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Submitted by: Submitted to: Dr. Yasmeen Sultana

Mamta Mehta

M.pharmacy(Ist semester)

Pharmaceutics

 

The term parenteral derived from the
Greek word “Para- outside” and
“enteron- intestine”. Meaning route
of administration other than oral route
which refers to the injectable routes.

 

Parenteral preparations are sterile preparations
containing one or more active ingredients intended for
administration by injection, infusion, or implantation
into the body.

They are packaged in either single dose or multi dose
containers.

 

• It may require the use of excipients such as solvents
substances to enhance solubility, suspending agents,
buffering agents, substances to make the
preparations isotonic with blood, stabilizers or
antimicrobial preparation.

• Water for injections is used as the vehicle for
aqueous injections.It is freshly distilled by the
process described under water for injections.

 

oSterility

oFree from pyrogens

oFree from particulate

oClarity

oStability

oSpecific and high quality

oIsotonicity

 

Solvents and vehicle used must have special purity and
other standard.

Do not use coloring agents.

Must be prepared under aseptic condition.

 

Parenterals are tested for particulate contamination:
sub-visible particles.

For preparations for human use, solutions for insulins or
solutions for injections supplied in containers with a
nominal content of more than 100ml comply with the
test.

Sterility- parenteral preparations comply with the test
for sterility.

 

Store in a sterile, airtight, tamper- proof container.

Labelling
The label states:-

The name and concentration of any added antimicrobial
preservative.

Where applicable, that the solution is to be used in conjunction
with a final filter.

Where applicable, that the preparation is free from bacterial
endotoxins or that it is apyrogenic.

 

The manufacturing process should meet the
requirements of GMP.
The addition of excipients is kept to a minimum.
When excipients are used they do not adversely affect
the stability, bioavailability, safety or efficacy of the
active ingredients or cause toxicity or undue local
irritation.
There must be no incompatibility between any of the
components.

 

Parenteral are classified into 2 main types:-

1. Small volume parenteral

2. Large volume parenteral

3. Powder parenteral

 

They include ampules of 1ml, 2ml, 3ml upto 30ml and vial of 1ml to
30ml.

According to USP

An injection that is packaged in containers labelled as
containing 100ml or less.

This is said to be small volume parenteral.

 

• All the sterile products packaged in vials, ampules, cartridges,
syringes, bottles or any other container that is 100ml or less fall
under the class of SVP.

• Ophthalmic products packaged in squeezable plastic
containers, although topically applied to the eye rather than
administered by injections, also fall under the classification of
small volume Injections (SVP) as long as the containers size is
100ml or less.

 

SVP aqueous solutions can be administered by IV route
because of local irritation.

Small volume parenteral products can be formulated and
packaged in several ways and includes a wide variety of
products like pharmaceutical products, biological
products, allergenic extracts, radio pharmaceutical
products, genetically engineered or biotechnology
products, liposome and lipid products.

 

Drug Injection

Drug for injection

Drug injectable emulsion

Drug injectable suspension

Drug for injectable suspension

 

1. Glass

Highly resistant borosilicate glass

Treated soda lime glass

Regular soda lime glass

N.P( Non parenteral) glass

Type 4 is not used for parenteral packaging, other all
are used for parenteral packaging.

 

2. Plastic

Plastic containers are used but they face
following problems

• Permeation

• Sorption

• Leaching

• Softening

 

3.Rubber
• To provide closure for multiple dose vials, IV fluid
bottles, plugs for disposable syringes and bulbs for
ophthalmic pipettes, Rubber is the material of choice.

• Problems associated with Rubber closures are
Incompatibility
Chemical instability
Physical instability

 

Characteristics of Good Pharmaceutical Rubbers

• Good ageing qualities

• Satisfactory hardness and elasticity

• Resistance to sterilization conditions

• Impermeable to moisture and air

Examples:– butyl rubbers, natural rubbers, neoprene
rubbers, poly isoprene rubbers, silicon rubbers etc.

