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Repected Sir Kindly mail me yours ppt of topic semisolid and sterile dossage form at my email id. Regards Rimpi

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SEMISOLID DOSAGE FORMS Presented By : Mr. Naresh Rajgor, Assistant Professor, M.P. Patel College of Pharmacy, Kapadwanj


SEMISOLID DOSAGE FORMS They are dermatological products and applied to the skin for therapeutic or protective action or cosmetic function.


Advantages Patient convenient. Easily compounded Melting & softening at body temperature Ease of application. Prevent first pass metabolism. Immediately available for absorption.

Disadvantages :

Disadvantages Some dosage form may irritate the skin. Barrier function changes from person to person and within the same person. Patients have no accurate measuring device. May not be economical.


TYPES OF SEMISOLID DOSAGE FORMS Ointment Cream Paste Gels Poultices Plasters


OINTMENT Any greasy or oily semi-solid preparation, usually medicated, that can be applied externally to the skin in order to heal, soothe or protect it. It is a viscous semisolid preparation used topically on a variety of body surfaces. Drug ingredients can be dissolved, emulsified or suspended in the ointment base.


CREAM Are ointments of a particularly soft consistency they are usually emulsion ointments. They are viscous liquid or semisolid emulsions of oil-in-water or water-in-oil type. Easier to spread and easier to remove than ointments.


PASTE Have very solid consistency and contain usually relatively large quantities of solids. Contain a larger percentage of solid material than ointments (thicker and stiffer). Will not soften and flow after application .


Gels Gels are aqueous colloidal suspensions of the hydrated forms of insoluble medications. Jellies are trasparent, nongreasy semisolid preparation mainly used externally. In gels and gellies, hydrated threads or granules of the disperse phase are intimately associated with the dispersion medium.

Mechanism of Drug Penetration through the skin :

Mechanism of Drug Penetration through the skin Epidermis: Stratum corneum (Horny cell layer) Stratum lucidum (Clear layer) Stratum granulosum ( Granular Layer) Stratum spinosum (Prickly layer) Stratum germinativum Dermis: Hypodermis or Subcutaneous layer: STRUCTURE OF SKIN:

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12 STRUCTURE OF SKIN : Epidermis: The outer layer of skin is made up of Stratified Squamous epithelial cells. Epidermis is thickest in palms and soles. The stratum corneum forms the outer most layer (10-15µm thick ) which consists of many layers of compacted , flattened, dehydrated keratinized cells. The stratum corneum is responsible for the barrier function of the skin and behaves as a primary barrier to the percutaneous absorption. Water content of stratum corneum is around 20%. The moisture required for stratum corneum is around 10% (w/w) to maintain flexibility and softness. It consists of Cermides and neutral lipids such as Sterols, free fatty acids and triglycerides.

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14 DERMIS: The dermis is made up of regular network of robust collagen fibers of fairly uniform thickness with regularly placed cross striations . This network or the gel structure is responsible for the elastic properties of the skin. It is supplied by blood to convey nutrients, remove waste & regulate body temp. Drug is well absorbed by this route. Upper portion of the dermis is formed into ridges containing lymphatics and nerve endings.

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15 SUBCUTANEOUS TISSUE: This is a sheet of the fat containing areolar tissue known as the superficial fascia, attaching the dermis to the underlying structures . SKIN APPENDAGES: Sweat glands produces sweat of pH 4-6.8 & absorbs drugs, secretes proteins, lipids and antibodies. Its function is to control heat. HAIR FOLLICLES: They have sebaceous glands which produces sebum and includes glycerides, cholesterol and squalene.

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16 Routes of drug absorption through skin: Trans follicular route Trans epidermal route 16

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17 TRANSFOLLICULAR ROUTE: Fractional area available through this route is 0.1 % Human skin contains 40-70 hair follicles, 200 to 250 sweat glands on every of skin area. Mainly water soluble substance are diffused faster through appendages than that of other layers. Sweat glands and hair follicles act as a shunt i.e. easy pathway for diffusion through rate limiting ST corneum .

