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Osmotic pump controlled release tablet of losartan potassium and hydrochlorothiazide solid dispersion or inclusion compound

A solid dispersion, osmotic pump controlled release technology, applied in the directions of non-active ingredients medical preparations, medical preparations containing active ingredients, drug combinations, etc., can solve problems such as increasing technical complexity, achieve high application value, Improve bioavailability and reduce peak-to-valley fluctuations

Active Publication Date: 2013-04-03
惠州市九惠药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Generally, the preparation of osmotic pump controlled-release tablets for insoluble drugs mostly adopts double-chamber or single-chamber multi-layer tablet technology, which increases the technical complexity

Method used

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  • Osmotic pump controlled release tablet of losartan potassium and hydrochlorothiazide solid dispersion or inclusion compound
  • Osmotic pump controlled release tablet of losartan potassium and hydrochlorothiazide solid dispersion or inclusion compound
  • Osmotic pump controlled release tablet of losartan potassium and hydrochlorothiazide solid dispersion or inclusion compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0083] The losartan potassium hydrochlorothiazide osmotic pump controlled-release tablet is composed of a tablet core and a coating film wrapping the tablet core, and a drug release hole of 0.3-0.9 mm is punched in the center of the coating side.

[0084] The tablet core consists of the following components:

[0085] Losartan Potassium 50mg

[0086] Hydrochlorothiazide-urea solid dispersion 87.5 mg

[0087] Lactose 125 mg

[0088] Sucrose 187.5 mg

[0089] It also contains magnesium stearate accounting for 1% of the mass of the tablet core, and povidone in a dose sufficient to bind the above substances;

[0090] The mass ratio of hydrochlorothiazide to urea in the hydrochlorothiazide-urea solid dispersion is 1:6.

[0091] The used coating liquid of described coating accounts for 3~5% of tablet core weight, and each component ratio of coating liquid is:

[0092] 30 parts of cellulose acetate,

[0093] Polyethylene glycol-4000 1.2 parts,

[0094] 6 parts of diethyl ph...

Embodiment 2

[0111] The hydrochlorothiazide-urea solid dispersion in Example 1 was replaced with the hydrochlorothiazide-polyvidone solid dispersion, and the others were the same as in Example 1.

[0112] The preparation method of the hydrochlorothiazide-povidone solid dispersion is as follows: weigh hydrochlorothiazide, povidone and poloxamer 188, place them in a container, add 2~5ml / 10mg of hydrochlorothiazide dehydrated alcohol, 35~45°C Stir to dissolve completely, evaporate the solvent in a water bath at 75-85°C to obtain a dry solid, then dry it in a desiccator for 24 hours, pass through a 60-mesh sieve, and seal it for later use.

[0113] The test method of the release of the two active ingredients of the losartan potassium hydrochlorothiazide osmotic pump controlled-release tablet prepared by the present embodiment is the same as in Example 1, and the release curve recorded is as follows: figure 2 .

[0114]

Embodiment 3

[0116] The hydrochlorothiazide-urea solid dispersion in Example 1 is replaced with hydrochlorothiazide-hydroxypropyl-β-cyclodextrin inclusion compound, and its addition amount is 200mg, the hydrochlorothiazide-hydroxypropyl-β-cyclodextrin inclusion compound The preparation method is:

[0117] Weigh hydrochlorothiazide, place it in a container, add 0.1mol / LNaOH, stir electromagnetically until hydrochlorothiazide dissolves, add hydroxypropyl-β-cyclodextrin, the molar ratio of added hydroxypropyl-β-cyclodextrin to hydrochlorothiazide is 3:1, add 0.1mol / L HCL drop by drop under electromagnetic stirring at 38°C, adjust the pH value to 5-7, rotate the water in the above solution at 70°C, and vacuum dry at 60°C to obtain Hydrochlorothiazide-hydroxypropyl-β-cyclodextrin inclusion compound solid dispersion.

[0118] Others are the same as in Example 1.

[0119] The test method of the release of the two active ingredients of the losartan potassium hydrochlorothiazide osmotic pump cont...

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Abstract

The invention belongs to the technical field of pharmacy, and in particular relates to a hydrochlorothiazide solid dispersion and hydroxypropyl-beta-cyclodextrin inclusion compound, and a preparation comprising losartan potassium and hydrochlorothiazide. The hydrochlorothiazide solid dispersion is prepared from hydrochlorothiazide and dispersion medium urea or povidone, and the hydrochlorothiazide hydroxypropyl-beta-cyclodextrin inclusion compound is prepared from hydrochlorothiazide and hydroxypropyl-beta-cyclodextrin inclusion. The preparation is an osmotic pump controlled release tablet comprising hydrochlorothiazide solid dispersion and inclusion compound and losartan potassium, consists of a tablet core and a coating for coating the tablet core, and a drug release hole with diameter of between 0.3 and 0.9mm is formed in the center of one side of the coating. The hydrochlorothiazide is compressed in the tablet core in a solid dispersion or inclusion compound mode together with losartan potassium, and is produced into a final product by utilizing an osmotic pump controlled release technology, so that the dissolubility of hydrochlorothiazide is improved, and the losartan potassium and the hydrochlorothiazide can be released at controlled speed in 0 to 24 hours in vitro. Therefore, the osmotic pump controlled release tablet has extremely high application value.

Description

[0001] technical field [0002] The invention belongs to the technical field of pharmacy, and in particular relates to a hydrochlorothiazide solid dispersion, a hydroxypropyl-β-cyclodextrin inclusion compound, and a preparation in which losartan potassium and hydrochlorothiazide are active ingredients. Background technique [0003] Losartan Potassium Hydrochlorothiazide is used for the treatment of hypertension and is suitable for patients treated with combination therapy. The commonly used starting and maintenance doses of losartan potassium and hydrochlorothiazide are once a day, one losartan potassium and hydrochlorothiazide 50-12.5mg each time (losartan potassium 50mg / hydrochlorothiazide 12.5mg). [0004] Losartan Potassium Hydrochlorothiazide Tablets (Losartan Potassium 50 mg + Hydrochlorothiazide Tablets 12.5 mg) is the first compound preparation consisting of angiotensin Ⅱ receptor (AT1 type) antagonists and diuretics. The two drugs in this compound preparation have ...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K9/22A61K9/36A61K31/549A61K47/16A61K47/32A61K47/48A61P9/12A61K31/4178A61K47/61
Inventor 高崇凯黄辉球李宁江洁
Owner 惠州市九惠药业有限公司
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