Chapter 20 Rektal medicinal
Forms. Suppozitoris. Technology suppozitoris. Formation and
Packing candles. Prospects of development rektal LF.
Rectal medicinal forms.
To rektalnym LF ointments, capsules concern suppozitorii (candles),
rektioli (mikromumy disposable application), solutions. Most
Widespread LF are suppozitorii (candles).
Suppozitorii.
According to GF XI suppozitorii - firm at room
To temperature and rasplavljajushchajasja or rastvorjajushchajasja at temperature
Bodies dosed out LF. Enter suppozitorii in a direct gut,
A vagina. In quality suppozitornoj bases use more often
A fatty basis. Weight of a fatty basis for preparation of one candle
From 1,2 up to 2,5ã. Structure of a fatty basis: fat gidrogenizirovannogo
(oils cotton - GHM, fat beef - GZH, oils
Sunflower - GPM), paraffin, oil of cocoa in parities
Accordingly from 49 up to 58 %, 12 - 21 % and 30 %.
Necessary temperature of fusion of alloys preliminary
Establish under the formula:
Ò1Q1 + Ò2Q2 + Ò3Q3 + ÊQ
T = -----------,
100
Where T - temperature of fusion of a mix;
Ò1, Ò2 and Ò3 - temperature of fusion of separate components;
Q1, Q2 and Q3 - their maintenance in %;
Q - the total maintenance of liquid components in %;
To - conditional factor for liquid components.
We shall assume, that it is necessary to prepare for an alloy as a basis
Structure: hydrofat of 50 %, paraffin of 20 % and oil of cocoa of 30 %. Taken
For preparation fats have the following melting points: hydrofat
36?, paraffin 54? And oil of cocoa 30?. Under the formula it is calculated (ÊQ
Disappear, as liquid fats do not enter into a basis):
(36 · 50) + (54 · 20) + (30 · 30)
T = ------------- = 37,8?
100
Whereas temperatures of fusion of components of a basis
Change in rather wide limits (hydrofat 28 - 37?,
Paraffin 50 - 57?, oil of cocoa 30 - 34?), actual temperature
Than fusion of the received alloy can be a little bit higher or is lower
Set. In this case in a basis add paraffin or hydrofat
In the quantities necessary for finishing of temperature of fusion
Mixes up to set. Thus use « the table of additives ».
Except for necessary temperature of fusion, a basis for svechej
Should possess corresponding mechanical properties also.
To judge them it is possible on time of full deformation of a candle,
Prepared from a tested basis. Definition of time full
Deformations make at temperature 37? In the special device.
In structure of bases often enter FALLING which not only improve
Structural - mechanical properties, but also influence on
kinetiku liberation and vsasyvanija medicinal substances. In
Quality of PEAHENS in technology suppozitoriev apply emulgator
?-2, twins, speny, sodium laurilsulfat, etc.
From gidrofilnyh bases apply: mylno-glyceric candles, PEO.
Technology suppozitoriev.
The basic method of reception suppozitoriev in industrial
Manufacture is vylivanie in forms.
The method will consist of the following stages:
Preparation of a basis;
Introduction in a basis of medicinal substances;
Formation and packing svechej.
Preparation of a basis. First give all components of a basis.
Into a reactor from stainless steel with a steam shirt load
Paraffin, include heating. In other reactor hydrofat and
rasplavljajut submission pair in a shirt of a reactor. Razogretyj hydrofat
With the help of the pump overload in a reactor with preliminary
The fused paraffin, and a mix heat up to temperature 60
-70? S.Zatem add oil of cocoa, but thus watch, that
Heating did not exceed 70? With also was not long, in avoidance
Changes of updating of oil of cocoa and increase on 2 - 3?
Temperatures of his fusion. After full fusion of its basis
Mix during 40? With with the help of a mixer. In a ready basis
Define temperature of fusion and time of full deformation. If
The temperature of fusion of a basis is more or less set, her
Correct introduction of paraffin or hydrofat, adding them in
podogretuju up to 60 - 70? About a basis at careful hashing.
A ready fatty basis filter through druk the filter, in quality
A filtering material - a fabric belting or a brass grid. And with
The help of compressed air pass in a reactor where are entered
Medicinal substances.
