Minophosphonic Acid Introduction

- Sep 05, 2019-

Osteoporosis (OP) is a systemic bone disease caused by a variety of causes. It is a systemic bone disease characterized by decreased bone strength and increased risk of fracture. It is prone to fracture due to increased fragility of the bone. Bone strength depends mainly on two factors: bone mineral density and bone mass. Factors affecting bone mass include bone microstructure, bone turnover, damage accumulation (such as microfractures), and mineralization of bone. The reduction in bone strength makes the bone prone to fracture when subjected to external forces. With the extension of human life, the problem of aging has brought new problems to human health. Osteoporosis and its fractures rank 7th among the current common diseases, which seriously threaten the health of middle and old people and become a global public health problem. Ethyl Trans-4-oxo-2-butenoate CAS 2960-66-9 is one of the important raw materials for osteoporosis minoxidin.

According to China's "Ninth Five-Year Plan" research topic, 48,615 people in five major administrative regions (North China, East China, Central South, Southwest China, Northeast China) (including 7182 people using dual-energy X-ray absorptiometry to measure lumbar spine and femur bone mineral density) epidemiological study The results showed that the prevalence of osteoporosis and low bone mass in women over 40 years old was 19.9% and 32.4%, respectively, and men were 11.5% and 45.8%, respectively. The prevalence of osteoporosis and low bone mass in the population over 60 years old was 28.6% and 13.8% for women, and 15% and 12.7% for men, respectively. The total prevalence rates were 22.6% and 13.3%, respectively. There are about 29 million patients with osteoporosis over 60 years old in China, and 17 million patients with low bone mass.

  Ethyl Fumaraldehydate factory told us that bisphosphonates are analogs of pyrophosphate compounds in the body. They are low in blood and once absorbed into the bone tissue, adsorbed on the surface of hydroxyapatite crystals, inhibiting the formation of calcium phosphate crystals. And dissolve, and inhibit soft tissue ectopic calcification, affecting the activity of osteoclasts. It was applied to the treatment of 0P in the mid-1970s, but long-term application can prevent normal bone tissue calcification and increase the incidence of fracture. By changing its structure in the late 1980s, it eliminated the defects of inhibiting bone calcification and enhanced the effect of inhibiting bone resorption. Bisphosphonate therapy has been shown to increase bone mass, but the potential protective effects of this drug on bone structural damage are unclear. The main adverse reactions are gastrointestinal irritation and kidney damage. At present, bisphosphonates have become one of the most potential drugs for the prevention and treatment of OP.

  Ethyl (2E)-4-Oxo-2-butenoate manufacturers mentioned that the development of bisphosphonate drugs can be divided into three generations according to pharmacodynamics. The first generation of nitrogen-free bisphosphonates, the earliest application of etidronate, was used clinically as early as the 1970s. Since long-term use at therapeutic doses can lead to bone softening, it is currently rarely used. The most widely used first generation bisphosphonate is sodium clodronate. The second-generation bisphosphonate has a significantly better anti-bone absorption effect than the first-generation product. In its structure, the amino group is the main feature. Pamidronate is the most widely used. The third generation is a heterocyclic nitrogen-containing bisphosphonate, which has a stronger anti-bone absorption effect and is more convenient for clinical application. Zoledronic acid is a representative of the third-generation bisphosphonate.

  The minodronate tablets are used to treat osteoporosis and belong to the third generation azaaryl bisphosphonate derivatives. The main component is minodronic acid hydrate, and its chemical name is: {1-hydroxy-2-[imidazo(1,2-a)pyridin-3-yl]ethylidene}bisphosphonic acid monohydrate.

  Patent W09400462A1 discloses a formulation of a minodronic acid formulation which is formulated into a tablet by adding lactose, corn starch, 10% aqueous hydroxypropylcellulose solution, magnesium stearate. Minoxidin is the latest product in the third generation of bisphosphonates. It is more prominent in terms of effectiveness and safety. The activity of minodronic acid (MED = 1 mg/kg p.ο.) is 30 to 100 times that of sodium alendronate (30 mg/kg ρ.ο.) and pamidronate (100 mg/kg p.ο.). A multicenter, randomized, placebo-controlled trial in postmenopausal Japanese women diagnosed with osteoporosis has validated the efficacy and safety of this product.

  Ethyl Trans-4-oxobutenoate manufacturers told us that minodronic acid has good clinical effect and outstanding safety, simple preparation process and high quality controllability. The population of osteoporosis in China is large and the market potential is huge. Has significant research, development and promotion value.