dissolution apparatus post-lab

37
DISSOLUTION APPARATUS POST-LAB DISCUSSION 6/24/15

Upload: juxtaglomerular-rx

Post on 31-Jul-2015

129 views

Category:

Health & Medicine


1 download

TRANSCRIPT

Page 1: Dissolution apparatus POST-LAB

DISSOLUTION APPARATUSPOST-LAB DISCUSSION

6/24/15

Page 2: Dissolution apparatus POST-LAB

Types of Dissolution Apparatus

• USP Dissolution apparatus (official):1. Basket type2. Paddle type3. Reciprocating cylinder4. Flow through cell5. Paddle over disc6. Rotating cylinder7. Reciprocating disc

Page 3: Dissolution apparatus POST-LAB

USP dissolution apparatus (non-official):

1. Rotating bottle method

2. Diffusion cell

3. Peristalisis method

4. Intrinsic dissolution method

Page 4: Dissolution apparatus POST-LAB

• IP Dissolution apparatus:1. Paddle type2. Basket type

BP Dissolution apparatus:1. Basket type apparatus2. Paddle type apparatus3. Flow through cell

Page 5: Dissolution apparatus POST-LAB

IDEAL FEATURES OF DISSOLUTION APPARATUS

• Fabrication dimensions and positioning of all components must be precisely specified and reproducible, run to run.

• Must be simply design easy to operate and useable under variety of conditions.

Page 6: Dissolution apparatus POST-LAB

IDEAL FEATURES OF DISSOLUTION APPARATUS

• Must be sensitive to reveal processes changes and formulations differences but still yield repeatable results under identical conditions.

Page 7: Dissolution apparatus POST-LAB

IDEAL FEATURES OF DISSOLUTION APPARATUS

• Should permit controlled but variable intensity of: mild uniform non-turbulent liquid agitation. Uniform flow is very essential because changes in hydrodynamic flow will modify dissolution

• Nearly perfect sink conditions should be maintained.

Page 8: Dissolution apparatus POST-LAB

• Provide easy means of introducing the dosage form into dissolution medium and holding it, once immersed in a regular and reliable fashion.

• Provide minimum abrasion to the dosage form during test period to avoid disruption of the microenvironment surrounding the dissolving form.

IDEAL FEATURES OF DISSOLUTION APPARATUS

Page 9: Dissolution apparatus POST-LAB

• Special care should be taken that medium must not evaporate from container of apparatus.

IDEAL FEATURES OF DISSOLUTION APPARATUS

Page 10: Dissolution apparatus POST-LAB

• Sample should be easily withdrawn for automatic or manual analysis without interrupting the flow characteristics of liquid.

• Should be capable of allowing the evaluation of disintegrating, non-disintegrating, floating tablets or capsules, finely powdered drugs and novel dosage forms.

IDEAL FEATURES OF DISSOLUTION APPARATUS

Page 11: Dissolution apparatus POST-LAB
Page 12: Dissolution apparatus POST-LAB
Page 13: Dissolution apparatus POST-LAB

APPARATUS NAME DRUG

PRODUCT

I ROATING BASKET

TABLETS

II PADDLE Tab, capsules modified drug products

III RECIPROCATING CYCLINDER

ER drug products

IV FLOW CELL Drugs w/ low water sol drug

Page 14: Dissolution apparatus POST-LAB

APPARATUS NAME DRUG

PRODUCT

V PADDLE OVER DISK

Transdermal

VI CYLINDER Transdermal

VII RECIPROCATING DISK

ER products

VIII NON USP NF ER products

Page 15: Dissolution apparatus POST-LAB

APPARATUS NAME DRUG

PRODUCT

IX NON USP NF Ointments creams

transdermal

Page 16: Dissolution apparatus POST-LAB

PADDLE TYPE

Page 17: Dissolution apparatus POST-LAB

PADDLE TYPE

Page 18: Dissolution apparatus POST-LAB

PADDLE TYPE

• Design

1. Vessel

2. Shaft: the blade passes through the shaft so that the bottom of blade fuses with bottom of shaft.

3. Stirring elements: Made of Teflon/ stainless steel

Page 19: Dissolution apparatus POST-LAB

PADDLE TYPE

4. Waterbath: Maintain at 37 + 0.5C

5. Sinkers: Platinum wire used to prevent capsule tablet from floating.

Page 20: Dissolution apparatus POST-LAB

PADDLE TYPE

Page 21: Dissolution apparatus POST-LAB

PADDLE TYPE

• Consist of a special, coated paddle that minimizes turbulence due to stirring.

