Phenobarbital sustained-release preparation and preparation method thereof

A technology of sustained-release preparations and phenobarbital, which is applied in pill delivery, pharmaceutical formulations, and medical preparations of non-active ingredients. Effects of absorption, enhanced bioavailability, and slow release rate

Pending Publication Date: 2020-08-18
北京清析技术研究院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Clinical studies have shown that phenobarbital is well absorbed in the small intestine and ascending colon, but after exceeding the hepatic flexure of the colon, its absorption is very poor, which means that the average absorption window of phenobarbital is 5h or less. In terms of medication for patients, If the drug can be developed into a once-daily sustained-release formulation, it can improve patient compliance, reduce or prevent dose-related adverse reactions, and improve efficacy
However, there are some problems in the common sustained-release preparations of phenobarbital developed at present. When the sustained-release preparations of phenobarbital are transferred to th

Method used

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Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0031] A preparation method of phenobarbital sustained-release preparation, the method comprises the following steps:

[0032] Step 1: Grinding and sieving each raw material to obtain raw material drug powder with a particle size of 180-220 mesh for subsequent use;

[0033] Step 2: The alginate and calcium salt obtained in the ratio of step 1 are stirred and mixed in a mixing furnace, the stirring speed is 350-450r / min, and the mixing time is 30-90 min to obtain the intermediate gel skeleton material;

[0034] Step 3: Add the proportioned amount of swelling material and diluent to the gel skeleton material obtained in step 2 and continue to stir and mix in the mixing furnace. The stirring speed is 350-450 r / min, and the mixing time is 30-90 min. Obtain excipient material blend stand-by;

[0035] Step 4: uniformly mixing the phenobarbital bulk drug with a pharmaceutically acceptable complex, salt, solvate or hydrate to prepare the phenobarbital pharmaceutical active ingredient...

Embodiment 1

[0040] A kind of phenobarbital sustained-release preparation, sustained-release tablet comprises phenobarbital pharmaceutical active ingredient, excipient and lubricant; Phenobarbital pharmaceutical active ingredient is made of phenobarbital or phenobarbital pharmacology Composition of acceptable complexes, salts, solvates or hydrates, wherein the phenobarbital pharmaceutical active ingredient accounts for 25% by weight of the sustained-release preparation; the excipient is made of gel matrix material, swelling material and diluent get; the gel matrix material is made up of alginate and calcium salt, and the gel matrix material accounts for 50% by weight of the sustained-release preparation; wherein, the alginate is sodium alginate, the calcium salt is calcium hydrogen phosphate, sodium alginate and phosphoric acid The weight ratio of calcium hydrogen is 2:1; the swelling material is polyoxyethylene, crospovidone composition, wherein the swelling material accounts for 10% of th...

Embodiment 2

[0050] A kind of phenobarbital sustained-release preparation, sustained-release tablet comprises phenobarbital pharmaceutical active ingredient, excipient and lubricant; Phenobarbital pharmaceutical active ingredient is made of phenobarbital or phenobarbital pharmacology Composition of acceptable complexes, salts, solvates or hydrates, wherein the phenobarbital pharmaceutical active ingredient accounts for 60% by weight of the sustained-release preparation; the excipient is made of gel matrix material, swelling material and diluent get; the gel matrix material is made up of alginate and calcium salt, and the gel matrix material accounts for 10% by weight of the sustained-release preparation; wherein, the alginate is sodium alginate, the calcium salt is calcium hydrogen phosphate, sodium alginate and phosphoric acid The weight ratio of calcium hydrogen is 8:1; the swelling material is polyoxyethylene, crospovidone composition, wherein the swelling material accounts for 29.3% of ...

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Abstract

The invention belongs to the field of medicinal materials and carriers, and particularly discloses a phenobarbital sustained-release preparation which comprises a phenobarbital pharmaceutical active component, an excipient and a lubricant. The phenobarbital pharmaceutical active component accounts for 25-60% of the weight of the sustained-release preparation. The excipient is prepared from a gel skeleton material, a swelling material and a diluent, the gel skeleton material accounts for 10-50% of the weight of the sustained-release preparation, the swelling material accounts for 10-30% of theweight of the sustained-release preparation, and the diluent accounts for 0-15% of the weight of the sustained-release preparation. The gel skeleton material is composed of alginate and calcium salt,and the weight ratio of alginate to calcium salt is 2: 1 to 8: 1. The lubricant accounts for 0.7-2.5% of the weight of the sustained-release preparation. After the sustained release preparation disclosed by the invention is used, acid-insoluble gel with good strength is rapidly formed, so that the phenobarbital drug release speed is reduced, the drug can be released and absorbed for a longer time,and the bioavailability of the drug is improved.

Description

technical field [0001] The invention relates to the field of medicinal materials and carriers, in particular to a phenobarbital sustained-release preparation and a preparation method. Background technique [0002] Phenobarbital is a white shiny crystalline powder, and its saturated solution is acidic. It is a long-acting barbiturate. It is mainly used clinically to treat antiepileptic and anticonvulsant and achieve sedative and hypnotic effects. Clinical studies have shown that phenobarbital is well absorbed in the small intestine and ascending colon, but after exceeding the hepatic flexure of the colon, its absorption is very poor, which means that the average absorption window of phenobarbital is 5h or less. In terms of medication for patients, If the drug can be developed into a once-daily sustained-release formulation, it can improve patients' medication compliance, reduce or prevent dose-related adverse reactions, and improve efficacy. However, there are some problems ...

Claims

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Application Information

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IPC IPC(8): A61K9/22A61K47/36A61K47/02A61K47/10A61K47/32A61K47/26A61K47/38A61K31/515A61P25/08A61P25/20
CPCA61K9/2009A61K9/2018A61K9/2027A61K9/2031A61K9/205A61K9/2054A61K9/2059A61K31/515A61P25/08A61P25/20
Inventor 盛四辈李成龙董珍许文友徐万飞刘煦旸潘士泉项婷
Owner 北京清析技术研究院
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