Chapter 5 Auxilary
Substances. Natural auxiliary substances. Synthetic and
polusinteticheskie auxiliary substanecs.
Auxiliary substances.
Auxiliary substances are additional substances,
Necessary for preparation of a medical product. Creation
Effective medical products demands application big
Numbers of auxiliary substances. Until recently to
To auxiliary substances demanded
Pharmacological and chemical indifference. However
Were found out, that these substances can influence substantially
On pharmacological activity of medicinal substances: to strengthen
Action of medicinal substances or to reduce their activity,
To change character of action under influence of the different reasons, namely
kompleksoobrazovanija, molecular reactions, an interference, etc.
Auxiliary substances are auxiliary components
Almost all medical products and at use enter
In contact to bodies and fabrics of an organism, therefore to them
The certain requirements are showed. Thus it is necessary
To take into account, that many auxiliary substances act from
The various enterprises of the ministries and departments (chemical,
Food the industries, etc.), therefore requirements to
Auxiliary substances should be uniform.
To auxiliary substances the following should be showed
Requirements:
Conformity to medical purpose of a medical product,
I.e. maintenance of display appropriate pharmacological
Actions of a medical product in view of his pharmacokinetics.
Auxiliary substances should not render influence and change
Biological availability of a medical product;
Used quantities should be biologically harmless and
biosovmestimy with fabrics of an organism and also to not render
allergizirujushchego and toxic action;
Conformity of form-building properties made medicinal
To the form. Auxiliary substances should give medicinal
To the form required properties: structural - mechanical,
Physical and chemical and, hence, to provide bioavailability.
Auxiliary substances should not render (-) influence on
organolepticheskie properties of medical products: taste,
A smell, color, etc.
Absence of chemical or physical and chemical interaction with
Medicinal substances, packing and corking
Means, and also a material of the process equipment in
Process of preparation of medical products and at them
Storage. Consequence of various interactions can be
Decrease in efficiency, and on occassion even display
Toxic properties of a medical product.
Conformity depending on a degree can be cleanliness
A made preparation (as end-product) to requirements
Maximum permissible microbic kontaminatsii; an opportunity
To be exposed to sterilization, as auxiliary substances
Sometimes are the basic source of microbic pollution
Medical products;
Economic availability. It is necessary to reduce the list of substances,
Used in the food-processing industry.
The nomenclature of the auxiliary substances used in technology
LF, it is rather numerous, therefore with the purpose of ordering and
Simplification of their further studying and correct selection
Their classification is expedient.
In a basis of classification of auxiliary substances a number lays
Attributes: 1) the nature (including chemical structure); 2)
Influence on technical characteristics and farmakonetiku LF.
Classification of auxiliary substances by the nature and chemical
To structure.
By the nature of auxiliary substance it is possible to divide on:
à) natural; á) synthetic and polusinteticheskie substances.
Natural organic connections
Inorganic connections
Auxiliary substances of a natural origin receive by
Processings raw material, raw material of a microbic origin and minerals.
(+) natural auxiliary substances: in their high
Biological harmlessness. Today 1/3 auxiliary substances
Falls natural. Vegetative biopolymers use in
Quality emulgatorov, stabilizers, prolongatorov and for other.
The purposes by manufacture LF.
(-) natural auxiliary substances:
They are subject high microbic kontaminatsii, in this connection
Solutions PS and fibers quickly spoil. Use of sterilization
And addition of preservatives can lower up to maximum permissible
Norms microbic kontaminatsiju natural auxiliary substances.
Synthetic and polusinteticheskie substances find wider
Application in technology LF. This is promoted by their availability,
I.e. an opportunity of synthesis of substances with the set properties.
For example, derivatives MTS: Na-salt MTS rastvorima in water, and
oksipropiltselljuloza not rastvorima, therefore she is used for
Coverings shells of tablets and drops with the purpose of protection
Medicinal substances from the sour environment of gastric juice, etc.
Derivatives of lanolin (atsetilirovannye, oksietilirovannye, etc.)
As against lanolin on structure are identical to skin fat
The person, do not cause allergic reactions and in view of smaller
In comparison with lanolin it is more convenient than viscosity at manufacturing
Ointments.
And more very important: synthetic and polusinteticheskie
Auxiliary substances can replace a number of foodstuff.
On chemical structure auxiliary substances are Naval Forces. To
Naval Forces concern natural and synthetic substances with M.m ≥ 10000.
