1 / 56

SUPPOSITORIES AND PESSARIES

SUPPOSITORIES AND PESSARIES. Department of pharmaceutics CHALAPATHI INSTITUTE OF PHARMACEUTICAL SCIENCES. CONTENTS. Introduction Classification of suppositories Advantages & disadvantages Ideal properties of suppositories Formulation of suppositories Preparation of suppositories

mboucher
Télécharger la présentation

SUPPOSITORIES AND PESSARIES

An Image/Link below is provided (as is) to download presentation Download Policy: Content on the Website is provided to you AS IS for your information and personal use and may not be sold / licensed / shared on other websites without getting consent from its author. Content is provided to you AS IS for your information and personal use only. Download presentation by click this link. While downloading, if for some reason you are not able to download a presentation, the publisher may have deleted the file from their server. During download, if you can't get a presentation, the file might be deleted by the publisher.

E N D

Presentation Transcript

  1. SUPPOSITORIES AND PESSARIES Department of pharmaceutics CHALAPATHI INSTITUTE OF PHARMACEUTICAL SCIENCES

  2. CONTENTS • Introduction • Classification of suppositories • Advantages & disadvantages • Ideal properties of suppositories • Formulation of suppositories • Preparation of suppositories • Evaluation & packing of suppositories

  3. Introduction • Suppositories are the solid dosage forms meant to be inserted into the body cavities like rectum , urethra and vagina ,where they melt or soften to release the drugs and exert local or systemic effects.

  4. Anatomy and Physiology of Rectum • The rectum is about 15 to 20 cm long. • It hooks up with the sigmoid colon to the north and with the anal canal to the south. • It is a hollow organ with a relatively flat wall surface, without villi and with only three major folds, the rectal valves

  5. Anatomy and Physiology of Rectum • The terminal 2 to 3 cm of the rectum is called the anal canal. • The opening of the anal canal to the exterior is called the anus. • The anus is controlled by an internal sphincter of smooth muscle and an external sphincter of skeletal muscle.

  6. Anatomy and Physiology of Rectum • Under normal conditions, the rectum is empty and filling provokes a defecation reflex which under voluntary control. • The transverse folds in rectum keep stool in place until the person is ready to go to the bathroom. Then, stool enters the lower rectum, moves into the anal canal, and then passes through the anus on its way out. • Rectum contains about 2 to 3 ml of mucous, which has a pH of 7.4 and little buffering capacity.

  7. Absorption of drugs from the rectum • Medicaments absorbed in the lower part of the rectum are delivered directly into the systemic circulation, thus avoiding any first-pass metabolism. • However, it has been found that suppositories can settle high enough in the rectum to allow at least some drug absorption into the superior vein. • Thus keeping the drug in the lower part of the rectum would be advisable.

  8. Absorption of drugs from the rectum • Insertion of a suppository into the rectum results in a chain of effects leading to the bioavailability of the drug. • Depending on the character of the base, a suppository will either dissolve in the rectal fluid or melt on the mucous layer. • Since the volume of rectal fluid is so small, complete dissolution of the base require extra water.

  9. Absorption of drugs from the rectum • Due to osmotic effects of the dissolved base, water is attracted with a painful sensation for the patient. • Independent on the base type, dissolved drugs in the suppository will diffuse out towards the rectal membrane. • The process of absorption will be passive diffusion.

  10. Classification Of Suppositories • Rectal suppositories • Vaginal suppositories ( PESSARIES ) • Urethral suppositories ( BOUGIES ) • Nasal suppositories • Ear suppositories

  11. VAGINAL SUPPOSITORY • They are also called as PESSARIES. • SHAPE : globular, oviform or cone-shaped. • Used occasionally. • Intended for local effects like contraceptives, antiseptics in feminine hygiene

  12. URETHRAL SUPPOSITORY • Also called as BOUGIES . • SHAPE – slender, pencil-shaped. • Intended for anti-bacterial or as a local anesthetic preparative for urethral examination. • Occasionally used.

