Development of fi lm forming formulation and technology of polymeric fi lm coating on Indotril tablets
DOI:
https://doi.org/10.14739/2310-1210.2013.5.18957Keywords:
indomethacin, thiotriazolin, tablets, polymeric coatAbstract
Introduction. In previous researches we grounded expedience of «Indotril» tablets development; formulation and technology of "Indotril" tablet cores were developed. Received tablet cores should be covered by protective polymeric film with the purpose of unpleasant taste elimination, increase of tablets expiration date.
Objective. The aim of our investigation was to develop the film forming composition and technology of polymeric film coating on «Indotril» tablets in pseudo-fluidized layer.
Materials and Methods. As “Indotril” tablets cores should be covered by protective polymeric film we performed research designed to select efficient film forming solution. Thus modern filming agents were studied, besides such factors were investigated: concentration of film forming suspension, increase of tablet coat in mass, air temperature under gas distribution grid. Obtained tablets were checked according to pharmacopeia methods.
Results and discussion. First we studied tablet compression force influence on main parameters of «Indotril» cores tablets: on crushing strength, abrasion in pseudo-fluidized layer unit and disintegration. Then for further investigation we chose «Indotril» cores tablets with crushing strength near 70 H, abrasion - up to 0,5% and disintegration time - not more than 10 minutes. We performed research to select film forming solution for covering “Indotril” tablets in pseudo-fluidized layer unit. As filming agents we used different samples of hydroxypropyl methylcellulose (HPMC) by Japan company Shin-Etsu Chemical Co and English company Colorcon. Water HPMC solutions were prepared which contained plasticizer (propylene glycol), pigment (titanium IV dioxide) and dye (tartrazine). Coating process of “Indotril” tablets was performed in laboratory pseudo-fluidized layer unit with the air temperature 75ºC under gas distribution grid.
Variance analysis of experimental data on quality of coat surface showed insignificance as for nature of studied filming agents. Homogeneity in bulk of coated “Indotril” tablets also did not differ significantly as for filming agents’ nature. Divergence in mass of coated tablets did not differ significantly from uncoated ones; it testifies identity of filming process over all tablets surface. Strength of coated “Indotril” tablets as compared with uncoated ones increases in average on 15-20 H.
Variance analysis of experimental data concerning tablets disintegration resistance showed that there was no significant difference between studied filming agents. While defining disintegration time statistical significance of filming agents’ nature was determined. Ranking is the following: 6% solution of HPMC Pharmacoat 603 > 5% solution of Opadray II WHITE > 5% solution of HPMC Pharmacoat 606 > 4% solution of HPMC Pharmacoat 615. But the difference between filming agents’ nature is not more than 2 minutes.
Opadray II WHITE has been chosen for further study; it comes to the enterprise (“Arterium” Corporation) where the results of investigation are planned to be introduced for the manufacture of other tablet dosage forms.
On the next stage of our investigation we defined optimal values of quantitative factors, notably the influence of air temperature under gas distribution grid, concentration of film forming suspension and film thickness on the properties of coated “Indotril” tablets.
Conclusion.
- Influence of filming agent nature on properties of coated tablets «Indotril» was studied, namely on appearance, homogeneity in bulk, mechanical strength, disintegration time.
- Opadray II WHITE was proposed for coating “Indotril” tablets by protective polymeric coat in pseudo-fluidized layer.
- Worked out formulation of filming agent solution and technology of its application were included into technological regulation of «Indotril» tablets production.
References
Зупанець І.А. Раціональне застосування нестероїдних протизапальних препаратів при лікуванні захворювань суглобів: метод. реком. / І.А. Зупанець. – Х., 2002. – 23с.
Державна Фармакопея України/ ДП «Науково-експертний фармакопейний центр» – 1-е вид. –Харків: РІРЕГ, 2001. – 556 с.
Державна Фармакопея України: Доповнення 1 / ДП«Науково-експертний фармакопейний центр» – 1 вид. – Х.: РІРЕГ, 2004.– 520 с.
Математичне планування експерименту при проведенні наукових досліджень в фармації / [Грошовий Т.А., Марценюк В.П., Кучеренко Л.І. та ін.]; під ред. Т.А. Грошового. – Тернопіль: ТДМУ, Укрмедкнига, 2008. – 367 с.
