems can form fine (oil in water) emulsion instantaneously. M.R. COLLEGE OF PHARMACY
  5. 5. MECHANISM According to Reiss: self-emulsification occurs when the entropy change that favors dispersion is greater than the energy required to increase the surface area of the dispersion. M.R. COLLEGE OF PHARMACY
  6. 6. LIPID FORMULATION CLASSIFICATION SYSTEM (LFCS) TYPE 1 DRUG + LIPID + LIPOPHILIC SURFACTANT HLB< 12 DRUG + LIPID DRUG + LIPID + COSOLVENT + HYDROPHILIC SURFACTANTS HLB>12 DRUG + COSOLVENTS + HYDROPHILIC SURFACTANTS TYPE 4TYPE 3TYPE 2 M.R. COLLEGE OF PHARMACY
  7. 7. Conducting binary screening Suitable formulation technique Invivo performance Optimizing the formulation FORMULATION DEVELOPMENT M.R. COLLEGE OF PHARMACY
  8. 8. EXCIPIENTS LIPIDS SURFACTANTS COSOLVENTS Solubilize lipophilic drug Promotes lymphatic transport protection of drugs Eg: Corn oil, Olive oil Usual surfactant concentration 30-60% w/w formulation Increases permeability Eg:Tween,Span, Labrafil,Cremophor Enhance the dissolution of surfactants & drug in lipid base Act as cosurfactants in SMEDDS Eg Ethanol, Propylene glycol,PEG M.R. COLLEGE OF PHARMACY
  9. 9. 1.Retards gastric emptying 2.Simulation of bile 3.Pancreatic secretion 4.Membrane lipid fluidity 5.Acts on Enterocyte transport 6.Opening of tight junctions 7.Inhibition of P-gp 8.Inhibits presystemic metabolism 9.Promotes lymphatic pathway EFFECT OF LIPID BASED EXCEPIENTS M.R. COLLEGE OF PHARMACY
  10. 10. Solid dosage forms with self emulsification properties SOLID SELF-EMULSIFYING DRUG DELIVERY SYSTEM (S-SEDDS) M.R. COLLEGE OF PHARMACY
  11. 11. CAPSULES DRY EMULSIONS SOLID DISPERSIONS SUPOSITORIES SUSTAINED/CONTROL LED RELEASE TABLETS PELLETS MICROSPHERES BEADS NANO PARTICLES IMPLANTS DOSAGE FORM DEVELOPMENT OF SOLID SEDDS M.R. COLLEGE OF PHARMACY
  12. 12. SOLIDIFICATION TECHNIQUES CAPSULE FILLING SPRAY DRYING SPRAY COOLING ADSORPTION ON SOLID CARRIERS M.R. COLLEGE OF PHARMACY
  13. 13. CAPSULE FILLING • Liquid or semisolid self emulsifying formulations are encapsulatedincapsulefororalroute SPRAY DRYING • Lipids, surfactants, drug, solid carriers are solubilized before spray drying. • The solubilized liquid formulation is then atomized in to a spray of droplets. • The droplets introduced in to a drying chamber , water evaporates forming dry particles • Such particles can be further prepared into tablets or capsules M.R. COLLEGE OF PHARMACY
  14. 14. SPRAY COOLING • Molten formula is sprayed in to a cooling chamber • On contact with cooling air, the matter droplets congeal re-crystallize in to spherical solid particles • To atomize the liquid mixture and to generate droplets rotary pressure, two fluid or ultrasonic atomizers are used ADSORPTION ON SOLID CARRIERS • SEDDS can be absorbed up to (70% w/w) on suitable careers • Solid cross linked polymers, nanoparticle adsorbents • Eg: Silica, slicates, magnesium tri silicate, magnesium hydroxide, talcum, cross povidone, cross linked Na CMC, cross linked poly methyl methacrylate, lactose,maltodextrin. M.R. COLLEGE OF PHARMACY
  15. 15. Droplet size Turbidity measurement Electron microscopic studies Emulsification time Zeta potential measurement Equilibrium phase diagram Liquefaction time Small angle neutron scattering Small angle x-ray scattering CHARECTERIZATION M.R. COLLEGE OF PHARMACY
  16. 16. M.R. COLLEGE OF PHARMACY
  17. 17. M.R. COLLEGE OF PHARMACY
  18. 18. M.R. COLLEGE OF PHARMACY
  19. 19. BIOPHARMACEUTICAL ISSUES Role of lipolysis M.R. COLLEGE OF PHARMACY
  20. 20. COMPOUND SELECTION Compounds which are in BCS type II drugs When conventional formulations approaches i.e salt or crystalline form , particle size reduction , solid dispersions or the addition surfactants have failed. ROLE OF LIPOLYSIS Digestion of lipid formulation could reduce the solubility of the drug in the GI gut lumen,which would result in precipitation of the drug and a decrease in the absorption rate. For such compounds type II, type III systems might be preferable , since the presence of surfactant can inhibit digestion of oil with in the formulation. M.R. COLLEGE OF PHARMACY
  21. 21. EFFECT OF P-GP Enhanced uptake of hydrophobic drugs formulated as SEDDS from the GI tract is also due to P-gp drug efflux. Excipients incorporated SEDDS/SMEDDS can inhibit both presystemic drug metabolism & intestinal efflux mediated by P-gp resulting in an increased oral absorption of cytotoxic drugs. LYMPHATIC TRANSPORT Primary physiological purpose of the intestinal lymphatic system is to assimilate dietary lipid from the gut. Lymphatic transport can be responsible for a portion of the total uptake of hydrophobic drugs. M.R. COLLEGE OF PHARMACY
