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HOMOGENEOUS OINTMENTS Author: as. Yu.Yu. Plaskonis Ointments are the soft medical form, appointed for causing on a skin, wounds and consist of basis and medicinal substances, evenly divided. •For physical and chemical classification: ointments are the free comprehensively dispersible shapeless structured systems from plastic-resiliently viscid dispersible environment. At the room temperature, ointment, as a result of high viscidity, keep a form and lose it at the increase of temperature, growing into thick liquids. From typical liquids they differ absence of noticeable fluidity. Negative qualities: some ointments have the limited spectrum of pharmacological action; some connections of ointments on hydrophobic bases can make the expressed «greenhouse» effect which limits their application in medical practice; some ointments can irritate the skin. Positive qualities: possibility of introduction in the complement of ointments different medicinal substances (liquid, soft, hard); possibility of prescription of ointments with the local action or resorbtion action; achievement of high concentration of medicinal substances in a skin, biological liquids of organism; simple and safe application of ointments is in comparing to other medical forms. Requirements to ointments Ointments must own certain consistency properties which are characterized by some indexes: by plasticity, viscidity, period, relaxations on which in a great extent depends the degree of pharmaceutical dynamics of ointments. Ointments must have optimum dispersion of medicinal substances and their distributing ,which guarantees a maximal therapeutic effect and invariability of connection at storage. At the same time they must be stable, without admixtures and with the exact concentration of medicinal substances. CLASSIFICATION OF OINTMENTS According to a place of application distinguish such ointments: dermatological (actually ointments) which are used on a skin eye which are used on the conjunctiva of eye for a nose vaginal urethral rectal By the type of the dispersible systems (in dependence on the degree of dispersion of medicinal substances and character of its distributing in basis) distinguish: homogeneous heterogeneous ointments. Depending on consistency distinguish: liquid ointments (whether liniments) creams gels actually ointments dense ointments - pastes On the type (by character) of ointment bases distinguish ointments, prepared on: hydrophobic hydrophilic diphilic (hydrophilic-hydrophobic) bases. PROPERTIES OF OINTMENT BASES Oleaginous Absorption Ointment Bases Ointment Bases Water/Oil Oil/Water Water-miscible Emulsion Emulsion Ointment Bases Ointment Bases Ointment Bases oleaginous base + oleaginous base + oleaginous base + Polyethylene w/o surfactant water (< 45% water (> 45% Glycols (PEGs) w/w) + w/o w/w) + o/w surfactant (HLB surfactant (HLB <8) >9) anhydrous hydrous hydrous anhydrous, hydrous hydrophilic hydrophilic hydrophilic hydrophilic Composition oleaginous compounds Water Content anhydrous Affinity for Water hydrophobic Spreadability difficult difficult Washability nonwashable nonwashable Stability Drug Incorporation Potential moderate to easy easy moderate to easy non- or poorly washable washable washable oils poor; oils poor; unstable, unstable, stable hydrocarbons hydrocarbons especially alkali especially alkali better better soaps and natural soaps and natural colloids colloids; nonionics better solids or oils (oil solids, oils, and solids, oils, and solid and aqueous solid and aqueous solubles only) aqueous solutions aqueous solutions solutions (small solutions (small amounts) (small amounts) amounts) Drug Release Potential* Occlusiveness Uses Examples Composition Oleaginous Ointment Bases Absorption Ointment Bases poor poor, but > oleaginous yes yes protectants, protectants, emollients (+/-), emollients (+/-), vehicles for vehicles for hydrolyzable aqueous solutions, drugs solids, and nonhydrolyzable drugs White Petrolatum, Hydrophilic White Ointment Petrolatum, Anhydrous Lanolin, Aquabase™, Aquaphor®, Polysorb® Oleaginous Absorption Ointment Bases Ointment Bases oleaginous compounds Water/Oil Emulsion Ointment Bases fair to good Oil/Water Emulsion Ointment Bases fair to good Water-miscible Ointment Bases sometimes no no emollients, emollients, cleansing creams, vehicles for solid, vehicles for solid, liquid, or nonliquid, or nonhydrolyzable hydrolyzable drugs drugs Cold Cream type, Hydrous Lanolin, Rose Water Ointment, Hydrocream™, Eucerin®, Nivea® Hydrophilic Ointment, Dermabase™, Velvachol®, Unibase® Water/Oil Oil/Water Emulsion Emulsion Ointment Bases Ointment Bases oleaginous base + oleaginous base + oleaginous base + w/o surfactant water (< 45% water (> 45% w/w) + w/o w/w) + o/w surfactant (HLB surfactant (HLB <8) >9) good drug vehicles PEG Ointment, Polybase™ Water-miscible Ointment Bases Polyethylene Glycols (PEGs) By the type of the dispersible systems ointment divided to: * homogeneous ointment ointments- solutions ointments- alloys extraction ointment * heterogeneous ointments- suspensions ointments - emulsion combined Heterogeneous Suspension ointments contain solid powder, grind medicinal substances which are insoluble