Parenterals Product: IP injections, Sterile powders, Implants, Emulsions, suspensions and MCQs for GPAT, NIPER, Pharmacist and Drug Inspector exam

Parenterals Product: IP injections, Sterile powders, Implants, Emulsions, suspensions and MCQs for GPAT, NIPER, Pharmacist and Drug Inspector exam

Sterile powders:

  • Dry sterile powder is aseptically added to a sterile vial.
  • The dry drug powder is reconstituted with a sterile vehicle before use.
  • Powders for injections are solid substances, distributed in their final containers and which, when shaken with the prescribed volume of the appropriate sterile liquid, rapidly form either clear and practically particle-free solutions or uniform suspensions.

Emulsions:

  • Can be given by I.M., S.C., or I.V. routes.
  • O/w systems are not used due to large interfacial area and rapid partitioning.
  • W/o emulsions are used for water soluble drugs.
  • Multiple emulsions are used generally such as w/o/w and o/w/o since an additional reservoir is presented to the drug for partitioning which can effectively retard its release rate.
  • Release of water soluble drugs can be retarded by presenting it as oil suspension and vice versa.
  • e.g. water soluble drug – 5-Fluorouracil, oil soluble drug – Lipidol.

Suspensions:

  • Suspension for injection contain less than 5% of drug solids with a mean particle diameter within the range 5-10µm.
  • During the manufacture of suspension for injection, the components are prepared and sterilized separately, then aseptically combined.
  • The final product cannot be filter sterilized owing to the presence of particles in the formulation.
  • Powders for use in sterile suspensions can be sterilized by gas residues must be avoided.

Aqueous suspensions –

  • Given by I.M. or S.C. routes.
  • Concentration of solids should be 0.5 to 5 %.
  • Particle size should be < 10 μm.
  • Drug is continuously dissolving to replenish the lost.
  • For oil soluble drugs – Only crystalline and stable polymorphic drugs are given by this form.
  • Viscosity builders can be used. – E.g., Crystalline zinc insulin.

Oil suspensions –

  • Given by I.M. route.
  • Process of drug availability consists of dissolution of drug particles followed by partitioning of drug from oil solution to aqueous medium.
  • More prolong dug action as compared to oil solution and aqueous suspension.
  • E.g., Penicillin G procaine in vegetable oil Suspensions.

Implants: Implants are small sterile solid masses consisting of a highly purified drug made by compression or molding or extrusion. Implants are drug delivery systems which provide controlled delivery of drug over a period of time at the site of implantation.

Implants are intended for implantation in the body subcutaneous or intramuscular tissue by a minor surgical incision or injected through a large bore needle. Implants are developed with a view to provide continuous release of the drug into the blood stream over long periods of time without the repeated insertion of needles.

Advantages –

  • Controlled drug delivery for over a long time.
  •  Improve patient compliance.
  • Targeted drug delivery.
  • Bypass first pass metabolism.
  • Decrease side effects.
  • Improved stability of drugs.
  • prove availability of drugs.

Disadvantages –

  • Mini-surgery is needed (Painful).
  • Uneasy to simply discontinue the therapy.
  • Local reactions.
  • Inadequate release.

Ideal properties of Implants –

  • Biostable.
  • Biocompatible.
  • Easily removable.
  • Nontoxic & non carcinogenic.
  • Minimum surface area & smooth texture.
  • ate controlled release of the drug.

Type of Implants –

  • Non Biodegradable
  • Biodegradable

Non Biodegradable – The drug is dispersed homogeneously, inside the polymeric matrix through which the drug diffuses slowly providing sustained release. This type of system has several disadvantages, the outer membrane is nondegradable. Thus minor surgery is necessary for the removal of the delivery system from the body. There is also a possibility that membrane rupture will potentially lead to “drug dumping” during therapy.

Biodegradable –  The inert polymers, used are eventually absorbed or excreted by the body. No need for surgical removal of the implant after the conclusion of therapy. Drug is dispersed in to a biodegradable polymer matrix like poly vinyl methyl ether and is coated with immobilized urease in a neutral pH. In the presence of urea, ammonia is released causing increase in PH at which polymer degrades leading to drug release.

