Chapter 3 Base sciences.
Biopharmacy. Pharmaceutical factors.
Base sciences.
Among other pharmaceutical sciences (pharmaceutical chemistry,
farmakognozija) technology LF borrows original position. On
To definition of professor A.A.Iovskogo, she is top
Pharmacy, its closing stage. Not knowing properties medicinal
Substances (are studied by pharmaceutical chemistry), medicinal
Vegetative raw material (it is studied farmakognoziej), it is impossible
Correctly to make LF.
Technology LF as science has applied character. Its development
Promotes achievements in the field of chemistry, physics, biology, etc.
For example, intensive development of chemistry Naval Forces mattered not
Only for engineering science, but also for medicine and pharmacy,
Physical and kolloidnoj chemistry (the doctrine about stabilization
Heterogeneous systems), microbiology (methods of sterilization) and
Developments of technology LF.
In technology the biopharmaceutical direction is new,
Which has developed in the independent doctrine in the beginning of 60th years
The current century.
Biopharmacy (the section of pharmaceutical science studying
Interrelation between physical and chemical properties medicinal
Means in concrete LF and their pharmacological action)
Has appeared after an establishment of the facts therapeutic
neekvivalentnosti medical products, i.e. LP one
Structure, but made by the different enterprises, differed on
Efficiency. It has been caused by a number of the reasons:
izmelchennostju medicinal substances; selection auxiliary
Components and distinction of technological processes - so-called.
Pharmaceutical factors. Each of the listed factors
In itself is determining in pharmacological action
Medical products.
Biopharmacy - a theoretical basis of technology medicinal
Forms.
Biopharmacy as an independent direction pharmaceutical
Sciences has developed in the beginning of 60th years. A push to occurrence
To biopharmacy have served received in experiment on animals
The data on significant distinction in biological activity
Medical products depending on used
The technologies, used auxiliary substances, their physical
Statuses.
At purpose in one of clinics the USA of tablets one
A medical product working specifically on processes
The curtailing of blood got from two various
The pharmaceutical firms containing identical dozes, unexpectedly
It was revealed, that tablets of one firm appeared in 2 times
More actively tablets from other firm. The chemical analysis not
It is revealed any deviations in the maintenance medicinal
Substances in tablets of both firms. It was the first case
(received wide publicity) precisely established therapeutic
Inadequacy, neekvivalentnosti the preparations containing
Identical dozes of the same working substance, but
Made by the different enterprises. The similar phenomenon is revealed
At many antibiotics (tetratsiklinov, levomitsetina, eritrometsina),
Steroid hormones, sulfanilamidnov, etc.
For the experts engaged in manufacture and the analysis
Medical products, this phenomenon was unexpected. All
Preparations corresponded the requirement of the pharmacopoeia, and consequently,
According to the standard concept, should be completely
Equivalent.
An explanation to this phenomenon of therapeutic inadequacy has given
New branch of pharmacy, medicine, biology - biopharmacy,
Marking a birth of a biological stage of pharmacy.
The biopharmacy can be defined as the science studying biological
Action of medical products depending on them
Physical and chemical properties, medicinal forms, technologies
Preparations. For the first time substantive provisions of biopharmacy
Are formulated in Wagner's jobs. In our country the first jobs
On biopharmacy are published by professor P.L.Senovym, And. And.
Tentsovoj, I.S.Azhgihinym.
The biopharmacy at all does not substitute itself pharmacology. She
Does not study the mechanism of action of biologically active substance,
Points of his application. The biopharmacy as though accepts from
Pharmacology of medicinal substance with the established spectrum
Actions, points of their application. But this biologically active
The substance is not yet suitable for application. And to create
A medical product in the certain medicinal form,
Convenient for reception, storage, transportation the pharmacy is called.
For this purpose medicinal substances crush, dissolve,
Mix. Give to them various medicinal forms, using
Various auxiliary substances, applying numerous
Mechanical receptions, machines, devices, etc.
Thus one parties of biological action can be
usileny, others are weakened silt in general activity of a preparation is shown
On no. Studying of these changes, processes, the factors influencing
On therapeutic efficiency of medical products and
Makes, the main task of biopharmacy.
Special influence on therapeutic efficiency medicinal
Preparations render the following factors which are named
Pharmaceutical.
Pharmaceutical factors.
(make 5 groups)
Chemical updating a preparation (salt, an acid, presence radio
Communications, complex connections);
Physical and chemical, a status of medicinal substance (the form
A crystal, the sizes of particles, presence or absence of a charge on them
Surfaces, etc.);
Auxiliary substances, their nature, quantity;
A kind of the medicinal form and a way of introduction;
Pharmaceutical technology.
Chemical updating medicinal substance it is necessary
It is taken into account by development of new medical products. She
Causes kinetiku liberation and vsasyvanija medicinal
A preparation. However in practical activities of the pharmacist-
This factor of value has no technologist. For the pharmacist - technologist
Such factors, as physical have the greatest value
A status of medicinal substance, presence auxiliary
Substances and their nature. These factors are necessary for taking into account at
A choice of technology of medical products.
