Chapter 21 Eye medicinal forms.
Maintenance of chemical stability. Maintenance of absence
Mechanical inclusions. Maintenance of comfort. Technology
Eye drops. Eye ointments. Eye a film. (GLP).
Ãëàçíûå medicinal forms.
Eye LF are allocated in special group in connection with their way
Applications. The known Soviet ophthalmologist academician V.P.
Filatov (1875 - 1956) wrote: « It is possible to say without exaggeration,
That among sense organs of the person the most precious is
Body of sight ». 90 % of the information on world around the person
Receives with the help of sight.
The mucous membrane of an eye is most sensitive of all
Mucous an organism. She sharply reacts on external razdrazhiteli
- mechanical inclusions, discrepancy of osmotic pressure
And values rN entered into eye LP to osmotic pressure and
To value rN a plaintive liquid. The plaintive liquid is protective
A barrier to microorganisms due to presence in her lizotsima
(enzyme muromidaza). At various diseases of eyes the maintenance
lizotsima in a plaintive liquid it is considerably reduced, that
Promotes duplication of microorganisms which cause
Heavy diseases. Therefore alongside with the general requirements for
Many LF to them increased requirements are showed:
Sterility, stability, izotonichnost, absence
Mechanical inclusions and irritating action, accuracy
Batchings.
Now at treatment and preventive maintenance of diseases of eyes
The following eye LF industrial production are used:
Drops, ointments, a film. The most widespread eye LF are
Drops.
The basic requirements to which should correspond eye
Drops:
Sterility;
Absence of mechanical inclusions;
Comfort (izotonichnost, optimum value rN);
Chemical stability;
Prolongation of action.
Maintenance sterility.
This one of the main requirements. Impurity is especially dangerous
Eye drops sinegnojnoj a stick and golden stafilokokkom.
A number of cases of blindness which came in result was
instilljatsii unsterile eye drops. Microbic kontaminatsija
Causes also instability of eye drops at storage.
In some days after manufacturing in unsterile eye
Drops seen attributes microbic kontaminatsii are found out-
Dregs, a mould, a deposit.
Sterility of eye drops is reached by the same methods, as
And sterility of solutions for injections - preparation in
asepticheskih conditions and use of this or that way
Sterilizations. The way of sterilization of eye drops depends from
Stability LV in solutions to temperature influence. In
Communications with it can be divided eye drops into three groups.
In 1-? group eye drops which can be enter
Are sterilized the ferry under pressure during 8 - 12 mines without
Additions of stabilizers. These are solutions amidopirina, atropine
Sulfate, an acid boric, dikoina, kalija jodida, calcium
Chloride, sodium of chloride, an acid nicotinic, pilokarpina
A hydrochloride, prozerina, riboflavina, sulfopiridazin - sodium,
furatsilina, zinc of sulfate, efedrina a hydrochloride, and also
The eye drops containing riboflavin in a combination with an acid
Ascorbic and glucose, etc.
In 2-? group eye drops with addition of stabilizers enter,
Which can be sterilized the ferry under pressure or
Fluid the ferry. Drops of this group are resulted below, at
Consideration chemical eye drops.
3-n the group includes the eye drops containing termolabilnye
Substances which cannot be sterilized by thermal methods
(benzilpenitsillin, streptomycin sulfate, kollargol, protargol,
rezortsin, etc.). For sterilization such laznyh drops can be
Filtering through microporous sterile is used
Filters.
The eye drops made asepticheski, or drops sterile,
Can become soiled microorganisms during use. In
Communications with it there is a necessity of addition to eye drops
Preservatives which interfere with growth and duplication
The microorganisms which have got in eye drops, also promote
To preservation of their sterility during all time of application.
The following preservatives are used: hlorbutanola hydrate (0,5 %),
Spirit benzilovyj (0,9 %), complex ethers paraoksibenzojnoj acids
(nipagin and nipazol, 0 » %), salts chetvertichnyh ammonievyh the bases
(benzalkonija chloride, 0) 1 %), an acid sorbinovaja (0,05 - 0,2 %).
Group of the Leningrad ophthalmologists it is offered in quality
Preservative for eye drops addition of the mix consisting from
0,2 % levomitsetina and 2 % of an acid boric.
Maintenance of absence of mechanical inclusions.
By analogy with inektsionnymi solutions eye drops are filtered
Through glass, paper or membrannye filters with
Simultaneous sterilization.
