Acetaminophen-pregabalin combinations and methods of treating pain

A technology of acetaminophen and pregabalin, applied in the field of manufacturing pharmaceutical preparations, pain in subjects, and pharmaceutical compositions for pain treatment, which can solve problems such as poor respiratory function

Pending Publication Date: 2020-07-17
NEVAKAR INJECTABLES INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the use of opioids or opioid-derived analgesics can lead to desirable side effects including, for example, nausea, vomiting, constipation, and poor respiratory function

Method used

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  • Acetaminophen-pregabalin combinations and methods of treating pain
  • Acetaminophen-pregabalin combinations and methods of treating pain
  • Acetaminophen-pregabalin combinations and methods of treating pain

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0111] Example 1: Effect of pH on the solubility of pregabalin and acetaminophen.

[0112] The solubility of pregabalin (PGB) and acetaminophen (APAP) in water was determined at different pH values ​​at room temperature. Samples were prepared by adding acetaminophen at a concentration of 50 mg / mL and pregabalin at a concentration of 100 mg / mL in water. The pH is then adjusted to the desired range. The concentration of the active ingredient was determined by HPLC-UV.

[0113] As can be seen from Table 1, no significant difference in the solubility of acetaminophen was observed within the pH range of 4-7.

[0114] As shown in Table 2, the solubility of pregabalin is higher at pH 4, being about 31 mg / mL in the pH range of 5-7.

[0115]

[0116]

[0117]

[0118] When pregabalin and acetaminophen are co-dissolved in the aqueous vehicle, the concentration of pregabalin and acetaminophen in the aqueous vehicle can be increased. Solubility samples were prepared by adding...

Embodiment 2

[0121] Example 2: Stability of acetaminophen and pregabalin formulations.

[0122] To determine the stability of acetaminophen and pregabalin co-formulations, citrate buffer (10 mM), acetate buffer (10 mM) and phosphate buffer (10 mM) were housed in four separate manufacturing tanks , as shown in Table 4. Pregabalin, acetaminophen, and other excipients were added to each tank and filled with the required amount of water (water for injection) to obtain concentrations of 4.5 mg / mL and 10 mg / mL, respectively.

[0123] Then, readjust the pH of each tank using HCl or NaOH. The volume of the tank can be topped up with deoxygenated water.

[0124] The bulk solution was filled into 100 mL polypropylene bags with a target fill volume of 100 mL, then stoppered and sealed. The bag is then further packed in an aluminum bag together with an oxygen scavenger and sealed.

[0125] Samples were assayed and tested for impurities. Table 4 shows four different formulations of pregabalin and ...

Embodiment 3

[0145] Example 3: Pharmacokinetic parameters of acetaminophen-pregabalin combination formulations.

[0146] Formulations for testing were prepared by weighing pregabalin and / or acetaminophen as indicated in Table 10 in glass vials. The active ingredient was dissolved in 0.9% saline (20 mL) to the desired concentration. Mix the brine and vial ingredients with gentle agitation until a clear solution is obtained. The obtained clear solution was filtered through a sterile 0.45 μm PVDF membrane syringe filter before being used for further studies.

[0147]

[0148]

[0149] Carry out paracetamol, pregabalin and paracetamol and pregabalin combination preparation after 15min infusion in rat body, analyze pharmacokinetic parameter in the period of time of 24h (table 11, figure 1 - Acetaminophen; Table 12, figure 2 - pregabalin).

[0150] The presence or absence of pregabalin did not affect the pharmacokinetics of acetaminophen in rats (Table 11; figure 1 ). No changes i...

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Abstract

Compositions and methods for an injectable liquid formulation for reducing consumption or need of a postoperative analgesic compound by a patient are presented. The pharmaceutical formulation can contain a non-opioid analgesic and a gabapentinoid, and can be administered prior to surgery to reduce postoperative pain.

Description

[0001] cross reference [0002] This application claims the benefit of U.S. Provisional Application No. 62 / 567,384, filed October 3, 2017, which is hereby incorporated by reference in its entirety. Background technique [0003] Postoperative pain management can involve the use of opioids or nonsteroidal inflammatory drugs (NSAIDs) after surgery. However, the use of opioids or opioid-derived analgesics can lead to desirable side effects including, for example, nausea, vomiting, constipation, and poor respiratory function. Analgesics that can be administered to patients prior to surgery could therefore eliminate the need for postoperative opioid administration and reduce the occurrence of unwanted side effects. [0004] Incorporate by reference [0005] Each patent, publication, and non-patent reference cited in this application is herein incorporated by reference in its entirety, as if each were individually incorporated by reference. Contents of the invention [0006] ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61P25/08A61K9/08A61K9/10A61K9/107A61K31/167A61K31/197
CPCA61K31/167A61K31/197A61P25/08A61K9/0019A61K45/06A61K47/02A61K47/12A61K47/183A61K31/195A61K2300/00A61P29/00A61K31/19A61K31/194A61K33/42
Inventor 瓦伦·库拉纳杰克·马丁·利普曼米兰·帕特尔尤里·伊利乔夫图沙尔·欣戈拉尼库玛列什·索皮马斯纳夫尼特·普瑞
Owner NEVAKAR INJECTABLES INC
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