Pregabalin CAS 148553-50-8 Raw Powder

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Product details

Pregabalin Powder Usage and Synthesis:

Pregabalin is a medication used to treat epilepsy, neuropathic pain, anxiety disorders, and fibromyalgia. It works by reducing the release of certain neurotransmitters in the brain, which can help to reduce seizures and relieve pain.

Pregabalin is typically taken orally, either as a capsule or tablet, and is usually taken two to three times a day. The dosage will depend on the condition being treated and the individual's response to the medication.

Common side effects of pregabalin include dizziness, drowsiness, dry mouth, blurred vision, and weight gain. In rare cases, it can also cause more serious side effects such as suicidal thoughts or behaviors.

As with any medication, it is important to follow the instructions of a healthcare provider and to report any side effects or concerns. Pregabalin can also interact with other medications, so it is important to inform a healthcare provider of any other medications being taken.

Pharmacokinetics of Pregabalin Powder:

Pregabalin is used for the treatment of peripheral neuralgia and adjuvant treatment of localized partial seizures. Pharmacological action Pregabalin has a good therapeutic effect on epilepsy. Studies on various animal epileptic seizure models have shown that pregabalin can obviously prevent epileptic seizure, and the dose of its active effect is 3-10 times lower than gabapentin. Pregabalin was found to reduce sensory and motor spinal reflex in rat grip toe stimulation, reduce behaviors associated with diabetes, peripheral nerve injury, or chemotherapy in neuropathic animal pain models, and inhibit or reduce pain-related behaviors caused by spinal giving stimuli. Animal studies have found that pregabalin may have advantages in combination with opioids. Pregabalin provides a new option for the clinical treatment of neuropathic pain.

Pregabalin, a non-gamma-aminobutyrate (GABA) receptor agonist or antagonist, is a novel calcium channel regulator that can block voltage-dependent calcium channels and reduce the release of neurotransmitters. It is mainly used in neuralgia associated with diabetic peripheral neuropathy, postherpetic neuralgia, and adjuvant treatment of adult partial seizures, generalized anxiety disorder, central neuralgia (including spinal cord injury, stroke, and neurogia associated with multiple sclerosis), and fibromyalgia.

Applications of Pregabalin Powder :

Pregabalin is an analogue of the neurotransmitter gamma-aminobutyric acid (GABA), sold under the trade name Lyrica. In December 2004, the FDA approved pregabalin to treat diabetic neuralgia and herpes zoster neuralgia. Pregabalin is the first drug approved in the United States and Europe for both types of pain. In June 2005, pregabalin was approved for adjuvant treatment of adult partial seizure epilepsy. In March 2006, the EU approved Pregabalin for the treatment of generalized anxiety disorder (GAD) and social anxiety disorder (SAD).

In December 2008, the U.S. Food and Drug Administration (FDA) approved Pregabalin (trade name "Relica") for the treatment of diabetic peripheral neuralgia (DPN) and postherpetic neuralgia (PHN), two of the most common types of neuropathic pain. Neuropathic pain is one of the most difficult chronic pain syndroms to treat. It is characterized by dull, burning, and stinging pain. Neuropathic pain is caused by many factors, including diabetes, infections (e.g., shingles), cancer, and AIDS.

Method of preparing Pregabalin Powder：

The condensation of diethyl malonate and 3-methylbutyral in the presence of diisopropylamine gives 98. The latter is double-bonded with KCN and hydrodissociated to obtain racemic pregabalin 96. Racemic pregabalin formed diastereoisomer salt with S-(+) -mandelic acid, which was crystallization and resolution to obtain optically pure S- isomer.

Pregabalin may reduce calcium-dependent release of some neurotransmitters by modulating calcium channel function. Although pregabalin is a structural derivative of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA), it does not directly bind to GABAA, GABAB or benzodiazepine receptors, does not increase the GABAA response of cultured neurons in vitro, does not change the concentration of GABA in the brain of rats, and has no acute effect on GABA uptake or degradation. However, in vitro neurons exposed to pregabalin for a long period of time, GABA transporter density and functional GABA transport rate increased. Pregabalin does not block sodium channels, has no activity on opioid receptors, does not change cyclooxygenase activity, has no activity on dopamine and serotonin receptors, and does not inhibit the reuptake of dopamine, serotonin or norepinephrine.

The preparation method of pregabalin capsule has the following steps: 

(1) The raw material of pregabalin in the swing particle machine through 30 mesh (aperture 600μm) screen, the raw material of pregabalin after 30 mesh screen then through 60 mesh (aperture 250μm) screen and 80 mesh (aperture 180μm) screen, take 60 mesh screen and not over 80 mesh of pregabalin particle powder, reserve;

(2) lactose was passed through 80 mesh (diameter 180μm) screen and 120 mesh (diameter 120μm) screen on the concussion screen, and lactose granule powder was taken through 80 mesh screen and not through 120 mesh screen, and set aside;

③ The pregabalin granule powder (D50 particle size of 180μm ~ 220μm, D90 particle size of 250μm ~ 280μm) obtained from step 1 was mixed evenly with adhesive in the multi-direction motion mixer, and then the lubricant and lactose granule powder obtained from step 2 (D50 particle size of 120μm ~ 140μm, D90 particle size is 160μm ~ 180μm), continue to mix evenly, and finally fill the evenly mixed material directly in the automatic capsule filling machine to get pregabalin capsules.

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