Conducting in a basis of medicinal substances. Thus take into account
Physical and chemical properties of components. Them dissolve in water
(novokain, rezortsin, zinc sulfate), ethanol (iodine
Crystal), to a basis (menthol) also prepare
Solutions - concentrates. Often into structure suppozitoriev enters
An extract krasavki dense which dissolve at hashing in
Equal quantity of water temperature 45 - 48? With.
Solutions - concentrates of medicinal substances filter through coarse calico
Also submit to a reactor.
Medicinal substances, insoluble in water, ethanol, fatty
To a basis entering as suspensions (zinc oksid, bismuth nitrate and
Other). Crushing of medicinal substances conduct on trehvaltsovoj
mazeterke, and largly crystal substances - in spherical
To a mill. The crushed medicinal substances mix in the boiler
With equal or one-and-a-half quantity of the basis which have been heated up up to 40-
50? With and acting from a reactor through the druk-filter. Received
A suspension - concentrate cool and grind on trehvaltsovoj
mazeterke with backlashes between rollers 5 - 10 microns. Razmalyvanie
Repeat some times for reception of necessary crushing.
For reception of suspensions - concentrates use and
Rotatsionno-gear pump Rz-3a.
A principle of job of the pump: the Mix of a basis and a powder medicinal
Substances from a reactor moves in soaking up cavity of the pump for
The bill of rotation shesteren towards to each other. A concentrate
Fills in gleams between zubjami and at the expense of it it is crushed.
Razmol in the pump continue during 40 - 60 minutes. The pump
Crushing medicinal substances a concentrate submit to a reactor with
A steam shirt and a turbine mixer. There acts through
The druk-filter and a fatty basis. From the rests of a concentrate a cavity
The pump clear submission of a fatty basis.
Ready suppozitornuju weight mix current of 45 mines,
Analyze and submit on packing.
Formation and packing svechej. Issue candles of two sizes:
¹1 (weight from 1,2 up to 1,5ã, length of 29 mm O8ìì), ¹2 (weight 2,3-
2,5ã, length of 35 mm O10ìì). Time of full deformation no more than 3-
4 '.
Vylivanie suppozitoriev make on automatic devices with divided
Operations of casting and packing ("Ex - Krespi" Italy) and
The automated lines (f. Heflinger and Hags « Servac - 200S-
GERMANY).
The basic parts of automatic device " Ex - Krespi " are three
Synchronously rotating a disk. Two extreme have forms for
vylivanija svechej. Cooling of forms up to-15 - 18? With it is made with
The help of the refrigerating device. The average disk serves for reception
The cooled forms with subsequent their pushing out in receptions
Baths.
Job of a semiautomatic device for packing suppozitoriev:
Suppozitorii from the receiver are manually stacked in cells
A rotating disk, from which a horizontal pusher they
Are pushed out through an entrance aperture formed cellophane
Tapes. Candles are accepted by the holder, are packed into cellophane.
To the help of the cutting device there is their division on 5 pieces
otrezajushchimi devices. Packing is made on 10 pieces in
Cardboard boxes which wrap on 50 pieces in paper
Kidneys. From 5 - 8 packs place a party in plywood boxes and
Mark.
More sovershennyi the automatic device « Servac - 200S » (Germany) is.
In the aluminium foil acting from two rolls, are formed
chasheobraznye half which incorporate and termosvarivajutsja.
Thus above each form remains open filling
An aperture through which a needle the weight moves suppozitornaja.
Thus packing simultaneously serves as the form for vylivanija
suppozitoriev. Suppozitornaja the weight acts from tanks,
Supplied with a mixer and a steam shirt. Batching
It is carried out by the pump. After filling forms of packing
It is hermetically closed and supplied between separate
Welded suppozitorijami cross-section edges of rigidity
(a cold stamping). Further from a tape narezajut a strip on
To the certain quantity suppozitoriev. The cut off strip
Cool also the automatic device throws out ready packing. External
The surface of a foil is covered stretched polipropilenovoj with a film,
Internal - it is polished or layered by polythene high
Pressure.
