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Composition capable of eliminating tpgs twilight phenomenon and its application in pharmaceutical preparations

A composition and phenomenon technology, which is applied in the directions of non-active ingredients medical preparations, medical preparations containing active ingredients, pharmaceutical formulas, etc., can solve the problem of preparation scrap, discount of application prospects, uncontrollable process randomness of qualified preparations, etc. question

Inactive Publication Date: 2016-02-10
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] If it is in large-scale industrial production, the serious consequences that may be caused by the phenomenon of TPGS clouding are: when a batch or even several batches of injections that use TPGS as a solubilizer are sterilized, the preparations will be scrapped due to clouding, which will not only cause labor costs for the enterprise. Multiple unnecessary losses of material resources, financial resources, etc., and also lead to uncontrollable process and randomness of qualified preparations in the preparation process of TPGS-related sterilization preparations
[0011] In addition, the serious consequences that may be caused by the phenomenon of TPGS clouding are that its application prospect is greatly reduced

Method used

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  • Composition capable of eliminating tpgs twilight phenomenon and its application in pharmaceutical preparations
  • Composition capable of eliminating tpgs twilight phenomenon and its application in pharmaceutical preparations
  • Composition capable of eliminating tpgs twilight phenomenon and its application in pharmaceutical preparations

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Example 1: Coenzyme Q solubilized with TPGS alone 10 Preparation of Injection

[0033] Prescription 1:

[0034] coenzyme Q 10 75mg

[0035] TPGS600mg

[0036] Water for injection 28mL

[0037]

[0038] 30mL

[0039] Process:

[0040] Weigh the prescribed amount of coenzyme Q 10 , TPGS to form the oil phase; measure the prescribed amount of water for injection as the water phase, and heat the two phases to 55°C respectively. After the substances in the oil phase are completely dissolved, under the condition of magnetic stirring, slowly add the water phase into the oil phase, continue to stir for 20 minutes, dilute to 30mL with water for injection, pass through a 0.22μm microporous membrane, subpackage, fill with nitrogen, and stopper , sealed with an aluminum cap, half of the preparation is sterilized at 100°C for 30 minutes, and the other half is sterilized at 121°C for 8 minutes.

[0041] Observe the state of the preparation before sterilization: the obtained...

Embodiment 2

[0043] Example 2: Coenzyme Q Solubilized with TPGS without Sudden Phenomenon 10 Preparation of injections (fixed TPGS: F68=1:1(m / m), polyol selection of different amounts of propylene glycol)

[0044] prescription:

[0045]

Prescription 2 Prescription 3 Prescription 4 Prescription 5 Prescription 6 Prescription 7 coenzyme Q 10 75mg 75mg 75mg 75mg 75mg 75mg TPGS 600mg 600mg 600mg 600mg 600mg 600mg F68 600mg 600mg 600mg 600mg 600mg 600mg Propylene Glycol 1800mg 2400mg 3000mg 3600mg 4800mg 6000mg Water for Injection Add to 30ml Add to 30ml Add to 30ml Add to 30ml Add to 30ml Add to 30ml

[0046] Process:

[0047] Weigh the prescribed amount of coenzyme Q 10 , TPGS to form the oil phase; take the prescribed amount of F68, propylene glycol and water for injection as the water phase, and heat the two phases to 55°C respectively. After the substances in the two phases are...

Embodiment 3

[0051] Example 3: Coenzyme Q Solubilized with TPGS without Sudden Phenomenon 10 Preparation of injections (fixed TPGS: F68=1:3(m / m), polyol selection of different amounts of glycerol)

[0052] prescription:

[0053]

Prescription 8 Prescription 9 Prescription 10 Prescription 11 Prescription 12 Prescription 13 coenzyme Q 10 75mg 75mg 75mg 75mg 75mg 75mg TPGS 600mg 600mg 600mg 600mg 600mg 600mg F68 1800mg 1800mg 1800mg 1800mg 1800mg 1800mg glycerin 1800mg 2400mg 3000mg 3600mg 4800mg 6000mg Water for Injection Add to 30ml Add to 30ml Add to 30ml Add to 30ml Add to 30ml Add to 30ml

[0054] Process:

[0055] Weigh the prescribed amount of coenzyme Q 10 , TPGS to form the oil phase; take the prescribed amount of F68, glycerin and water for injection as the water phase, and heat the two phases to 55°C respectively. After the substances in the two phases are completely d...

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PUM

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Abstract

The present invention is a composition capable of eliminating TPGS twilight phenomenon and its application in pharmaceutical preparations. It includes insoluble drug, TPGS, polyoxyethylene polyoxypropylene copolymer and / or polyoxyethylene castor oil polyol and water, in which insoluble drug: TPGS: polyoxyethylene polyoxypropylene copolymer: polyol The weight ratio is 0.001-2:1:0.5-5:2-20, and the balance is water. When this combination is used in the preparation of common poorly soluble drug injections, the resulting preparation can withstand 100°C, 30min and 121°C8? Min sterilization, without seeing the phenomenon of clouding, ensures the controllability of the whole preparation process, the combination disclosed by the invention eliminates the phenomenon of clouding of TPGS, and solves the serious problem existing in the application of TPGS in large-scale industrial production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a combination capable of eliminating TPGS flash phenomenon and its application in pharmaceutical preparations. Background technique [0002] α-tocopheryl polyethylene glycol (PEG) 1000 succinate, or TPGS, is obtained from the esterification reaction of α-tocopheryl succinate and PEG1000, containing tocopheryl lipophilic groups and polyethylene glycol long chains The hydrophilic group is a non-ionic surfactant that has been listed in the United States Pharmacopoeia. Its average molecular weight is about 1513, and its structural formula is as follows: [0003] [0004] TPGS was first produced and marketed by Eastman Company of the United States in 1950. It was discovered in 1960 that it could be used as a solubilizer, and then reports on its toxicity and safety also appeared. In the 1980s, TPGS was used to treat tocopherol deficiency. After that, more and more research...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/44A61K47/34A61K31/122
Inventor 邓意辉商磊程晓波王春玲王宇付强
Owner SHENYANG PHARMA UNIVERSITY