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18 TRANS EPIDERMAL ROUTE Epidermal barrier function mainly resides in horny layer The viable layer may metabolize, inactivate or activate a prodrug. Dermal capillary contains many capillaries so residence time of drug is only one minute. Within stratum corneum molecule may penetrate either transcellularly or intercellularly. Intracellular region is filled with lipid rich amorphous material.

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20 Process of permeation.

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22 FACTORS AFFECTING TRANSDERMAL PERMEABILITY Physico chemical properties of parent molecule Solubility and partition co- efficient pH condition Penetrant concentration Physico chemical properties of drug delivery system Release characteristic Composition of drug delivery system Permeation enhancer used

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23 Physiological and pathological condition of skin Lipid film Skin hydration Skin temperature Effect of vehicle Pathological injury to skin Biological factors Skin age Thickness of S. Corneum Skin condition 23

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Semisolid base

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Ideal requirements of Semisolid Base

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2. ABSORPTION BASE The absorption bases are formed by the addition of substances miscible with hydrocarbons and possessing polar grouping, such as the sulphate , sulfonates , carboxyl, hydroxyl or an ether linkage. Lanolin, lanolin isolates, cholesterol, lanosterol may be added to make the hydrocarbon bases hydrophilic. The bases do not absorb water on contact but with sufficient agitation, they do absorb aqueous solutions and can be considered W/O emulsion.

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The maximum amount of water that can be added to 100 g of such a base at a given temperature is known as the water number. To determine the water number, the base is stirred continuously as the water is being added. Distilled or deionized water should. The end point is reached when no more water can be absorbed into base, as evidenced by droplets of water remaining in the container. Type a. anhydrous form b.hydrous/emulsion form

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a. anhydrous form

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a. Hydrous form

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(b) Oil in water Emulsion Base: They are Hydrous Hydrophilic Insoluble in water Water washable O/W emulsion Non-greasy Capable of dilution with water

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MANUFACTURING OF SEMISOLID DOSAGE FORMS: Time, temperature and mechanical work are the three variables in the manufacturing of emulsified semisolid. The three factures are interrelated and must be carefully controlled if the same high quality batches are to be manufactured repeatedly. Equipments available are automatically controlled the above variables.

Preparation of oil and aqueous Phases:

Preparation of oil and aqueous Phases The components of the oil or fat mixture are placed into a stainless steel steam-jacketed kettle, melted and mixed. Some of the solid components like stearic acid, cetyl alcohol are available in many different forms: cakes, flakes or powder. The flakes are preferable because of the convenience of handling. The powder form may have metal contamination while size reduction.

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Petrolatum is inconvenient to handle unless it is melted and transferred by pumping or pouring from its drum. The liquefied petrolatum can then be transferred to the mixing kettle by metering pump. The oil phase is then strained through several layers of cheese cloth to remove any foreign matter or it can be passed through the filter medium particularly for ophthalmic preparation. The kettle is heated to a temperature of the oil phase to prevent some of its higher melting components from congealing. The components of the aqueous phase are dissolved in the purified water and filtered. A soluble drug may be added to the aqueous phase at this time. Provided the high temperature does not degrade of active substance.

Basic components of semisolid Preparations:

Basic components of semisolid Preparations 1 Emulsifiers Sorbitan monostearate Sorbitan monooleate Sodium lauryl sulphate Polysorvate 80 2 Fat Phase Components Glyceryl monostearate , Cetyl alcohol, Spermiceti , Steryl alcohol, Stearic acid, Petrolatum, Liquid paraffin Cetostearyl alcohol, Isopropyl palmitate 3 Polyols Glycerin Propylene glycol pEG 400 PEG 600 4 Antimicrobial agents Methylparaben , Propylparaben , Ethylparaben , Butylparaben Chlorocresol , Thimersol , Sorbic acid, Potassium sorbate 5. Buffering agents Citric acid Phosphoric acid Monobasic sodium phosphate

Mixing of Phases:

Mixing of Phases The phases are usually mixed at a temperature of 70-72 0 C, because at this temperature intimate mixing of the liquid phases can occurs. The phase mixing temperature can be lowered a few degrees if the melting point of the fat phase is low enough to prevent the premature crystallization. The phase can be mixed by three ways, 1. Simultaneous blending of the phase 2.Addition of the discontinuous phase into continuous phase 3.Addition of the continuous phase into discontinuous phase.

