All known drug forms are prepared by using excipients. Excipients are additional material which is required to give appropriate drug dosage form. Forming effective drugs are required a large number of excipients. Until recently, to excipients were demanded of pharmacological and chemical indifference. However, it was found out that these substances may significantly affect to the pharmacological activity of drugs: increase the effects of drugs or reduce their activity, to change the nature of the action under the influence of different reasons, chelation, molecular reactions, and other interference. Excipients influence not only on the therapeutic efficacy of the drug, but also on the physico-chemical characteristics of the dosage form during manufacture and storage.
Key words: Excipients, synthetic chemistry, pharmacological activity of the drug, therapeutic effectiveness, substances, pharmaceutical technology, technical equipments.
Introduction. Excipients - a substance of an organic or inorganic nature, which are used in the manufacturing process and manufacturing dosage forms to impart desired properties. To create the drug forms in all cases, must be usedthis or that excipient. Moreover, thanks to the success of synthetic chemistry and pharmacology were created hormone drugs action. Single doses of such drugs comprise milligrams or even fractions of a milligram, and this leads to the need of the obligatory use of excipients in the drug forms, and increasing their role in the pharmacokinetics of the drug. In the manufacture of drugs were used excipients which are allowed for medical use appropriate to RD or special standarts USST and UST. Until recently, the substances to make demands only on pharmacological and chemical indifference. However, it was found out that these substances can significantly affect on the pharmacological activity of the drug. Affecting to the pharmacological activity of the drug, excipients are able to strengthen or weaken (lower activity) of the drug, to provide local or systemic effect on the body, measuring the speed of onset of effect (speed up or prolong the action), aiming to provide transport or controlled release of drugs.
Methods and materials. These substances influence not only on the therapeutic effectiveness of the drug, but also on the stability of the drug form during manufacturing and storage, which has not only medical, but also economic importance, as it allows to increase the shelf life of drugs. The substances has its certain requirements. They must be biologically, non-toxic, chemically indifferently to the substances which is contained in the preparation, materials of technical equipments, including information, of environmental factors in the manufacturing process of the drug and during storage. It should not cause allergic reactions, attach to the required properties. These substances should take the necessary functional properties with a minimum content in the product.
Effect of excipients on the efficacy and quality of pharmaceuticals.
- Excipients influence on: therapeutic efficiency, resorption, localized action, pharmacokinetics, pharmacodynamics.
- Quality of drugs: stability, prolongation of action, taste masking.
Discussion. Based on the functions of the adjuncts as formative they can be classified into the following groups: solvents; bases for ointments; suppository bases; The excipient used in powders, tablets or pills; coating substances; surfactants; substances that increase the viscosity; stabilizers; preservatives; flavoring substances; coloring substances; gases.
Soaps are widely used in medical practice in a topical medication as liniments, lotions, ointments. Another more widely used organic soap - trietanolaminostearat and sodium lauryl sulfate, a sodium salt and a high molecular sulfoefira alcohol poluchaemogoiz coconut oil.
Cationic surfactants due to adverse biological action and relatively low stabilizing effect found limited use in pharmacy as a means of lowering the surface tension. The best known of this group of surfactants - dimetiltsetilbenzilammoniya chloride, cetyl trimethyl ammonium chloride - are used more because of its bactericidal activity. The most acceptable in pharmaceutical technology nonionic surfactant
Natural excipients have the advantage to compare with synthetic due to high biological safety. Therefore, of all the excipients for about 2/3 is natural.
Currently natural excipients are used as shaping devices (excipients), binders, prolongators, taste masking, etc.
Natural excipients have significant disadvantages, they are subject to microbial contamination, so the drug forms, especially solutions, is prone to loss of its quality. In addition, the content of the microflora can be detected not only opportunistic but also pathogens. In this case, using of suitable methods of sterilization, the addition of antimicrobial agents (preservatives) to a large extent can be reduced to the maximum allowable microbial contamination of natural substances.
Conclusion. Remains of ampoules, aerosol cans, bags and bottles are taken as the production or household garbage; Hard drug forms (powders, tablets, capsules and etc.) containing of water-soluble substance drugs are crushed to a powder, diluted with water in the ratio of 1: 100 and merge into industrial sewers.
Solid drug forms (powders, tablets, capsules, etc.), containing substances which are insoluble in water, soft drug forms (ointment, suppositories and etc.), transdermal forms of drugs and pharmaceutical substances are burned; narcotic drugs and psychotropic substances are included in lists II and III of the list of narcotic drugs are destroyed in the accordance of the law of the RK, flammable, explosive drugs, radiopharmaceuticals, and medicinal herbs with a high content of radionuclides destroyed in special circumstances by a special technology available to the organization for the destruction.
- Azhgikhin. I.S. “Технология лекарств.” 2nd edition. Moscow. Medicine, 1980 - p.440
- Gretsky V.M.”PyKoeogcTBO к практическим занятиям по технологии лекарств”Moscow. Medicine, 1984 p351.
- Kondratyeva T. S. “Технология лекарственных форм.” Moscow. Medicine. 1991 p 496.
- Kondratyeva T. S. “Руководство к лабораторным занятиям по аптечной технологии лекарственных форм.” Moscow. Medicine.1986 p286.
- Krasnyuk I. N. “Фармацевтическая технология: Технология лекарственных форм.” Moscow. “Academy” 2004 p464.
- Milovanova L. N. “Технология изготовления лекарственных форм” Rostov na Donu: Medicine, 2002 p448.