Chapter 6 Other
Auxiliary substances. Form-building substances.
Stabilizers. Protivomikrob stabilizers. Soljubilizators.
Prolongators. Korrigents.
Auxilary substances.
ZHirosahara - incomplete complex ethers of saccharose with the maximum fat
Acids (stearin, palmitinovaja, laurinovaja, etc.). It
A new class FALLING, in an organism break up to fat acids,
Fructose and saccharose. Are applied in quality soljubilizatorov,
emulgatorov, stabilizers.
Silikony - kremnijorganicheskie polymers. The greatest application
Have received kremnijorganicheskie liquids (esilon - 4 and esilon - 5).
In connection with absence of chemically active groups silikony
Are characterized by high chemical inertness: are not oxidized,
Did not treat to action of excited environments, possess waterproof
Properties, termostojki. They are used as carriers in
Medical products at various ways of introduction. For
silikonizirovanija glass container with the purpose of increase chemical and
Thermal stability. Silikonovye liquids are used for
zashity leather as cream losjonov and ointments.
Continuation.
2) Classification of auxiliary substances
(on influence on physical and chemical characteristics and
Pharmacokinetics LF).
Depending on influence on physical and chemical characteristics and
Pharmacokinetics LF of auxiliary substance can be divided on
The following groups: form-building, stabilizers, prolongatory,
soljubilizatory, korrigenty.
à) Form-building substances.
This group of auxiliary substances is used in quality
Dispersive environments (water or not water environments) in technology liquid
LF, napolnitelej for firm LF (powders, pills, tablets and
Other), bases for ointments, bases for suppozitoriev. Form-building
Substances enable to create necessary weight or volume,
To give the certain geometrical form. Among dispersive
Environments for preparation liquid LF most often it is used
Water (cleared or for injections) as not water
Solvents - ethanol, glycerin, oils fat, vazelinovoe
Oil, polietilenoksid, propilenglikol, etiloleat, silikonovye
Liquids (esilony), benzil - benzoat, etc. For manufacturing
Firm LF as auxiliary substances (it is frequent them
Name napolniteljami) use sugar dairy or white,
Starch, talc, powders of medicinal plants and their extracts
(Dry) and many other components depending on kind LF. In
Technologies of ointments as bases most often apply
vjazkoplastichnye substances (vaseline, fats, silikonovye bases and
Other); gidrofilnye (polietilenoksidnye, krahmalno-glyceric,
Solutions MTS and its derivatives). For manufacturing suppozitoriev
Use substances and their combinations as insoluble in water
(oil of cocoa, butiroja, oils gidrogenizirovannye), and
Soluble (gelatin, polietilenoksidy, etc.).
á) Stabilizers.
Stability - property of medical products to save
Physical and chemical and m - properties during certain
Time from the moment of release.
Classification of stabilizers:
Physical and chemical (disperse) systems:
zhelatoza; derivatives MTS; microbic PS; PVP; bentonity, the twin-
80, etc.
Chemical substances:
The substances braking gidroliticheskie processes (acids, alkalis,
Buffer systems); the substances braking about - in processes (sodium
Metabisulphite, tiomochevina, trilon, etc.)
protivomikrobnye stabilizers (preservatives):
metallorganicheskie connections; organic connections (spirits
Phenols, acids, complex ethers, salts chetvertichnyh ammonievyh
Connections, radio oils).
Stabilizers of physical and chemical systems are of great importance
For heterogeneous systems (suspensions and emulsy), used in
To medical practice due to valuable properties: an opportunity
Manufacturing and use of medical products from t/r or
n/r medical products; prodlennost actions medicinal
Substances; practicability of various ways of introduction, including
And inektsionnogo. So, stable suspensions of barium of sulfate,
Allow to diagnose in due time changes mucous
Shells of a gastroenteric path; emulsii oils vazelinovogo
Are necessary for patients with atoniej intestines, for his stimulation
Functions.
Stabilizers of chemical substances are used in process
Manufacturing and long storage of medical products.
This kind of stabilization is of great importance for LF,
Exposed to various kinds of sterilization, especially
Thermal. In this case the chemical method is used
Stabilization which is especially necessary for liquid LF.
