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Indissolvable drug oral sustained-release dry emulsion tablet and preparation method thereof

A technology of insoluble drugs and dry milk tablets, which is applied in the fields of pharmaceutical formula, drug combination, drug delivery, etc., can solve the problems of short half-life, short duration of drug effect, prolonged duration of drug effect, peak and valley phenomenon of blood drug concentration, etc. Achieve the effects of reducing the first-pass effect of the liver, taking less times, and improving oral bioavailability

Inactive Publication Date: 2015-12-23
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The first-generation DHP calcium antagonists are also known as short-acting DHP calcium antagonists, and representative drugs include nifedipine and nicardipine, which have short half-lives and duration of drug effects in vivo; second-generation DHPs such as nisoldipine, nicardipine, etc. Qundiping, compared with the first generation of DHP calcium antagonists, the drug effect duration is significantly prolonged, but its water solubility is poor, even if the drug is completely released in the body, the bioavailability is also low; the third generation of DHP calcium antagonists It overcomes the shortcomings of the short duration of drug effect and low bioavailability of the previous two generations of DHP calcium antagonists
[0013] Most of the first- and second-generation DHP calcium antagonists are water-insoluble compounds, and the first-pass effect may occur during the absorption process, resulting in low bioavailability; these drugs usually have a short duration of efficacy, and patients need to frequently Taking medicine, so the compliance is low; in addition, this kind of medicine is easy to have obvious peak and valley phenomenon of blood drug concentration, which is easy to cause toxic side effects such as rapid reflex heart rate
However, these drugs have their unique clinical value and cannot be replaced

Method used

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  • Indissolvable drug oral sustained-release dry emulsion tablet and preparation method thereof
  • Indissolvable drug oral sustained-release dry emulsion tablet and preparation method thereof
  • Indissolvable drug oral sustained-release dry emulsion tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Prescription composition:

[0043]

[0044] 3% PVPK30 in 70% ethanol solution as adhesive, made 1000 pieces in total

[0045] Preparation Process:

[0046] 1) The drug is completely dissolved in the self-emulsifying system to obtain the drug-loaded self-emulsifying system;

[0047] 2) adding a small amount of water to the drug-loaded self-emulsifying system to make it self-emulsified, and then mixing it with an aqueous solution of HPMCK4M for spray drying to obtain a material liquid for spray drying;

[0048] 3) spray drying;

[0049] 4) Sieve and mix dry milk powder with extra HPMC and lactose, use 3% PVPK30 in 70% ethanol solution as binder, sieve and granulate at 20 mesh, dry at 45°C for 4 hours, granulate at 20 mesh, and finally add lubricant Tablet.

[0050] The obtained felodipine oral sustained-release dry milk tablet was tested for release according to the following dissolution method. Its drug release curve is shown in figure 1 .

[0051] According to...

Embodiment 2

[0053] Prescription composition:

[0054]

[0055]

[0056] A 70% ethanol solution of 3% PVPK30 was used as an adhesive to make a total of 1000 dosage units. The preparation process was the same as in Example 1.

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Abstract

The invention belongs to the field of medicinal preparations, and discloses an indissolvable drug oral sustained-release dry emulsion tablet and a preparation method thereof. The preparation method for the oral sustained-release dry emulsion tablet comprises the steps that after an oil phase, a surface active agent and cosurfactant are evenly mixed, an indissolvable drug is added till the drug is dissolved completely, and accordingly a medicine-carried self-emulsifying system is prepared; after the medicine-carried self-emulsifying system and an aqueous solution of a hydrophilic gel framework material are evenly mixed, spray drying is conducted, and sustained-release dry emulsion powder is obtained; after the sustained-release dry emulsion powder and a conventional tablet auxiliary material needed for preparation are mixed, wet granulation is carried out; at last, tabletting is performed. The sustained-release dry emulsion tablet can improve the dissolution and dissolving-out performance of the indissolvable drug, the bioavailability of the indissolvable drug is improved, a stable blood concentration is formed, and the compliance of patients is improved. The sustained-release dry emulsion tablet is not complex in composition of prescription, and the preparation technology is suitable for industrial production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to slow-release preparations for insoluble drugs, in particular to oral slow-release dry milk tablets for insoluble drugs and a preparation method thereof. Background technique [0002] About 40% of the active substances obtained by high-throughput drug screening are insoluble in water. Insoluble drugs have poor dissolution and dissolution properties in the body, so there are problems such as poor body absorption, low oral bioavailability, and difficulty in achieving diversification of dosage forms; some insoluble drugs also have a faster elimination rate in the body, and the blood drug concentration is prone to peaks and valleys. features. [0003] Sustained or controlled released dosage forms (sustainedorcontrolledreleasedosageforms) have the advantages of reducing the total dose and frequency of medication, avoiding the peak and valley phenomenon of blood concentration, ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K45/00A61K31/4422A61K47/38A61P9/12
Inventor 蒋曙光袁惠卿刘楚怡俞宏智
Owner CHINA PHARM UNIV
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