1、 Product introduction

【Indication】

       Pyrimidine is suitable for reducing elevated intraocular pressure in the following cases: high intraocular pressure open-angle glaucoma can be used as an ineffective β - receptor blocker, or as a separate treatment drug for patients with contraindications, or as a synergistic treatment drug for β - receptor blocker.

【Reportable Dosage Form &Strength】

       Eye drops 5ml: 50mg (1%) / branch

【Usage and Dosage】

        When it is used as a single or cooperative treatment drug, the dosage is to drop 1 drop of pyrimidine into the conjunctival sac of the affected eye twice a day. Some patients are more effective three times a day.

【Mechanism of Action】

      Carbonic anhydrase (CA) exists in many body tissues, including tissues. Carbonic anhydrase catalyzes the hydration of carbon dioxide into carbonic acid, and the reversible reaction of carbonic acid dehydration. Inhibition of carbonic anhydrase in the ciliary body of the eye can reduce the secretion of aqueous humor. It is possible that the transport of sodium and water can be reduced by reducing the formation of carbonate ions, and finally the intraocular pressure can be reduced. Intraocular pressure is an important risk factor for optic nerve damage and glaucomatous visual field defect. Brinzolam mainly inhibited the dominant carbonic anhydrase type 2 isoenzyme in eye tissue. In vitro, 50% of the effective inhibition concentration was 3.2NM, and the Ki value for carbonic anhydrase type 2 isoenzyme was 0.13nm.

【Development Progress】

  Our company is translating and sorting out the application materials, and it is expected to apply for the registration of imported raw materials by the end of 2015.

【Research and production at home and abroad】

         Alcon eye products Co., Ltd. products, 1998 in the United States. At present, it has been listed in nearly 30 countries in the world, and it was approved to import in 2002 in China. There is no preparation produced domestically.

2、 Product Features

A. It is a local carbonic anhydrase inhibitor with good selectivity, high affinity, strong inhibition activity to type II carbonic anhydrase isoenzyme related to the secretion of aqueous humor. Its physiological pH value and suspension design make the drug eye comfortable.

B. The sales situation is very good, which is favored by doctors and patients. As the first eye drops of carbonic anhydrase inhibitor in China, the amount of drugs purchased by the hospital rose all the way after brinzolam went on the market. In 2005 and 2006, the money growth rate of the drug was 297.21% and 30.20% respectively. The market share of brinzolam in the first quarter of 2007 was 28.16%.

C. Type of medical insurance, national medical insurance class B.

3、 Clinical Advantages   

  This product is suitable for the treatment of elevated intraocular pressure in patients with high intraocular pressure or open-angle glaucoma. It can be used as a separate treatment for patients with ineffective or contraindicated β - receptor blockers, or as a synergistic treatment for β - receptor blockers.

  Several clinical trials showed that the effect of this eye drop was the same as that of 0.5% metoprolol, but slightly worse than that of 0.5% timolol. There was no significant difference between dozoamine and dozoamine. This product has the best effect on reducing intraocular pressure in patients with primary open-angle glaucoma and high intraocular pressure, and has little adverse reactions.

  In addition, through a multicenter, double-blind, placebo-controlled prospective study, the efficacy and safety of 0.5% timolol in combination with this product for 3 months in 132 patients with open-angle glaucoma and high intraocular pressure were evaluated. The results showed that the effect of timolol + this product group on reducing intraocular pressure (3.3-4.1mmhg from baseline) was better than timolol + type agent (0.9-2.5mmhg from baseline) control group.

   According to foreign research data, among the drugs combined with β - blocker, 2% bromonidine, 2% pilocarpine, 0.1% dipivoline, and 1% brinzolam, 1% brinzolam eye drops showed the greatest drop in IOP.

   The tolerance and safety of brinzolam are good, the adverse reactions are few and not serious, and it usually relieves itself without treatment. A comparative study with dozoamine showed that the adverse reactions of this product were significantly less than 2% dozoamine.

4、 Patent information

        It is found that the basic patent ep0527801, the patent priority date is April 9, 1990 (US), and the expiry date is August 2010. Application for supplementary protection: from France to December 17, 2014, and from the Netherlands to March 8, 2010. This product has not applied for compound patent in China, and has applied for drug use patent, patent No.: 98811745, which has been authorized and expires in 2018. Alcon pharmaceutical, 98811745.

5、 Quality comparison

        The comparison between our raw material quality standard and usp35-nf30 shows that the limit and number of single impurity are better than USP

6、Domestic Declaration

Guangzhou Tosun Pharmaceutical Ltd

FL 4-5,No.3, 2nd Kehui street, Science Park, Guangzhou High-tech Industrial Development Zone, Guangzhou, China. 510663

Tel: +86-20-66392521； Fax: +86-20-66392525