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Sustained and
controlled release drugs
Submitted by:
AISHWARYA ANAND
ID NO. 42469
DRUG DELIVERY SYSTEM
• Drug delivery systems refer to the technology
utilized to present the drug to the desired
body site for drug release and absorption.
• Newer discoveries and advancements in
technology has lead to various new
techniques of delivering the drugs for
maximum patient compliance at minimal dose
and side effects.
Ideal drug delivery system
• First, it should deliver drug at a rate dictated by the needs of the body over the
period of the treatment.
• Second it should channel the active entity solely to the site of action.
• This is achieved by development of new various modified drug release dosage
forms, like-
 Control release dosage forms
 Time release dosage forms
 Sustained release dosage forms
 Site specific or targeted drug delivery systems etc
SUSTAINED RELEASE DRUGS
Any of the dosage form that maintains the
therapeutic blood or tissue levels of drug by
continuous release of medication for a prolonged
period of time, after administration of a single dose.
The basic goal of therapy is to achieve steady
state blood level that is therapeutically effective and
non toxic for an extended period of time.
CONTROLLED RELEASE DRUG
DELIVERY :
• Delivery of the drug at a predetermined rate
and /or to a location according to the needs of
the body and disease states for a definite
period of time.
• Controlled release is perfectly zero order
release that is the drug release over time
irrespective of concentration.
Sustained and controlled release drugs
Merits :
Reduction in dosing frequency.
Enhanced patient convenience and compliance.
Reduction in adverse effects(both systemic and
local), esp. of potent drugs, in sensitive patients.
Reduction in health care costs.
Improved efficiency of treatment.
Reduces nursing and hospitalizing time.
Maximum bioavailability with a minimum dose.
Reduction in blood level fluctuations of drug, thus
better management of the disease.
DEMERITS:
 Probability of dose dumping.
 Reduced potential for dose adjustment.
 Cost of single unit higher than conventional dosage
forms.
 Increase potential for first pass metabolism.
 Requirement for additional patient education for proper
medication.
 Decreased systemic availability in comparison to
immediate release conventional dosage forms.
 Poor invitro and invivo correlations.
PHYSIOCHEMICAL PROPERTIES OF
DRUGS
1) Aqueous solubility & PKaː–
Aqueous solubilityː–
• A drug with good aqueous solubility,
especially if pH independent, serves as a good
candidates
• Drug to be absorbed it first must dissolve in
the aqueous phase surrounding the site of
administration and then partition into
absorbing membrane.
Noyes Whitney Equation
dc = KDACs
dt where ,dc/dt= dissolution rate
Kᴅ = Dissolution rate constant.
A = total surface area of drug.
Cs = aqueous saturation solubility.
Drugs with low aqueous solubility have low dissolution
rate and have oral bioavailability problems. E.g.:
Tetracycline.
 Drugs with high aqueous solubility are undesirable to
formulate SRDF’s.
• E.g.: Paracetamol
pKaː–
• The aqueous solubility of weak acids & weak bases is
governed by the pKa of the compound and pH of the
medium.
• Weakly acidic drug exist as unionized form in the
stomach absorption is favored by acidic medium.
FOR WEAK ACID
St = So(1+Ka[H ] =So(1+10pH-pKa)
where, St – Total solubility of the weak acid
So – Solubility of the un-ionized form
Ka – Acid dissociation constant
H - Hydrogen ion concentration
FOR WEAK BASES
Where, St – Total solubility of both conjugate and free base form of weak base.
So– Solubility of the free base.
• Weakly basic drug exists as ionized form in the
stomach hence absorption of this type is poor in this
medium .
St = So(1+[H ] Ka) =So(1+pKa-pH)
2) Partition coefficientː
• Between the time a drug is administered and is
eliminated from the body, it must diffuse through a
variety of biological membranes.
• Partition coefficient is the fraction of drug in an oil
phase to that of an adjacent aqueous phase.
K=Co/Cs
where, Co= Equilibrium concentration
in organic phase.
Cs= Equilibrium concentration
in aqueous phase.
• Drugs with extremely high partition coefficient are very oil soluble
and penetrates in to various membranes very easily.
• High partition coefficient compound are predominantly lipid
soluble and have very low aqueous solubility and thus these
compound persist in the body for long periods.
3) Drug stabilityː–
 Solid state undergoes degradation at much slower rate than
in the suspension or solution etc..
 Drugs stable in stomach gets released in stomach and which
are unstable gets released in intestine.
 Drugs with stability problems in any particular area of G.I.T
are less suitable for the formulation.