 

Cleaning of materials, closures and equipments
Collection of materials
Preparation of parenteral products
Filtration
Filling the preparation in final containers
Sealing the containers
Sterilization
Evaluation of parenteral preparation
Labelling and packaging

 

In the preparation of parenteral products the following
substances are added to make a stable preparation;

The active drug

Vehicles

-Aqueous vehicles[ e.g. Water for injection, water for injection
free from CO2]

-Non-Aqueous vehicles [e.g. Ethyl alcohol, propylene glycol,
almond oil]

 

Solubilizing agents [e.g. Tweens and polysorbates]

Stabilizers and antioxidants [thiourea, ascorbic acid]

Buffering agents[citric acid, sodium citrate]

Antibacterial agents [benzyl alcohol, metacresol, phenol]

Chelating agents[EDTA]

Suspending,emulsifying and wetting agents[MC, CMC]

Toxicity factor[ Sodium chloride, dextrose]

 

Aqueous vehicle:

• Types:- purified water, WFI, sterile WFI, bacteriostatic WFI,
sterile WF Irrigation.

• Preparation:- Distillation, ion exchange or reverse osmosis.

• Except purified water all are pyrogen free

Non-aqueous vehicle:

• Because of safety, purity and biocompatibility.

• Several SVPs are marketed as oily solutions

 

The oil must be vegetable in origin( sesame, olive, or cottonseed
oil).

• Co -Solvents:-

• Are used to increase the stability of poorly soluble drug in
water and prevent drug chemical degradation by hydrolysis.

Eg. Propylene glycol or in combination with ethanol and
polyethylene glycol.

 

• Antimicrobial preservatives

• Buffers

• Antioxidants

• Tonicity adjusters

• Other ingredients

 

Sterility test

Clarity test

Leakage test

Pyrogen test

Assay

 

Volume of these parenterals varies from 500ml and
above. They are administered as single dose injections
at a slow rate.

Example: infusion fluids, total parenteral nutrition
solutions, patient controlled analgesia,dialysis fluids etc.

These generally provide electrolytes, nutrition to the
body.

These are delivered through IV route.

 

• Sterile, Non pyrogenic, free from particulate matter.

• Volume 101-1000ml,

• Single dose unit,

• No preservatives,

• Clear solution except fat emulsion,

• Isotonic, but hypertonic also administered in TPN.

 

1. Hyper alimentation solutions

2. Cardiolpagic solutions

3. Peritoneal dialysis solutions

4. Irrigating solutions

 

Administration of large amount of nutrients to patients who
unable to take food orally, at caloric intake of 4000 kcal/day.

 Subclavian vein cannulation: Infusion of hypertonic solution.

Formulation: mixture of dextrose, amino acids, lipids,
electrolytes and vitamins.

USE

oAdministration of life saving/sustaining drug to comatose
patient.

oPatient undergoing t/t of GI disease.

 

oAre LVP used in heart surgery to prevent injury to
myocardium during reperfusion, as well as to maintain
bloodless operating field.

oMaintains the diastolic arrest.
oAdministration in cold form.
oSlightly alkaline to compensate metabolic acidosis,
oHypertonic
USE
To minimize reperfusion injury resulting from tissue

edema.

 

Infused continuously into abdominal cavity, bathing
peritoneum and are then continuously withdrawn.

Formulation:- glucose, antibiotics as prophylactic

USE

oRemoval of toxic substances from body.

oTo aid and accelerate excretion normal.

oTo treat acute renal insufficiency

 

To irrigate, flush and aid in cleansing body cavities
and wounds.

Certain IV solution (normal saline) may be used as
irrigating solution, but solution designed as irrigating
solution should not be used parententrally.

USE

Treatment of serious wounds infused into blood
stream.

 

The production area where the parenteral
preparation are manufactured can be divided into
five sections:
Clean-up area
Preparation area
An aseptic area
Quarantine area
Finishing and packaging area

 

• Lachman/Lieberman ‘s “ The Theory and Practice of Industrial
Pharmacy” Fourth Edition 2013, Edited by: Roop K khar, SP Vyas,
Farhan J Ahmad, Gautama k Jain, CBS publishers and
distributors Pvt Ltd, New Delhi.

• The science and practice of Pharmacy, By Remington, Vol-01,
21st Edition, lippincott Publication, pg 838-840.

• Mordern Pharmaceutics Fourth Edition, Revised and Expanded,
Edited By G.S. Banker and C.T. Rhodes, Marcel Dekker pg 387-
389.

• www.weiler-bfs.com