Механізм проти ішемічної та антиоксидантної дії тіотриазоліну / І.Ф. Бєленічев, І.А. Мазур, М.А. Волошин [та ін.] // Новости медицины и фармации. – 2007. – №2 (206). – С. 8–9.
Молекулярный механизм энерготропного и антиоксидантного действия тиотриазолина / И.Ф. Беленичев, И.А. Мазур, И.С. Чекман, Н.А. Волошин // Ліки. – 2006. – №3–4. – С. 12–16.
Морфологические изменения в органах желудочно-кишечного тракта крыс при изучени их ронической токсичности индотрила и препаратов сравнения / В.И. Мамчур, Е.А. Подплетняя, И.А. Мазур [и др.] // Актуал. питання фармац. та мед.науки та практики: зб. наук. ст. Запоріжжя: Вид-во ЗДМУ, 2006. – Вип. ХV, т. ІІІ. – С. 597 599.
Насонова В.А. Рациональная фармакотерапия ревматических заболеваний / В.А. Насонова, Е.Л. Насонов. – М.: Литтерра, 2003. – С. 22–34.
Новые подходы к прогнозированию риска развития гастропатий, индуцированных нестероидным и противовоспалительными средствами / Л.Е. Зиганшина, А.Ф. Султанова, В.Н. Хазиахметова [и др.] // Эксперим. и клинич. фармакология. – 2002. – Т. 65, №2. – С. 49–52.
Основные направления поиска и создания нових лекарственных средств сотрудниками Запорожского государственного медицинского университета / А.Д. Визир, В.В. Дунаев, В.А. Визир, И.А. Мазур // Актуал. питання фармац. та мед. науки та практики: зб. наук. ст. – Запоріжжя, 1997. – Вип. 1. – С. 3–13.
Патент на винахід №74920 Україна, МПК (2006): A61K31/4015,A61K31/41 A61K9/20. Спосіб виготовлення таблеток, покритих оболонкою, що містять пірацетам і тіотриазолін/ Мазур І.А., Дячок В.В., Грошовий Т.А. [та ін.] //Промислова власність. – 2006. – №2.
Современные пленочные покрытия в технологии таблеток /Алексеев К.В., Дитковская А.Г., Алексеев С.К.// Фармация. –2009.–N 8.–С.45–49.
Protective effect of thiaton, an antispasmodic drug, against indomethacin-induced intestinal damage in rats / T. Kunikata, T. Miyazawa, K. Kanatsu [atal.] // Jpn. J. Pharmacol. – 2002. – Vol. 88, № 1. – Р. 45-54.
Crystal. Molecular structure and tautomerism of (5-methyl -1H-[1,2,4]triazol-3-ylsulfanyl)-acetic acid / Roman I. Zubatyuk, Svetlana V. Shichkina, Lyudmila I. Kucherenko, Ivan A. Mazur, Oleg V. Shichkin // Struct. Chem. – 2008. – Vol. 19. – P. 407–412.
Two polymorphs of morpholin-4-ium 2-(5-methyl-1H 1,2,4tryazol- 3yisulfanyl) acetate / Svetlana V. Shichkina, Roman I. Zubatyuk, Lyudmila I. Kucherenko, Ivan A. Mazur, Oleg V. Shichkin // CrystalStruct. Communications – 2009. – Vol. C65. – P. o24–o26.
Comparative tablet and rheological properties of new microcrystalline cellulose: Direct compression and wet granulation methods / D. Opota, P. Prinderre, J. Kaloustian [etal.] // DrugDev. and Ind. Pharm. – 1999. – Vol. 25, №6. – P. 795–799.
Downloads
How to Cite
Issue
Section
License
Authors who publish with this journal agree to the following terms:
- Authors retain copyright and grant the journal right of first publication with the work simultaneously licensed under a Creative Commons Attribution License that allows others to share the work with an acknowledgement of the work's authorship and initial publication in this journal.
- Authors are able to enter into separate, additional contractual arrangements for the non-exclusive distribution of the journal's published version of the work (e.g., post it to an institutional repository or publish it in a book), with an acknowledgement of its initial publication in this journal.
- Authors are permitted and encouraged to post their work online (e.g., in institutional repositories or on their website) prior to and during the submission process, as it can lead to productive exchanges, as well as earlier and greater citation of published work (See The Effect of Open Access)