 Drugs may be protected from enzymatic degradation by
incorporation in to a polymeric matrix
4) Protein bindingː–
 Drug binding to plasma proteins (albumins) & resulting retention of
the drug in the vascular space.
 Drug-protein binding serve as a depot for drug producing a prolonged
release profile, especially it is high degree of drug binding occurs.
 Main forces for binding are Vander Waal forces, hydrogen
bonding , electrostatic forces.
 Charged compounds has greater tendency to bind proteins
than uncharged ones.
 Extensive binding of plasma proteins results in longer half-life
of elimination for the drug.
 E.x..95% binding in Amitriptyline , diazepam , diazepoxide.
5) Molecular size & diffusivityː
• The ability of a drug to diffuse through membranes is called
diffusivity which is a function of molecular weight.
• In most polymers it is possible to relate log D to some
function of molecular size as,
Log D = - Sv log v + Kv = - SM log M + Km
where, V – Molecular volume.
M – Molecular weight.
Sv, Sm, Kv & Km are constants.
• The drugs with high molecular weight show very slow kinetics.
6) Dose sizeː–
 For those drugs requiring large conventional doses, the
volume of sustained dose may be too large to be practical.
 The compounds that require large dose are given in
multiple amounts or formulated into liquid systems.
 The greater the dose size,greater the fluctuation.
 So the dose should have proper size.
Biological half life
The usual goal of sustained release product is to
maintain therapeutic blood level over an extended
period, to this drug must enter the circulation at
approximately the same rate at which it is eliminated.
The elimination rate is quantitatively described by the
half-life (t1/2)
Therapeutic compounds with short half life are
excellent candidates for drug preparation since these
can reduce dosing frequency.
 Drugs with half-life shorter than 2 hours. Such as
e.g.: Furosemide, levodopa are poor for sustained
release formulation because it requires large rates
and large dose compounds with long half-life. More
than 8 hours are also generally not used in sustaining
forms, since their effect is already sustained.
E.g.; Digoxin, Warfarin, Phenytoin etc.
Margin of safety (Therapeutic index)
In general the larger the volume of therapeutic index
safer the drug. Drug with very small values of
therapeutic index usually are poor candidates for
SRDF due to pharmacological limitation of control
over release rate .e.g.- induced digtoxin,
Phenobarbital, phenotoin.
Larger the TI ratio the safer is drug.
It is imperative that the drug release pattern is precise
so that the plasma drug concentration achieved in
under therapeutic range.
Formulations Methods
Embedding the drug in matrix :
Matrix may be defined as uniform dispersion of
drug in solid which is less soluble than a drug in the
dispersion fluid, & which for the continuous external
phase of the dispersion effectively impeder the passage
of the drug from the matrix to the dispersion fluid.
•Drug release through-diffusion
•Least complicated approaches to manufacture
sustained release dosage form involves the direct
compression of drug, materials & additives to form a
tablet .
Polymers:-
•Insoluble, inert - polyethylene, polyvinyl chloride,
methyl acrilate, ethylcellulose.
•Insoluble, erodible – carnauba wax, stearyl alcohol,
castor wax.
•Hydrophilic – methyl cellulose, hydroxyl ethyl cellulose,
sodium carboxymethyl cellulose, sodium alginate.
In a matrix system the drug is dispersed as solid
particle within a porous matrix formed of a water
insoluble polymer, such as poly-vinyl chloride.
Microencapsulations
• method for retarding drug release by coating its surface with a
material(polymers) that retards penetration by the dispersion
fluid.
• it is a mean of applying relatively thin coating to small particles
of solid or droplets of liquids and dispersion.
Can be done by-
 spray congealing
 spray drying
Polymers used
• Polyvinyl alcohol
• Polyacrylic acid
• Ethyl cellulose(pH sensitive)
• Polyethylene
• Polymethacrylate
• Poly (ethylene-vinyl acetate)
• Cellulose nitrite
• Silicones
• Poly (lactide-co-glycolide)
Ion exchange resins
• Ion exchange resins are polymers that are capable of
exchanging particular ions within the polymer with ions in a
solution that is passed through them.
• Sustained delivery of ionizing acidic & basic drug can be
obtained by complexing them with insoluble non-toxic anion
exchanger & cation exchanger resin respectively.
• Release by diffusion .
• The complex can be prepared by incubating the drug-resin
solution or passing the drug solution through a column
containing ion exchange resin.
