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Immune System Diseases

Respiratory Diseases

Small molecule drug

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Disease Domain	Count

Immune System Diseases	1

Top 5 Drug Type	Count

Small molecule drug	1

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CysLT x CysLT1	1

BACKGROUNDStatins are the first-line therapy for lowering high lipid levels. Atorvastatin calcium (AtC) is the most commonly prescribed statin. It inhibits 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase which converts HMG-CoA into mevalonic acid, a cholesterol precursor.OBJECTIVETo compound and evaluate the stability of AtC suspension (0.4% w/v) using commercial tablets or pure AtC powder as the source of the active pharmaceutical ingredient.METHODSeveral AtC suspension formulations were produced using commercial AtC tablets or AtC pure powder as the source of the active ingredient. The most suitable one in terms of general organoleptic properties and dissolution was selected for stability studies. For this purpose, samples of final suspensions were stored at room temperature and in the refrigerator. Assay, pH, organoleptic properties and microbial contamination were evaluated according to the USP specifications. High performance liquid chromatography was used for the analysis and quantification of AtC in the studied samples.RESULTSThe obtained suspension (S4) had good organoleptic properties. It showed complete dissolution of AtC within 30 min. However, the suspension prepared from crushed tablet (S_t4) showed a better dissolution profile than that prepared from pure powder (S_p4). The prepared formula had unchanged pH, which remained around 9.9. S_t and S_p formulas were both free from microbial contamination. Both products showed good stability within at least the period of use of the 100 mL AtC bottles.CONCLUSIONSAtC extemporaneous suspension was successfully prepared using tablets as a source of AtC or pure AtC powder. However, S_t4 had a better dissolution profile than S_p4. This study provides a solution for patients with swallowing difficulties or feeding tubes who are unable to take medicines in solid oral dosage forms. Community pharmacists can prepare the suspension using AtC tablets as the source of the active ingredient.

International Journal of NanomedicineQ2 · MEDICINE

<p>Strategic approach to developing a self-microemulsifying drug delivery system to enhance antiplatelet activity and bioavailability of ticagrelor</p>

Q2 · MEDICINE

ArticleOA

Author: Kim, Sung-Jin ; Wang, Miao ; Huh, Hyun Wook ; Lee, Hong-Ki ; Jeon, Sung-Hoon ; Byeon, Jin-Ju ; Son, Gi-Ho ; Cho, Cheong-Weon ; Bang, Ki-Hyun ; Lee, Hye-Jin ; Na, Young-Guk

BACKGROUNDTicagrelor (TCG) is used to inhibit platelet aggregation in patients with acute coronary syndrome, but its poor solubility and low bioavailability limit its in vivo efficacy. The purpose of this study was to manufacture an optimized TCG-loaded self-microemulsifying drug delivery system (SMEDDS) to enhance the oral bioavailability and antiplatelet activity of TCG.MATERIALS AND METHODSSolubility and emulsification tests were conducted to determine the most suitable oils, surfactants, and cosurfactants. Scheffé's mixture design was applied to optimize the percentage of each component applied in the SMEDDS formulation to achieve optimal physical characteristics, ie, high solubility of TCG in SMEDDS, small droplet size, low precipitation, and high transmittance.RESULTSThe optimized TCG-loaded SMEDDS (TCG-SM) formulation composed of 10.0% Capmul MCM (oil), 53.8% Cremophor EL (surfactant), and 36.2% Transcutol P (cosurfactant) significantly improving the dissolution of TCG in various media compared with TCG in Brilinta^® (commercial product). TCG-SM exhibited higher cellular uptake and permeability in Caco-2 cells than raw TCG suspension. In pharmacokinetic studies in rats, TCG-SM exhibited higher oral bioavailability with 5.7 and 6.4 times higher area under the concentration-time curve and maximum plasma concentration, respectively, than a raw TCG suspension. Antiplatelet activity studies exhibited that the TCG-SM formulation showed significantly improved inhibition of platelet aggregation compared with raw TCG at the same dose of TCG. And, a 10 mg/kg dose of raw TCG suspension and a 5 mg/kg dose of TCG-SM had a similar area under the inhibitory curve (907.0%±408.8% and 907.8%±200.5%⋅hours, respectively) for antiplatelet activity.CONCLUSIONThese results suggest that the developed TCG-SM could be successfully used as an efficient method to achieve the enhanced antiplatelet activity and bioavailability of TCG.

100 Deals associated with SAMA Pharma Co. Ltd.

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100 Translational Medicine associated with SAMA Pharma Co. Ltd.

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Pipeline

Pipeline Snapshot as of 23 Dec 2024

The statistics for drugs in the Pipeline is the current organization and its subsidiaries are counted as organizations,Early Phase 1 is incorporated into Phase 1, Phase 1/2 is incorporated into phase 2, and phase 2/3 is incorporated into phase 3

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