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Вестник КазНМУ, №5(3)- 2013
А. БАКЫТ, У.М. ДАТХАЕВ, Ж. АБЫЛАЙ¥ЛЫ, К-К- КОЖАНОВА
ЛЕКАРСТВЕННАЯ ТЕРАПИЯ ПРИМЕНЯЕМАЯ ДЛЯ ЛЕЧЕНИЯ ЗАБОЛЕВАНИЙ ЩИТОВИДНОЙ ЖЕЛЕЗЫ, АНТИТИРЕОИДНЫЕ ПРЕПАРАТЫ
Резюме: В статье приведены статистика распространения заболеваний щитовидной железы не только в Республике Казахстан, но и во всем мире, влияние щитовидной железы на организм человека, видыболезни и методы лечения. Описан механизм действия антитиреоидных препаратов, рассмотрены показания к применению и особенности использования тиреостатиков в терапевтической клинике. Приведены основные побочные эффекты антитиреоидных препаратов. Указана актуальность внедрения современных лекарственных форм в фармацевтическую практику. Ключевые слова: щитовидная железа, антитиреоидные препараты, тиамазол.
A.BAKYT, U.M.DATKHAEV, ZH.ABYLAYULY, K.K.KOZHANOVA
DRUG THERAPY IS USED TO TREAT THYROID DISEASE, ANTITHYROID DRUGS
Resume: The articlepresents statistics ofthe spread of diseasesof the thyroidgland is notonlyin the Republic ofKazakhstan, and around the world, said the impactof the thyroidglandin thehuman body, the types of illnesses andtreatments. A mechanism ofaction ofantithyroiddrugsare consideredindications for useand featuresthyreostaticsusein therapeuticclinic.The mainside effectsof antithyroid drugs.Indicatedthe relevance ofthe introduction of moderndosage forms inpharmaceutical practice. Keywords: thyroid,antithyroid drugs, tiamazol.
UDC 615.453.62:615.281:615-011-078
D.V. BARINOV A.S. KALYKOVA Z.B. SAKIPOVA 1
1 S.D. Asfendiyarov Kazakh National Medical University, Module «Pharmacist-Technologist» 2 Scientific Center for Anti-Infectious Drugs
STUDY OF SOME PHYSICAL ANDTECHNOLOGICAL CHARACTERISTICS OF THE FS-1SUBSTANCE
Resume:Some physical and technological characteristics of the FS-1 substance were studied: calculated the porosity by the bulk and true density, pressability and compression ratio, also the lyophilic property and wettability.
Keywords: FS-1 substance, technological parameters, porosity, bulk density, true density, Hausner ratio, compression ratio, wettability, pressability.
Introduction.Value of iodine-containing preparations as antiseptics that all agents of wound infection naturally sensitive to them and the formation of acquired resistance to them are not typical, so iodine is still in the leading position among modern antiseptics.
Widely used in medical practice found iodophores - iodine preparations based on non-toxic soluble polymers. They are complexes of iodine with polymers of different structures "lodinol"- polyvinyl alcohol "Yodopiran"-
polyvinylpyrrolidone, "Amiloiodil"- with the starch. The developed FS-1 substance [1] is a complex compound with iodine polidental ligands, which serve associates of carbohydrates and peptides. The active component of FS-1 substance is iodine polymer complex that serves as a matrix capable of retaining a molecule of iodine in the blood included in the preparation, thereby allowing transportation and placement of I2 in the intercellular space. The main stages of the synthesis of substance FS-1 is:
1- preparationofmatrixpolymer;
2- intercalationofactiveiodine;
3- preparation of FS-1 liquid drug form;
4- lyophilizationofsolution.
To obtain the most effective dosage form based on the dry powder substance FS-1 is necessary to study a number of
characteristics which have a direct effect on the manufactured form.
Thesecharacteristicscanbeclassifiedintomajorgroups:
1- phisical;
2- technological.
This article discusses the methodological approaches to the study of some characteristics of FS-1 substance, which is a dry heat labile and hygroscopic dark color powder. On the chemical nature the FS-1 substance is an ionic compound nanostructured complex.
Materials and methods. To investigate the physico-chemical and technological characteristics were synthesized four series of FS-1substance. The synthesis conditions were the same, except the molecular weight of the synthetic polymer matrix.
In the production of solid dosage forms of FS-1 substance the important characteristic is the porosity as one of the flowability factors.
Powder porosity (P, %) was determined from the values of bulk and true density.
The bulk density (pb, kg/m3) were determined by weighing a graduated cylinder with thesubstance after multiple seals. Hausner ratio was calculated (H), which described the degree of FS-1substance flowability.