Examples:
• Nifedipine sustained-release tablets
Treating high blood pressure. Some brands of
nifedipine sustained-release tablets may also be used
to manage certain kinds of angina (chest pain).
Nifedipine sustained-release tablets are a calcium
channel blocking agent. It works by dilating
(widening) blood vessels
Paroxetine controlled-release tablets
• Treating depression, panic disorder, or social
anxiety disorder. It may also be used to treat
premenstrual dysphoric disorder (PMDD), a
severe form of premenstrual syndrome. It may
also be used for other conditions as determined
by your doctor.
• Paroxetine controlled-release tablets are a
selective serotonin reuptake inhibitor (SSRI). It
works by restoring the balance of serotonin, a
natural substance in the brain, which helps to
improve certain mood problems.
Xiral SR Sustained-Release Tablets
• Relieving congestion, sneezing, runny nose, and itchy,
watery eyes due to colds, flu, or hay fever. It may also
be used for other conditions as determined by your
doctor.
• Xiral SR Sustained-Release Tablets are an antihistamine,
decongestant, and anticholinergic combination. It
works by blocking histamine, a substance in the body
that causes sneezing, runny nose, and watery eyes. It
also relieves nasal congestion by shrinking the nasal
mucous membranes, which promotes nasal drainage,
and dries the chest by decreasing lung secretions.
Sustained-release metformin
hydrochloride
• Metformin hydrochloride(HCI), the only available biguanide,
remains the first-line drug therapy for patients with Type 2
diabetes mellitus (T2DM), acting by decreasing the hepatic
glucose output and peripheral insulin resistance. The
advantages of metformin are a very low risk of hypoglycemia,
weight neutrality and reduced risk of cardiovascular morbidity
and mortality. It is an oral anti-hyperglycemic agent, shows
incomplete absorption from the gastrointestinal tract and the
absolute bioavailability is 50–60% with a relatively short
plasma half-life of 1.5–4.5 h
• An obstacle to more successful use of metformin therapy is the
high incidence of concomitant gastrointestinal symptoms such
as abdominal discomfort, nausea and diarrhea that especially
occur during the initial weeks of treatment.
• Side-effects and the need for administration two or three times
per day when larger doses are required can decrease patient
compliance.
• A SR formulation that would maintain plasma levels of the
drug for 10–16 hours might be sufficient for once-daily dosing
of metformin. SR products are needed for metformin to
prolong its duration of action and to improve patient
compliance.
Sustained and controlled release drugs

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Sustained and controlled release drugs

  • 1. Sustained and controlled release drugs Submitted by: AISHWARYA ANAND ID NO. 42469
  • 2. DRUG DELIVERY SYSTEM • Drug delivery systems refer to the technology utilized to present the drug to the desired body site for drug release and absorption. • Newer discoveries and advancements in technology has lead to various new techniques of delivering the drugs for maximum patient compliance at minimal dose and side effects.
  • 3. Ideal drug delivery system • First, it should deliver drug at a rate dictated by the needs of the body over the period of the treatment. • Second it should channel the active entity solely to the site of action. • This is achieved by development of new various modified drug release dosage forms, like-  Control release dosage forms  Time release dosage forms  Sustained release dosage forms  Site specific or targeted drug delivery systems etc
  • 4. SUSTAINED RELEASE DRUGS Any of the dosage form that maintains the therapeutic blood or tissue levels of drug by continuous release of medication for a prolonged period of time, after administration of a single dose. The basic goal of therapy is to achieve steady state blood level that is therapeutically effective and non toxic for an extended period of time.
  • 5. CONTROLLED RELEASE DRUG DELIVERY : • Delivery of the drug at a predetermined rate and /or to a location according to the needs of the body and disease states for a definite period of time. • Controlled release is perfectly zero order release that is the drug release over time irrespective of concentration.
  • 7. Merits : Reduction in dosing frequency. Enhanced patient convenience and compliance. Reduction in adverse effects(both systemic and local), esp. of potent drugs, in sensitive patients. Reduction in health care costs. Improved efficiency of treatment. Reduces nursing and hospitalizing time. Maximum bioavailability with a minimum dose. Reduction in blood level fluctuations of drug, thus better management of the disease.
  • 8. DEMERITS:  Probability of dose dumping.  Reduced potential for dose adjustment.  Cost of single unit higher than conventional dosage forms.  Increase potential for first pass metabolism.  Requirement for additional patient education for proper medication.  Decreased systemic availability in comparison to immediate release conventional dosage forms.  Poor invitro and invivo correlations.