in the basis and distributed it by type of suspension Emulsion ointment characterized by the presence of the liquid component that is insoluble in basis and distributed it to the type of emulsion. Combined ointment - a combination of different disperse systems The main task of technology in the manufacture of ointments is that the drugs have been possible dispersed and evenly distributed throughout the mass basis; consistency would provide easy dab and uniform distribution of the skin or mucous membrane, the stability of the ointment would ensure consistency in the application of their composition and storage Prescription OF OINTMENTS 1. With indication of basis and amount of medicinal substances in units of mass: Rp.: Mеntholi 0,1 Vaselini 10,0 Miscе, fiat unguеntum Da. Signa: Ointment is for a nose. 2. Without indication of basis: а) with pointing of concentration of medicinal substance Rp.: Unguenti Zinci oxydi 3 % 10,0 Da. Signa: Ointment is for hands. б) without pointing of concentration of medicinal substance Rp.: Unguenti Xеroformii 100,0 Da. Signa: Zmazuvati the staggered areas of skin. GENERAL RULES OF PREPARING OINTMENTS Calculations of amounts of medicinal substances and basis If the concentration of medicinal substance was`t noted in a recipe, it is followed to prepare 10 % ointment. Ointments the samples of which are standardized. prepare according to concentration of medicinal substances, marked in NTD. Introductions of medicinal substances in ointment conduct taking into account their physical and chemical properties and written amounts. Medicinal substances, soluble in fats (Camphor, Mentholum, Thymolum, , a crystalline Fenolum, Anaesthesinum less than 2 %, Salol but, other) enter in monophase ointments-solutions, dissolving them in fat basis or its component part. If total amount of these substances less than 5 %, they are ground with a liquid, what similar after properties to basis: Vaseline -Vaseline oil, fatty basis drupaceous butter. Liquids take so much, how many matters. If total amount of these substances more than 5 %, they are ground with an even amount to mass of dry substances of molten basis. In hydrophilic bases these substances enter like suspensions. Preparing of homogeneous ointments Ointments-alloys are connection of a few mutually fusible and mutually soluble components. Fats can enter in the complement of such ointments, beeswax, hydrocarbons, resins, plasters, butters, and other substances. Ingredients can be both hard and soft or liquid. The alloy of components is conducted on an aquatic bath in a porcelain or enameled cup. General technology of ointmentsalloys consists in the following: in the first turns melt the most refractory substance to the got fusion add other ingredients in order of decline of temperature of melting; liquid components add in the last turn this liquid fusion if necessary strain through a gauze in a warmed-up mortar (50-55 °С) mix to cooling essential oils add in the last turn at a temperature not higher 40 С. Comparative fusibility of substances which enter in the complement of ointments-alloys is resulted below in such order: 1. Tserezin 2. Ozocerite 3. A beeswax is yellow 4. A beeswax is white 5. Petrolatum 6. Paraffin hard 7. Spermaceti 8. Beef fat 9. Lanolin is waterless 10. Vaseline 11. Hydrogenated fats 12. Naphthalanum 13. Butters vegetable and artificial 14. Essential oils Rp.: Naphthalani liquidi raffinati 70,0 Paraffini 18,0 Petrolati 12,0 Misce, fiat unguentum Da. Signa. For bandages. Medicinal preparation – ointment alloy with mutually fusible components which have a different temperature of drowning. Melt petrolatum (t - 60-62 °С), to the got fusion at stirring add a paraffin (t - 50-54 °С) and in the last turn - oil naphthalini. An alloy is mixed in a warm mortar to the complete cooling-down. WPC (f.s.) Date № recipe Petrolati 12,0 Paraffini 18,0 Naphthalani of liquidi raffinati 70,0 m= 100,0 Prepared: (signature) Checked: (signature) Medicinal substances, soluble in fats (camphor, Mentholum, Thymolum, a crystalline phenolum, Anaesthesinum to 2 %, salol but other) enter in mono phase ointments-solutions, dissolving them in fat basis or its component part. Ointment- solution If total amount of these substances is less than 5 %, they are ground with a liquid, what similar by the properties to basis: Vaseline is Vaseline butter, fatty basis is drupaceous butter. Liquids take so much, how many matters If total amount of these substances is more than 5 %, they are ground with an even amount to mass of dry substances of molten basis. At preparing of ointments-solutions it is needed to take into account the following rules: if a medicinal substance has a volatile characteristics (camphor, Mentholum, other), then it is dissolved in the cold fusion (45-50 °С); it is not followed to prepare satiate solutions, because permeates can crystallize at cooling; many medicinal preparations, soluble in hydrophobic bases, reduce the temperature of melting of the last as a result of education eutectic, that is why for a receipt enough dense ointmentssolutions in the contain of ointment bases enter making more compact components (10% beeswax or paraffin) on a concordance with a doctor. THANK YOU FOR ATTENTION !