The physical and chemical status of medicinal substance renders
Significant influence on his biological activity. It is known,
Ability of chemical compounds to have various structure,
Described in each concrete case specific
Set of properties. The geometrical form and structure
Formed crystals essentially depend on character
Solvent, speed of crystallization, temperature of process, from
Impurity, size of pressure, etc. factors. Consider for example,
That 30-60 % sulfanilamidov, 70 % barbituratov polimorfny, 1/3
All organic connections has at least two
Crystal forms. Enough is saved up
An experimental material about dependence of structure of substances and
Their biological availability. To questions of crushing in
To pharmaceutical technology attaches special significance. It is known,
That with reduction of the size of particles sharply increases
Superficial energy of crushed medicinal substance. At
Thin crushing medicinal substance are better dissolved,
Participate in chemical reactions, etc. fastly and more full.
Crushing can influence significally on therapeutic
Activity of medicinal substances owing to change of processes
Them vsasyvanija. It occurs at change of solubility
Medicinal substances, which speed in direct ratio
The areas of a surface and in inverse proportion to size of particles
Substances. For example, at purpose of identical dozes sulfadimezida
mikronizirovannogo and received in factory manufacture without
Additional crushing it is revealed, that in the first case in
To plasma of blood of people the maintenance of substance is higher 40 %, maximal
Concentration is reached at 2 o'clock earlier, and total
On 20 % it is more than soaked up substance, than in the second case. At
Reduction of the size of particles of an acid atsetilsalitsilovoj up to
mikronizirovannyh has increased approximately in 2 its times
analgeticheskoe, febrifugal and anti-inflammatory
Action. In chemist's practice the necessary size of particles of a powder
Receive at observance of the following conditions of crushing: a choice
Mortars, time of crushing, application of devices, the order
Mixing, special corrected also receptions of technology.
Not less the great value in technology of medicinal forms has
A correct choice of auxiliary substances. Up to the most recent
Time in auxiliary substances saw only
Indifferent formoobrazovateli which value were reduced to
To giving the corresponding form and volume of medicinal substance
With the purpose of convenience of his reception, transportation, storage. However
Opening last decades have led to to comprehension biological
Roles of auxiliary substances. They can strengthen, reduce
Action of medicinal substances or to change his character under
Influence of the various reasons (kompleksoobrazovanie, molecular
Reactions, etc.)
Application of thin high-sensitivity methods of the analysis
Preparations (gazo-liquid, tonkoslojnaja a chromatography,
rentgenostrukturnyj the analysis, spektrofotometrija) have allowed
To establish the closest mutual relations medicinal and
Auxiliary substances. Such usually used
Auxiliary substances, as gelatin, krahmaly,
polietilenoksidy, derivative cellulose, neionoaktivnye PEAHENS
Are capable to enter reactions of interaction (in particular,
kompleksoobrazovanie) with medicinal substances most
The various nature, forming the connections described by others,
Than initial substances, properties. As an example we shall consider
Influence of auxiliary substances on activity medicinal
Substances in ointments and suppozitorijah. Among the factors influencing on
Liberation of medicinal substances in ointments, the greatest attention
Give a basis. Influence such as a basis variously depending on
A way of introduction of medicinal substance. It is established, for example,
That the acid boric does not render bakteriostaticheskogo action
At use of fatty bases, but it is effective at manufacturing
Ointments on gidrofilnyh bases in which contains big
Quantity of water. Apparently, therapeutic action shows
A formed solution of an acid boric. Iodine, on the contrary, maloaktiven
In the bases containing a plenty of water.
Introduction in structure mazevyh and suppozitornyh bases emulgatorov,
PEAHENS, etc. activators vsasyvanija is one of important
The factors influencing activity medicinal
Substances. Sodium laurilsulfat promotes increase rezorbtsii
Microcrystalline sulfapiridazina from gidrofilnoj bases.
It is shown, ability dimetilsulfoksida it is easy to penetrate through
The intact leather to transport, deposit and
prolangirovat thus receipt of medicinal substances in
An organism.
Perspective auxiliary substance in technology of ointments,
suppozitoriev, solutions for injections, eye medicinal
plenok, etc. medicinal forms collagen is.
It is supposed, that medicinal substance, getting in "loops"
Molecules of collagen, forms connection - inclusion of type
klatratov, providing thus prolonged action.
Auxiliary substances should respond the basic requirement-
To open all scale of pharmacological properties of a preparation,
To provide optimum action of medicinal substance.
The correct choice of auxiliary substances allows to lower
Concentration of medicinal substance at preservation
Therapeutic effect.
Value of the medicinal form. Optimum activity
Medicinal substance it is reached only by his purpose in
Rational, scientifically proved LF. Choice LF defines and
A way of introduction of medicinal substance in an organism.
Efficiency of medicinal substance depends on what
The way will be made with it before gets in blood. At rektalnom
A way the medicinal substance gets in blood, passing a liver, and
Is not exposed to chemical influence of its enzymes,
Gastric juice and bile. Therefore it, is soaked up through 7 ', and
At peroralnom - through 30 '.
Value of technology factors. A way of reception LF
In many respects defines stability of a preparation, speed
His liberation from LF, intensity vsasyvanija-
More shortly, therapeutic efficiency. For example, a choice
A way granulirovanija tablets it is caused
Safety of medicinal substance in LF. Are perspective
Technologies of multilayered tablets and spansul (gelatinous
The capsules filled with granules) for maintenance
The prolonged and differentiated action.
