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A quick-acting and safe ticagrelor oral spray and preparation method thereof

A technology of oral spray and ticagrelor, which is applied in the field of ticagrelor oral spray and its preparation, to achieve the effect of stable dispersion system, good taste and stability, and convenient taking

Active Publication Date: 2022-04-22
HEFEI IND PHARMA INST CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] At present, there are no relevant patents and literature reports on ticagrelor spray formulations at home and abroad

Method used

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  • A quick-acting and safe ticagrelor oral spray and preparation method thereof
  • A quick-acting and safe ticagrelor oral spray and preparation method thereof
  • A quick-acting and safe ticagrelor oral spray and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Example 1: Effect of Particle Size of Ticagrelor API on Solubilization Effect

[0037] The raw material of ticagrelor was micronized using a jet mill, and the results are shown in Table 1. The measurement results showed that micronizing the raw material was helpful to improve the solubility of ticagrelor, but adding a solubilizer was still needed to further improve the solubility. where, * indicates D compared with the particle size of 20 μm 90 There was a significant difference in the solubility of ticagrelor at ≤10 μm.

[0038] Table 1 The influence of the particle size of raw materials on the solubilization effect of ticagrelor

[0039] API Particle Size solvent Solubility (mg / mL) D. 90 :20μm

Embodiment 2

[0040] Embodiment 2: prepare the product of different particle size, solubility

[0041] Table 2 Product Prescription Form

[0042]

[0043]

[0044] Preparation method: a. Add RC-591 microcrystalline cellulose-carboxymethyl cellulose sodium into purified water under stirring, and stir well until the swelling is complete; b. Micronize the raw material drug to a suitable particle size Adding a wetting agent and a transdermal absorption-promoting agent to the powder and fully stirring to obtain a stable and uniform raw material drug mixture; c. Adding the colloid solution obtained in step a to step b and fully stirring to obtain a stable and uniform dispersion system; d .Add taste regulator, pH regulator and other auxiliary materials to the uniform dispersion system obtained in step c, fully stir and adjust the pH to between 5.0 and 9.0; obtain the drug-containing solution, and fill the drug-containing solution, Promptly obtain described ticagrelor oral spray.

[0045] T...

Embodiment 3

[0046] Embodiment 3: pharmacokinetic animal experiment

[0047] In vivo absorption experiments were carried out on the prepared seven products. Test method is as follows: get 45 beagle dogs fasting, be divided into 9 groups, every group of 5: one group is given normal saline gavage (negative control), one group is given commercially available tablet (trade name: ) orally (positive control), and the other seven groups were given seven product sprays in Table 3 respectively. Oral group given Tablet 90mg, experimental group oral administration spray 30mg / spray, totally 3 sprays. When spraying, fix the dog's head to keep the mouth level, spray the drug quantitatively into the mouth, and keep the dog's head in a horizontal position for more than 1 minute after administration to prevent the liquid from flowing out. There must be an appropriate interval after administration of each dosage form to ensure sufficient time for blood collection.

[0048] Before administration (0h) and...

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Abstract

The invention belongs to the field of pharmaceutical preparations, and in particular relates to a quick-acting and safe ticagrelor oral spray and a preparation method thereof, which comprises an active ingredient ticagrelor, a suspending agent, a wetting agent, a taste regulator and a pharmaceutically acceptable Other excipients, characterized in that the content of ticagrelor is 5% to 15% (w / v), the solubility is at least 0.02 mg / mL, and the particle size of insoluble crystals is D 90 ≤10μm. The oral spray solves the problem of achieving consistent exposure in the body under the same dosage as the tablet () and through different administration routes, and T max 1.0~1.5h≤tablet 1.5h, rapid onset of action ensures the efficacy and safety of the drug.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a quick-acting and safe ticagrelor oral spray and a preparation method thereof. Background technique [0002] Studies have shown that coronary arteriosclerosis accounts for 22.3% of the global causes of death, much higher than cancer and AIDS. Among them, acute coronary syndrome (ACS) is a serious type of coronary heart disease, and patients often present with paroxysmal chest pain, Symptoms such as chest tightness can lead to sudden death and seriously affect the quality of life and longevity of patients. [0003] Ticagrelor, whose chemical structural formula is: [0004] [0005] Ticagrelor is a direct-acting, reversibly binding P2Y12 platelet inhibitor, which belongs to a new type of anti-platelet drug. Compared with clopidogrel, it does not need to be activated by liver metabolism, and has the characteristics of faster and more potent inhibition of p...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/12A61K47/10A61K47/38A61K31/519A61P7/02A61P9/10
CPCA61K9/006A61K47/10A61K47/38A61K31/519A61P7/02A61P9/10A61K9/12
Inventor 何广卫刘为中陈娟娟苏峰王奎李颖
Owner HEFEI IND PHARMA INST CO LTD
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