Stabilizers of this group oppress processes gidroliticheskogo or
About - in decomposition of medicinal substances. Are especially sensitive to
To oxidation nonsaturated fats and oils, connections with aldegidnymi and
Phenolic groups. Reactions of oxidation can be ingibirovany
By addition of small amounts of auxiliary substances,
Are called as antioxidants (protivookisliteljami). On the mechanism
Actions, divide joint-stock company into 3 groups:
1. joint-stock companies, which ingibirujut process of oxidation, reacting with
Free radicals of primary products of oxidation, than
Stop development of chain reaction.
2. joint-stock companies which have lower about - in potential, than
Oxidized connections taking place in system, and which
Are oxidized the first.
3. Sinergisty joint-stock company, own a/o action which
Insignificantly, however they promote amplification of action of others
JOINT-STOCK COMPANY.
Protivomikrobnye stabilizers (preservatives) use for
Protection of medical products from microbic
Influences. Conservation does not exclude observance sanitary
Rules of production which should promote
Maximal snizheni microbic kontaminatsii medicinal
Preparations. Preservatives are ingibitorami growth of those
Microorganisms which get in medical products. They
Allow to save sterility of medical products or
Maximum permissible number of not pathogenic microorganisms in not
Sterile LP. To preservatives same requirements are showed,
As to other auxiliary substances.
In GF XI as antiseptic substances for inektsionnyh
Solutions, others LF, wheys and vaccines are switched on:
hlorbutanolgidrat (0,05 - 0,5 %); phenol (0,25 - 0,3 %); chloroform
(0,5 %); mertiolat (0,01 %) nipagin (0,1 %); nipazol, an acid
sorbinovaja (0,1 - 0,2 %), etc. As against previous
Pharmacopoeias, in GF XI the preservatives intended for are resulted
All not inektsionnyh LF.
Metalloorganic connections of mercury - for example, mertiolat.
Possesses high antimicrobic activity small dozes not
Are toxic for the person. Mertiolat it is applied to eye drops
(0,005 %), eye ointments (0,002 %), inektsionnyh solutions
(0,01 %), ointments (0,1 %).
Organic connections:
Spirits (etilovyj, benzilovyj, hlorbutanolgidrat);
Phenols (phenol, hlorkrezol);
Organic acids (benzojnaja and sorbinovaja);
Complex ethers paragidroksibenzojnoj acids;
Salts chetvertichnyh ammonievyh connections;
Radio oils.
Spirit etilovyj - ekstragent at reception of tinctures, extracts and
Concentrates from medicinal vegetative raw material. Simultaneously
Carries out a role of preservative. In emulsijah ethanol in quantity
10-12 % from a water phase, in galenovyh and novogalenovyh preparations-
Up to 20 %. The best a/s properties 70 % ethanol possess.
Spirit benzilovyj - a liquid with a pleasant aromatic smell.
0,9 % - for eye drops, emulsionnyh mazevyh bases.
Hlorbutanolgidrat - colorless crystals with a smell of camphor. For
Conservations ekstraktsionnyh preparations, juices fresh
Plants, organopreparatov.
Phenol. 0,25 - 0,5 % solutions of phenol - for preparations of insulin,
Vaccines and wheys.
Hlorkrezol. In 10 - 13 times are more active some phenol, but is less toxic.
For conservation of eye drops (0,05 %); inektsionnyh
Solutions (0-,1 %), ointments (0,1 - 0,2 %).
An acid benzojnaja. It is usually applied as natrievoj salts.
Use for conservation of a syrup sugar, emulsii oils
vazelinovogo, suspensions with a/b.
An acid sorbinovaja. It is resolved in many countries for
Conservations of foodstuff, it is harmless even in big
Quantities. For conservation of syrups and extracts, sodium
Bromide, calcium of chloride, ointments and linimentov.
Complex ethers paragidroksibenzojnoj acids
- parabeny. A methyl ether - nipagin and propilovyj an ether-
nipazol. Stronger action at a combination 0,025ã propilovogo
And 0,075ã methyl ethers (1:3). Small toxicity parabenov
Allows to use them for LP for internal application-
Syrups, tinctures, broths, a/b, peroralnyh emulsy,
Gelatinous capsules, ointments.
The representative of salts chetvertichnyh ammonievyh connections (BAH)
benzalkonija chloride. It is effective concerning many
gramotritsatelnyh, grampolozhitelnyh bacteria also does not possess
Toxicity.