Table 1 – Classification of implantable drug delivery system

a)Controlled drug release by diffusion b)Controlled drug release by activation c)Controlled drug delivery by feedback regulated mechanism
1.Membrane permaeation controlled release system

2.Matrix diffusion controlled release system

3.Micro reservoir dissolution controlled release system

4.Membrane matrix hybrid type controlled release system

1.Osmotic pressure activated e.g. Alzet pump

2.Vapour pressure activated e.g. infusaid pump

3.Magnetically activated

4.Phonophoresis

5.Hydrolysis activated e.g. for control release of levonorgestrel

6.Hydration activated e.g Hydron implant

1.Bioerosion regulated drug delivery system

2.Bioresponse activated drug delivery system

 

Table 2 – Controlled drug release by diffusion

Approach Mechanism Example
Membrane permaeation controlled release Drug encapsulated in capsule/spherical compartment Norplant subdermal implant
Matrix diffusion controlled release Homogenous dispersion of drug in lipophilic/hydrophilic polymer matrix Compudose implant
Micro reservoir dissolution controlled release Drug in suspension in aqueous solution of water miscible polymer forms dispersion of drug reservoir in polymer matrix Syncro mate implant
Membrane matrix hybrid type controlled release Hybrid of polymer membrane permeation controlled DDS and polymer matrix diffusion controlled DDS Norplant II

 

Table 3 – Controlled drug release by activation

Approach Mechanism Example
Osmotic pressure activated Drug reservoir solution or semisolid placed within semipermeable housing with controlled water permeability Alzet pump
Vapour pressure activated Drug reservoir solution is placed inside infusate chamber Infusaid pump

 

Magnetically activated Magnetic wave triggering mechanism is incorporated into drug delivery device  
Hydrolysis activated Solid drug is homogenously dispersed throughout polymer matrix of bioerodible or biodegradable polymer Levonorgestrel using poly ortho esters biodegradable polymer
Hydration activated Solid drug is coated by hydrophilic polymer Hydron implant

 

Table 4 – Controlled drug delivery by feedback regulated mechanism

Approach Mechanism
Bioerosion regulated Drug dispersed in bioerodible matrix fabricated with polymer coated with immobilized urease
Bioresponse activated Drug eclosed in bioresponsive polymer whose permeability is controlled by concentration of biochemical agent in tissue

IP injections:

  • Frusemide injection IP 10mg/ml
  • Meropenem injection IP

 Multiple choice questions:

1.Dry sterile powder is aseptically added to a sterile

a)ampoule

b)vial

c)both of these

d)plastic containers

2.Powders for injections are solid substances, distributed in their final containers and which, when shaken with the prescribed volume of the appropriate sterile liquid, rapidly form either clear and practically particle-free solutions or uniform suspensions.

a)true

b)false

3.Emulsions Can be given by

a)I.M. route

b)S.C. route

c)I.V. route

d)All of these

4.Suspension for injection contain less than ____ of drug solids with a mean particle diameter within the range 5-10µm.

a)1%

b)5%

c)10%

d)0.1%

5.Aqueous suspensions can be given by

a)I.M. route

b)S.C. route

c)Both of these

d)None of these

6.Particle size in aqueous suspensions should be

a)< 10 μm

b)> 10 μm

c) = 10 μm

d)1 μm

7.Oil suspensions can be given by

a)I.M. route

b)S.C. route

c)I.V. route

d)All of these

8.Implants are intended for implantation in the body subcutaneous or intramuscular tissue by a minor surgical incision or injected through a large bore needle.

a)true

b)false

9.Which of the following is not an advantage of implants?

a)Local reactions

b)Improve patient compliance.

c)Targeted drug delivery.

d)Bypass first pass metabolism

10.Disadvantages of implants is/are

a)Mini-surgery is needed (Painful)

b)Uneasy to simply discontinue the therapy

c)Inadequate release

d)All of these

11.Ideal properties of implants are

a)Biostable

b)Biocompatible

c)Easily removable

d)All of these

12.Classification of implantable drug delivery system include

a)Controlled drug release by diffusion

b)Controlled drug release by activation

c)Controlled drug delivery by feedback regulated mechanism

d)All of these

13.Norplant subdermal implant is an example of

a)Membrane permaeation controlled release system

b)Matrix diffusion controlled release system

c)Micro reservoir dissolution controlled release system

d)Membrane matrix hybrid type controlled release system

14.Drug reservoir solution is placed inside infusate chamber in

a)Osmotic pressure activated system

b)Vapour pressure activated system

c)Magnetically activated system

d)Hydration activated system

15.Hydron implant is an example of

a)Osmotic pressure activated system

b)Vapour pressure activated system

c)Magnetically activated system

d)Hydration activated system

Solutions:

  1. b)vial
  2. a)true
  3. d)All of these
  4. b)5%
  5. c)Both of these
  6. a)< 10 μm
  7. a)I.M. route
  8. a)true
  9. a)Local reactions
  10. d)All of these
  11. d)All of these
  12. d)All of these
  13. a)Membrane permaeation controlled release system
  14. b)Vapour pressure activated system
  15. d)Hydration activated system

References:

  1. Pharmaceutical product development by N K Jain, 2nd edition 2011.
  2. Theory and practice of industrial pharmacy by Lachman and Leiberman, 4th edition.

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