HOMOGENEOUS HOMOGENEOUS OINTMENTSOINTMENTS

Author: as. Yu.Yu. Author: as. Yu.Yu. PlaskonisPlaskonis

Ointments are the soft medical Ointments are the soft medical form, appointed for causing on a form, appointed for causing on a skin, wounds and consist of basis skin, wounds and consist of basis and medicinal substances, evenly and medicinal substances, evenly divided.divided.

•For physical and chemical classification: For physical and chemical classification: ointments are the free comprehensively ointments are the free comprehensively dispersible shapeless structured systems dispersible shapeless structured systems from plastic-resiliently viscid dispersible from plastic-resiliently viscid dispersible environment.environment.At the room temperature, ointment, as a At the room temperature, ointment, as a result of high viscidity, keep a form and lose result of high viscidity, keep a form and lose it at the increase of temperature, growing it at the increase of temperature, growing into thick liquids. From typical liquids they into thick liquids. From typical liquids they differ absence of noticeable fluidity.differ absence of noticeable fluidity.

Negative qualities:Negative qualities:

some ointments have the limited some ointments have the limited spectrum of pharmacological action;spectrum of pharmacological action;

some connections of ointments on some connections of ointments on hydrophobic bases can make the hydrophobic bases can make the expressed «greenhouse» effect which expressed «greenhouse» effect which limits their application in medical limits their application in medical practice;practice;

some ointments can irritate the skin.some ointments can irritate the skin.

Positive qualities:Positive qualities: possibility of introduction in the possibility of introduction in the

complement of ointments different complement of ointments different medicinal substances (liquid, soft, hard);medicinal substances (liquid, soft, hard);

possibility of prescription of ointments possibility of prescription of ointments with the local action or resorbtion action;with the local action or resorbtion action;

achievement of high concentration of achievement of high concentration of medicinal substances in a skin, medicinal substances in a skin, biological liquids of organism;biological liquids of organism;

simple and safe application of ointments simple and safe application of ointments is in comparing to other medical forms.is in comparing to other medical forms.

Requirements to Requirements to ointmentsointments

Ointments must own certain consistency Ointments must own certain consistency properties which are characterized by some properties which are characterized by some indexes: by plasticity, viscidity, period, indexes: by plasticity, viscidity, period, relaxations on which in a great extent depends relaxations on which in a great extent depends the degree of pharmaceuticalthe degree of pharmaceutical dynamics of dynamics of ointments.ointments.

Ointments must have optimum dispersion of medicinal Ointments must have optimum dispersion of medicinal substances and their distributing ,which guarantees a substances and their distributing ,which guarantees a maximal therapeutic effect and invariability of maximal therapeutic effect and invariability of connection at storage. At the same time they must be connection at storage. At the same time they must be stable, without admixtures and with the exact stable, without admixtures and with the exact concentration of medicinal substances.concentration of medicinal substances.

CLASSIFICATION OF CLASSIFICATION OF OINTMENTSOINTMENTS

According to aAccording to a place of place of application application distinguish such ointments:distinguish such ointments:

dermatological (actually ointments) which dermatological (actually ointments) which are used on a skinare used on a skin

eye which are used on the conjunctiva of eye which are used on the conjunctiva of eyeeye

for a nosefor a nose vaginal vaginal urethral urethral rectalrectal

By the type of the dispersible systems (in By the type of the dispersible systems (in dependence on the degree of dispersion dependence on the degree of dispersion of medicinal substances and character of of medicinal substances and character of its distributing in basis) distinguish:its distributing in basis) distinguish:

homogeneous homogeneous heterogeneous ointments.heterogeneous ointments.

Depending on consistency distinguish:Depending on consistency distinguish: liquid ointments (whether liniments) liquid ointments (whether liniments) creams creams gels gels actually ointments actually ointments dense ointments - pastes dense ointments - pastes

On the type (by character) of On the type (by character) of ointment bases distinguish ointment bases distinguish ointments, prepared on:ointments, prepared on:

hydrophobic hydrophobic hydrophilic hydrophilic diphilicdiphilic (hydrophilic-hydrophobic) bases. (hydrophilic-hydrophobic) bases.

