The study of structural-mechanical characteristics of suppositories with clopidogrel
Keywords:clopidogrel, suppositories, thixotropy, technology pharmaceutical
During last years clopidogrel keeps leading positions among medicines with platelet antiaggregation mechanism.
The rectal dosage form with clopidogrel, namely suppository containing 0.075 g of active substance on hydrophilic base with addition of 2 % twin-80 was proposed by the Department of Medicinal Preparations Technology (Zaporizhzhia State Medical University on the base of complex investigations.
The aim of present work is the study of structural-mechanical characteristics of rectal dosage form with clopidogrel depending on the temperature of technological process of supposirory manufacturing.
The study of structural-mechanical characteristics of suppository mass with clopidogrel was carried out using the rotational viscosimeter “Rheotest2”with cylinder device at the human body temperature (37 ºС) and at temperature of manufacturing technological process.
Results. Results testify presence of structure in suppository mass system, because limit shear stress increases and effective viscosity decreases with deformation speed rising.
Conclusions. Study of consistent characteristics of suppository mass with clopidogrel on polyethylenoxyde base with addition of 2 % twin-80 at the human body temperature was carried out. It was established that it is structural system with expressed thixotropic properties and with the uniform distribution of active substance and excipients both at the moment of manufacturing and during administration or long storage. It was revealed that increasing of temperature of suppository mass to 50 ºС doesn't lead to essential modification of its structural-mechanical characteristics and transformation into Newtonian system. Taking obtained results into account it was determined that temperature rate of manufacturing of rectal suppositories with clopidogrel on the hydrofiflic base (processes of mixing, homogenization, pouring into forms) within 50–55 ºС creates sufficient fluidity of mass for unhampered technological process and thixotropy of suppository mass providing the uniform distribution of active substance and excipients in this dosage form.
Lipoveckij, B. (2012). Dislipidemii, ateroskleros і ikh svyaz' s ishemicheskoj bolezn'yu serdca і mozga [Dislipidemia, atherosclerosis and their connection with ischemic heart and brain trouble]. Saint Petersburg: Eko Vektor [in Russian].
Bolotnova, T. V. & Efanova, A. Yu. & Sherstobitova, A. F. (2015) Rol' vracha obshchej praktiki v profilaktike faktorov riska koronarnogo ateroskleroza [A role of general practitioner is in the prophylaxis of risk of coronal atherosclerosis factors]. Universitetskaya medicina Urala, 2–3, 15–18. [in Russian].
Yakusevich, V. V. & Yakusevich, V. Vl. & Pozdnyakova, E. M. (2015). Rol' dezagregantov v lechenii stabil'noj stenokardii: ustoyavshijsya vzglyad i nerazreshennye problemy [Role of the antiplatelet drugs in treatment of stable angina: common sense and non-resolved issues]. Rossijskij kardiologicheskij zhurnal, 7(123), 120–126. [in Russian]. http://dx.doi.org/10.15829/1560-4071-2015-07-120-126.
Orlova, T. (2014). Sovremennye rektal'nye, vaginal'nye і uretral'nye lekarstvennye formy [Modern rectal, vaginal and urethral medicinal forms]. Vestnik Voronezhskogo gosudarstvennogo universiteta. Seriya: Khimiya. Biologiya. Farmaciya, 1, 126–133. [in Russian].
Redkina, Ye. А., Gladyshev, V. V., Burlaka, B. S., & Pukhalskaya, I. A. (2018). Vyvchennia vplyvu dopomizhnych rechovyn na vyvilnennia klopidogreliu z rektalnych supositoriiv [The study of excipients’ influence on Clopidogrel releasing from the rectal suppositories]. Current issues in pharmacy and medicine: science and practice, 1(26), 74–78. [in Ukrainian]. doi: 10.14739/2409-2932.2018.1.123717.
Redkina, Ye. А., Gladyshev, V. V., Burlaka, B. S., & Kechin, I. L. (2018). Vyvchennia vplyvu kontsentratsii poverchnevo-aktyvnykh rechovyn na vyvilnennіa klopidogreliu z rektalnykh supozitoriiv [Study of influence of the surface-active substances concentration on clopidogrel releasing from the rectal suppository]. Current issues in pharmacy and medicine: science and practice, 2(27), 185–189. [in Ukrainian]. doi: https://doi.org/10.14739/2409-2932.2018.2.133214.
Kuchina, L. K., Gladysheva, S. A. & Puchalskaya, I. A. (2015). Izuchenie strukturno-mekhanicheskikh svojstv suppozitoriev s diltiazemom [The study of structural-mechanical properties of diltiazem suppositories]. Current issues in pharmacy and medicine: science and practice, 2(18), 41–44. [in Russian]. doi: http://dx.doi.org/10.14739/2409-2932.2015.2.45197.
Fadi Al Zedan, Gladyshev, V. V., Burlaka, B. S., & Nagorny, V. V. (2013). Izuchenie strukturno-mekhanicheskikh svojstv suppozitoriev s amlodipinom [Studying of structural-mechanical characteristics of suppositories with amlodipine]. Zaporozhye medical journal, 1(76), 63–66. [in Russian]. doi: https://doi.org/10.14739/2310-1210.2013.1.15509.
Tikhonov, O. I., Krivovyaz, O. V., & Zubchenko, T. M. (2010). Vyvchennia strukturno-mechanichnykh vlastyvostei suposytoriiv z vmistom fenolnoho preparatu propolisu ta lipofilnoho ekstraktu pylku kvitkovoho [The study of structural and mechanical properties of suppositories containing FGPP and LEBP]. Visnyk farmatsii, 4(64), 3–6. [in Ukrainian].
Nagornaya, N. A. & Burlaka, B. S. & Gladysheva, S. A. (2014). Izuchenie strukturno-mekhanicheskikh svojstv suppozitoriev s vinpocetinom [Study of structural-mechanical properties of vinpocetine suppositories]. A Current issues in pharmacy and medicine: science and practice, 1(14), 39–42. [in Russian]. doi: https://doi.org/10.14739/2409-2932.2014.1.24654.
Al Zedan Fadi (2013). Razrabotka sostava, tekhnologii i issledovanie myagkikh lekarstvennykh sredstv antigipertenzivnogo dejstviya s amlodipinom (Dis…kand. farm. nauk). [The development of technology and research of soft drugs antihypertensive action of amlodipine Dr. farm. sci. diss.]. Zaporizhzhya: ZSMU [in Russian].
How to Cite
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)