Preparations in the form suppozitoriev:
"tsefekon" (salitsilamida 0,6ã, amidopirina 0,2ã, fenatsetina 0,2ã,
Caffeine 0,05ã);
"betiol" (an extract krasavki 0,015ã, ihtiola 0,2ã);
"anuzol" (an extract krasavki 0,02ã, kseroforma 0,1ã, zinc
Sulfate 0,05ã, glycerin 0,12ã);
"anestezol" (benzocaine 0,1ã, dermatola 0,04ã, menthol 0,004ã,
Zinc oksida 0,02ã);, etc.
Prospects of development rektalnyh LF.
liofilizovannye suppozitorii.
A great bulk liofilizovannyh suppozitoriev is active
The substance, quantity of a basis - is minimal. A principle of manufacturing
suppozitoriev will consist in freezing at temperature - 50-70? With
emulsii or suspensions LV in suppozitornoj to the form. Frozen
suppozitorii take from the form and subject liofilizatsii with
The subsequent addition suppozitornoj bases. Suppozitorii,
Received in such a way, are quickly dissolved in a direct gut,
Not causing its irritation. However, as well as all liofilizirovannye
Preparations, this LF gidrolabilna also demands special conditions
Storages.
Pressed (or tabletirovannye) suppozitorii.
Preparation such suppozitoriev is based on transformation
Fatty suppozitornyh weights in the form of a powder that allows him
Freely to get enough sleep from loading voronki and to prepare
suppozitorii, similarly to tablets, a method of pressing, using
Matrixes and punches of the corresponding form. For achievement
Accuracy of batching, flowability from the loading bunker,
suppozitornuju weight cool in the refrigerating chamber up to
Temperatures 3 - 5? With, crush and sift through a sieve. For
Improvements of technological properties in weight enter thinners
(lactose, saccharose, aeroforces) in quantity up to 10 - 20 %,
Sliding substances - starch and aeroforces (up to 3 - 5 %).
The given method turns out suppozitorii with LV
Anti-inflammatory action of not steroid nature: an acid
mefenaminovaja, paracetamol.
Two-layer or two-compound suppozitorii.
The shell such suppozitoriev make of a basis with less
A heat of fusion, for example gidrogenizat beef
Fat from 10 % propilenglikolmonostearata.
She contains LV local action (benzocaine, an extract
krasavki). In a core enter the substances rendering rezorbtivnoe
Action on an organism (vitamin Â15). For a core use
A basis having more a heat of fusion-
Above mentioned gidrogenizat with addition of 3 % emulgatora ?-2.
rektalnye ointments.
On fatty and gidrofilnyh bases. In quality gidrofilnyh bases
- polietilenglikoli, gels MTS, oksipropilmetiltselljulozy, NàÊÌÖ.
Significant, up to 50ã, unitary introduction of an ointment allows
To increase quantity used LV. For set a plenty
Bases can be applied LV, which introductions at other ways
Can call irritation. Rektalnye ointments are issued in a syringe-
Tubes with long tips.
rektalnye capsules.
The shell of a capsule - an alloy of 70 % of gelatin and 30 % of glycerin. A cavity
Capsules it is filled with oil suspension of working substance or
His solution with emulgatorom type emulsii water in oil. At
Introduction in a direct gut the shell of a capsule inflates and bursts, and
Its contents are distributed on a surface vsasyvanija.
Advantages rektalnyh capsules: they save the form at
To temperature up to 40? C; LV capsules it is soaked up faster, than from
suppozitoriev, due to that the shell of a capsule bursts under
Pressure of muscular walls of a direct gut.
rektalnye pipettes - rektioly.
They represent elastic p/e the container in volume 3 - 5
The ml containing solution LV, and supplied with a tip. Use
rektioloj as klizmoj, applying her with the purpose of reception fast
Therapeutic effect, since from the water solutions entered in
A direct gut in the form klizmy, LV are soaked up much faster,
Than from suppozitoriev on a fatty basis.
rektalnye tampons.
It is the plastic core which has been wrapped up by cotton wool with adsorbed on
Her LV. The wadded tampon is covered with a thin layer alginata. Before
The use a tampon immerse in water, the shell from alginata
nabuhaet also does not interfere with process of diffusion LV. A tampon enter in
A direct gut at 2 o'clock (treatment of a hemorrhoids).
Special value rektalnye LF have in children's practice and for
Older persons.
