selection of dissolution medium And dissolution study of solid dosage form

University seminar On

Selection Of Dissolution Media & Dissolution Study Of Solid Dosage

Form

H.R.Patel Institute of Pharmaceutical

Education & Research , Shirpur.

Guided by:DR. P. K. DESHMUKH(Department of pharmaceutics)

Presented by:PATIL ASHWIN ANIL(F. Y. M. Pharm Department of pharmaceutics)

CONTENT Introduction & Defination Human GI tract pH Selection criteria of dissolution medium Types of dissolution media Selection of RPM Selection of dissolution time interval Selection of other parameters like, media volume, temperature, etc. Dissolution test of colonic drug delivery system Dissolution of solids ---Powders ---Tablet ---Capsules Mechanism of dissolution Apparatus type 1 & 2 Advantages and disadvantages Conclusion Reference

06/10/2015ASHWIN PATIL Selection Of Dissolution Media & Dissolution Study Of Solid Dosage Form 2

INTRODUCTION1

Dissolution testing of dosage forms is considered one of the most important quality control tools while assessing the efficacy of a product in vitro

The process of dissolution of an active ingredient from solid pharmaceutical dosage forms involves several intermediate physiochemical steps, such as wetting, swelling, capillarity, solubility, and diffusion


DEFINATION2

“Dissolution is the process by which a solid substance enters the solvent phase to yield a solution i.e. mass transfer from solid surface to liquid phase”.

Dissolution Rate: It is the amount of drug substance that goes in solution per unit time under standardized conditions of temperature and solvent composition.


IMPORTANCE2

Dissolution testing is mainly used to confirm product quality and batch-to-batch consistency.

Dissolution testing finds application in bioavailability problems and bioequivalence studies.

In R&D department, comparing In vitro dissolution data with In vivo bioavailability, we would greatly facilitate product development.



HUMAN GI TRACT pH9

pH in different parts of GIT


Part of GIT pHStomach Fasted state 1.5-2

Fed state 2-6Small intestine 6.6- 7.5ColonAscending colon 6.4Transverse colon 6.6Descending colon 7.0

SELECTION OF DISSOLUTION MEDIUM3

Selection of dissolution medium depends upon following parameters. Type of formulation (Immediate or modified

release). Solubility characteristics of active component. Type formulation design, e. g. Soft gel capsule,

Hard gel capsule, Tablets, Suspension, powder etc.


TYPES OF DISSOLUTION MEDIA2

1. COMPENDIAL DISSOLUTION MEDIA:a) Simulated Gastric Fluid:b) Water:c) Simulated Intestinal Fluid:2. BIORELEVENT MEDIA:a) Fasted State Gastric Conditions: FaSSGF:b) Fasted State Small Intestinal Conditions:

FaSSIF:c) Fed State Gastric Conditions:


SELECTION OF RPM3

The selection of RPM depends upon type of formulation, solubility characteristics of active substances and apparatus used for dissolution study.

For capsules (both soft gel and hard gel), USP-I i. e. Basket apparatus is recommended, rotation speed for basket shall be 50 to 75 RPM.

For tablets, USP-II i. e. paddle apparatus is recommended, rotation speed for paddle shall be 75 to 100 RPM.

Any change in apparatus and RPM other than recommended parameters should be justified.


SELECTION OF DISSOLUTION TIME INTERVEL3 Dissolution time is defined as the time in minutes

at which maximum amount of drug is dissolved. For immediate release dosage forms, dissolution

time from 30min. to 60min. In some cases dissolution time may be higher i. e.

up to 90min. to l20min. For modified release formulations (delayed release,

enteric coated and sustained release), time depends upon design of formulation, site of action and therapeutic use. Time for such formulations may be from about 6 hrs. to 24 hrs. or may be higher.


SELECTION OF OTHER PARAMETERS LIKE, MEDIA VOLUME, TEMP., ETC.3

The volume of dissolution media is ideally 900ml, however if label claim is less than 5mg and if active substances has less absorbance at selected wavelength, then in that case dissolution volume can be reduced to 500ml.

The dissolution media temperature is fixed i. e. 37.0 (±0.5)ºC

Clean the dissolution apparatus and jars with suitable detergent, but do not wash with organic solvent.


DISSOLUTION TEST OF COLONIC DRUG DELIVERY SYSTEM.8

The dissolution testing is done using the conventional basket method. The dissolution testing is done in different buffers to characterize the behavior of formulations at different pH levels.

The different media that are used for the dissolution testing of colon targeted drug delivery are


CDDs are Tested forpH 1.2 To Simulate Gastric Fluid

2hr In 0.1N HCl

pH 6.8 To Simulate Small Intestine

3hr In pH 6.8 Phosphate Buffer

pH 7.4 To Simulate Large Intestine.