• The paddle is attached vertically to a variable-speed motor that rotates at a controlled 40 speed.

Page 22: Dissolution apparatus POST-LAB

PADDLE TYPE

• The tablet or capsule is placed into the round bottom dissolution flask, which minimizes turbulence of the dissolution medium.

• The apparatus is housed in a constant-temperature water hall maintained at 37C similar to a rotating basket method.

Page 23: Dissolution apparatus POST-LAB

• The position and alignment of the paddle are specified in the USP. The paddle method is very sensitive to tilting. Improper alignment may drastically affect the dissolution results with some drug products.

PADDLE TYPE

Page 24: Dissolution apparatus POST-LAB

• The most common operating speed for apparatus II are 50 rpm for solid oral dosage forms and 25 rpm for suspensions

PADDLE TYPE

Page 25: Dissolution apparatus POST-LAB

• Apparatus II is generally preferred for tablets.

• A sinker such as a few turns of platinum wire may be used to prevent a capsule or tablet from floating.

PADDLE TYPE

Page 26: Dissolution apparatus POST-LAB

Dissolution Sampling

• Use of Water is LIMITED

• Additives (enzymes and salt)

• Agitation (50-100 rpm)

• Media temp (37 +/- 0.5C oral)

(38 +/- 0.5C special; rectal)

( 32 +/- 0.5C transdermal)

•Use of sinkers

Page 27: Dissolution apparatus POST-LAB

Dissolution media

• Required major characteristics of a dissolution medium

1. Should be a representative of the liquid phase present in the tract (aqueous)

2. Physiologically, the dissolution medium has to be water or water based.

Page 28: Dissolution apparatus POST-LAB

Dissolution media

Potassium or NaOH soln, although water-based, their use is restricted by their high pH values not found in the GI tract

Page 29: Dissolution apparatus POST-LAB

Types of dissolution media

• Purified water• Dilute acid (0.001 N- 0.1 HCl)• Simulated gastric fluid (w or without

enzymes)• Simulated intestinal fluid(w or wo enzyme)Surfactants ( w or w/o acids or buffers)Buffered aqueous sol’n (pH 4-8)

Page 30: Dissolution apparatus POST-LAB

Selection of dissolution media

• Oral formulation

-physiological pH

pH 1.2-6.8 for IR formulations

pH 1.2- 7.5 for MR formulations

Page 31: Dissolution apparatus POST-LAB

Selection of dissolution media

• Low solubility compounds

Surfactants (eg polysorbate, SLS, bile)

Wetting agent

Solubilizing agent

Page 32: Dissolution apparatus POST-LAB

CALCULATIONS

1. mg/ tablet = Au/ As x conc of std(ug/mL)/1000 X DF X average wt of tab

weight of tab

Where: Au - absorbance reading of sample

As - absorbance reading of standard

DF - Dilution factor

900 X 50 mL = 50,000

0.9 1 tab

Page 33: Dissolution apparatus POST-LAB

2. % of labeled claim=actual amount obtainedX100

labeled claim

USP LIMITSNot less than 80% of the labeled amount of acetaminophen is dissolved in 30 mins.

CALCULATIONS

Page 34: Dissolution apparatus POST-LAB

DISSOLUTION

• Drug Dissolution testing is routinely used to provide critical in vitro drug release information for QC purpose.

Uses:

1. To assess batch consistency of solid DF

2. To predict in vivo drug release profiles

3. To assist in decisions concerning need for bioavailability studies.

Page 35: Dissolution apparatus POST-LAB

Sample Calculation:

Find: mg/ tablet% labelled claim

DATA : 500 mg Mefenamic acidAs - 3.214Au - 3.210Wt of 10 tabs - 6.53 gAve wt - 0.65 gActual wt - 0.653 g

Page 36: Dissolution apparatus POST-LAB

SOLUTION

1. mg/ tablet = Au/ As x conc of std(ug/mL)/1000 X DF X average wt of tab

weight of tab

= __________________

= __________________

Page 37: Dissolution apparatus POST-LAB

SOLUTION

2. % of labeled claim=actual amount obtainedX100

labeled claim

= _______________

= _______________