Abstract

TICAGRELOR-EXCIPIENT COMPATIBILITY STUDIES FOR ADVANCED DRUG DELIVERY SYSTEMS DEVELOPMENT

Mahmoud Mahyoob Alburyhi*, Abdalwali Ahmed Saif and Maged Alwan Noman

ABSTRACT

Ticagrelor is one of the most recent antiplatelet agents used to inhibit platelet aggregation via blocking the Adenosine diphosphate (ADP) receptors of the subtype P2Y12, it used in patients with a history of myocardial infarction or with acute coronary syndrome (ACS) to prevent future myocardial infarction, stroke and cardiovascular death. Ticagrelor is used to prevent a serious or life-threatening heart attack or stroke, or death in people who have had a heart attack or who have acute coronary syndrome (ACS; blockage of blood flow to the heart). The main objective of the present study was to the preformulation studies were performed to know the development of formulation and evaluation of Ticagrelor Orodispersible Tablets to improve the bioavailability of Ticagrelor which shows 36%, Ticagrelor is classified as a biopharmaceutics classification system (BCS) class IV drug with highly lipophilic having poor aqueous solubility and permeability increasing the solubility, improve the bioavailability and onset of action Ticagrelor has been done. In API development process, a detailed characterization of the API and other formulation componentsis usually carried out during the preformulation stage. The drug-excipient compatibility studies were conducted to characterize the drug Ticagrelor present in Orodispersible Tablets Delivery System ODTs. Preformulation, formulation and evaluation of Ticagrelor to avoid problems associated with conventional delivery system such as limited permeation, low dissolution and bioavailability and also to improve bioavailability and one of the most recent antiplatelet agents. In the present study that the compatibility was assessed by, FTIR spectroscopy, and melting point apparatus, precompression parameters and powder flow properties. Results showed that physical mixtures of Ticagrelor and various excipients as mannitol, and avicel PH 102 as diluents, and sodium starch glycolate, croscarmellose sodium, and crospovidone as superdisintegrants and sodium lauryl sulfate as wetting agent were evaluated for preformulation studies parameters. It was concluded that the drug Ticagrelor was found to be compatible with various excipients which were selected for the formulation development of the Ticagrelor ODTs. Formulation scientist from his experience and knowledge have to significantly in the preformulation study stage and is an important factor in the ADDS (Advanced Drug Delivery Systems) product development process.

Keywords: Ticagrelor, Compatibility, Excipients, Development, Preformulation, Formulation, Antiplatelet agents.