As at filtering there are big losses, and it
It is reflected in accuracy of concentration LV in eye drops,
Especially at very low concentration LV, resort to
To use of the concentrated solutions.
Maintenance of comfort.
In most cases the discomfortable phenomena at use
Eye drops are caused by discrepancy osmotic
Pressure and values rN eye drops those in plaintive
Liquids.
In norm the plaintive liquid has osmotic pressure, same
As plasma of blood and as izotonichesky (0,9 %) a solution of sodium
Chloride. It is desirable, that also eye drops had such
Osmotic pressure. Deviations are supposed and is shown, that
Eye drops cause unpleasant sensations at concentration from
0,7 up to 1,1 %.
Sometimes doctors write out hypertonic eye drops, since they
Render faster, especially antimicrobic action. But
Hypertonic eye drops are badly transferred by children.
On comfort of eye drops the big influence renders
Value rN. The majority of eye drops has rN within the limits of 4,5
- 9.
Optimum value - 7,4. At values rN > 9 and < 4,5 eye
Drops cause at zakapyvanii strong slezotechenie, feeling
Burnings, rezi.
Maintenance of chemical stability.
The basic ways of stabilization of eye drops are
Regulation of values rN and introduction in structure of solutions,
Containing legkookisljajushchiesja substances, antioxidants. For
Regulations of value rN are used buffer solvents.
More often as buffer solvent it is applied boric
An acid 1,9 - 2 %. As antioxidants: sodium
Sulphite, sodium metabisulphite and trilon Á.
Maintenance of prolonged action.
Lack of eye drops is the short period
Therapeutic action. It causes their necessity
Often instilljatsii, and also represents danger to an eye.
For example, a maximum gipotenzivnogo effect of a water solution
pilokarpina a hydrochloride at patients with a glaucoma it is observed only
Within 2 hours, therefore it is necessary to make up to 6 times in
svutki instilljatsiju eye drops. Often instilljatsii water
A solution wash off the plaintive liquid containing lizotsim, and that
Most create conditions for occurrence of an infection.
To reduce frequency istilljatsy eye drops and simultaneously
To increase time of contact to fabrics of an eye it is possible in the way
Prolongations inclusion in structure of eye drops is
Viscous solvents which slow down fast washing away LV from
konjuktivalnogo a bag. As such substances earlier
Used oils (sunflower refined, peach or
Apricot). However more effective prolongatorami for
Eye drops there were synthetic gidrofilnye Naval Forces, such,
As MTS (0,5 % - 2 %), Nà - salt KMTS (0,5 - 2 %) polivinol (1,5 %),
Microbic PS aubazidan (0,1 - 0,3 %), poligljukin, etc. These
Substances do not irritate a mucous membrane of an eye, and also
Are compatible with many LV and preservatives.
Amplification and prolongation action speaks increase
Durations of a presence of substances in konktivalnom a bag,
Slow, but full vsasyvaniem them through a cornea. For example,
Quantity instilljatsy 2 % of solutions pilokarpina a hydrochloride,
Prepared about 2 % Nà KMTS at patients about 3 times have been reduced in
Day instead of 6 instilljatsy a water solution without addition
prolongatorov.
Technology of eye drops.
Eye drops represent water or oil solutions,
The most thin suspensions and emulsii for instilljatsii in konjuktivalnyj
A bag. As solvents water for injections, sterile serves
Fat oils - peach, almond and paraffin liquid.
Features of their industrial manufacture is application,
Except for antioxidants, gas protection for legkookisljajushchihsja
Substances (morfina a hydrochloride, sodium sulfatsila, acids
Ascorbic), perfection of packing (a tube - drops-
Droppers).
Solutions in a tube droppers prepare in 2-nd class
Cleanliness in conditions aseptiki. Dissolution spend in reactors with
Mixers, a solution release from mechanical inclusions,
Subject to sterile filtering and collect in sterilized
The device for the subsequent filling a tube - droppers.
In parallel with it make korpusy and kolpachki a tube-
Droppers. Capacity of 1,5 ml receive the case on the automatic device in
Some stages blowing and punching from granules of polythene
A high pressure. Kolpachki with the probe for piercing
Are poured out under pressure of fused granules PE low
Pressure. After manufacturing them wash out water cleared, dry
Also subject to gas sterilization at 40 - 50? With a mix
etilenoksida and 10 % ÑÎ2 within 2 hours. Etilenoksid delete from
Products their keeping within 12 hours in sterile
A premise.