Now almost in all foreign countries it is applied
For conservation eye LF, drops for a nose where are required
Absence of irritating action and fast bactericidal
Effect.
Domestic preservative of this group-
dimetildodetsilbenzilammonija chloride. (DMDBAH). In comparison with
BAHom DMDBAH is more active in the attitude sinegnojnoj than a stick, which
Usually is the representative of accompanying flora at eye
Diseases.
Radio oils use as preservatives for LP
External application (an ointment, emulsii, linimenty). Radio oils
Containing phenolic connections - laurel, ukropnoe,
lavandovoe, pink, anisic, citric. They possess not only
Preserving properties, but also bactericidal activity in
The attitude of pathogenic microflora of a leather, including yeast,
Causing candidiases. An example of increase of stability LP at
Addition of preservatives:
Preparations Without preservative With preservative Just prepared
Drops, sut 33010
Plugins, sut 33010
â) soljubilizatory.
With the purpose of increase in solubility difficultly soluble or not
Soluble medicinal substances are applied FALLING, for example,
The twin - 80, bilious acids. These substances are called
soljubilizatorami.
Soljubilizatsija - process of spontaneous transition not
Soluble substance in water in a water solution of PEAHENS. Application
soljublizatorov allows to prepare LF with insoluble
Medicinal substances. These are groups a/b, tsitostatikov,
Hormonal preparations. At use of the twin - 80 are received
inektsionnye solutions of hormones (instead of tablets), water
Solutions of camphor (instead of oil), etc. Thus it is reached
Fast and full rezorbtsija medicinal substance that can
To lead to to decrease in a dosage of medicinal substance. In a case
With camphor the water solutions appointed the patient at
Cardiovascular diseases, badly resolve and it is frequent
Form oleomy - tumours which no at introduction water
Solutions of camphor.
ã) Prolongatory.
The auxiliary substances increasing time of a presence
Medical products in an organism, are called prolongatorami. At
Medical products of prolonged action it is increased
Duration of action.
At fast deducing medicinal substances from an organism or
Fast destruction in him a/b, vitamins, hormones, etc.
There is a necessity of often introduction of medicinal substances,
That results in change of their concentration in an organism and
Causes undesirable by-effects (allergic
Reactions, irritation, etc.). Creation medicinal is necessary
Preparations, which unitary reception, saving in an organism in
Current of long time terapevticheski active concentration
Medicinal substance, including receipt medicinal
Substances with the set speed.
To prolonging components, besides the requirements showed to
To auxiliary substances, it is necessary to attribute and maintenance
An optimum level of medicinal substance in an organism,
Absence of sharp fluctuations of his concentration. A maximum
Concentration of medicinal substance in blood it is direct
To proportionally entered doze, speed vsasyvanija and back
Proportionally speeds of allocation of substance from an organism.
There are various technological methods of prolongation LP:
Increase of viscosity of the dispersive environment (the conclusion
Medicinal substance in a gel); the conclusion medicinal
Substances in film shells; suspendirovanie soluble
Medicinal substances; creation eye medicinal plenok
Instead of solutions, etc.
The most preferable is the conclusion medicinal
Substances in a gel or use as the dispersive environment
Not water solvents (PEO - 400, oils, etc.). As a gel
For prolonged LP use solutions Naval Forces various is more often
Concentration that allows to adjust time of prolongation.
To such substances concern MTS, KMTS and sodium KMTS (1 %), PVP,
Collagen, etc. Naval Forces. (an example - eye drops as 10 % of a solution
sulfatsil - the sodium, the prolonged 1 % MTS).
ä) Korrigenty.
Auxiliary substances which enable concern
To correct taste, color, a smell of various medicinal substances.
Use in children's practice is more often. In quality korrigirujushchih
Substances use natural and synthetic substances as
Solutions, syrups, extracts, essences. Syrups: sugar,
Cherry, crimson, solodkovyj. Podslashchivajushchie substances-
Saccharose, lactose, fructose, sorbite, saccharin. Most
Perspective - sorbite which is also preservatives. To
korrigentam various Naval Forces which envelop concern
Medicinal substances and flavouring receptors of language - an agar,
alginaty, MTS and pectins. Radio oils: mint, anisic,
Orange.
