Suppository mfg and evaluation

SUPPOSITORY: 

1 SUPPOSITORY Presented By : Mr. Naresh Rajgor, Assistant Professor, M.P. Patel College of Pharmacy, Kapadwanj

DEFINITION: 

2 DEFINITION Suppositories are MEDICATED solid dosage forms of various shapes and sizes meant for insertion into body cavities like rectum, vagina, urethra, ear and nose.

Suppositories : 

3 Suppositories Suppositories are medicated, solid bodies of various sizes and shapes suitable for introduction into body cavities for local or systemic effect. The medicament is incorporated into a base such as cocoa butter which melts at body temperature, or into one such as glycerinated gelatin or PEG which slowly dissolves in the mucous secretions. Suppositories are suited particularly for producing local action, but may also be used to produce a systemic effect or to exert a mechanical effect to facilitate emptying the lower bowel.

Suppository Base: 

Suppository Base 1- Oleaginous (fatty) bases: Cocoa butter or Theobroma oil 2- Water soluble or miscible bases: Glycerinated gelating, polyethylene glycol 4

METHODS OF PREPARATION : 

5 METHODS OF PREPARATION Suppositories can be prepared by one of three methods. 1. Hand Rolling It is the oldest and simplest method of suppository preparation and may be used when only a few suppositories are to be prepared in a cocoa butter base. It has the advantage of avoiding the necessity of heating the cocoa butter. A plastic-like mass is prepared by triturating grated cocoa butter and active ingredients in a mortar.

PowerPoint Presentation: 

6 The mass is formed into a ball in the palm of the hands, then rolled into a uniform cylinder with a large spatula or small flat board on a pill tile. The cylinder is then cut into the appropriate number of pieces which are rolled on one end to produce a conical shape. Effective hand rolling requires considerable practice and skill. The suppository "pipe" or cylinder tends to crack or hollow in the center, especially when the mass is insufficiently kneaded and softened.

2. Compression Molding: 

7 2. Compression Molding Compression molding is a method of preparing suppositories from a mixed mass of grated suppository base and medicaments which is forced into a special compression mold using suppository making machines. The suppository base and the other ingredients are combined by thorough mixing. The friction of the process causing the base to soften into a past-like consistency.

PowerPoint Presentation: 

8 On a small scale, a mortar and pestle may be used (preheated mortar facilitate softening of the base). On large scale, mechanically operated kneading mixers and a warmed mixing vessel may be applied. In the compression machine, the suppository mass is placed into a cylinder which is then closed. Pressure is applied from one end to release the mass from the other end into the suppository mold or die.

PowerPoint Presentation: 

9 When the die is filled with the mass, a movable end plate at the back of the die is removed and when additional pressure is applied to the mass in the cylinder, the formed suppositories are ejected. The end plate is returned, and the process is repeated until all of the suppository mass has been used. The method requires that the capacity of the molds first be determined by compressing a small amount of the base into the dies and weighing the finished suppositories. When active ingredients are added, it is necessary to omit a portion of the suppository base, based on the density factors of the active ingredients.

3. Fusion Molding: 

10 3. Fusion Molding Fusion Molding involves: 1- Melting the suppository base 2- Dispersing or dissolving the drug in the melted base. 3- The mixture is removed from the heat and poured into a suppository mold. 4- Allowing the melt to congeal 5- Removing the formed suppositories from the mold. The fusion method can be used with all types of suppositories and must be used with most of them.

Suppository molds: 

11 Suppository molds Small scale molds are capable of producing 6 or 12 suppositories in a single operation. Industrial molds produce thousands of suppositories per hour from a single molding.

Packaging: 

Packaging Suppositories must be packed in such a manner that they do not touch each other. Staining, breaking or deformation by melting caused by adhesion can result from poorly wrapped and packaged suppositories. Suppositories usually are foiled in tin or aluminium, paper or plastic strips. Overwrapping is done with hand or machine. Hand packing yields a nonuniform products. Machines overcome this problem and can wrap 8000 suppositories per hour . 12

Storage: 

Storage Suppositories should be protected from heat, preferably by storing in the refrigerator. Polyethylene glycol suppositories and suppositories enclosed in a solid shell are less prone to distortion to temperature slightly above body temp. STORE IN A COOL PLACE OR REFRIGERATOR FOR EXTERNAL USE ONLY 13

Testing/Evaluation of suppositories: 

14 Testing/Evaluation of suppositories Finished suppositories are routinely inspected for: Appearance. Content uniformity Melting range test Breaking Test Drug release test Disintegration test Dissolution Testing Liquefaction or Softening time

Breaking test (Hardness): 

15 Breaking test (Hardness) To measure the brittleness of suppository Double wall chamber in which the test suppository is placed. Water at 37ºC is pumped through the double wall. The suppository supports a disc to which rod is attached. The other end of the rod consist of another disc to which weights are applied.

PowerPoint Presentation: 

16 The test was conducted by placing the suppository to support the axis of 600 g weight. At one minute intervals 200 gm weights are added. The weight at which the suppository collapses is the breaking point When the breaking point reached in the first 20 sec, the added weight was not calculated When the breaking point reached in the second 20 sec, half the added weight was calculated When the breaking point reached in the third 20 sec, all the added weight was calculated

Melting range test: 

17 Melting range test Macro-melting range is a measure of the time it takes for the entire suppository to melt when immersed in a constant-temperature (37ºC) water bath. The apparatus commonly used for measuring the melting range of the entire sppositories is a USP tablet Disintegration Apparatus.

In-vitro drug release: 

18 In-vitro drug release In-vitro drug release pattern is measured by using the same melting rang apparatus. Aliquots of the release medium were taken at different time intervals within the melting period. The drug content in the aliquots was determined. The drug release pattern was plotted (time versus-drug release curve)