This document provides an overview of dissolution testing. It defines dissolution as the process by which a solid solute enters into a solution. The document discusses the importance of dissolution studies for quality control and product development. It describes the common types of dissolution apparatus, including baskets, paddles, reciprocating cylinders, and flow-through cells. The document also discusses biopharmaceutics classification systems and factors to consider for developing dissolution methods such as choice of medium, solubility, and stability testing.

1. Hello Everyone ,
I am KINJAL PANCHAL
Expert ,
Thane R & D ,
Analytical Department.
You can find me at
k.panchal@omniactives.com
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2. DISSOLUTION

3. Content
.
1) What is dissolution
2) What is in-vitro and in-vivo dissolution
3) BCS CLASSIFICATION
4) Types of Dissolution apparatus
5) Usage of Dissolution Apparatus in industry
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4. What is Dissolution :
.

5. WHY DISSOLUTION STUDY?
.
▸ Definition
▸ Dissolution is the process by which
a solid solute enters in to a solution
i.e. , mass transfer from solid
surface to liquid phase.
1) Estimation of amount of drug released per
unit time.
2) Batch to batch Quality control.
3) It is the rate limiting factor for poorly soluble
drugs.
4) For Product development.
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6. Choosing a Medium and Volume
.
When developing a dissolution procedure, one goal is to have sink
conditions, which are defined as having a volume of medium at
least three times the volume required to form a saturated solution
of drug substance.
Commonly Used Dissolution Media:
▸ 1. Purified water
▸ 2. Dilute acid (0.001N – 0.1N HCl)
▸ 3. Stimulated gastric fluid
▸ 4. Stimulated intestinal fluid
▸ 5. Surfactants (e.g. Polysorbate, SLS)
▸ 6. Aqueous buffers (pH 5-7)
The use of enzymes in the
dissolution medium is
permitted, in accordance with
Dissolution 711, when dissolution
failures occur as a result of
cross-linking with gelatin
capsules or gelatin-coated
products
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7. Determining Solubility and Stability of Drug
Substance in Various Media
.
▸ When deciding the composition of the medium for dissolution testing, it is
important to evaluate the influence of buffers, pH, and if needed, different
surfactants on the solubility and stability of the drug substance
▸ Typical media for dissolution may include the following (not listed in order of
preference): diluted hydrochloric acid, buffers (phosphate or acetate) in the
physiologic pH range of 1.2–7.5, simulated gastric or intestinal fluid (with or
without enzymes), and water
▸ Use of Surfactants for poorly soluble drugs
.
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8. USP Monograph
.
▸ •USP 711 (Dissolution) late 1960
▸ •USP 724 (Drug Release) 1985
▸ •USP 1088 (In Vitro and In Vivo Evaluation of Dosage Forms) 1995
▸ •USP 1092 (The Dissolution Procedure Development and Validation): Total Revision August 2015
▸ •USP 1094 CAPSULES—DISSOLUTION TESTING AND RELATED QUALITY ATTRIBUTES
▸ •USP 2040 Disintegration and Dissolution of Dietary Supplements
▸ •EP 2.9.3 Dissolution late 1960
▸ •EP 2.9.4 Dissolution for Transdermal Systems late 1970
.
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9. What is in-vitro and in-vivo dissolution?
▸ Generally, the in-vitro property
is the rate or extent of drug
dissolution or release.
▸ in-vivo response is the plasma
drug concentration or amount
of drug absorbed. ...
To use dissolution test as a
surrogate for human studies
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10. BCS CLASSIFICATION
The BCS places a given API in one of four
categories depending on its oral dosing
solubility and permeability.
Solubility is the maximum concentration
of a solute that can dissolve in a solvent at
a given temperature.
Permeability The ability of a drug to pass
across biological membrane
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11. ▸ According to the Biopharmaceutics
Classification System referred to in several
FDA Guidance's, highly soluble, highly
permeable drugs formulated into very rapidly
dissolving products need not be subjected to
a profile comparison if they can be shown to
release 85% or more of the drug substance
