Tamsulosin hydrochloride double-layer osmotic pump controlled-releasing tablet and preparation method thereof

Abstract

The invention provides double-layer osmotic pump tablets of tamsulosin ehydrochloride and a process for preparation. The medicament contains tamsulosin ehydrochloride and acceptable medical polymeric excipient, and is characterized in that the invention has excellent zero-level controlled releasing, pH level of environment, movements of the stomach and intestine, and food, has little effect on releasing action and food, and has no effect on the internal pharmacokinetics parameter. According to the percentage by weight, the preparation contains tamsulosin ehydrochloride 0-2%, excipient in pastille layer with the function of controlled-releasing 30-70% excipient in boosting layer with the function of controlled releasing 30-70%, and the rest percentage of other excipient. The of process for preparation the double layer permeable pump controlled-release tablets of tamsulosin ehydrochloride comprises (1) the preparation of pastille layer, (2) the preparation of boosting layer, (3) the compressing of the two layers, (4) the coating of the double layer tablets, (5) the perforating of the coated tablets, (6) the packing of moisture proof cost. The invention is clinically used for the treatment of paruria symptom like frequent micturition, diuresis at night, dysuria caused by prostatic hyperplasia.

Description

technical field [0001] The invention relates to a tamsulosin hydrochloride double-layer osmotic pump controlled-release tablet for treating abnormal urination symptoms caused by benign prostatic hyperplasia, such as frequent urination, nocturia, and dysuria, and a preparation method thereof. Background technique [0002] Benign Prostate Hyperplasia (BPH) is a benign adenomatous hyperplasia of cells in the periurethral zone of the prostate. Progressive enlargement of the gland can narrow the prostatic urethra and cause obstruction of urine outflow from the bladder. The clinical manifestations are urgency, frequency, and residual urine, which often lead to urinary tract infection, urinary retention, bladder infection, bladder stones, and renal failure. Data show that the incidence rate of benign prostatic hyperplasia is very low before the age of 40, 40% of the 50-year-old, nearly 90% of the 80-year-old, and almost 100% of the 90-year-old suffer from the disease. Therefore, b...

AI Technical Summary

Problems solved by technology

But it may have the following disadvantages: since the prescription contains high-viscosity polyoxyethylene as a sustained-release gel material, the release rate of the drug from the tablet is mainly affected by the hydration and erosion speed of polyoxyethylene, and the in vitro release rate Experiments have shown that the release rate of the preparation varies greatly with different dissolution paddle speeds; therefore, in the human gastrointestinal tract, the intensity of gastrointestinal peristalsis may have a greater impact on the release rate of the preparation, so that the preparation can be used as a drug for the human body. Kinetic features have large variability

But it has the following problems: (1) it has a time lag of about 2 hours, so that the drug cannot take effect quickly after taking it; (2) the main auxiliary material polyoxyethylene used is a kind of poor thermal stability and low glass transition temperature (62~67℃) high molecular polymers have the following problems in the preparation and storage process of industrial production: ①It is difficult to dry the solvent in the granulation process

Since the drying temperature should generally not exceed 40°C, it is easy to cause a high residual amount of organic solvents; if the drying is to be relatively complete, a relatively long drying time is required; Change the physical and chemical properties of polyoxyethylene, thereby affecting the release behavior of the tablet; ③During the high-speed tablet compression process, if the die generates heat after repeated use and the temperature reaches about 50°C, unfavorable phenomena such as sticking and punching are prone to occur , so special cooling facilities are needed to control the temperature of the die

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