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EVALUATION-
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Nitrendipine film consistency evaluation
time：2020-03-03 
browse：1994second
一、Basic information
Common name: Nitrendipine film
English name: Nitrendipine Tablets
Pinyin: NiQunDiPingPian
Chemical name: 2,6dimethyl-4- (3-nitrophenyl) -1,4-dihydro-3,5-pyridinedicarboxylate
Molecular formula: C18H20N2O6
Molecular weight: 360.37
二、Introduction to varieties
Liniqundipine tablets were first marketed in Germany and developed by Bayer Pharmaceuticals under the trade name Bayotensin. They are available in 10mg and 20mg specifications. The original research unit was Bayer Pharmaceuticals.
API properties
Dissociation constant: without dissociation group
Stability in various dissolution media:
Decanter water: 37 ℃ / 4 hours stable
In each pH dissolution medium:
Stable in dissolution media at pH 1.2, pH 4.0 and pH 6.8 at 37 ° C / 4 hours.
Kuang Guang: Not determined.
BCS classification: Ⅱ
1. This product is a dihydropyridine calcium channel blocker.
2. This product inhibits the transmembrane calcium ion inflow of vascular smooth muscle and myocardium, but it is mainly vascular, so its vascular selectivity is strong.
3. This product causes dilation of systemic blood vessels such as coronary arteries and renal arterioles, resulting in hypotensive effects. Carcinogenic, mutagenic, and reproductive toxicity. Oral administration of similar drugs nifedipine to rats has not shown carcinogenic effects for two years. In vivo mutagenicity studies were negative.
This product is well absorbed orally, but there is a clear first pass effect. Protein binding rate was 98%. Earlier studies reported that t1 / 2 was 2 hours, and recent studies reported that T1 / 2 was between 10 and 22 hours due to the use of more sensitive measuring equipment. This product peaked at about 1.5 hours after oral administration. The systolic blood pressure began to decrease 30 minutes after oral administration, and the diastolic blood pressure began to decrease after 60 minutes. The antihypertensive effect was greatest at 1 to 2 hours after oral administration and lasted 6 to 8 hours. This product is metabolized in the liver, 70% of its metabolites are excreted by the kidney, and 8% are excreted with feces. Increased plasma concentration and elimination half-life in patients with liver disease.
三、 Domestic and foreign listings
Nitrendipine tablets in China have a total of 186 symbols with three specifications: 5mg, 10mg and 20mg.
No imported drugs are on the market.
No imported localized products went on the market.
Currently listed in European countries such as Germany, Spain and France.
This product is not available in the United States.
Japan has this product on the market, the specifications include 5mg and 10mg, there are multiple manufacturers.
四、Reference preparation
Original development agent listed in Germany (Bayer Pharmaceuticals) is preferred.
The reference preparation contained in the Japanese Orange Book is Nitrendipine tablets produced by Tanabe Mitsubishi Pharmaceutical Co., Ltd.