Cooling of semisolid Preparation:

Cooling of semisolid Preparation Following addition of the phases, the rate of cooling is generally slow to allow for adequate mixing while the emulsion is still liquid. The temp. of the cooling medium in the kettle jacket should be decrease gradually and at a rate consistent with the mixing of the emulsion and scrapping of the kettle walls to prevent formation of congealed masses of the ointment or cream. If perfume should be added at a 43-45 O C temp. The drug is added in solution form, if not already incorporated or as a crystal if it is soluble in external phase. An insoluble powder should be dispersed in the continuous prior to removing the semisolid from the kettle for homogenization and or storage.


Homogenization The creams or ointments that require further treatment are then transferred or pumped to the proper homogenizer, the selection of which is governed by the degrees and the rate of shear stress required. The choices include a low-shear pump, a roller mill, a colloid mill and a valve type homogenizer. Uniform dispersion of an insoluble drug in a semisolid, as well as reduction of the size of the fatty aggregates can be achieved by the passage of the warm ointment or cream through a homogenizer or mill.

Storage of semisolids:

Storage of semisolids The specified quality control tests have been completed before packaging into appropriate containers like tubes, jars or single-dose packets are used. A product is considered to be “in-process” until it has been packaged. These preliminary quality control tests are time consuming and delay the packaging process. Some semisolid becomes viscous when storage , such products cannot be stored for any length of time. To prevent water evaporation , the container is to be closed until packaging.

Transfer of material for packaging:

Transfer of material for packaging Once a formal manufacturing procedure has been established, there should be no deviation from it. If a change is necessary, the problem should be carefully re-evaluate, first in R & D and then pilot plant and manufacturing level. Homogenizers, pumps and filling equipments that have areas wherein pockets f water or product may accumulate and that are ordinarily inaccessible must be completely disassembled, cleaned, sanitized and dried before reassembly.

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Semisolids are usually dispersed in either jars or tubes. Jars are available in brown, green white glass or plastic bottle. Aluminum and tin tubes are also used. Now a days plastic tubes are also available. The Packed material should be labeled with the following instruction FOR EXTERNAL USE ONLY STORE IN A COLL AND DRY PLACE


EVALUATION PARAMETERS 1.Penetration of the base through the skin 2.Absorption of the drug into the blood Stream 3.Rate of release of the drug from the base

1. Tests for penetration:

1. Tests for penetration A. Wild Test He has taken fixed quantity of various base (X gm) Rubbed on fixed area for fixed time. The unabsorbed base was carefully collected from the skin and weighs (Y gm). The difference (X–Y gm)gave amount of penetrate. B. STRAKOSCH Test Fixed amount of base rubbed on skin in well defined conditions Historical examinations of human skin biopsies at different interval of 24 hrs made to determine the amount of penetration.

2. Test for absorption:

2. Test for absorption A. Bliss Test: Fixed amount of medicated base rubbed on fixed area for fixed time. The concentration of drug measured in urine. Drugs used are Methyl salicylate, Iodine, Pot. Iodide. B. Johnson Test: He used Radio active sod. Chloride as the medicament. Radioactive substance was measured in the tissues and in the urine.

3. Rate of Release :

3. Rate of Release A. In vivo Test (performed by Skimmer) He used Na-flourescein as a drug. Mixed with different base. Rubbes on fixed area for a fixed time. Intensity of pigmentation (coloration) measured. More pigmentation indicates more release.

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B. In Vitro Test:


GELS Gels are aqueous colloidal suspensions of the hydrated forms of insoluble medicaments. In gels hydrated threads or granules of the disperse phase are infinitely associated with the dispersion medium. Gels contain polymer less than 10% and they may be clear to turbid depending upon aggregation formation of polymer. The gels forming polymers are Natural Polymers like tragacanth, pectin, agar, carrageen, alginic acid, gelatin. Synthetic & semi synthetic Polymers like Methyl Cellulose, HMC, Carbopols , CMC. Fluid phase may be water or water miscible organic solvents. Evaporation of the water produces a pleasant cooling.

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