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Development of Irbesartan Sustained Released Tablets

Author: XiongSiMin
Tutor: LvZhuFen；ChenYanZhong
School: Guangdong College of Pharmacy
Course: Pharmacy
Keywords: Irbesartan Physical and Chemical Properties Solubility Solid dispersion Differential scanning calorimetry
CLC: R94
Type: Master's thesis
Year: 2008
Downloads: 442
Quote: 1
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Abstract

Irbesartan angiotensin II receptor antagonists, specificity antagonize angiotensin II and angiotensin converting enzyme 1 receptor (AT1) the combination of inhibition of vasoconstriction and aldosterone release, resulting in the antihypertensive effect . Irbesartan is mainly used in the clinical treatment of hypertension, is now approved in the European Union for a new indication, the treatment of hypertension in patients with type II diabetes, kidney disease, the EU approved for the prevention of diabetes early and advanced kidney disease, the first anti-hypertensive drugs. Compared with similar AT1 receptor antagonist, great differences in the pharmacokinetic parameters of these drugs in the oral bioavailability of irbesartan the buck smooth and well tolerated, the role is more durable, and its absorption from food, the lowest protein binding rate, currently no reports of interactions with other drugs. Good patient compliance, suitable patients can not intolerant to angiotensin-converting enzyme inhibitors (ACEI), the probability of occurrence of severe coughing was significantly less than the use of ACEI patients. In view of this, irbesartan clinical promising anti-hypertensive drugs, has a good prospect. Clinical studies have shown that oral irbesartan 150mg / d (once daily) is effective in treating mild to moderate essential hypertension. CV131-030 the Sai Nuofei reported to the U.S. Food and Drug Administration in 1997 clinical trials of new drugs that a daily dose of 150mg, twice taking effect in taking the first, low incidence of adverse reactions. Irbesartan buck optimum plasma concentration range is unclear. The study shows that only in the case of irbesartan low blood concentration (lt; = 40ng/mL) have blood concentrations and between the antihypertensive efficacy of the positive effect of the presence of the dose - response. Thus, we consider irbesartan made dose for 24h sustained-release tablets of 150mg, wants to achieve and compared to conventional tablets: release the drug slowly to avoid a sudden increase of the concentration of the drug, and reduce to a sudden increase in the plasma concentration caused by the occurrence of adverse reactions; sustained release drugs, the drug concentration is maintained in the lower range, thereby generating a continuous and stable antihypertensive effect. The solution equilibrium solubility of irbesartan visit, the solubility of the drug with the change of pH value and showing a \is small, in order to ensure the release of the drug in the late, therefore contemplated that the sustained-release tablets made of double-layer tablets, double layer is divided into two parts of the sustained release layer and a rapid release layer. Of the drug in the sustained release layer to the water soluble material PEG6000 as carrier, prepared as a solid dispersion in order to increase the solubility of the drug in the intestine so as to increase the drug release rate of the late solvent method. Identified by differential scanning calorimetry of the solid dispersion, and no chemical reaction occurs in the results between table 明厄贝沙坦 carrier the dispersion a simple eutectic shaped state. Solid dispersions significantly increased the rate of release of irbesartan, which is stable, while the temperature and humidity stability Poor glare, need to be stored at room temperature in a moisture-proof container. Established vitro release, content and related substances determination method, select determination in vitro release of sustained release tablets irbesartan, select the HPLC determination of content and related substances, these methods are good linear range, high recovery method is accurate and reliable. Prescription process through the single factor screening and optimization. Release Tablets impact factors were investigated; using a variety of release model equation the release curve fitting, and explore the drug release mechanism. The results showed that the release test should use the paddle method; to speed drug release significant impact; said 明厄贝沙坦 sustained-release tablets release mechanism of the main skeleton dissolution, diffusion release mechanism, supplemented.

Development of Irbesartan Sustained Released Tablets

Abstract

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