Linezolid oral suspension and preparation method theroef

An oral suspension, linezolid technology, applied in the directions of liquid delivery, pharmaceutical formulation, emulsion delivery, etc., can solve the inconvenience of clinical medication, the difficulty of dividing linezolid into doses, and the inconvenience of divided doses or divided doses of oral solid preparations. Accuracy and other issues to achieve the effect of good physical and chemical compatibility

Active Publication Date: 2016-08-17
CHONGQING HUAPONT PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is still the problem that children need to give linezolid according to body weight and it is difficult to divide the dose; in addition, even if the orally disintegrating tablet of the present invention is fast, it needs to go through the process of disintegrating in a solid state and then dispersing to exert its drug effect. Compared with liquid preparations, its Disintegration and efficacy are still slow
In addition, the present invention uses freeze-drying method to prepare tablets, which requires special freeze-drying equipment, long and complicated process cycle, and high manufacturing cost. The main drug specification of linezolid itself is relatively large. For example, the main drug specification of the marketed oral tablet is 0.6g. The high cost of raw materials, coupled with high manufacturing costs, will inevitably increase the financial burden on patients
[0014] Due to the characteristics of carrying large-capacity injections, inconvenient clinical medication, poor patient compliance, and difficult or inaccurate dosage of oral solid preparations, it is currently necessary to develop a preparation that is convenient to take, easy to divide and accurate in dosage

Method used

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  • Linezolid oral suspension and preparation method theroef
  • Linezolid oral suspension and preparation method theroef
  • Linezolid oral suspension and preparation method theroef

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0068] Example 1 Linezolid oral suspension formula 1 and preparation method

[0069] (1) Preparation prescription: (total made into 1000ml)

[0070]

[0071] (2) Preparation method:

[0072] 1) Weigh 4 / 5 of the prescription amount of purified water, add the prescription amount of suspending agent sodium carboxymethyl cellulose to it, heat to 80-100°C, stir to swell and clarify, and cool to room temperature to obtain solution I;

[0073] 2) Add the wetting agent polysorbate 80 to solution I, stir and dissolve it to obtain solution II;

[0074] 3) Add linezolid micropowder to solution II, homogenize at 5000 rpm and disperse for 5 minutes, mix well, and flocculate to obtain suspension III;

[0075] 4) Adding the pH regulators sodium citrate and citric acid to suspension Ⅲ to obtain suspension Ⅳ;

[0076] 5) Finally, add the prescription amount of preservative sodium benzoate, sweetener sorbitol and corrective cherry powder flavor to suspension IV, stir at 30Hz for 10min, after dissolving, ad...

Embodiment 2

[0077] Example 2 Linezolid oral suspension formulation 2 and preparation method

[0078] (1) Preparation prescription: (total made into 1000ml)

[0079]

[0080] (2) Preparation method:

[0081] 1) Weigh 4 / 5 of the prescription amount of purified water, add the prescription amount of suspending agent sodium carboxymethyl cellulose to it, heat to 80-100°C, stir to swell and clarify, and cool to room temperature to obtain solution I;

[0082] 2) Add the wetting agent polysorbate 80 to solution I, stir and dissolve it to obtain solution II;

[0083] 3) Add linezolid micropowder to solution II, homogenize at 5000 rpm and disperse for 8 minutes, mix and flocculate to obtain suspension III;

[0084] 4) Adding the pH regulators sodium citrate and citric acid to suspension Ⅲ to obtain suspension Ⅳ;

[0085] 5) Finally, add the prescription amount of preservative sodium benzoate, sweetener sorbitol and corrective cherry powder flavor to suspension IV, stir at 30Hz for 10min, after dissolving, add ...

Embodiment 3

[0086] Example 3 Linezolid oral suspension formulation 3 and preparation method

[0087] (1) Preparation prescription: (total made into 1000ml)

[0088]

[0089]

[0090] (2) Preparation method:

[0091] 1) Weigh 4 / 5 of the prescription amount of purified water, add the prescription amount of suspending agent sodium carboxymethyl cellulose to it, heat to 80-100°C, stir to swell and clarify, and cool to room temperature to obtain solution I;

[0092] 2) Add the wetting agent polysorbate 80 to solution I, stir and dissolve it to obtain solution II;

[0093] 3) Add linezolid micropowder to solution II, homogenize at 5000 rpm and disperse for 8 minutes, mix and flocculate to obtain suspension III;

[0094] 4) Adding the pH regulators sodium citrate and citric acid to suspension Ⅲ to obtain suspension Ⅳ;

[0095] 5) Finally, add the prescription amount of preservative sodium benzoate, sweetener sorbitol and corrective cherry powder flavor to suspension IV, stir at 30Hz for 10min, after dissolv...

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Abstract

The invention belongs to the field of pharmaceutic preparation, and specifically a linezolid oral suspension and a preparation method thereof. The linezolid oral suspension comprises the following components by weight: 0.5-2.0 parts of linezolid, 0.5-5.0 parts of sodium carboxymethyl cellulose, 0.05-0.5 part of polysorbate 80, 0.15-0.20 part of sodium citrate, 0.08-0.10 part of citric acid, 0.22-0.28 part of a preservative, 22-28 parts of sweetener, 1.2-1.8 parts of a correctant and an aqueous medium. The present invention fills the market blank of only containing tablet or injection, and provides a novel dosage form choice. The linezolid oral suspension product has good quality, can be accurately divided into the dosage based on body weight, and is easy to swallow. The preparation process is simple, feasible and reproducible, and can consistently produce linezolid oral suspension with quality meeting the requirements.

Description

Technical field [0001] The invention belongs to the field of pharmaceutical preparations, and specifically relates to a linezolid oral suspension and a preparation method thereof. Background technique [0002] Linezolid is the first new type of antibiotic to obtain marketing approval among the oxazolidinone compounds. It was developed by Upjohn. In 2000, the FDA approved its marketing for the treatment of gram-positive (G+) cocci. Infections, including suspected or confirmed hospital-acquired pneumonia (HAP), community-acquired pneumonia (CAP), complicated skin or skin and soft tissue infections (SSTI), and vancomycin-resistant enterococcus (VRE) infections caused by MRSA. [0003] Linezolid is a bacterial protein synthesis inhibitor that acts on the 50S ribosomal subunit of bacteria and is closest to the site of action. Unlike other drugs, linezolid does not affect the activity of peptidyl transferase, but acts on the initial stage of the translation system, inhibiting the connec...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K31/5377A61K47/38A61K47/12A61K47/34A61K47/26A61P31/04
CPCA61K9/0053A61K9/10A61K31/5377A61K47/12A61K47/26A61K47/38
Inventor 徐飞
Owner CHONGQING HUAPONT PHARMA
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