BecTHUK Ka3HMY, №5(3)- 2013
Determination of true density (pg, kg/m3) was performed on a Pycnomatic - ATC, Porotec GmbH., Germany. One of the important technological parameters for dry substances is the compaction factor (Kc), which characterizes the time of pressing and pushing force of the formulation during tabletting.Compaction ratio or compression ratio -the ratio of the height of the substance in the press-form prior to compression to the height of the resulting tablets after compression.
Compressibility of substance (Kp, g/mm) - the ability of the particles of FS-1 substance for mutual attraction and mechanical interlocking to form a solid tablet model. Since the FS-1 substance includes components differing hygroscopicity, it was determined parameter -hygroscopicity - is the ability of dry substance to absorb moisture from the environment. Degree of hygroscopic substances is generally measured in two conditions: room temperature and 100% humidity. Room humidity should not exceed 80%.
The bioavailability of the dosage form influence the ability of the substance to dissolve and its rate of dissolution which, in turn, depends on the hydrophilicity of FS-1 substance. The
hydrophilicity is due to the nature and amount of hydrophilic groups on the surface of the particles of FS-1 substance. Hydrophilicity substance studied by determining the degree of wetting in two mechanical states: finely dispersed powder phase and film.
Results and discussion. Evaluation of some technological parameters FS-1 substance was carried out on the basis of the study factors affecting the production of mainly solid dosage forms. Among them: porosity, Hausner ratio, bulk density, true density, compression ratio, compressibility, hygroscopicity and wettability. The research results are shown in table 1.
Obtained data indicate that as a result of laboratory syntheses were obtained FS-1 substance series with varying porosity and particle size, and therefore with different flow properties. Comparison studied physical and technological characteristics are presented as a histogram (fig. 1). FS-1 Substance series # 01130312 is the most optimal for the production of solid dosage forms, when substance has considered ideal flowability characteristics, as evidenced by Hausner ratio (1.09) and good porosity (43.9%).
Table 1 - The results of studies of FS-1 substance
Substance's batches Parameter The results of studies of FS-1 substance
01110113 02110113 03170113 04180113 01130312
Hausner ratio (H) 1,23 1,29 1,26 1,21 1,09
Porosity (P), % 37,2 36,6 38,5 40,0 43,9
Bulkdensity (pb), kg/m3 1,0513 1,0644 1,0314 0,9798 0,9276
True density (pg), kg/m3 1,6751 1,6783 1,6782 1,6325 1,6537
Compressionratio (Kc) 1,15 1,32 1,44 1,34 1,35
compressibility (Kp), g/mm 0,183 0,187 0,183 0,191 0,190
FS-1 substance series # 04180113, in its parameter had sufficient technological properties, for use in the manufacture of solid dosage forms. This series has a moderate flowability, porosity and particle size. Other FS-1 substances series (01110113, 02110113 and 03170113), had insufficient flowability due to low porosity and small particle size. The described deficiency will have considerable difficulty in using a substance with such features during the manufacture of solid dosage forms, when dosing.
All substances series FS-1 had good compression characteristics and the compression ratio.
FS-1 substance has a pronounced hygroscopic in conditions of maximum humidity and mild conditions in the room humidity. After 72 hours study under the maximum humidity FS-1 substance absorbed to go to viscous fluid state, which is unacceptable. Whereas, the hygroscopicity study in room conditions showed that after 100 hours humidity at room upper layer of FS-1 substance contact with medium weak solidified (flowability lost), but at weak hit again acquired flowability. The dependence of the amount of moisture absorbed presented as the kinetic curves in Figure 2 for maximum humidity and Figure 3 for the room humidity
BecTHUK Ka3HMY, №5(3)- 2013
Figure 1 - Comparison of the studied physical and technological characteristics of the FS-1 substance
Kinetic diagram depending chart of moisture absorption by substance FS-1 under the maximum humidity Moisture absorption, % o nnn
7,000 6,000 5,000 4,000 3,000 2,000 1,000 0,000
===== gSS
m
/
X
Period, h ) 24 48 72 96 120 144 168 192 FS-1 substance series -1110113 -2110113 -3170113 -4180113 -1130312
Figure 2 - The dependence of moisture absorbed of FS-1 substance with over time under the maximum air humidity
Figure 3 - The dependence of moisture absorbed substance FS-1 with over of time under room humidity
All substances series FS-1 are well wetted irrespective pH, and therefore are hydrophilic.
Conclusions: Conducted researches have shown that in the application of FS-1 substance for the manufacture of solid dosage forms must be administered excipients in tablet mass:
Вестник КазНМУ, №5(3)- 2013
- to improve the flowability of substance FS-1 is advisable to use an emulsifier - magnesium stearate;
- to improve the disintegration - croscarmellose sodium (Ac-Di-Sol);
- as a filler, to reduce the hygroscopicity of the FS-1 substance - dextrates or a macrocrystalline cellulose.