PROPERTIES OF OINTMENT BASESPROPERTIES OF OINTMENT BASESOleaginous

Ointment BasesAbsorption

Ointment BasesWater/Oil Emulsion

Ointment Bases

Oil/Water Emulsion

Ointment Bases

Water-miscible Ointment Bases

Composition oleaginous compounds

oleaginous base + w/o surfactant

oleaginous base + water (< 45% w/w) + w/o

surfactant (HLB <8)

oleaginous base + water (> 45% w/w) + o/w

surfactant (HLB >9)

Polyethylene Glycols (PEGs)

Water Content anhydrous anhydrous hydrous hydrous anhydrous, hydrous

Affinity for Water hydrophobic hydrophilic hydrophilic hydrophilic hydrophilic

Spreadability difficult difficult moderate to easy easy moderate to easy

Washability nonwashable nonwashable non- or poorly washable

washable washable

Stability oils poor; hydrocarbons

better

oils poor; hydrocarbons

better

unstable, especially alkali soaps and natural

colloids

unstable, especially alkali soaps and natural

colloids; nonionics better

stable

Drug Incorporation

Potential

solids or oils (oil solubles only)

solids, oils, and aqueous solutions (small amounts)

solids, oils, and aqueous solutions (small amounts)

solid and aqueous solutions (small

amounts)

solid and aqueous solutions

Oleaginous Ointment Bases

Absorption Ointment Bases

Water/Oil Emulsion

Ointment Bases

Oil/Water Emulsion

Ointment Bases

Water-miscible Ointment Bases

Drug Release Potential*

poor poor, but > oleaginous

fair to good fair to good good

Occlusiveness yes yes sometimes no no

Uses protectants, emollients (+/-),

vehicles for hydrolyzable

drugs

protectants, emollients (+/-),

vehicles for aqueous solutions,

solids, and non-hydrolyzable

drugs

emollients, cleansing creams, vehicles for solid,

liquid, or non-hydrolyzable

drugs

emollients, vehicles for solid,

liquid, or non-hydrolyzable

drugs

drug vehicles

Examples White Petrolatum, White Ointment

Hydrophilic Petrolatum, Anhydrous

Lanolin, Aquabase™, Aquaphor®, Polysorb®

Cold Cream type, Hydrous Lanolin,

Rose Water Ointment,

Hydrocream™, Eucerin®, Nivea®

Hydrophilic Ointment,

Dermabase™, Velvachol®,

Unibase®

PEG Ointment, Polybase™

Oleaginous Ointment Bases

Absorption Ointment Bases

Water/Oil Emulsion

Ointment Bases

Oil/Water Emulsion

Ointment Bases

Water-miscible Ointment Bases

Composition oleaginous compounds

oleaginous base + w/o surfactant

oleaginous base + water (< 45% w/w) + w/o

surfactant (HLB <8)

oleaginous base + water (> 45% w/w) + o/w

surfactant (HLB >9)

Polyethylene Glycols (PEGs)

By the type of the dispersible By the type of the dispersible systems ointment divided to:systems ointment divided to:

* homogeneous ointment * homogeneous ointment ointmentointmentss- solutions- solutions ointments- alloys ointments- alloys extraction ointmentextraction ointment

* heterogeneous* heterogeneous ointments- suspensions ointments- suspensions ointments - emulsion ointments - emulsion combinedcombined

HeterogeneousHeterogeneous

Suspension ointments contain solid Suspension ointments contain solid powder, grind medicinal substances powder, grind medicinal substances which are insoluble in the basis and which are insoluble in the basis and distributed it by type of suspensiondistributed it by type of suspension

Emulsion ointment characterized by the Emulsion ointment characterized by the presence of the liquid component that is presence of the liquid component that is insoluble in basis and distributed it to the insoluble in basis and distributed it to the type of emulsion. type of emulsion.

Combined ointment - a combination of Combined ointment - a combination of different disperse systemsdifferent disperse systems

The main task of technology in the The main task of technology in the manufacture of ointments is that the manufacture of ointments is that the drugs have been possible drugs have been possible dispersed dispersed and and evenly distributed throughout the mass evenly distributed throughout the mass basis;basis;

consistency would provide easy consistency would provide easy dab dab and and uniform distribution of the skin or mucous uniform distribution of the skin or mucous membrane, the stability of the ointment membrane, the stability of the ointment would ensure consistency in the would ensure consistency in the application of their composition and application of their composition and storagestorage