  • 9. PHYSIOCHEMICAL PROPERTIES OF DRUGS 1) Aqueous solubility & PKaː– Aqueous solubilityː– • A drug with good aqueous solubility, especially if pH independent, serves as a good candidates • Drug to be absorbed it first must dissolve in the aqueous phase surrounding the site of administration and then partition into absorbing membrane.
  • 10. Noyes Whitney Equation dc = KDACs dt where ,dc/dt= dissolution rate Kᴅ = Dissolution rate constant. A = total surface area of drug. Cs = aqueous saturation solubility. Drugs with low aqueous solubility have low dissolution rate and have oral bioavailability problems. E.g.: Tetracycline.  Drugs with high aqueous solubility are undesirable to formulate SRDF’s. • E.g.: Paracetamol
  • 11. pKaː– • The aqueous solubility of weak acids & weak bases is governed by the pKa of the compound and pH of the medium. • Weakly acidic drug exist as unionized form in the stomach absorption is favored by acidic medium. FOR WEAK ACID St = So(1+Ka[H ] =So(1+10pH-pKa) where, St – Total solubility of the weak acid So – Solubility of the un-ionized form Ka – Acid dissociation constant H - Hydrogen ion concentration
  • 12. FOR WEAK BASES Where, St – Total solubility of both conjugate and free base form of weak base. So– Solubility of the free base. • Weakly basic drug exists as ionized form in the stomach hence absorption of this type is poor in this medium . St = So(1+[H ] Ka) =So(1+pKa-pH)
  • 13. 2) Partition coefficientː • Between the time a drug is administered and is eliminated from the body, it must diffuse through a variety of biological membranes. • Partition coefficient is the fraction of drug in an oil phase to that of an adjacent aqueous phase. K=Co/Cs where, Co= Equilibrium concentration in organic phase. Cs= Equilibrium concentration in aqueous phase.
  • 14. • Drugs with extremely high partition coefficient are very oil soluble and penetrates in to various membranes very easily. • High partition coefficient compound are predominantly lipid soluble and have very low aqueous solubility and thus these compound persist in the body for long periods.
  • 15. 3) Drug stabilityː–  Solid state undergoes degradation at much slower rate than in the suspension or solution etc..  Drugs stable in stomach gets released in stomach and which are unstable gets released in intestine.  Drugs with stability problems in any particular area of G.I.T are less suitable for the formulation.  Drugs may be protected from enzymatic degradation by incorporation in to a polymeric matrix
  • 16. 4) Protein bindingː–  Drug binding to plasma proteins (albumins) & resulting retention of the drug in the vascular space.  Drug-protein binding serve as a depot for drug producing a prolonged release profile, especially it is high degree of drug binding occurs.  Main forces for binding are Vander Waal forces, hydrogen bonding , electrostatic forces.  Charged compounds has greater tendency to bind proteins than uncharged ones.  Extensive binding of plasma proteins results in longer half-life of elimination for the drug.  E.x..95% binding in Amitriptyline , diazepam , diazepoxide.
  • 17. 5) Molecular size & diffusivityː • The ability of a drug to diffuse through membranes is called diffusivity which is a function of molecular weight. • In most polymers it is possible to relate log D to some function of molecular size as, Log D = - Sv log v + Kv = - SM log M + Km where, V – Molecular volume. M – Molecular weight. Sv, Sm, Kv & Km are constants. • The drugs with high molecular weight show very slow kinetics.
  • 18. 6) Dose sizeː–  For those drugs requiring large conventional doses, the volume of sustained dose may be too large to be practical.  The compounds that require large dose are given in multiple amounts or formulated into liquid systems.  The greater the dose size,greater the fluctuation.  So the dose should have proper size.
  • 19. Biological half life The usual goal of sustained release product is to maintain therapeutic blood level over an extended period, to this drug must enter the circulation at approximately the same rate at which it is eliminated. The elimination rate is quantitatively described by the half-life (t1/2) Therapeutic compounds with short half life are excellent candidates for drug preparation since these can reduce dosing frequency.
  • 20.  Drugs with half-life shorter than 2 hours. Such as e.g.: Furosemide, levodopa are poor for sustained release formulation because it requires large rates and large dose compounds with long half-life. More than 8 hours are also generally not used in sustaining forms, since their effect is already sustained. E.g.; Digoxin, Warfarin, Phenytoin etc.