REFERENCES
1. IlinA.I., KulmanovM.E. PatentAppl. № 2010/1816.1, Republic of Kazakhstan (30 December 2010).
2. Чуешов В.И., Гладух Е.В., Ляпунова О.А., Сайко И.В., Сичкарь А.А., Рубан Е.А., Крутских Т.В. Промышленная технология лекарств. - 2010. Электронный учебник.: http://ztl.nuph.edu.ua/html/medication/index.html
3. Podczeck, Fridun& Brian E. Jones, eds. 2007. Pharmaceutical Capsules. - London: Pharmaceutical Press, - 111 p.
4. Mark Gibson (2001). Pharmaceutical Preformulation and Formulation: A Practical Guide from Candidate Drug Selection to Commercial Dosage Form. Boca Raton: CRC Press. ISBN 1-57491-120-1.
Д.В. БАРИНОВ, А.С. КАЛЫКОВА, З.Б. САКИПОВА
ФС-1 Ш1К1ЗАТЫНЫЦ Б1РНЕШЕ ФИЗИКАЛЫК; ЖЭНЕ ТЕХНОЛОГИЯЛЫК; К0РСЕТК1ШТЕР1НЗЕРТТЕУ
Туйш: ФС-1 шМзатыньщ бiрнеше физикалыщ жэне технологиялыщ параметрлердщ зерттелген: ^ысу коэффициент^ пресстелуi, лиофильдiгi, дым^ылдануы, нагыз жэне себтпштк тыгыздыгына негiзделе ^уыстыщ тесiктерi есептелген. ТYйiндi сездер: ФС-1 шЫзаты, технологиялыщ кврсеткiштер, ^уыстыщ тесiктер, нагыз жэне себтпштк тыгыздыщ, Хауснердщ коэффициент^ ^ысу коэффициентi, пресстелуi, дым^ылдануы.
Д.В. БАРИНОВ, А.С. КАЛЫКОВА, З.Б. САКИПОВА
ИЗУЧЕНИЕ НЕКОТОРЫХ ФИЗИЧЕСКИХ ИТЕХНОЛОГИЧЕСКИХ ХАРАКТЕРИСТИК СУБСТАНЦИИ ФС-1
Резюме:Изучены некоторые физические и технологические характеристики субстанции ФС-1: рассчитана пористость на основании изученных насыпной плотности и истинной плотности, коэффициент сжатия и прессуемость, а также лиофильность и смачиваемость.
Ключевые слова: Субстанция ФС-1, технологические параметры, пористость, насыпная плотность, истинная плотность, коэффициент Хауснера, коэффициент сжатия, смачиваемость, прессуемость.
УДК 615.322:615:014:633.88.005(15)
Д.Е. ЕСБОЛАТОВА, А.Б. БЕЛГИЖАН, А.А. АКЫЛБЕК, Э.Н. КАПСАЛЯМОВА
АНАЛИЗ ПРОИЗВОДСТВА ЛЕКАРСТВЕННОГО РАСТИТЕЛЬНОГО СЫРЬЯ В МИРЕ
В данной работе, основной целью было провести анализ мирового и фармацевтического рынка Казахстана по производству лекарственного растительного сырья. Объектами исследования стали страны Европы и Азии; использовались аналитические, статистические методы исследования и анкетирование. В наших исследованиях мы опирались на опыт зарубежных компаний, которые занимают ведущие места в таблице рейтинга по экспорту растительного сырья. Используя опыт этих предприятий, мы предложили освоение данного сегмента рынка на территории РК. Как показал мировой опыт, практика культивирования и сбора лекарственного растительного сырья, нуждается в специализированных руководствах. Для перехода, после тщательного изучения данного направления, мы предлагаем использование стандарта GACP (Good Agricultural and Collection Practice for Medicinal Plants), которые повсеместно используются ведущими странами в политике производства лекарственного растительного сырья. Ключевые слова: лекарственное растительное сырье, GACP, экспорт, Казахстан, надлежащие руководства.
Ежегодно в мире заготавливают сотни тысяч тонн лекарственного сырья, причиной тому значительная потребность в данном виде продукта. Наряду с фармацевтическим рынком лекарственных средств, изделий медицинского назначения и медицинской техники, существует рынок лекарственного растительного сырья, на данный момент ведущими в этом направлении являются такие страны как Китай, Индия, Мексика, Германия, США.
В период с 1991 по 2003 гг., по данным базы КОМТРЕЙД, ООН Статистического отдела, глобальный экспорт лекарственного растительного сырья по миру составил в среднем 467 000 тонн на сумму 1,2 млрд. долларов США. Главной особенностью этого экспорта является преобладание лишь несколько стран: около 80%, по всему миру, экспорта отведено только 12 странам, из которых страны Азии занимают 48% годовых в мировом экспорте лекарственного растительного сырья.