Their molecules represent the long strings bound
Among themselves or curtailed in balls. Naval Forces are used in
Technologies of all LF: as bases for ointments, suppozitoriev, pills
, etc., kakt stabilizers, as prolonging components, as
The substances correcting taste. Introduction in technology new Naval Forces
Has allowed to create new LF: multilayered tablets long
Actions, spansuly (the granules impregnated with a solution Naval Forces)
Microcapsules; eye medicinal a film; nurseries
Medicinal forms.
Wide application Naval Forces in technology LF is based as well on
Surface-active properties. Depending on chemical
Structures distinguish 3 types of PEAHENS: kationnye, anionnye,
neionogennye. All types are to some extent used in
Pharmaceutical technology as gidrofilizatory, soljubilizatory,
emulgatory, stabilizers, etc.
Among various groups of PEAHENS kationoaktivnye PEAHENS - the strongest
Bactericidal means. Due to a combination
Surface-active and bactericidal properties they are perspective
For application in pharmaceutical technology. These are salts mono
chetvertichnyh ammonievyh connections (etonija chloride, tionija
Chloride).
However the greatest application recently find
neionogennye PEAHENS (NPAV). This group make oksietilnye
Derivatives of some organic connections, monoethers of saccharose,
glitseridy VM fat acids, ethers of fat acids and multinuclear
Spirits and them oksietilnye the derivatives which have received the name
spenov, etc.
Researches have shown, that FALLING, changing physical and chemical
Properties LF, can render also appreciable influence on
Therapeutic efficiency of medical products. Low
Concentration of PEAHENS increase vsasyvanie sulfanilamidov,
barbituratov, some ethers of an acid salicylic
gidrokortizona and, on the contrary, high concentration of many PEAHENS
Lower rezorbtsiju medicinal substances from solutions.
Natural auxiliary substances.
Starch. Will consist of 2 fractions - amilazy and amilopektina.
Amiloza it is dissolved in warm water, and amilopektin only
nabuhaet. Starch is used in firm LF. In quality
The stabilizer of suspensions and emulsy 10 % a solution are used.
Alginaty - an acid alginic and its salts. An acid alginic-
Naval Forces, it turns out from sea seaweed. It is used in quality
Loosening, emulgirujushchih, jrologirujushchih, film-forming
Auxiliary substances, and also for preparation of ointments and pastes.
Agaroid. Into structure enter glucose and galaktoza, and also
Mineral elements (Sa, Ìg, S, etc.). Receive from sea
Seaweed. In 0,1 % of concentration possesses stabilizing,
Loosening and sliding properties, in a mix with glycerin in
1,5 % of concentration are used in quality mazevoj bases.
Pectin - is part of cellular walls of many plants.
Possesses zhelatinirujushchej ability. It is used for creation
Children's medicinal forms.
Microbic PS - it is most distributed aubazidan - received at
M - synthesis with the help of yeasty mushroom Àèreobasidium
pullulans. Aubazidan (0,6 %) form gels which are used
As a basis for ointments, 1 % - for plenok and gubok. Konts. 0,1 - 0,3 %
- as prolongator eye drops. Thus the solution is steady at
Thermal sterilization up to 120°C. The effective stabilizer and
emulgator.
Collagen. A source is the leather of large horned livestock.
Receive by shelochno salt processing. Collagen is applied
For a covering of wounds as plenok with furatsilinom, an acid boric,
Oil oblepihovym, metiluratsilom, and also as eye plenok
With a/b.
Gelatin - receive at evaporation of scraps of a leather, Naval Forces albuminous
The nature, contains glikokol, alanin, arginin, lejtsin, lizin,
gljutaminovaja an acid. Due to high geleobrazujushchim to properties
It is used for manufacturing ointments, gelatinous capsules,
suppozitoriev.
ZHelatoza - a product of incomplete hydrolysis of gelatin. Does not possess
Ability zhelatinirovatsja, but has high emulgirujushchie
Properties.
From inorganic polymers are used bentonit, aeroforces is more often,
Talc.
Bentonit - as minerals of crystal structure in the size
Particles of 0,01 mm. Have complex structure. The general formula: Al2O3 ·
SiO2 · n H2O (contains 90 % oksidov Al, Si, Mg, Fe, still kationy
K +, Na +, Ñà2 +, Ìg2 + - enter in and - about reaction). Ability to
To swelling and geleobrazovaniju allows to use them in
Manufacture of ointments, tablets, powders, granules. Bentonity
Provide to medical products softness, dispersiveness,
High adsorbtsionnye properties, easy feedback medicinal
Substances.