Prescription OF OINTMENTSPrescription OF OINTMENTS1. With indication of basis and amount of medicinal 1. With indication of basis and amount of medicinal

substances in units of mass: substances in units of mass: Rp.: Mеntholi 0,1 Rp.: Mеntholi 0,1 Vaselini 10,0 Vaselini 10,0 Miscе, fiat unguеntum Miscе, fiat unguеntum Da. Signa: Ointment is for a nose.Da. Signa: Ointment is for a nose.2. Without indication of basis:2. Without indication of basis:а) with pointing of concentration of medicinal substanceа) with pointing of concentration of medicinal substance Rp.: Unguenti Zinci oxydi 3 % 10,0 Rp.: Unguenti Zinci oxydi 3 % 10,0 Da. Signa: Ointment is for hands.Da. Signa: Ointment is for hands.б) without pointing of concentration of medicinal б) without pointing of concentration of medicinal

substancesubstance Rp.: Unguenti Xеroformii 100,0Rp.: Unguenti Xеroformii 100,0 Da. Signa: Zmazuvati the staggered areas of Da. Signa: Zmazuvati the staggered areas of

skin.skin.

GENERAL RULES OF GENERAL RULES OF PREPARING OINTMENTSPREPARING OINTMENTS

Calculations of amounts of medicinal substances and Calculations of amounts of medicinal substances and basisbasis

If the concentration of medicinal substance was`t noted If the concentration of medicinal substance was`t noted in a recipe, it is followed to prepare 10 % ointment. in a recipe, it is followed to prepare 10 % ointment.

Ointments the samples of which are standardized. Ointments the samples of which are standardized. prepare according to concentration of medicinal prepare according to concentration of medicinal substances, marked in NTD.substances, marked in NTD.

Introductions of medicinal Introductions of medicinal substancessubstances in ointment in ointment conduct taking into account their physical and conduct taking into account their physical and chemical properties and written amounts.chemical properties and written amounts.

Medicinal substances, soluble in fats (Camphor, Medicinal substances, soluble in fats (Camphor, Mentholum, Thymolum, , a crystalline Fenolum, Mentholum, Thymolum, , a crystalline Fenolum, Anaesthesinum less than 2 %, Salol but, other) Anaesthesinum less than 2 %, Salol but, other) enter in monophase ointments-solutions, enter in monophase ointments-solutions, dissolving them in fat basis or its component part.dissolving them in fat basis or its component part.

If total amount of these substances less If total amount of these substances less than 5 %, they are ground with a liquid, than 5 %, they are ground with a liquid, what similar after properties to basis: what similar after properties to basis: Vaseline -Vaseline oil, fatty basis -Vaseline -Vaseline oil, fatty basis -drupaceous butter. Liquids take so much, drupaceous butter. Liquids take so much, how many matters.how many matters.

If total amount of these substances more If total amount of these substances more than 5 %, they are ground with an even than 5 %, they are ground with an even amount to mass of dry substances of amount to mass of dry substances of molten basis.molten basis.

In hydrophilic bases these substances In hydrophilic bases these substances enter like suspensions.enter like suspensions.

Preparing of Preparing of homogeneous ointmentshomogeneous ointments Ointments-alloys are connection of a few Ointments-alloys are connection of a few

mutually fusible and mutually solublemutually fusible and mutually soluble components. Fats can enter in the components. Fats can enter in the complement of such ointments, beeswax, complement of such ointments, beeswax, hydrocarbons, resins, plasters, butters, hydrocarbons, resins, plasters, butters, and otherand other substances. Ingredients can be substances. Ingredients can be both hard and soft or liquid.both hard and soft or liquid.

The alloy of components is conducted on The alloy of components is conducted on an aquatic bath in a porcelain or an aquatic bath in a porcelain or enameled cup.enameled cup.

General technology of ointments-General technology of ointments-alloys consists in the following:alloys consists in the following:

in the first turns meltin the first turns melt the most refractory the most refractory substancesubstance

to the got fusion add other ingredients in order to the got fusion add other ingredients in order of decline of temperature of melting; of decline of temperature of melting;

liquid components add in the last turnliquid components add in the last turn this liquid fusion if necessary strainthis liquid fusion if necessary strain through a through a

gauze in a warmed-up mortar (50-55 °С) gauze in a warmed-up mortar (50-55 °С) mix to coolingmix to cooling essential oils add in the last turn at a essential oils add in the last turn at a

temperature not higher 40 С. temperature not higher 40 С.