  • 21. Margin of safety (Therapeutic index) In general the larger the volume of therapeutic index safer the drug. Drug with very small values of therapeutic index usually are poor candidates for SRDF due to pharmacological limitation of control over release rate .e.g.- induced digtoxin, Phenobarbital, phenotoin. Larger the TI ratio the safer is drug. It is imperative that the drug release pattern is precise so that the plasma drug concentration achieved in under therapeutic range.
  • 22. Formulations Methods Embedding the drug in matrix : Matrix may be defined as uniform dispersion of drug in solid which is less soluble than a drug in the dispersion fluid, & which for the continuous external phase of the dispersion effectively impeder the passage of the drug from the matrix to the dispersion fluid. •Drug release through-diffusion •Least complicated approaches to manufacture sustained release dosage form involves the direct compression of drug, materials & additives to form a tablet .
  • 23. Polymers:- •Insoluble, inert - polyethylene, polyvinyl chloride, methyl acrilate, ethylcellulose. •Insoluble, erodible – carnauba wax, stearyl alcohol, castor wax. •Hydrophilic – methyl cellulose, hydroxyl ethyl cellulose, sodium carboxymethyl cellulose, sodium alginate. In a matrix system the drug is dispersed as solid particle within a porous matrix formed of a water insoluble polymer, such as poly-vinyl chloride.
  • 24. Microencapsulations • method for retarding drug release by coating its surface with a material(polymers) that retards penetration by the dispersion fluid. • it is a mean of applying relatively thin coating to small particles of solid or droplets of liquids and dispersion. Can be done by-  spray congealing  spray drying
  • 25. Polymers used • Polyvinyl alcohol • Polyacrylic acid • Ethyl cellulose(pH sensitive) • Polyethylene • Polymethacrylate • Poly (ethylene-vinyl acetate) • Cellulose nitrite • Silicones • Poly (lactide-co-glycolide)
  • 26. Ion exchange resins • Ion exchange resins are polymers that are capable of exchanging particular ions within the polymer with ions in a solution that is passed through them. • Sustained delivery of ionizing acidic & basic drug can be obtained by complexing them with insoluble non-toxic anion exchanger & cation exchanger resin respectively. • Release by diffusion . • The complex can be prepared by incubating the drug-resin solution or passing the drug solution through a column containing ion exchange resin.
  • 27. Examples: • Nifedipine sustained-release tablets Treating high blood pressure. Some brands of nifedipine sustained-release tablets may also be used to manage certain kinds of angina (chest pain). Nifedipine sustained-release tablets are a calcium channel blocking agent. It works by dilating (widening) blood vessels
  • 28. Paroxetine controlled-release tablets • Treating depression, panic disorder, or social anxiety disorder. It may also be used to treat premenstrual dysphoric disorder (PMDD), a severe form of premenstrual syndrome. It may also be used for other conditions as determined by your doctor. • Paroxetine controlled-release tablets are a selective serotonin reuptake inhibitor (SSRI). It works by restoring the balance of serotonin, a natural substance in the brain, which helps to improve certain mood problems.
  • 29. Xiral SR Sustained-Release Tablets • Relieving congestion, sneezing, runny nose, and itchy, watery eyes due to colds, flu, or hay fever. It may also be used for other conditions as determined by your doctor. • Xiral SR Sustained-Release Tablets are an antihistamine, decongestant, and anticholinergic combination. It works by blocking histamine, a substance in the body that causes sneezing, runny nose, and watery eyes. It also relieves nasal congestion by shrinking the nasal mucous membranes, which promotes nasal drainage, and dries the chest by decreasing lung secretions.
  • 30. Sustained-release metformin hydrochloride • Metformin hydrochloride(HCI), the only available biguanide, remains the first-line drug therapy for patients with Type 2 diabetes mellitus (T2DM), acting by decreasing the hepatic glucose output and peripheral insulin resistance. The advantages of metformin are a very low risk of hypoglycemia, weight neutrality and reduced risk of cardiovascular morbidity and mortality. It is an oral anti-hyperglycemic agent, shows incomplete absorption from the gastrointestinal tract and the absolute bioavailability is 50–60% with a relatively short plasma half-life of 1.5–4.5 h
  • 31. • An obstacle to more successful use of metformin therapy is the high incidence of concomitant gastrointestinal symptoms such as abdominal discomfort, nausea and diarrhea that especially occur during the initial weeks of treatment. • Side-effects and the need for administration two or three times per day when larger doses are required can decrease patient compliance. • A SR formulation that would maintain plasma levels of the drug for 10–16 hours might be sufficient for once-daily dosing of metformin. SR products are needed for metformin to prolong its duration of action and to improve patient compliance.