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Midazolam combination as well as preparation method and application thereof

A midazolam and composition technology, applied in the field of medicine and pharmacy, can solve problems such as unsatisfactory effect, and achieve the effects of good physical and chemical stability, reducing first-pass effect and high concentration

Active Publication Date: 2012-05-23
INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Compared with the pH value of adding acid and forming salt, it is still slightly acidic, and the effect is not satisfactory (Knoester, P.D., D.M.Jonker, et al.Pharmacokinetics and pharmacodynamics of midazolam administered as a concentrated intranasal spray.A study in healthy Volunteers. Br J Clin Pharmacol.2002.53(5):501-507.; Loftsson, T., H. Gudmundsdottir, et al. -40.)

Method used

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  • Midazolam combination as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Example 1: Preparation of midazolam composition sample 1

[0044] This product is a nasal spray (nasal spray) with a specification of 5mg / 100μL / spray (calculated as midazolam).

[0045] prescription:

[0046] Midazolam 5g

[0047] Propylene glycol: 40ml

[0048] Glycerin: 10ml

[0049] β-cyclodextrin 15g

[0050] Add water for injection to 100ml

[0051]

[0052] Preparation Process:

[0053] Accurately weigh 5g of midazolam and dissolve it in 30ml of propylene glycol. After fully dissolving, add 15ml of glycerin and an appropriate amount of β-CD aqueous solution, stir well or ultrasound to dissolve and mix, cool to room temperature and add water for injection to the full amount (add to 100ml). After the content determination is qualified, carry out sub-packaging. Thus, sample 1 of the midazolam composition was prepared. The pH of the preparation was measured with a pH meter to be 7.6.

[0054] Those skilled in the art can understand that although the...

Embodiment 2

[0055] Example 2: Preparation of midazolam composition sample 2

[0056] This product is a solution for the nasal cavity and is administered by dripping (nasal drops), with a specification of 50mg / ml (calculated as midazolam).

[0057] prescription:

[0058] Midazolam 5g

[0059] Propylene glycol: 60ml

[0060] Glycerin: 5ml

[0061] Hydroxypropyl-βcyclodextrin 21g

[0062] Add water for injection to 100ml

[0063]

[0064] Preparation Process:

[0065] Accurately weigh 5g of midazolam and dissolve it in 60ml of propylene glycol. After fully dissolving, add 5ml of glycerin and an appropriate amount of Hp-β-CD aqueous solution, stir well or ultrasound to dissolve and mix, cool to room temperature and add water for injection to the full amount ( Add to 100ml). After the intermediate content is qualified, it is divided into packaging. Thus, sample 2 of the midazolam composition was prepared. The pH of the preparation was determined to be 7.8.

[0066] Those ...

Embodiment 3

[0067] Example 3: Preparation of midazolam composition sample 3

[0068] This product is a solution that is administered through the nasal route, and the concentration of the solution is 50mg / ml (calculated as midazolam).

[0069] prescription:

[0070] Midazolam maleate 6.8g

[0071] Propylene glycol: 50ml

[0072] β-cyclodextrin 5g

[0073] Add water for injection to 100ml

[0074]

[0075] Note: In the above prescription, the main medicine used is midazolam maleate, 6.8g midazolam maleate, which is equivalent to 5g midazolam. Since different salt types are involved, in order to facilitate the measurement and comparison of the concentration of different solutions, the free midazolam is uniformly converted to express the drug concentration. In other words, in this prescription, the concentration of the solution is still 50mg / ml (in midazolam).

[0076] Preparation Process:

[0077] Accurately weigh 6.8g of midazolam maleate and dissolve it in 50ml of propy...

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Abstract

The invention belongs to the field of medicines and pharmaceutics, and relates to a midazolam combination, a preparation method of the midazolam combination, and the application of the midazolam combination. Specifically, the midazolam combination comprises 2.5 to 8.0 percent (g / ml) of midazolam, 5 to 30 percent (g / ml) of cyclodextrin and 30 to 80 percent (ml / ml) of polyols through being calculated according to the total volume of the midazolam combination, wherein the cyclodextrin is carefully selected from one or more of beta cyclodextrin, hydroxypropyl-beta cyclodextrin, gamma cyclodextrin, dimethyl beta cyclodextrin, trimethyl beta cyclodextrin, hydroxypropyl beta cyclodextrin and HE-beta cyclodextrin; and the polyols are selected from one or more of propylene glycol, glycerol, polyoxyethylene castor oil and polyethylene glycol. The concentration of the midazolam in the combination can reach above 25mg / ml and the pH (potential of hydrogen) value of the midazolam is between 4.5 and 10.0. The invention additionally relates to the preparation method of the combination and the application of the combination during the preparation of medicines for curing epilepsy and achieving the effects of anti-anxiety, sedation, peaceful sleeping, muscular relaxation or anti-convulsion.

Description

Technical field [0001] The invention belongs to the field of medicine and pharmacy, and relates to a midazolam composition, its preparation method and application. Background technique [0002] Midazolam (Midazolam) is a benzodiazepine derivative, which has anti-anxiety, sedation, sleeping, muscle relaxation and anticonvulsant effects. Studies have found that midazolam at an appropriate dose has good anti-epileptic effects and can be used for the treatment of acute epilepsy and febrile seizures or for the acute treatment of epileptic seizures in patients with epilepsy (Minagawa, K. and S. Yanai.Efficacy of continuous intravenous infusion of midazolam in the treatment of status epilepticus in children. No To Hattatsu. 1998.30(4): 290-294.). [0003] Clinically, midazolam medicine has two dosage forms: tablet and injection. Midazolam is absorbed rapidly after oral administration, and its plasma concentration reaches its peak value in 1 / 2 to 1 hour. However, because it is mainly oxi...

Claims

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Application Information

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IPC IPC(8): A61K31/5517A61K47/40A61P25/08A61P25/22A61P25/20A61P21/02
Inventor 郑爱萍张晓燕毕芸祺孙建绪
Owner INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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