Terbutaline impulse formulation and preparation method thereof

A terbutaline and pulse technology, applied in the field of terbutaline pulse preparation and its preparation, can solve the problems of increasing adverse reactions, affecting sleep, waste and the like

Inactive Publication Date: 2008-12-10
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, since the disease symptoms of asthma patients often appear or intensify in the early morning, the patients are generally still in a sleep state at this time, and usually cannot take medicine in time to prevent the onset of the disease or relieve symptoms, thereby seriously affecting normal sleep; In order to ensure that the blood drug concentration in the early morning reaches the effective blood drug concentration, it is necessary to increase the dose of the drug taken, which not only causes waste but also increases the risk of adverse reactions

Method used

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  • Terbutaline impulse formulation and preparation method thereof
  • Terbutaline impulse formulation and preparation method thereof
  • Terbutaline impulse formulation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Recipe 1:

[0050]

[0051] 100 pieces

[0052] Take terbutaline sulfate, mannitol, and L-HPC to pass through a 80-mesh sieve, and mix evenly; take starch, add 10 mL of water to boil, let it cool to make starch slurry, add mixed raw and auxiliary materials to prepare soft materials, and pass through 16 mesh Sieve and granulate, dry at 65°C for 4 hours, granulate with 18 mesh, add magnesium stearate and mix. Use a 5.0mm shallow arc punch as a die, and press on a tablet press (TDP single-punch tablet press) to obtain a tablet core. Tablet weight 101mg, hardness 3.5±0.5kg.

[0053]

[0054] Suspend hydroxymethylcellulose, carnauba wax, talcum powder, and polyethylene glycol in 20mL of water to make a coating solution; place the tablet core in the coating pan, adjust the rolling coating pan (BY300A type coating pan) Coating pan) angle is 30 degrees, rotating speed is 30rpm, add the coating solution in the spray gun and spray it on t...

Embodiment 2

[0059] Recipe 2:

[0060]

[0061] 100 pieces

[0062] Take terbutaline sulfate, starch, PVPP and potassium chloride and pass through 80-mesh sieve respectively, mix well, take povidone k29 and dissolve in 10mL of ethanol, add mixed raw and auxiliary materials to make soft material, pass through 16-mesh sieve to granulate , dried at 65°C for 3 hours, granulated with 18 mesh, mixed with magnesium stearate. Use a 5.0mm shallow arc punch as a die, and press a tablet machine to obtain tablet cores. Tablet weight 102mg, hardness 4.5±0.5kg.

[0063]

[0064] Hydroxyethyl cellulose, ethyl cellulose, glycerol monostearate, triethyl citrate are dissolved in 50mL of ethanol to make coating solution; the tablet core is placed in a fluidized bed, and the airflow is introduced, The tablet core is in a fluidized state by the rapidly rising airflow, the coating liquid is input into the fluidized bed and atomized, so that a layer of coating material ...

Embodiment 3

[0067] Recipe 3:

[0068]

[0069] 100 pieces

[0070] Take terbutaline sulfate, microcrystalline cellulose PH101, CCNa, povidone k29, micropowder silica gel, and sorbitol and pass through 80-mesh sieve respectively, mix evenly, and use the method of powder direct compression, and use 5.0mm shallow arc punching Punching dies to make tablet cores. Tablet weight 102mg, hardness 3.5±0.5kg.

[0071]

[0072] Mix polyethylene glycol, beeswax, glycerin monostearate, glycerin triacetate and other components, heat and melt in a water bath at 65°C, mix well, cool slowly at room temperature to solidify, grind and pulverize ;Take 10.2mg of coating material and a piece of prepared tablet core, directly dry-press the coating on the tablet machine, the tablet weight is 112.2mg, the hardness is 5.5±0.5kg, and the weight gain of the coating is 10%, which is to make terbu sulfate Taline Pulse Tablets.

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Abstract

The invention discloses a terbutaline pulse preparation used for relieving asthma. The terbutaline pulse preparation comprises a tablet core containing the active ingredient of the terbutaline or the salt thereof and one or two coating layers. The tablet core is made by tabletting. Rollover coating in a coating pan, dry pressure coating or fluidized-bed coating is adopted for preparing the terbutaline pulse tablet, and the terbutaline pulse tablet can be further used for filling to prepare a terbutaline capsule. The time lag of the terbutaline preparation is controlled according to the weight increment and the proportion of the ingredients of the coating layer during the process of coating. The invention is designed by being based on the principles of chrono-pharmacology and chrono-therapeutics. If taken at bed-time, the ingredient of the terbutaline or the salt thereof can be released quickly at the preset time lag, thus preventing and relieving the clinical symptoms of asthma attacks quickly in a wee hour.

Description

technical field [0001] The present invention relates to a medicine for preventing and treating bronchial asthma, in particular to a terbutaline pulse preparation capable of preventing and treating bronchial asthma and a preparation method thereof. The pulse preparation includes a tablet core (containing active ingredient terbutaline terbutaline or its salt) and a coating layer (one or two layers) whose release is characterized by a rapid release of a dose of the contained active ingredient terbutaline or its salt over a period of time lag. Background technique [0002] Asthma is a common allergic disease. During the onset, due to the patient's bronchial smooth muscle spasm, mucosal swelling, narrowing of the lumen, and accumulation of secretions, ventilation obstruction and dyspnea are caused. In the past ten years, with climate warming and environmental pollution becoming more and more serious, the incidence of asthma has shown a global upward trend. The latest data shows ...

Claims

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Application Information

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IPC IPC(8): A61K9/28A61K9/22A61K9/52A61K31/137A61K47/38A61K47/34A61K47/44A61P11/06A61K47/10A61K47/32
Inventor 李亚平顾王文陈伶俐
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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