  13. RECTAL SUPPOSITORY • Intended for local action to relieve constipation, irritation, itching and inflammatory associated to hemorrhoids

  14. Classification Of Suppositories Via Position Of Action LOCAL EFFECT : • In case of pain, itching and hemorrhoid. • Locally active drugs include astringents, antiseptics, local anesthetics, vasoconstrictors, anti-inflammatory, soothing and protective agents and some laxatives. SYSTEMIC EFFECT : • Anti-asthmatics, anti rheumatics, anti-pyretic and analgesics

  15. ADVANTAGES • EASILY ADMINSTERED to children, old persons, to unconscious or sometimes to mentally unstable persons who cannot swallow the drug. • Convenient mode of administration for drugs which irritate the GIT, causing vomiting and destroyed in acidic ph of stomach and enzymes of GIT. • FASTER ONSET OF ACTION as compared to oral administration because absorption of drug through rectal mucosa directly reaches blood

  16. DISADVANTAGES • They are not acceptable by the patients. • The manufacturing process is difficult. • The drugs which cause irritation to the mucous membrane cannot be administered as suppositories. • Most of the suppositories should be stored at low temperature10-20°c in a refrigerator , other wise the base gets liquified.

  17. IDEAL PROPERTIES OF SUPPOSITORY BASES • It should melt at body temperature or dissolve or disperse in body fluids. • It should release any medicament easily. • It should keep its shape when being handled. • It should be non-toxic and non-irritant to the mucous membrane. • It should be stable on storage and also stable if heated above its M.P.

  18. IDEAL PROPERTIES OF SUPPOSITORY BASES • It should be easily molded and should not adhere to the mold. • It should possess good wetting and emulsifying properties. • It should be able to incorporate a high percentage of water. • It should be chemically and physically stable

  19. IDEAL PROPERTIES OF SUPPOSITORY BASES If the base is fatty, it has the following additional requirements: • Acid value is below 0.2. • Saponification value ranges from 200 to 245. • Iodine value is less than 7. • The interval between melting point and solidification point is small.

  20. Specifications of suppository bases 1- Origin and chemical composition • The source of origin (i.e. entirely natural or synthetic or modified natural). • Physical and chemical incompatibilities with additives (i.e. preservatives, antioxidants and emulsifiers)

  21. Specifications of suppository bases 2- Melting range • Since fats do not have sharp melting point, their melting characteristics are expressed as a range indicating the temperature at which the fat start to melt and the temperature at which it is completely melted.

  22. Specifications of suppository bases 3- Solidification point • This value indicates the time required for base solidification when it is chilled in the mold. • If the interval between the melting range and solidification point is 10ºC or more, the time required for solidification may have to be shortened for a more efficient manufacturing procedure by augmenting refrigeration.

  23. Specifications of suppository bases 4- Saponification value • The number of milligrams of potassium hydroxide required to neutralize the free acids and to saponify the esters contained in 1 gm of fat is an indication of the type of glyceride (mono- or tri-) as well as the amount of glyceride present.

  24. Specifications of suppository bases 5- Iodine value • This value express the number of grams of iodine that react with 100 gm of fat or other unsaturated material. • The possibility of decomposition by moisture, acids, and oxygen (leads to rancidity in fats) increases with high iodine values.

  25. Specifications of suppository bases 6- Water number • The amount of water in grams, which can be incorporated in 100 gm of fat is expressed by this value. • The water number can be increased by addition of surface active agents.

  26. Specifications of suppository bases 7- Acid value • The number of milligrams of potassium hydroxide required to neutralize the free acid in 1 gm of substance is expressed by this value. • Low acid values or complete absence of acid are important for good suppository bases. • Free acids complicate formulation work, because they react with other ingredients and can also cause irritation when in contact with mucous membranes.

  27. Formulation of suppositories • Bases • Anti- oxidants • Emulsifying agents • Hardening agents • Preservatives • Thickening agents • Plasticizers

  28. SUPPOSITORY BASES • Bases :They are of two types • Hydrophilic bases • water-dispersible bases: • properties: These are mixtures of non-ionic surfactants which are chemically related to polyethylene glycols. • These are used alone or in combination with other types of bases • Cellulose derivatives like methylcellulose sodium carboxy methylcellulose also come under this class. Eg; polyoxyethylenesorbitan fatty acid (tween)

  29. ii)Water soluble bases: • Glycero-gelatin • This occurs as a gel .It is a mixture of gelatin, glycerol and water. • According to B.P the composition of the base is gelatin-14%w/w ,glycerol-70%w/w • To get a stiff mass, the quantity of gelatin should be increased to32%w/w and that of glycerol reduced to 40%w/w.

  30. b) Lipophilic bases • Coca butter: • Properties: It is a natural triglyceride • It can exist in more than one crystalline form i.e., it exhibits polymorphism • It consists of mixture of oleic acid , palmitic acid , stearic acid .

