Tablet containing valsartan and hydrochlorothiazide

A technology of hydrochlorothiazide and valsartan granules, applied in the field of medicine, can solve the problems of low bulk density, adverse reactions, and large drugs of valsartan oral dosage forms, and achieve the effect of reducing the incidence of adverse reactions and the incidence of adverse reactions

Active Publication Date: 2010-07-21
LUNAN BETTER PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Furthermore, the challenge of developing a patient-friendly oral dosage form of valsartan is its low bulk density
The absolute bioavailability of hydrochlorothiazide is higher than that of valsartan, and due to these complex biopharmaceutical properties, it is challenging to develop a solid dosage form of a fixed combination of valsartan and hydrochlorothiazide that is bioequivalent or synergistic with free combination
[0007] The compound preparations of valsartan / hydrochlorothiazide currently used clinically are tablets and capsules. / 25mg, in order to increase the efficacy of the drug, the dosage of the drug is generally greatly increased, which will inevitably lead to greater adverse drug reactions

Method used

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  • Tablet containing valsartan and hydrochlorothiazide
  • Tablet containing valsartan and hydrochlorothiazide
  • Tablet containing valsartan and hydrochlorothiazide

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 180

[0033] Embodiment 180mg / 12.5mg bilayer tablet

[0034] Composition Weight / g Content / %

[0035] Valsartan layer

[0036] A Valsartan 80.00 8.70

[0037] B Microcrystalline cellulose 312.00 33.91

[0038] C Crospovidone 60.00 6.52

[0039] D Colloidal silicon dioxide 6.00 0.65

[0040] E Magnesium stearate (I) 12.00 1.30

[0041] F Magnesium (II) stearate 6.00 0.65

[0042] Subtotal 476.00 51.74

[0043] Hydrochlorothiazide layer

[0044] G Hydrochlorothiazide 12.50 1.36

[0045] H Microcrystalline cellulose 400.40 43.52

[0046] I Sodium starch glycolate 28.00 3.04

[0047] G Iron oxide 0.20 0.02

[0048] K Magnesium (III) stearate 1.30 0.14

[0049] L Magnesium (IV) stearate 1.60 0.17

[0050] Subtotal 444.00 48.26

[0051] Total 920.00 100

[0052] Preparation Process:

[0053] First, combine ingredients A-E in a diffusion blender for valsartan granulation; sieve the blended mat...

Embodiment 2

[0057] Embodiment 2 The effect of valsartan / hydrochlorothiazide compound on hypertensive model rats

[0058] 1. Grouping

[0059] A total of 50 10-week-old spontaneously hypertensive rats (SHR) were randomly divided into model group, valsartan group, hydrochlorothiazide group, compound I group, and compound II group, with 10 rats in each group, half male and half male.

[0060] 2 Administration method

[0061] Rats in each group were administered intragastrically for 12 weeks, and the doses were as follows:

[0062] Model group: intragastric administration of 0.9% normal saline with the same volume;

[0063] Valsartan group: 8.0mg / (kg.d) valsartan;

[0064] Hydrochlorothiazide group: 1.25mg / (kg.d) hydrochlorothiazide;

[0065] Compound group I: 8.0mg / (kg.d) valsartan+1.25mg / (kg.d) hydrochlorothiazide, the preparation process is the same as in Example 1, valsartan / hydrochlorothiazide 80mg / 12.5mg;

[0066] Compound group II: 8.0mg / (kg.d) valsartan + 1.25mg / (kg.d) hydrochlor...

Embodiment 3

[0078] Embodiment 3 valsartan / hydrochlorothiazide compound antihypertensive clinical trial research

[0079] 1. Case selection

[0080] Elderly hypertensive patients between 60 and 70 years old, without other obvious history of cardiovascular and cerebrovascular diseases, and patients with poor clinical efficacy after traditional antihypertensive treatment are eligible to participate in this trial.

[0081] 2. Medication regimen

[0082] A total of 160 patients participated in this test, and all patients participating in this test were randomly divided into two groups according to the level of systolic blood pressure and age, that is, compound group I and compound group II, with 80 cases in each group. The compound group I is administered the double-layer tablet valsartan / hydrochlorothiazide 80mg / 12.5mg prepared in Example 1 provided by the present invention, once a day for 8 consecutive weeks; the compound group II is administered orally by Nanbeite Pharmaceutical Co., Ltd. ...

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Abstract

The invention belongs to the filed of medicines, in particular relates to a tablet containing valsartan and hydrochlorothiazide. The double-layer tablet with synergy antihypertension function provided by the invention contains 80mg/12.5mg of the valsartan and hydrochlorothiazide. Compared with a compound unilayer tablet and a capsule containing 80mg/12.5mg of the valsartan / hydrochlorothiazide, the curative effect of the tablet provided by the invention is improved, and the incidence rates of adverse effects such as hacking cough, headache and dizziness are notably reduced, and p is less than 0.05.

Description

technical field [0001] The invention belongs to the field of medicine, in particular to a tablet containing valsartan and hydrochlorothiazide. Background technique [0002] Valsartan / hydrochlorothiazide compound preparation is a safe and orally effective antihypertensive drug widely used in clinic. Valsartan specifically antagonizes the angiotensin II receptor type I (AT 1 ) to inhibit the activity of angiotensin II (AII), thereby reducing blood pressure. Hydrochlorothiazide is a thiazide diuretic, which directly increases the secretion of sodium ions and chloride ions by affecting the reabsorption of electrolytes by the renal tubules, resulting in increased urine output and decreased blood volume. At the same time, hydrochlorothiazide reduces plasma volume through its diuretic effect, indirectly increases plasma renin activity, increases aldosterone secretion, increases urinary potassium excretion, and reduces blood potassium. The role of renin-aldosterone system is media...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/549A61K31/41A61K9/20A61P9/12A61K9/28
Inventor 赵志全张帅
Owner LUNAN BETTER PHARMA
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