within 15 min. For these types of products, a
one-point test or disintegration will suffice.
However, most products do not fall into this
category. Dissolution profiles of immediate-
release products typically show a gradual
increase reaching 85%–100% at about 30–45
min.
BCS CLASSIFICATION
.
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12. Types of dissolution apparatus
.
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13. USP TYPE 1 = BASKET
 DESIGN:
 Vessel: -Made of borosilicate glass.
 -Semi hemispherical bottom
 -Capacity 1000ml
 Shaft : -Stainless steel 316
 -Speed 50-100 rpm.
 Water bath :-Maintained at 37±0.5ºC
 Dosage form is kept in basket.
 USE: Tablets, capsules, floating
dosage forms.
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14. USP TYPE 2 = PADDLE
▸ DESIGN:
▸ Vessel: -Same as basket apparatus
▸ Shaft: - Fused with blade at bottom
▸ Stirring elements:- Coated with teflon
▸ For laboratory purpose
▸ stainless steel is used
▸ Rotation Speed:- 25-50 rpm
▸ Water-bath: -Maintains at 37±0.5°C
▸ Sinkers : -Platinum wire used to prevent
▸ tablet/capsule from floating.
▸ Dosage form should remain at the bottom
center of vessel
▸ USE: Orally disintegrating tablets, Chewable
tablets etc.
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15. USP TYPE 2 = PADDLE
with Sinkers
▸ Sinkers are often used to adjust the
tendency to float of dosage forms that
would otherwise float during testing
with Apparatus 2. For materials, use
316 stainless steel wire, typically 0.032
inch/20 gauge, or other inert material
and wind the wire around cylinders of
appropriate diameter (e.g., cork borers)
for an appropriate number of turns to
fit the capsule shell type
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16. USP Type 3=Reciprocating
cylinder
▸ DESIGN:
▸ Vessel: -Set of cylindrical flat bottom glass
vessels
▸ -Set of reciprocating cylinders
▸ -stainless steel fittings.
▸ Agitation type: -Reciprocating
▸ (Upward & downward)
▸ Volume of dissolution medium:-200-250ml
▸ Water bath:- Maintain at 37±0.5°C
▸ Dosage form is placed in cylinder
▸ USE: Tablets, beads, controlled and
▸ extended release formulations
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17. USP Type 4=Flow through cell
▸ DESIGN:
▸ Reservoir :- For dissolution medium
▸ Pump :- Forces dissolution medium through
cell (upward
▸ direction)
▸ -Flow rate 10-100ml/min
▸ -Laminar flow is maintained
▸ -Centrifugal pumps are not recommended
▸ Water bath:- Maintained at 37±0.5°C
▸ USE: Low solubility drugs, micro
particulate, implants,
▸ suppositories, controlled release
formulations.
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18. USP Apparatus 5 : Paddle-over-Disk Apparatus
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 DESIGN:
 Vessel & Shaft:- Same as paddle apparatus
 Rotation Speed:- 25-50 rpm
 Sample holder:-disk assembly that holds
 product in such a way that release surface
 is parallel with paddle blade
 -Distance 25 ± 2 mm
 -Samples are drawn between
 surface of the medium &
 the top of the paddle blade
 Temperature:32 ± 0.5°C
 USE: Transdermal products, emulsions.

19. USP Apparatus 6 : Rotating Cylinder
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• DESIGN:
• Vessel:- Same as of basket apparatus
• Shaft & Cylinder:- Stainless steel
• Sample :- inner porous cellulosic material
• an entire system is adhered to cylinder.
• - Dosage unit is placed in cylinder and release
from side out.
• Rotation Speed:- 25-50 rpm
• Water-bath: maintained at 32±0.5°C
• USE:
• Mainly transdermal products

20. USP Apparatus 7 : Reciprocating Holder
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• DESIGN:
• Vessel:- A set of cylindrical vessels connected to
• each other
• Volume of dissolution medium 50-200 ml
• Shaft
Holder:- Spring holder/ Reciprocating disk/
• Teflon cylinder/ Acrylic rod
• Sample : - Placed on holders
• Agitation:- Reciprocating frequency 30 cycle/sec
• Water-bath:- Maintained at 32±0.5°C
• USE:
• Controlled release dosage form, non disintegrating
oral formulations.

21. FDA Dissolution Methods
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.
https://www.accessdata.fda.gov/scripts/cder/dissolution/dsp_getallData.cfm

22. Thanks!
Any questions?
You can find me at:
▸ k.Panchal@omniactives.com
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