  22. 22. RECENT ADVANCES • Helps to reduce or prevent drug precipitation upon GI fluid dilution. •Cellulose polymer, hydroxy propyl methylcellulose (HPMC), was used as a viscosity enhancer SUPERSATURATED SEDDS • Incorporation of a small amount of cationic lipid (2.5±3%), oleylamine. • Positively charged droplets attracted to the negatively charged physiological compounds in lumen. POSITIVELY CHARGED SEDDS M.R. COLLEGE OF PHARMACY
  23. 23. LITERATURE UPDATES ON BIOAVAILABILITY ENHANCEMENT USING SELF EMULSIFYING FORMULATIONS DRUG ENHANCEMENT DOSAGE FORM SPECIES Acyclovir 3.5 fold Pure drug solution Male albino rats Anethole Trithione 2.5 fold Tablets rabbits Carvedilol 4.13 fold Commercial tablet Beagle dogs Gentamycin 5 fold i.v saline Beagle dogs Oleanolic acid 2.4 fold Tablet Rats M.R. COLLEGE OF PHARMACY
  24. 24. Drug name Compound Dosage form Company Neoral Cyclosporin Soft gelatin capsules Novartis Norvir Ritonavir Soft gelatin capsules Abott laboratories Fortavase Saquinavir Soft gelatin capsules Hoffmann- LaRoche Inc. Agenerase Amprenavir Soft gelatin capsules Glaxosmithkline Solufen Ibuprofen Hard gelatin capsules Sanofi-Aventis Lipirex Finofibrate Hard gelatin capsules Sanofi-Aventis M.R. COLLEGE OF PHARMACY
  25. 25. REFERENCES 1 Kanchan Kohli, Sunny Chopra, Deepika Dhar, Saurabh Arora and Roop K. Khar. Self emulsifying drug delivery system : an approach to enhance oral bioavailabilty. Drug Discovery Today Volume 15, Numbers 21/22 November 2010. 2 Bo Tang, Gang Cheng, Jian-Chun Gu and Cai-Hong Xu: development of solid self emulsifying drug delivery systems: preparation techniques and dosage forms. Drug Discovery Today Volume 13, Numbers 13/14 July 2008. 3 Martin Kuentz. Lipid-based formulations for oral delivery of lipophilic drugs. Drug Discovery Today: Technologies | Formulation technologies to overcome poor drug-like properties Vol. 9, No. 2 2012. 4 Colin W. Pouton. Self-emulsifying drug delivery systems: assessment of the efficiency of emulsification. International Journal of Pharmaceutics, 27 (1985) 335-348. 5 Tatyana Gershanika, Simon Benita, Self-dispersing lipid formulations for improving oral absorption of lipophilic drugs. European Journal of Pharmaceutics and Biopharmaceutics 50 (2000) 179-188. M.R. COLLEGE OF PHARMACY
  26. 26. 6 C.W. Pouton. Lipid formulations for oral administration of drugs: non- emulsifying, self-emulsifying and ‘self-microemulsifying’ drug delivery systems. European Journal of Pharmaceutical Sciences 11 Suppl. 2 (2000) S93 –S98. 7 Gursoy, S.Simon Benita. Self-emulsifying drug delivery systems (SEDDS) for improved oral delivery of lipophilic drugs. Biomedicine & Pharmacotherapy 58 (2004) 173–182. 8 C.W. Pouton, C.J.H. Porter. Formulation of lipid-based delivery systems for oral administration: Materials, methods and strategies. Advanced Drug Delivery Reviews 60 (2008) 625-637. 9 V. Jannin et al. Approaches for the development of solid and semi-solid lipid-based formulations. Advanced Drug Delivery Reviews 60 (2008) 734–746 10 D.J. Hauss. Oral lipid-based formulations. Advanced Drug Delivery Reviews 59 (2007) 667–676. 11 C.W. Pouton. Formulation of self-emulsifying drug delivery systems. Advanced Drug Delivery Reviews 25 (1997) 47-58. M.R. COLLEGE OF PHARMACY
  27. 27. 12 Christopher J.H. Porter, Colin W. Pouton, Jean F. Cuine, William N. Charman. Enhancing intestinal drug solubilisation using lipid-based delivery systems. Advanced Drug Delivery Reviews 60 (2008) 673–691. 13 Patel D and Sawanth kk. Oral bioavailabilty enhancement of acyclovir by self micro emulsifying drug delivery System (SMEDDS). Drug Dev Ind Pharm. 2007,33(12): 1318-26 14 Jing Q, Shen Y, Ren F, Chen J, Jiang Z, Peng B, Leng Y and Dong J. HPLC determination of anethole trithione and its application to pharmacokinetics in rabbits . J Pharm Biomed Anal. 2006;42(5):613-7 15 Wei L,Sun P, Nie S and Pan W . Preparation and evaluation of sedds and smedds containing carvedilol. Drug Dev Ind Pharm. 2005;31(8):785-94. 16 Ito Y, Kusawake T, Ishida M, Tawa R. Oral solid gentamicin preparation using emulsifier and adsorbent. J control release, 2005;105 :23–31. 17 Woo JS, Kim TS, Park JH and Chi SC. Formulation and biopharmaceutical evaluation of sylimarin using smedds. Arch Pharm Res.2007;30(1):82-9 M.R. COLLEGE OF PHARMACY
  28. 28. M.R. COLLEGE OF PHARMACY

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