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Solubilization systems, solid dispersions and pharmaceutical preparations

A solid dispersion and system technology, which can be used in pharmaceutical combinations, medical preparations without active ingredients, and medical preparations containing active ingredients, etc., can solve the problems of complex process, low preparation formability, low solubility, etc. The effect of specific surface area, improvement of hydrophilic properties, and improvement of solubility

Active Publication Date: 2019-05-07
BEIJING COLLAB PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, lofprodine or its salt has very low solubility, and it is difficult to dissolve in the gastrointestinal tract. The preparation containing loflupridine hydrochloride cannot achieve a good dissolution state by the existing common preparation technology, and the absorption in the body is also dissolved outside the body. limitations, and loflupridine or its salt also has strong adhesion and aggregation properties, so it may stick to punches or dies when it is made into capsules or tablets, thus showing low formulation formability
[0007] The Chinese patent with the publication number CN101600419B discloses a solid dispersion containing revaprazan and its preparation method. The surface of the raw material is modified by adding special excipients, and the solid dispersion is prepared by spray drying, but it still has complex processes. , Difficult to control, high environmental temperature and humidity requirements in the preparation process, high energy consumption in the production process, etc., and the solubilizing system excipients used are unconventional excipients

Method used

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  • Solubilization systems, solid dispersions and pharmaceutical preparations
  • Solubilization systems, solid dispersions and pharmaceutical preparations
  • Solubilization systems, solid dispersions and pharmaceutical preparations

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Tablets with a content of 200mg / tablet of loflupridine hydrochloride are composed as shown in Table 1.

[0036] Table 1 Composition of Loflupridine Hydrochloride Tablets

[0037]

[0038]

[0039] 1.1 Mix 200g of loflupridine hydrochloride, 100g of polyethylene glycol-6000, 10g of sodium lauryl sulfate and 50g of macrogolglycerol laurate, heat and melt it into a white suspension to obtain the first mid product.

[0040] 1.2 Mix 150 g of microcrystalline cellulose and 20 g of croscarmellose sodium evenly, add the first intermediate product, wet granulate, dry, granulate, add magnesium stearate, mix, and tablet to obtain tablets.

Embodiment 2

[0042] The composition of the capsules with a loflupridine hydrochloride content of 200mg / capsules is shown in Table 2.

[0043] Table 2 Composition of Loflupridine Hydrochloride Capsules

[0044]

[0045] 2.1 Dissolve 200g of PEG-4000 in 50g of purified water, add 5g of sodium lauryl sulfate and stir to dissolve, then add 20g of macrogol glycerol stearate, stir to dissolve, and add 200g of loflupridine hydrochloride at 60°C The water bath was stirred at least 1000 rpm to make it homogenized, and the first intermediate product was obtained.

[0046] 2.2 Add 100g of mannitol and 10g of crospovidone into the fluidized bed, then spray into the first intermediate product obtained in 2.1, granulate in the fluidized bed, pass through a 20-mesh sieve for granulation, add 5g of silicon dioxide, and mix Evenly, put it into capsules.

Embodiment 3

[0048] The composition of the granule of loflupridine hydrochloride content 100g / bag is as shown in table 3.

[0049] Table 3 Composition of Loflupridine Hydrochloride Granules

[0050]

[0051] Dissolve 300g of povidone K30 in 1000g of water, add 5g of sodium lauryl sulfate and 10g of macrogolglycerol laurate and stir to dissolve, then add 100g of loflupridine hydrochloride and stir at high speed to fully suspend , using a spray drying method to prepare granules, add 5g of magnesium stearate, and pack in sachets.

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PUM

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Abstract

The invention provides a solubilization system, a solid dispersion and a pharmaceutical preparation. The solid dispersion comprises the solubilization system and raw medicines, the solubilization system comprises high molecular polymer, anionic surfactant and grease, and the grease is polyethylene glycol fatty glyceride. Compared with the prior art, the high molecular polymer in the solid dispersion can enable the gathered raw medicines to be better dispersed so as to increase the specific surface area of the raw medicines; the surface activity of the raw medicines is modified by the anionic surfactant in the whole system, so that the solubility of the raw medicines can be improved; the grease has a solubilization effect and can improve the hydrophilicity of the raw medicines, so that the solubility of the raw medicines is improved; and the three substances are synergistic to form a strong solubilization system, so that the solubility of the raw medicines can be improved in many ways.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, in particular to solubilizing systems, solid dispersions and pharmaceutical preparations. Background technique [0002] Solid dispersion refers to a dispersion system in which a drug is highly dispersed in a solid carrier material in the form of molecules, colloids, microcrystals or amorphous states. Solid dispersion can increase the solubility and dissolution rate of poorly soluble drugs, delay or control drug release, and reduce drug side effects. [0003] The chemical name of lofopridine or revaprazan is 5,6-dimethyl-2-(4-fluorophenylamino)-4-(1-methyl-1,2,3,4-tetrahydro isoquinolin-2-yl)pyrimidine. Loflupridine or its salt reversibly binds to the proton pump H present in parietal cells + / K + exchange site (H + / K + ATPase) binding to competitively inhibit H + Secreted into the gastric cavity. Loflupridine or its salt also with H + / K + ATPase-specific site bindi...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/14A61K31/506A61K9/20A61K9/48A61K9/16A61P1/04
Inventor 申超邱敦有赵大龙王珂
Owner BEIJING COLLAB PHARMA
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