Dynamic release measuring device for microsphere preparation
By designing a dynamic release assay device for microsphere formulations, which uses a squeezing rod and a flexible squeezing block to simulate in vivo mechanical tension, the problem that traditional devices cannot simulate in vivo release behavior is solved, enabling more accurate release testing and improving R&D efficiency and experimental reliability.
Patent Information
- Application Number
- CN202422935630.X
- Authority / Receiving Office
- CN · China
- Patent Type
- Utility models(China)
- Current Assignee / Owner
- Filing Date
- 2024-11-29
- Publication Date
- 2026-01-02
- Estimated Expiration
- 2034-11-29
AI Technical Summary
Traditional microsphere formulation release testing devices cannot effectively simulate the mechanical tension caused by muscle and joint movements in the body, resulting in a large deviation between experimental results and actual conditions, which affects research and development efficiency and clinical application effectiveness.
A device for measuring the dynamic release of microsphere formulations was designed, comprising a dissolution cup, a squeezing rod, and a release assembly. By cooperating with the flexible squeezing block and the squeezing rod, the mechanical tension generated by the movement of muscles and joints in the body is simulated to achieve dynamic release testing of microsphere formulations.
It can more accurately simulate the release environment of microsphere formulations in vivo, improve the efficiency of drug formulation development, reduce the difficulty and cost of experimental operation, and is suitable for microsphere formulation release testing in joint cavities and other moving parts.
Smart Images
Figure CN223756728U_ABST
Abstract
Description
TECHNICAL FIELD
[0001] The utility model relates to an experimental device, specifically a kind of microsphere preparation dynamic release determination device. BACKGROUND
[0002] In the research and development of pharmaceutical preparations, microsphere preparations are highly concerned due to their unique sustained-release and targeting properties. However, the release behavior of microsphere preparations in vivo is influenced by multiple factors, among which the most critical factor is mechanical tension. In particular, in the movement parts such as joint cavity, the release behavior of microsphere preparations will be significantly affected by the mechanical tension generated by joint movement.
[0003] Traditional microsphere preparation release testing devices, such as static dissolution test devices, can simulate the dissolution of microsphere preparations by dissolution medium, but cannot effectively simulate the mechanical tension caused by muscle and joint movement in vivo, thus cannot accurately reflect the real release behavior of microsphere preparations in vivo. This limitation leads to a large deviation between experimental results and actual situation, which further affects the research and development efficiency and clinical application effect of microsphere preparations. SUMMARY
[0004] The purpose of the utility model is to provide a kind of microsphere preparation dynamic release determination device to solve the problem that traditional static dissolution test device cannot simulate the influence of mechanical tension of muscle and joint movement in vivo on the release behavior of microsphere preparations.
[0005] The utility model is realized as follows: a kind of microsphere preparation dynamic release determination device, its structure includes dissolution cup, extrusion rod and the release component being arranged in the dissolution cup, the dissolution cup includes cup body and cup cover, and the through hole and sampling hole for extrusion rod insertion are opened on cup cover;The release component includes two uprights being symmetrically arranged on the inner bottom of the cup body, two fixed rings and a release ring being commonly penetrated on the two uprights, flexible extrusion block being penetrated in the fixed ring and screen mesh cage being arranged in the release ring;Release ring is located between two fixed rings, the bottom of flexible extrusion block on upper fixed ring abuts on the top surface of screen mesh cage, the top of flexible extrusion block on lower fixed ring abuts on the bottom surface of screen mesh cage, and the bottom of flexible extrusion block on lower fixed ring abuts on the inner bottom of cup body.
[0006] Further, the release ring includes upper convex disc and lower concave disc, a downward extending recess is formed in the upper end center of the concave disc, a downward extending convex part is provided in the lower end center of the convex disc, and the shape of the recess matches the convex part.
[0007] Further, the height of the convex part is less than the depth of the recess, the screen mesh cage is arranged between the recess and the convex part, and the diameter of the screen mesh cage is adapted to the diameter of the recess and the convex part.
[0008] Further, bolt through holes are formed on the convex disc and the concave disc, and bolts are inserted through the bolt through holes.
[0009] Further, the mesh size of the mesh cage is smaller than the diameter of the microspheres.
[0010] Further, the dissolution cup and the extrusion rod are provided in plurality, the upper end of the extrusion rod is connected with a connecting plate, and a telescopic driving element is connected to the connecting plate.
[0011] Further, the telescopic driving element is a pneumatic cylinder, an electric rod, a hydraulic cylinder or a servo motor.
[0012] Further, the flexible extrusion block is a sponge.
