Medicine composition contg. Tamsulosin and calcium antagonist

Abstract

A composite medicine for treating hypertension and the diseases associated with prostatoplasia contains Tansuoluoxin or its active metabolite or its precursor or its addition salt, antagon or its metabolite or its salt, and medicinal carrier or excipient.

Description

technical field [0001] The invention relates to a pharmaceutical composition containing tamsulosin and a calcium antagonist, and the use of the composition in preparing medicines for treating hypertension or / and diseases related to benign prostatic hyperplasia. The present invention belongs to the field of pharmacy. Background technique [0002] Hypertension is the most common cardiovascular disease that endangers human health and is a major public health issue worldwide. A large number of evidence-based medical studies have confirmed that with the increase of blood pressure, the risk of cardiovascular disease increases significantly. From 115 / 75mmHg onwards, every 20 / 10mmHg increase in blood pressure doubles the risk of cardiovascular disease; while active antihypertensive treatment can Effectively reduce cardiovascular events, reduce the morbidity and mortality of stroke, myocardial infarction and heart failure, and reduce the consumption of medical resources [Shi Xubo. H...

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Problems solved by technology

[0006] In the scientific research on antihypertensive drugs, we found that the pharmaceutical compositions reported in the above published literature have insurmountable shortcomings: 1. The combined application of nifedipine and α-AR blocker drugs: nifedipine is a fast-acting Antihypertensive drugs, the half-life of antihypertensive drugs after oral administration is biphasic, the α phase is 2.5 to 3 hours, and the β phase is 5 hours [Edited by Zhang Xianglin. Drug clinical information reference. Drug Evaluation Center of the State Drug Administration, Sichuan Meikang Pharmaceutical Software Research and Development Publishing Ltd. 2003, 353]

Because nifedipine takes effect quickly after oral administration, the time to peak blood concentration is short, and the half-life is short, it is used in combination with α-AR blockers, and the probability of adverse reactions such as orthostatic hypotension, headache, flushing, and palpitations is higher. , the patient's medication compliance decreased significantly, and the long-term antihypertensive effect decreased accordingly

2. Combination of doxazosin and calcium antagonists: ALLHAT trial [Messerli FH. Doxazosin and congestive heart failure. J Am Coll Cardiol. 2001, 38(5): 1295-1296; 2000, 355(9207) : 863-864.] The results of the study suggest that doxazosin may aggravate cardiac insufficiency in patients with hypertension, so the above-mentioned drug combination will increase the difficulty of curing patients due to potential risks and bring additional risks to patients; at the same time, due to the The announcement of the research results shows that patients with hypertension have poor compliance when taking doxazosin, which is not suitable for clinical application

5α-reductase inhibitors prevent and treat benign prostatic enlargement but have side effects of adverse sexual events

At the same time, α-adrenergic receptor blockers also have limitations in the application process: SugayaK et al. reported that after treatment with terazosin, the systolic and diastolic blood pressures of hypertensive patients with BPH decreased. No change in non-hypertensive patients; hypertensive patients with BPH still had significantly higher systolic blood pressure than non-hypertensive patients with BPH【Sugaya K, et al.Influence of hypertension on lower urinary tract symptoms inbenign prostatic hyperplasia.Int J Urol, 2003, 10(11): 569-574]

Our study found that: diltiazem is an adjuvant drug for the treatment of hypertension, and its antihypertensive effect is poor. It has the potential to inhibit heart function or inhibit myocardial contractility. Another compound, alfuzosin, has almost no antihypertensive effect.

The patent also discloses that α-adrenoceptor blockers include alfuzosin (alfuzosin), prazosin (prazosin), terazosin (terazosin), doxazosin (doxazosin), trimazosin ( trimazosin, bunazosin, urapidil, and indoramin, and calcium antagonists, including diltiazem, nifedipine, and verapamil, The pharmaceutical compositions disclosed in this patent also include alfuzosin and verapamil, alfuzosin and nifedipine, diltiazem and prazosin, diltiazem and terazosin, diltiazem and doxazosin, diltiazem with trimazosin, diltiazem and bunazosin, diltiazem and urapidil, diltiazem and indolamine, however the patent document does not sufficiently disclose other drug combinations

The patent also indicates that the pharmaceutical composition protected by the patent application can be used to treat urinary tract diseases, but it does not give full disclosure and specific instructions

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