Further in asepticheskih conditions in the unit with superfluous pressure
Sterile air occurs navinchivanie kolpachkov on the case,
Filling by his solution LV with the help of dosing out pumps and
zapajka termosvarivaniem.
Filled - droppers supervise a tube visually on
Absence of mechanical inclusions on a black and white background
Illumination elektro-a lamp in 60 Vt.
Eye ointments.
Eye ointments are applied by zakladyvanija for veko. Structure
Ointments it is various - with a/b, sulfanilamidami, from mercury oksidom and
Other. The purpose of application can be various (disinfection,
Anesthesia, expansion or narrowing of a pupil, downturn
Intraocular pressure).
To eye ointments, besides the general requirements, (uniformity
Distributions LV, indifference and stability of a basis),
Show a number of additional requirements that speaks
In the way of their application:
mazevaja the basis should not contain any strangers
Impurity, should be neutral, sterile, in regular intervals
To be distributed on a mucous membrane of an eye;
It is necessary to prepare for eye ointments with observance of conditions aseptiki;
LV in eye ointments should is in maximum disperse
A status in order to prevent damage of a mucous membrane.
As a basis of an eye ointment used a mix earlier,
Consisting of 10 parts of lanolin b/v and 90 parts of vaseline (a grade
For eye ointments). His preparation consists that
Usual vaseline dissolve in the enameled reactor and add
There 1 - 2 % of the activated coal. After the further heating up to
150? With during 1 - 2 hours filter a mix. Recently in
Quality of bases for eye ointments even more often use gels Naval Forces:
Gum, sodium alginat, íàòðè1 KMTS, etc. As well as all gidrofilnye
Bases, they are well distributed on a mucous membrane of an eye,
Easily give LV. Lack of them: give in to damage under action
Microorganisms also require preservatives (nipagin + nipazol,
0,12 % + 0,02 %; an acid sorbinovaja 0,1 - 0,2 %).
The technology of eye ointments takes into account se requirements to this LF.
Packing: the most convenient - tubas with navinchivajushchejsja a cover.
Tubas can be supplied navinchivajushchimisja with tips,
Allowing to enter an ointment for veko.
Eye a film. (GLP).
Represent firm a plate of the oval form with equal
Edges (length 6 - 9 mm, width 3 - 4,5ìì, thickness 0,35 mm,
Weight 0,015 ã).
GLP have a number of advantages before others eye LF: from them
The help possible to prolong action and to raise concentration LV in
Fabrics of an eye to reduce number of introductions with 5 - 8 up to 1 - 2 times in
Day. GLP pawn in konjunktivalnyj a bag, for 10 - 15
Seconds they are moistened with a plaintive liquid and become
Elastic. Through 20 - 30 minutes the film turns in viscous
A clot of polymer, which in approximately 90 minutes
It is completely dissolved, creating a thin uniform film.
In quality plenkoobrazovatelja - poliakrilamid or his copolymers
With monomeasures akrilovogo and vinylic lines, spirit polyvinyl,
NàÊÌÖ. The basis for GLP is offered: 60 parts of a copolymer
akrilamid, 20 parts vinilpirrolidona, 20 parts etilakrilata and
50 parts of softener - polietilenglikolsuktsinata.
Technology GLP: in a reactor receive 16 - 18 % a solution of polymer,
Mix from 96 % ethanol for razryhlenija components, add
Water, a mix heat up up to 50? With also mix up to full
Dissolution, cool up to 30? With also filter. Separately prepare
Solution LV also enter in a solution of polymer. The received structure
Mix within 1 hour and tsentrifugirujut 2 hours for
Removals puzyrkov air. The received solution render on
A surface of a metal tape also dry in the chamber at temperature
40 - 48? With, then cool up to 38? With also remove from a tape a film in
A kind of a roll. Leave on 6 - 8 hours for removal deformation
Pressure. Pack received with the help of stamp GLP in
konturno-jachejkovuju packing on 10 pieces also stack in cardboard
Boxes. Sterilization - a mix etilenoksida with ÑÎ2.
The perspective form - intraokuljarnye LP, received on a basis
Collagen from gentamycin sulfate and trimekainom. They are filed
In the forward chamber of an eye at surgical operations, gradually
Liberating LV. GLP are completely dissolved for 10 day.
Contact lenses - gelatinous in the form of the cups filled LV,
Which provide prolonged action.
