Ifenprodil tartrate freeze-dried powder injection and preparation method thereof

A technology of ifenprodil tartrate and freeze-dried powder injection, which is applied in the field of ifenprodil tartrate freeze-dried powder injection and its preparation, which can solve the problems of easy oxidation, substance increase, high-heat instability, etc., to improve stability, Good stability and high quality effect

Inactive Publication Date: 2011-07-27
BEIJING SIHUAN KEBAO PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Although the injection can avoid the first-pass metabolic effect after oral administration, because its structure contains phenolic hydroxyl groups, it can complex with heavy metal ions to develop color, and it is easy to oxidize when exposed to air; it is unstable to high heat; so in the injection During the production process, it is necessary to add antioxidants or pass isolation gas to prevent ifenprodil tartrate from being oxidized, and related substances increase significantly after sterilization

Method used

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  • Ifenprodil tartrate freeze-dried powder injection and preparation method thereof
  • Ifenprodil tartrate freeze-dried powder injection and preparation method thereof
  • Ifenprodil tartrate freeze-dried powder injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

experiment example 1

[0042] Experimental Example 1 Prescription Screening Experiment

[0043] Using mannitol, lactose, dextran, maltose, and glycine as excipients, weigh the main ingredients and excipients as shown in Table 1, and prepare freeze-dried powder injections according to the following preparation methods. , main drug content and related substances are the evaluation indicators, respectively investigate the formability of ifenprodil tartrate freeze-dried powder injection, the results are shown in Table 1:

[0044] The preparation method of freeze-dried powder injection is as follows:

[0045] ①Weigh the prescribed amount of ifenprodil tartrate and excipients, add 90% of the prescribed amount of water for injection to dissolve at 50°C, add 0.03% (g / ml) of activated carbon for needle adsorption for 30min, add water for injection to the full amount, filter to remove carbon;

[0046] ② Check the pH value and content of the filtrate, calculate the filling volume, filter the solution through...

experiment example 2

[0062] Experimental example 2 preparation process research

[0063] 1. Effect of activated carbon dosage and decarbonization method on main drug content and related substances

[0064] Activated carbon for needles is used in the preparation of injections to adsorb heat sources, impurities and pigments in raw and auxiliary materials to improve product quality; but if the amount is too large, it will adsorb the main drug to reduce the content of the main drug or introduce other impurities into the finished preparation. The decarbonization method in the liquid preparation process will have a certain impact on the related substances of this product, so the amount of activated carbon and the decarburization method are screened and studied with the content of the main drug and related substances as the assessment indicators.

[0065] Table 3 Effects of activated carbon dosage and decarbonization method on the main drug content and related substances

[0066]

[0067]

[0068]...

Embodiment 1

[0085]

[0086] ① Weigh the prescribed amount of mannitol and add about 90% water for injection, stir to dissolve it, add 0.05% (g / ml) activated carbon for needles into the solution, absorb for 30 minutes, filter and decarbonize;

[0087] ② Add the prescribed amount of ifenprodil tartrate raw material to the filtrate (temperature controlled at 50°C), stir to dissolve completely, cool down to room temperature, and add water for injection to the full amount;

[0088] ③ Check the pH value and content of the solution, calculate the filling volume, filter the solution through a 0.22 μm microporous membrane, and fill it;

[0089] ④ Freeze drying:

[0090] a. Turn on the cooling of the front box to reduce the temperature of the product to about -40°C and keep it for 2 to 3 hours;

[0091] b. Turn on the cooling of the rear box to reduce the temperature of the condenser to about -50°C;

[0092] c. Evacuate the vacuum of the freeze-drying box to below 10Pa;

[0093] d. One-time s...

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Abstract

The invention discloses an ifenprodil tartrate freeze-dried powder injection, and belongs to the technical field of medicine. The ifenprodil tartrate freeze-dried powder injection comprises the following raw materials: 2 to 10 weight parts of ifenprodil tartrate (C21H27NO2)2.C4H6O6 and 20 to 200 weight parts of excipients. The invention also discloses a preparation method of the freeze-dried powder injection. The ifenprodil tartrate freeze-dried powder injection prepared by the method only contains the excipients required by the freeze-dried powder injection, so that possible adverse reaction caused by the addition of other auxiliary materials is avoided. Besides, the ifenprodil tartrate freeze-dried powder injection is high in stability and convenient to store and transport.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a freeze-dried powder injection of ifenprodil tartrate and a preparation method thereof. Background technique [0002] Ifenprodil Tartrate (Ifenprodil Tartrate), also known as benzphenamine tartrate, chemical name: (1RS, 2RS)-2-(4-benzylpiperidinyl)-1-(4-hydroxyphenyl)-1 -Propanol-(2R,3R)-hemitartrate hemihydrate. It is a new type of selective NMDA receptor antagonist, and its effect is highly selective , to avoid adverse reactions of non-selective NMDA receptor antagonist drugs, so it has a high degree of safety. Long-term pharmacology, toxicology and clinical trials have proved that it has good therapeutic effect and low toxicity, and it is a drug with good market prospect. [0003] Ifenprodil tartrate has the effect of dilating blood vessels, it is mainly used for the treatment of mental depression symptoms related to insufficient cerebral blood supply; the treatm...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K31/445A61P9/10A61P25/00
Inventor 张建强李海冰马月梅吴王民
Owner BEIJING SIHUAN KEBAO PHARM CO LTD
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