Comparative fusibility of substances which Comparative fusibility of substances which enter in the complement of ointments-alloys is enter in the complement of ointments-alloys is

resulted below in such order:resulted below in such order:

1. Tserezin 1. Tserezin 2. Ozocerite2. Ozocerite 3. A beeswax is yellow 3. A beeswax is yellow 4. A beeswax is white 4. A beeswax is white 5. Petrolatum5. Petrolatum 6. Paraffin hard6. Paraffin hard 7. Spermaceti 7. Spermaceti 8. Beef fat8. Beef fat 9. Lanolin is waterless 9. Lanolin is waterless 10. Vaseline 10. Vaseline 11. Hydrogenated fats11. Hydrogenated fats 12. Naphthalanum12. Naphthalanum 13. Butters vegetable and artificial13. Butters vegetable and artificial 14. Essential oils14. Essential oils

Rp.: Naphthalani liquidi raffinati 70,0 Rp.: Naphthalani liquidi raffinati 70,0

Paraffini 18,0 Paraffini 18,0

Petrolati 12,0 Petrolati 12,0

Misce, fiat unguentum Misce, fiat unguentum

Da. SignaDa. Signa.. For bandages. For bandages.

Medicinal preparation – ointment alloy Medicinal preparation – ointment alloy with mutually fusiblewith mutually fusible components which components which have a different temperature of drowning.have a different temperature of drowning.

Melt petrolatum (t - 60-62 °С), to the got Melt petrolatum (t - 60-62 °С), to the got fusion at stirring add a paraffin (t - 50-54 fusion at stirring add a paraffin (t - 50-54 °С) and in the last turn - oil naphthalini. °С) and in the last turn - oil naphthalini. An alloy is mixed in a warm mortar to the An alloy is mixed in a warm mortar to the complete cooling-down.complete cooling-down.

WPC (f.s.)WPC (f.s.)

Date Date № recipe № recipe

Petrolati 12,0 Petrolati 12,0

Paraffini 18,0 Paraffini 18,0

Naphthalani of liquidi raffinati 70,0Naphthalani of liquidi raffinati 70,0

m = 100,0m = 100,0

Prepared: (signature)Prepared: (signature)

Checked: (signature)Checked: (signature)

Medicinal substances, soluble in fats Medicinal substances, soluble in fats (camphor, Mentholum, Thymolum, a (camphor, Mentholum, Thymolum, a crystalline phenolum, Anaesthesinum crystalline phenolum, Anaesthesinum to 2 %, salol but other) enter in mono to 2 %, salol but other) enter in mono phase ointments-solutions, dissolving phase ointments-solutions, dissolving them in fat basis or its component them in fat basis or its component part.part.

Ointment- solutionOintment- solution If total amount of these substances is less than If total amount of these substances is less than

5 %, they are ground with a liquid, what similar 5 %, they are ground with a liquid, what similar by the properties to basis: Vaseline is Vaseline by the properties to basis: Vaseline is Vaseline butter, fatty basis is drupaceous butter. Liquids butter, fatty basis is drupaceous butter. Liquids take so much, how many matterstake so much, how many matters

If total amount of these substances is more If total amount of these substances is more than 5 %, they are ground with an even than 5 %, they are ground with an even amount to mass of dry substances of molten amount to mass of dry substances of molten basis.basis.

At preparing of ointments-At preparing of ointments-solutions it is needed to take into solutions it is needed to take into

account the following rules:account the following rules:

if a medicinal substance has a volatile if a medicinal substance has a volatile characteristics (camphor, Mentholum, other), then characteristics (camphor, Mentholum, other), then it is dissolved in the cold fusion (45-50 °С);it is dissolved in the cold fusion (45-50 °С);

it is not followed to prepare satiate solutions, it is not followed to prepare satiate solutions, because permeates can crystallize at cooling;because permeates can crystallize at cooling;

many medicinal preparations, soluble in many medicinal preparations, soluble in hydrophobic bases, reduce the temperature of hydrophobic bases, reduce the temperature of melting of the last as a result of education eutectic, melting of the last as a result of education eutectic, that is why for a receipt enough dense ointments-that is why for a receipt enough dense ointments-solutions in the contain of ointment bases enter solutions in the contain of ointment bases enter making more compact components (10% beeswax making more compact components (10% beeswax or paraffin) on a concordance with a doctor.or paraffin) on a concordance with a doctor.

THANK YOUTHANK YOU FOR FOR

ATTENTION !ATTENTION !