  31. Anti-oxidants • They protect the drug and the base from getting degraded due to oxidation. • Examples : • Ethyl or propylgallate • Ascorbic acid and its esters • Hydroquinone • Tocopherols

  32. Emulsifying agents: • They increase the water-absorbing capacity of fatty bases. This makes it possible to include aqueous solutions in the formulation. • Examples : polysorbates (tween 61) • Wool alcohol ,wool fat Hardening agents: • These are included in those formulations where the melting point of the base is decreased by the drug.

  33. These agents bring the melting point to normal. • Examples : macrogols with high molecular weight. • Preservatives : They should be included in suppositories which contain water soluble bases to prevent microbial growth. • Examples :methyl paraben , propylparaben • Thickening Agents: They increase the viscosity of molten base and prevent sedimentation of suspended insoluble solids. • Examples: Aluminium monostearate ,collodial silica ,magnesium stearate.

  34. Plasticizers • They impart plasticity to the fatty base and makes it less brittle. • Examples : • Castor oil • Glycerine or propylene glycol • Glycol • Tween 80 • Tween 85

  35. Preparation of suppositories

  36. PREPARATION METHODS • Suppositories are prepared by four methods:- • HAND MOLDING METHOD • COMPRESSION MOLDING METHOD • POUR MOLDING METHOD • AUTOMATIC MOLDING METHOD.

  37. HAND MOLD SUPPOSITORIES

  38. HAND MOLD SUPPOSITORIES • Advantages:- • Suitable for thermo labile ingredients. • Economical for the manufacture of small number of suppositories. • Disadvantages:- • No uniformity in shape & size of suppository.

  39. COMPRESSION MOLD SUPPOSITORIES [ COLD COMPRESSION]

  40. COMPRESSION MOLD SUPPOSITORIES [ COLD COMPRESSION] • Advantages:- • Suitable for thermo labile drugs. • No possibility of settling of the insoluble solids in base. • Disadvantages:- • Rate of production is low so not suitable for large scale. • Air get entrapped in the mass which leads to oxidation of ingredients.

  41. FUSION OR MELT OR POUR MOLD SUPPOSITORIES

  42. FUSION OR MELT OR POUR MOLD SUPPOSITORIES • Incorporation of drug: • Solid:-drug and additive powder mixed on warm tile • Semisolid:-triturate the ingredients on warm tile with water. this decrease the viscosity and give homogenous liquid. • Liquid:- • Volatile liquid:-they can be added to the molten base directly. • Nonvolatile liquid:- same as semisolid.

  43. AUTOMATIC MOLD MACHINE • All filling , ejection and mold cleaning operations are fully automatic • Output – 3500 to 6000 suppositories per hour • Suppository mold is lubricated with brushing or spraying and then filled to a slight excess • Excess material is removed after the mass gets solidified and collected for re – use

  44. PACK AND LABEL Packing of suppositories:- • It can be foiled in aluminum ,plastic, paper, tin strip. • Modern packing machine: nearly 8000 suppositories can be wrapped per hour. • In packing molding : In this ,the suppository mass is directly move into the series of molds which are made up of plastic. After cooling , excess mass is trimmed of . By this technique 12,000 to 15,000 suppositories can be produce per hour. • Disposable molds:- They are suitable for tropical climate. They are made up of plastic or aluminum . Labeling:- “store in a cool place.” “Not to be taken orally.”

  45. DISPLACEMENT VALUE • The volume of suppository from particular mold is uniform but its weight will vary because the density of medicament usually differ from the density of base . • To prepare product accurately , allowance must be made for the change in density of mass due to added medicament • The most convenient way of making this allowance is to use the displacement value-“ THE NUMBER OF PART BY THE WEIGHT OF MEDICAMENT THAT DISPLACE THE ONE PART BY WEIGHT OF BASE”

  46. Recent development(new trend in suppository) • Capsule suppositories • Coated suppositories • Layer suppositories • Tablet suppositories; • Compressed tablet • Effervescent base tablet

  47. EVALUATION OF SUPPOSITORIES • Appearance • Uniformity of weight • Disintegration • Test for uniformity of drug content • Breaking test • Softening time • Test of melting rang • Test for Dissolution rate

  48. APPEARANCE • Odor • Color • Surface condition • Shape • They may contain several layers • Instabilities are identified based on changes in surface texture ,color,odor

  49. WEIGHT VARIATION • Weigh individually 20 suppositories • Weigh 20 at a time • Calculate average weight • Limit: not more than 2 suppository differ from the average weight by more than 5% and no suppository differs from average weight by more than 10%

  50. HARDNESS or BREAKING TEST PLACE THE SUPPOSITORY IN THE INSTRUMENT ADD 600g, leave it for 1min If not broken add 200 gm every 1minute untill suppository is broken

More Related