Aeroforces - silicon dioksid SiO2, very easy mikronizirovannyj
A powder with expressed adsorbtsionnymi properties. Apply for
Stabilization of suspensions. Zagushchennuju ability aeroforce
Use at poluchenipi gels for mazevyh bases. Adsorbtsionnye
Properties use with the purpose of stabilization of dry extracts
(their hygroscopicity) decreases. In powders apply at
Manufacturing gigroskopichnyh mixes and as dispergator.
Synthetic and polusinteticheskie auxiliary substances.
The special place in this group is borrowed with ethers of cellulose. They
Represent products of replacement of hydrogen atoms
gidroksilnyh groups of cellulose on spirtovye the rests - alkidy (at
Reception of simple ethers) or the acid rests - atsily (at
Reception of complex ethers).
Metiltselljuloza soluble - a simple ether of cellulose and metanola.
Water solutions MTS possess high sorbtsionnoj, emulgirujushchej and
Moistening ability. In technology apply 0,5 - 1 % water
Solutions as thickeners and stabilizers, for
gidrofilizatsii waterproof bases of ointments and linimentov, in quality
emulgatora and the stabilizer at manufacturing suspensions and
emulsy, and also as a prolonging component for eye
Drops.
Other substances of this group: sodium - karboksimetiltselljuloza (Na
- KMTS), oksipropilmetiltselljuloza and atsetiltselljuloza.
Concentrated solutions MTS at drying form transparent
A strong film - film coverings. M.m. MTS 150 - 300 thousand
Polivinol - synthetic water-soluble polymer vinilatsetata,
Polyvinyl spirit - PVS. The structural formula [-ÑÍ2 - SN-]
n, where n - number of structural units in a macromolecule.
HE
On size M.m. PVS divide into 4 groups: oligomery (4000-
10000); low-molecular (10000 - 45000); sredne molecular
(45000 - 150000); high-molecular (150000 - 500000).
Solutions PVS apply in quality emulgatora, a thickener and
The stabilizer of suspensions.
Polivinilpirrolidon (PVP) - polymer N - vinilpirrolidona
- ÑÍ2 - SN -
N
Í2Ñ Ñ=Î
Í2Ñ ÑÍ2 n
M.m. 10000 - 100000. He we shall dissolve in water, spirits, glycerin,
Easily forms complexes with vitamins, a/b. It is used as
The stabilizer emulsy and the suspensions, a prolonging component,
napolnitel for tablets and drops. PVP is part
Plasma substitutes, aerosols eye medicinal plenok. Gels
On basis PVP use for preparation of ointments, including
Intended for drawing on mucous membranes.
Poliakrilamid - ÑÍ2 - SN -
ABOUT =Ñ - NÍ2 n
PAA we shall dissolve in water, glycerin, it is received also biosoluble
Polymer, he is used for medicinal biosoluble
Eye plenok which provide maximal time of contact
With a surface konjuktivy. 1 % use solutions PAA for
Prolongations of action of eye drops.
Polietilenoksidy. N (-ÎÑÍ2 - ÑÍ2-) n HE M.m. From 400 up to 4000
PEO - 400 - a viscous colorless liquid, PEO - 1500 - voski
(temperature of fusion 35 - 41°C). Rastvorimy in water, ethanol.
Are used in technology of ointments, emulsy, suspensions,
suppozitoriev.
Speny - ethers sorbitana with the maximum fat acids. Spen-20-
An ether laurinovoj acids, spen - 40 - an ether palmitinovoj acids,
spen - 60 - an ether of a stearin acid, spen - 80 - an ether oleinovoj
Acids. Speny are lipofilnymi connections. They
rastvorimyv oils, ethanol. Form emulsii type water / oil
ABOUT
N
Í2Ñ WITH
N ÑÍ2 - ABOUT - WITH - R SPEN
WITH
BUT ABOUT
WITH
N HE
Twins - monoethers polioksietilirovannogo sorbitana (spena) and
The maximum fat acids. Twins receive by processing spenov
etilenoksidom at presence NaOH (kataliz). Twins are dissolved in
Water and organic solvents. In medicine the twin is applied-
80 - for stabilization emulsy and suspensions, including for
inektsionnogo introductions.
