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Injectable long-acting local anesthetic semi-solid formulations

A semi-solid and gel technology, applied to non-active ingredient medical preparations, active ingredient-containing medical preparations, anti-inflammatory agents, etc., can solve the problem of poor repeatability, complicated and expensive manufacturing process, and drug release kinetics poor study, etc.

Active Publication Date: 2021-08-17
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

[0007] 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 known as "burst release") in the early post-injection period, and the drug release kinetics are not good and the reproducibility is poor

Method used

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

Examples

Experimental program
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Effect test

preparation example Construction

[0100] Preparation of castor oil semi-solid gel preparation

[0101] The castor oil semi-solid gel formulation containing active substances of the present invention can be prepared by directly mixing castor oil and a gelling agent, 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 agent and castor oil into solution and dissolve or grind the active drug by any mechanical means to form a clear solution or a 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.

[0102] Semisolid gel formulation composition comprising active ingredient

[0103] Preferred active ingredients for topical d...

Embodiment 1

[0146] Example 1. SUP D

[0147] 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.

[0148] 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.

[0149] Table 3: Castor Oil and SUP D Ratio Study

[0150] Sample serial number Castor oil (g) SUP D(g) Bupivacaine (mg...

Embodiment 2

[0151] Example 2. SUP CM

[0152] 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.

[0153] Since SUP CM has a lower melting point, SUP CM takes longer than SUP DM to initiate and complete gelation.

[0154] 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.

[0155] Table 4: Castor Oil and SUP CM Ratio Study

[0156] Sample serial number Castor oil (g) SUP CM(g) Bupivacaine (mg) SUP CM F01 1.64...

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Abstract

The invention discloses an injectable long-acting semi-solid gel preparation which comprises a mixture containing ricinoleic acid triglyceride and a gelling agent and an active ingredient, and the active ingredient comprises loteprednol, latanoprost, celecoxib, triamcinolone acetonide or betamethasone. The pharmaceutical composition provided by the invention is a biologically erodible semisolid carrier gel preparation, has the advantage of sustained release of drugs, and does not have an obvious burst release phenomenon.

Description

technical field [0001] The invention provides an injectable long-acting semi-solid gel preparation, the pharmaceutical composition comprising loteprednol, latanoprost, celecoxib, triamcinolone acetonide and / or Tamethasone, the semi-solid lipid carrier comprising a triglyceride of ricinoleic acid and a gelling agent. [0002] Background of the invention [0003] Controlled-release formulations for topical administration may be used specifically for the treatment of inflammation and pain resulting from disease or tissue damage. The drug delivery carrier is usually composed of a polymer carrier matrix, and the drug is released through the degradation of the matrix and the diffusion of the drug to achieve the purpose of controlled release. The active ingredient is usually embedded or encapsulated in microspheres or microparticles, which can be applied in the form of implants by injection or infusion into the surgical cavity. [0004] Researchers have done extensive research wor...

Claims

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Application Information

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IPC IPC(8): A61K45/00A61K45/06A61K31/635A61K31/58A61K31/573A61K31/56A61K31/5575A61K47/14A61K9/06A61K9/00A61P29/00A61P19/02A61P35/00A61P11/02A61P37/08A61P25/00A61P19/08A61P37/02A61P27/02A61P11/04
CPCA61K45/00A61K45/06A61K31/635A61K31/58A61K31/573A61K31/56A61K31/5575A61K47/14A61K9/06A61K9/0019A61P29/00A61P19/02A61P35/00A61P11/02A61P37/08A61P25/00A61P19/08A61P37/02A61P27/02A61P11/04
Inventor 沈惠荣
Owner HUZHOU HUI ZHONG JI SHI BIOTECHNOLOGY CO LTD
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