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Netilmicin sulfate lyophiled powder injection and preparation method thereof

A technology of netilmicin sulfate and freeze-dried powder injection is applied in freeze-dried delivery, powder delivery, pharmaceutical formulation and other directions, which can solve the problems of large amount of excipients, complicated preparation methods, hidden safety hazards of injection drugs, etc., and reduce irritation. and toxic and side effects, improve drug stability, improve bioavailability

Active Publication Date: 2012-07-04
WUHAN PUSHENG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The patented nanomicelle encapsulates netilmicin sulfate in the hydrophobic core and administers it intravenously in the form of a nanomicelle freeze-dried preparation. Although the stability of the preparation is increased, the amount of excipients added during the preparation process is too large. Bringing safety hazards to injecting drugs
On the other hand, the preparation method of this patent is relatively complicated, the preparation cost is high, and the solution ratio is not satisfactory. For example, the total amount of substances added in Example 2 reaches 4310g, and the amount of solvent required is too large. Calculated based on the total amount of substances added, insoluble freeze-dried
According to the principle of freeze-drying, this method cannot obtain the target product in industrial production, and is not suitable for large-scale industrial production. At the same time, the micelles themselves are micellar substances and macromolecular substances, which are not conducive to the effective utilization of drugs.

Method used

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  • Netilmicin sulfate lyophiled powder injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Recipe: Netilmicin Sulfate 100g

[0022] Bletilla striata polysaccharide 75g

[0023] Sodium carbonate 0.5g

[0024] Makes 1000 bottles

[0025] Preparation:

[0026] (1) Preparation: Routinely handle the pipes and containers used for dosing, and then wash them with water for injection; the vials and rubber stoppers should be roughly washed and then rinsed, then dried, sterilized, and cooled for later use.

[0027] (2) Liquid preparation: first weigh the prescribed amount of Bletilla striata polysaccharide, add 800ml of water for injection to make a 40% solution, add netilmicin sulfate and 1200ml of water for injection, stir until the whole amount is dissolved.

[0028] (3) Decolorization: add medicinal charcoal with 0.1% of the total volume of the solution, stir and absorb at room temperature for more than 30 minutes to obtain a suspension of netilmicin sulfate, take a sample, measure the pH value of the liquid, add sodium carbonate to adjust the pH to...

Embodiment 2

[0033] Recipe: Netilmicin Sulfate 100g

[0034] β-cyclodextrin 85g

[0035] Sodium bicarbonate 0.6g

[0036] Makes 1000 bottles

[0037] Preparation:

[0038] (1) Preparation: Routinely handle the pipes and containers used for dosing, and then wash them with water for injection; the vials and rubber stoppers should be roughly washed and then rinsed, then dried, sterilized, and cooled for later use.

[0039] (2) Dosing: first weigh the prescribed amount of β-cyclodextrin, add 800ml of water for injection to make a 40% solution, add netilmicin sulfate and 1200ml of water for injection, stir until the whole amount is dissolved.

[0040] (3) Decolorization: add 0.1% of the total volume of medicinal charcoal in the solution, stir and absorb at room temperature for more than 30 minutes to obtain a suspension of netilmicin sulfate, take a sample, measure the pH value of the liquid, add sodium bicarbonate to adjust the pH to 5.0 , the measured content was 48.7mg / ml....

Embodiment 3

[0045] Recipe: Netilmicin Sulfate 100g

[0046] Urea 90g

[0047] Ammonia 0.8g

[0048] Makes 1000 bottles

[0049] Preparation:

[0050] (1) Preparation: Routinely handle the pipes and containers used for dosing, and then wash them with water for injection; the vials and rubber stoppers should be roughly washed and then rinsed, then dried, sterilized, and cooled for later use.

[0051] (2) Dosing: first weigh the prescribed amount of urea, add 900ml of water for injection to make a 45% solution, add netilmicin sulfate and 1100ml of water for injection, stir until the full amount is dissolved.

[0052] (3) Decolorization: Add 0.3% medicinal charcoal in the total volume of the solution, stir and adsorb at room temperature for more than 30 minutes to obtain a suspension of netilmicin sulfate, take a sample, measure the pH value of the liquid, add ammonia water to adjust the pH to 5.3, and measure The content is 49.2mg / ml.

[0053] (4) Filtration and subpackagi...

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Abstract

The invention discloses netilmicin sulfate lyophiled powder injection and a preparation method of the netilmicin sulfate lyophiled powder injection. Netilmicin sulfate and additives are added with water to be prepared into netilmicin sulfate injectable suspension, and the netilmicin sulfate lyophiled powder injection is obtained through freeze drying, wherein the additives are inclusion moleculesand pH conditioning agents, the inclusion molecules are selected from bletilla striata polysaccharide, beta-cyclodextrin, urea, thiourea, beta-cyclodextrin derivatives, deoxycholic acid and starch, and the pH conditioning agents are selected from sodium carbonate, sodium bicarbonate, ammonia water, sulfuric acid and phosphoric acid. Required auxiliary materials are few, the preparation process issimple, the freeze drying process is particularly screened and optimized, and the netilmicin sulfate lyophiled powder injection and the preparation method has the characteristics that the stability is high, the biological availability is high, the production cost is low, the quality is safe and reliable, and the like.

Description

technical field [0001] The invention belongs to a pharmaceutical preparation, and in particular relates to the preparation of netilmicin sulfate freeze-dried powder for antibiotic injection by using clathrate technology and a preparation method thereof. Background technique [0002] Netilmicin Sulfate, NTM is a new generation of semi-synthetic aminoglycoside antibiotics introduced in 1994, which works by inhibiting the normal protein synthesis of sensitive microorganisms. It is mainly used for infections in the respiratory tract, digestive tract, genitourinary system, skin and soft tissue, bone and joints, abdominal cavity and other parts caused by Gram-negative bacteria such as Escherichia coli, Klebsiella, Proteus, and Enterobacter. It has a strong effect on drug-resistant bacteria and β-lactam-resistant bacteria, and has become the drug of choice for clinical application indications of aminoglycosides. Netilmicin sulfate is not easy to absorb when taken orally, but it is...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K31/7036A61P31/04
Inventor 刘浏刘昔平徐林华陈葵祖梅媛陈杰枫王萍
Owner WUHAN PUSHENG PHARMA
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