Finally at pH 7.4 Phosphate Buffer

IN-VITRO ENZYMATIC TEST8

There are 2 tests for the in-vitro enzymatic test.1) The carrier drug system is incubated in fermenter

containing suitable medium for bacteria. The amount of drug released at different time intervals is determined.

2) Drug release study is performed in buffer medium containing enzymes pectinase, dextranase or guinea pig or rabbit cecal contents. The amount of drug released in a particular time is directly proportional to rate of degradation of polymer carrier



Eudragit L

Eudragit E

DISSOLUTION OF SOLIDS1

In the dissolution of solids, we have

1.Powders

2.Tablets

3.Capsules


DISSOLUTION OF POWDERS1

Wettability and Dissolution Rate of Powders The first step in the process of dissolution is wetting of the

dissolving surface, which is in contact with the dissolution medium.

The condition for complete wetting of a solid surface is that the contact angle should be Zero.

This condition is fulfilled only when the forces of attraction between the liquid and solid are equal to or greater than those between liquid and liquid.


DISSOLUTION OF TABLET1


Tablet Disintegration Granules

Non - Disintegration

Drug in the solution in GI fluid

Drug in blood

Disaggregation drug particles in suspension

DISSOLUTION OF CAPSULES1


Drug in capsule massDrug in capsule

Drug particle in Suspension

Drug in solution

Drug in blood

Dissolution of Capsule shell

MECHANISM OF DISSOLUTION1 Initial mechanical lag Wetting of dosage form Disintegration Deaggregation Dissolution Occlusion



Apparatus Type 1:Rotating Basket Type4,6

Construction-

A) Shaft-

B) Cylindrical Vessel-

C) Cylindrical Basket-

D)Variable speed motor-

E) Water bath -

Uses-capsule, tablet, floating dosage form, controlled release formulation, Conventional tablet.


Apparatus Type 1: Paddle Type4,5

Construction -

A) Shaft -

B) Vessel -

C) Paddle -

D) Water bath -

Uses- Tablets orally disintegrating

tablet, chewable tablet, capsule,

controlled release products.


USP APPARATUS 1 & 2 HAVE SOME COMMON ADVANTAGES AND DISADVANTAGES.7

ADVANTAGES apparatus of first choice for solid oral dosage

forms standardized easy to operate robust broad experience


DISADVANTAGESsimulation of the gastrointestinal transit is

not possiblehydrodynamic conditions are not knownbasket screen clogged by gummy particles


CONCLUSIONThe study of “selection of dissolution media”

is very important, because it gives an idea that which type of dissolution medium have to be use for particular oral formulation

Different dissolution media have different effect on solubility on drug or dosage form

Selection of dissolution also depends on different dosage form and formulation

So, selection of dissolution medium play important role in In-Vitro dissolution study.


REFERENCE1. Umesh V. Banakar ,Pharmaceutical dissolution testing, volume 49,informa healthcare,

new york, london.251-277.2. http://www.pharmatutor.org/articles/review-selection-of-dissolution-media (Access on

dated 22/09/2015)3. Sp. karuppiah, Analytical method development for dissolution release of finished solid

oral dosage forms int j curr pharm res, vol 4,issue 2, 2012, 48-53 4. C.V.S. Subrahmanyam, Textbook of physical pharmaeutics,2012,vallabh

prakashan,delhi.85,102.5. http://www.metrolab.gr/Uploads/QLA_Paddles_01.JPG (Access on dated 2/10/2015)6. http://statics.smi-labhut.com/uploads/images/rotating-basket.gif

(Access on dated 2/10/2015)7. Riaz Uddin, Nadia Saffoon and Kumar Bishwajit Sutradhar Dissolution and Dissolution

Apparatus Review Int J Cur Biomed Phar Res.2011; 1(4): 201-207

8. Singh Amritpal, Sharma Ankush, Pooja, Anju Novel approaches for colon targeted drug delivery system int. J. Res. Dev. Pharm. L. Sci. February - march, 2014, 3(2), 877-886

9. http://image.slidesharecdn.com/jmsirius2009b-091125074146-phpapp01/95/measuring-pkas-logp-and-solubility-by-automated-titration-9-728.jpg?cb=1259134981(Access on dated 05/10/2015)


http://www.pharmatutor.org/articles/review-selection-of-dissolution-media

http://www.metrolab.gr/Uploads/QLA_Paddles_01.JPG

http://www.metrolab.gr/Uploads/QLA_Paddles_01.JPG

http://statics.smi-labhut.com/uploads/images/rotating-basket.gif

http://statics.smi-labhut.com/uploads/images/rotating-basket.gif

http://image.slidesharecdn.com/jmsirius2009b-091125074146-phpapp01/95/measuring-pkas-logp-and-solubility-by-automated-titration-9-728.jpg?cb=1259134981




06/10/2015

ASHWIN PATIL Selection Of Dissolution Media & Dissolution Study Of Solid Dosage Form 28

selection of dissolution medium And dissolution study of solid dosage form

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