Unlock instant, AI-driven research and patent intelligence for your innovation.

Composition capable of eliminating clouding formation phenomenon of TPGS and application thereof in medicinal preparation

A composition and phenomenon technology, applied in the directions of non-active ingredient medical preparations, active ingredients-containing medical preparations, pharmaceutical formulas, etc., can solve the problems of discount of application prospects, scrapped preparations, and loss of human, material and financial resources of enterprises

Inactive Publication Date: 2014-05-21
SHENYANG PHARMA UNIVERSITY
View PDF3 Cites 1 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] In the case of large-scale industrial production, the serious consequences that may be caused by the phenomenon of TPGS flashing are: a batch or even several batches of injections that use TPGS as a solubilizer are being sterilized At the same time, the scrapping of the preparation due to the occurrence of the disease not only caused multiple unnecessary losses in manpower, material resources, and financial resources of the enterprise, but also led to the uncontrollability of the process in the preparation process of TPGS-related sterilization preparations and the randomness of qualified 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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Composition capable of eliminating clouding formation phenomenon of TPGS and application thereof in medicinal preparation
  • Composition capable of eliminating clouding formation phenomenon of TPGS and application thereof in medicinal preparation
  • Composition capable of eliminating clouding formation phenomenon of TPGS and application thereof in medicinal preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

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

[0033] Prescription 1:

[0034]coenzyme Q 10 75mg

[0035] TPGS 600mg

[0036] Water for injection 28 mL

[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 min, dilute to 30 mL with water for injection, pass through a 0.22 μm microporous membrane, aliquot, and fill with nitrogen , stoppered, sealed with an aluminum cap, half of the preparation was sterilized at 100°C for 30 minutes, and the other half was sterilized at 121°C for 8 minutes.

[0041] Observe...

Embodiment 2

[0043] Example 2 : Coenzyme Q without flashing phenomenon solubilized by TPGS 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 phase...

Embodiment 3

[0051] Example 3: Coenzyme Q without sparkle solubilized by TPGS 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 dissolved,...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention relates to a composition capable of eliminating HS15 clouding formation phenomenon of TPGS (tocopheryl polyethylene glycol succinate), which comprises an insoluble drug, TPGS, polyethylene oxide-polypropylene oxide copolymer, a polyhydroxylated compound and water, wherein the weight ratio of insoluble drug to TPGS to polyethylene oxide-polypropylene oxide copolymer to the polyhydroxylated compound is (0.001-2):1:(0.5-5):(2-20), and the rest is water. When the composition is used for preparing injection of common insoluble drug, the obtained preparation can bear sterilization at 100DEG C for 30 min and 121 DEG C for 8 min without clouding formation, so as to ensure the controllability of the entire preparation process and avoid negative results arising from clouding formation phenomenon during sterilization of the preparation. The composition disclosed by the invention eliminates the clouding formation phenomenon of TPGS, and solves the serious problem when TPGS is applied in 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 researc...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): A61K47/44A61K47/34A61K31/122
Inventor 邓意辉程晓波王春玲王宇付强
Owner SHENYANG PHARMA UNIVERSITY