Paliperidone CAS 144598-75-4

Paliperidone powder, as the main active metabolite of Risperidone, is an effective antagonist of serotonin-2A and dopamine-2 receptor. Its molecular formula is C23H27FN4O3, its density is 1.45 g/cm3, and it is a gray-white to light orange solid, which belongs to one of the high-end raw materials for treating and relieving mental disorders.

paliperidone sustained-release tablets (pal 3)are made of paliperidone powder, and the release rate of product efficacy is delayed by special techniques, such as adding sustained-release agent into finished tablets, wrapping products with special films, adopting porous preparation structure, or adjusting the properties of wrapping materials or the size of pores. So as to prolong the residence time of the effective components of the product in the human body and make the use effect of the product more obvious.

Many factors should be considered in the design and preparation of sustained-release tablets, such as the chemical properties, physiological characteristics and therapeutic needs of raw materials.

Is using paliperidone a psychiatric patient?

paliperidone belongs to the second generation of antipsychotics, which is used to treat schizophrenia. Its pathological mechanism involves dopamine D2 receptor and D3 receptor in the central nervous system, and it is widely used in clinic. In particular, after combining research and development costs and market position, some scientific research institutions classify paliperidone raw materials as high-end spiritual raw materials.
However, it should be noted that besides schizophrenia, paliperidone may also be used for the treatment of bipolar disorder and other diseases (at this time, the patient is not mentally ill). In addition, because this product is an active metabolite of risperidone, an atypical antipsychotic product, it is often made into a scientific research reagent and widely used in molecular biology, pharmacology and other scientific research. Our company is one of the few companies in Xi 'an that can provide paliperidone powder and Risperidone powder research reagents in batches. If you have research plans and procurement needs, please leave a message through the email:sales6@faithfulbio.com

Product Specification

Which effect is better, paliperidone or risperidone?

Paliperidone is an active metabolite of risperidone in the body, and the only difference in their chemical structures is that Paliperidone has an additional hydroxyl group at the 9th carbon atom compared to risperidone; However, there are significant differences in the receptor action spectrum and metabolic pathways between the two.

Compared to risperidone, paliperidone not only has good D2 receptor affinity, but also stronger α 2, D3, and 5-HT7 receptor affinity. The above pharmacological characteristics can help comprehensively improve multidimensional symptoms such as positive, negative, emotional, cognitive, and sleep symptoms of schizophrenia, achieving multiple benefits with one action.

Paliperidone is mainly eliminated by kidney in vivo, about 59% is excreted from kidney in prototype, and less than 10% is eliminated by oxidation of cytochrome P450 enzyme in liver cells. This feature effectively reduces the risk of interaction between paliperidone and other products.

Thanks to the development of sustained-release technology, paliperidone sustained-release tablets can achieve an effective plasma concentration of more than 7.5ng/ml and a D2 receptor occupancy rate of more than 65% within 24 hours, while the fluctuations of plasma concentration and D2 receptor occupancy rate are obviously smaller than those of quick-release preparations. However, the efficacy of risperidone is relatively short, and it usually requires multiple daily uses to maintain blood active substance concentrations within an effective range.

Why should we use paliperidone for depression?

Because the patients' body state is different and the severity of their illness is different, there will be great differences in the way and time.
The treatment of depression needs to be individualized. Most patients with depression can be treated with antidepressant products alone or physical therapy, such as transcranial magnetic stimulation and non-convulsive electroconvulsive therapy, which can relieve the symptoms of depression at an early stage. In addition, it can also be combined with psychotherapy, which also has a good therapeutic effect on mild and moderate depression.
Some patients with depression, especially moderate and severe depression, are often accompanied by psychotic symptoms such as hallucinations and delusions. The use of antidepressant products can not completely improve such psychotic symptoms, so it is necessary to increase small doses of antipsychotic products, such as risperidone, olanzapine and paliperidone, to better alleviate the symptoms. There are also some patients with depression who have agitation symptoms, such as fidgeting, and the brain can't stop thinking about problems often, similar to the symptoms of forced thinking; Some patients have obvious symptoms of impulsiveness and emotional instability. The use of paliperidone powder and other new antipsychotic products can stabilize the mood and enhance the therapeutic effect.
If the patient is sensitive to paliperidone, the general use time will be shorter, and the psychotic symptoms may be improved after 4 -5 weeks of use. At this time, the dosage can be reduced under the guidance of a doctor until it stops. However, if the patient is not sensitive to this product, it may be necessary to appropriately increase the use time, which takes about 6 months or even longer to improve the above serious symptoms.
When using paliperidone sustained-release tablets, it should be noted that people who are allergic to the ingredients of this product, moderate and severe liver dysfunction and other people are prohibited from using it. Pay attention to rest during use, maintain emotional stability, and avoid being too excited, so as not to affect the recovery of the disease. At the same time, we should also pay attention to a reasonable diet, avoid eating irritating foods, such as peppers and hot and sour powder, and try to give priority to light and digestible foods so as not to aggravate the condition.

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Our strengths:

Our company has passed FDA and ISO19001 quality management system certification. And we have internal cooperation agreements with multiple factories and laboratories in China, so we can not only provide customers with the required paliperidone or paliperidone sustained-release tablets products, but also support the development and provision of new products.
We not only have unique advantages in transportation, but also support multiple payment methods, whether you use US dollars, euros, Australian dollars, or local currencies from Singapore, Malaysia, Thailand, and so on. We can also support local currencies in these regions and countries. In addition, we also support bank cards (credit cards, etc.) for payments.

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