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Injectable long-acting local anesthetic semi-solid gel formulations

A technology of semi-solid and pharmaceutical preparations, applied in the field of semi-solid gel preparations of injectable long-acting local anesthetics, which can solve the problems of unreliability, complicated and expensive manufacturing process, and poor repeatability

Pending Publication Date: 2020-09-11
HUZHOU HUI ZHONG JI SHI BIOTECHNOLOGY CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0016] While the above systems are useful, their manufacturing processes are complex, cumbersome and expensive
In addition, these products have a large amount of drug release (also called "burst release") in the early stage after injection, and the kinetics of drug release are not good, and the repeatability is poor, so the analgesic effect in animal experiments and human experiments is not ideal. Unreliable

Method used

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  • Injectable long-acting local anesthetic semi-solid gel formulations
  • Injectable long-acting local anesthetic semi-solid gel formulations
  • Injectable long-acting local anesthetic semi-solid gel formulations

Examples

Experimental program
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Effect test

preparation example Construction

[0116] Preparation of castor oil semi-solid gel preparation

[0117] The castor oil semi-solid gel formulation containing active substances of the present invention can be prepared by directly mixing castor oil and gelling excipients, or by mixing with an already formed semi-solid gel matrix. The mechanical mixing process is carried out at a suitable temperature, usually between 60°C and 90°C, to completely melt the gelling excipient and castor oil into solution and dissolve or grind the active drug by any mechanical means to form a clear solution or homogeneous suspension. Vacuum can be applied to avoid air bubbles, and nitrogen can be applied to reduce oxidation of the active drug and delivery vehicle components. After obtaining a homogeneous pharmaceutical composition, the active substance semi-solid gel formulation can be cooled to room temperature.

[0118] Semi-solid gel drug composition of local anesthetic

[0119] Local anesthetics can cause temporary nerve conducti...

Embodiment 1

[0169] Example 1. SUP D

[0170] C 12 to C 18 SUP D mixture of triglycerides, melting point 42°C to 45°C. The results of the ratio study of castor oil and SUP D are shown in Table 3. Target amounts of each component were weighed into glass vials and heated to approximately 50°C. Place in 75°C water bath and mix / vortex until all components are completely dissolved and a clear solution forms.

[0171] SUP D takes about a similar time to start and complete gelation as SUP DM because they have similar properties and melting points. Approximately 1 mL of the hot solution was filled into a 5 mL prefilled syringe and steam sterilized at 121 °C for 20 min. Whether steam sterilized or not, after cooling to room temperature at 10-20 wt% gelling agent levels, they all appeared as homogeneous opaque gels and were injectable with a 21 gauge needle.

[0172] Table 3: Castor Oil and SUP D Ratio Study

[0173] Sample serial number Castor oil (g) SUP D(g) Bupivacaine (mg...

Embodiment 2

[0174] Example 2. SUP CM

[0175] C 12 to C 18 The SUP CM mixture of triglycerides has a melting point of 37.8 to 39.8°C. Castor oil and SUP CM ratio studies are shown in Table 4. Target amounts of each component were weighed into glass vials and heated to approximately 75°C in a water bath and mixed / vortexed until all components were completely dissolved and a clear solution formed.

[0176] Since SUP CM has a lower melting point, SUP CM takes longer than SUP DM to initiate and complete gelation.

[0177] Approximately 1 mL of the hot solution was filled into a 5 mL prefilled syringe and steam sterilized at 121 °C for 20 min. Whether steam sterilized or not, after cooling to room temperature at 10-20 wt% gelling agent levels, they all appeared as homogeneous opaque gels and were injectable with a 21 gauge needle.

[0178] Table 4: Castor Oil and SUP CM Ratio Study

[0179] Sample serial number Castor oil (g) SUP CM(g) Bupivacaine (mg) SUP CM F01 1....

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Abstract

What is disclosed is a controlled release pharmaceutical composition comprising a biocompatible and bioerodible semi-solid gel comprising a triglyceride of ricinoleic acid, a gelling agent, bupivacaine and, optionally, a corticosteroid, an analgesic, or an anti-inflammatory agent.

Description

[0001] Related patent application reference [0002] This patent claims priority to U.S. Patent Application Serial No. 15 / 833,899, filed December 6, 2017. technical field [0003] The invention provides a semi-solid pharmaceutical composition for drug controlled release, the pharmaceutical composition includes a local anesthetic and an anti-inflammatory drug in a semi-solid lipid carrier, and the semi-solid lipid carrier contains castor oil and a gelling agent , the pharmaceutical composition for the controlled delivery of a local anesthetic in injectable form for the treatment of postoperative pain. [0004] Background of the invention [0005] In the United States, where approximately 100 million procedures are performed each year, systemic opioids are used to manage postoperative pain, and only half of patients have adequate pain control. Prescribing opioid postoperative pain management is fueling the opioid epidemic, as 1.6 million U.S. surgical outpatients become chroni...

Claims

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Application Information

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IPC IPC(8): A61K9/06A61K47/14A61K47/44A61K31/445A61K31/192A61K31/5415A61K31/5575A61K31/56A61P29/00A61P29/02A61K31/58A61K31/57A61K31/573
CPCA61K9/0024A61K47/14A61K9/06A61K47/44A61K31/192A61K31/445A61K31/5415A61K31/5575A61K31/56A61K31/57A61K31/573A61K31/58A61P29/02A61P29/00
Inventor 沈惠荣甘娜
Owner HUZHOU HUI ZHONG JI SHI BIOTECHNOLOGY CO LTD
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