[0013] The extrusion rod and the flexible extrusion block are used in cooperation, the mechanical tension generated by the muscle and joint movement in the body can be simulated, the release environment of the microsphere preparation in the body can be more accurately simulated, and the problem that the traditional test device cannot simulate the influence of the mechanical tension generated by the muscle and joint movement in the body on the release behavior of the microsphere preparation is solved. BRIEF DESCRIPTION OF DRAWINGS
[0014] Figure 1 is a structural schematic view of the utility model.
[0015] Figure 2 is a structural schematic view of the dissolution cup.
[0016] Figure 3 is a structural schematic view of the extrusion rod. Figure 2 is a structural schematic view of the release ring.
[0017] Figure 4 is a sectional view of the extrusion rod. Figure 2
[0018] Figure 5 is an exploded view of the release ring.
[0019] Figure 6 is a sectional view of the release ring. Figure 5
[0020] In the figure: 1, cup body, 2, cup cover, 3, stand, 4, fixed ring, 5, release ring, 6, flexible extrusion block, 7, convex disc, 8, concave disc, 9, screen cage, 10, sampling hole, 11, extrusion rod, 12, connecting plate, 13, telescopic drive element, 14, bolt through hole. DETAILED DESCRIPTION
[0021] As Figure 1 and Figure 2 shown, the utility model includes a dissolution cup, an extrusion rod 11 and a release assembly arranged in the dissolution cup, the dissolution cup includes a cup body 1 and a cup cover 2 covering the cup body. The dissolution cup is made of glass or acrylic material, has the characteristics of acid and alkali resistance, is not easy to erode and break. The inner diameter of the dissolution cup is 50±0.5 mm, and the height is 85±0.5 mm. The height of the cup cover 2 is 60±0.5 mm, the outer diameter is 55±0.5 mm, and the inner diameter is 50.5±0.5 mm. A through hole is formed in the middle of the cup cover 2 for the extrusion rod 11 to pass through, the extrusion rod 11 is arranged in the through hole, and a sampling hole 10 is also formed in the cup cover 2, which is used for measurement and sampling. The size of the sampling hole 10 is very small to reduce the volatilization of the solution in the cup body 1. The release assembly is used to simulate the pressure environment in the body.
[0022] As Figure 3 and Figure 4As shown, the release assembly includes two upright columns 3 symmetrically arranged on the inner bottom of the cup body 1, two fixed rings 4 and a release ring 5 commonly threaded on the two upright columns, a flexible extrusion block 6 threaded in the fixed ring 4, and a screen cage 9 arranged in the release ring 5. The release ring 5 is located between the two fixed rings 4, and a central hole is formed in each of the two fixed rings 4. A release hole corresponding to the central hole is formed in the release ring 5, and the central hole and the release hole are both through holes. The flexible extrusion block 6 is threaded in the central hole of the fixed ring 4, and the thickness of the flexible extrusion block 6 is greater than the thickness of the fixed ring 4. The fixed ring 4 is used to fix the flexible extrusion block 6, and the flexible extrusion block 6 is in interference fit with the fixed ring 4. The screen cage 9 is arranged at the release hole of the release ring 5, and the screen cage 9 is used to hold the microsphere preparation. The screen cage 9 is in contact with the two flexible extrusion blocks 6 respectively. The bottom of the flexible extrusion block of the upper fixed ring protrudes into the inner top of the release hole of the release ring 5 and abuts against the top surface of the screen cage 9, so as to provide a pressure F1 to the screen cage 9. The top of the flexible extrusion block of the lower fixed ring protrudes into the release hole of the release ring 5 and abuts against the bottom surface of the screen cage 9, so as to relieve the extrusion force caused by the compression of the flexible extrusion block of the upper fixed ring and provide a counterforce F2. Before the experiment, the specific pressure value F (F = F1-F2) is measured by using a pressure sensor, so as to adjust the pressure value required by the experiment. The upper end of the flexible extrusion block 6 of the upper fixed ring is in contact with the lower end of the extrusion rod 11, and the flexible extrusion block 6 of the upper fixed ring uniformly transmits the pressure applied by the extrusion rod 11 to the screen cage 9. The bottom of the flexible extrusion block of the lower fixed ring is in contact with the inner bottom of the dissolution cup and is responsible for maintaining the stability of the bottom of the release ring. The extrusion rod 11 repeatedly extrudes the screen cage 9, so as to simulate the diffusion process of the microsphere preparation under the extrusion force of the joint cavity and the impact of the synovial fluid when the joint is flexed and extended.
[0023] Two grooves are formed in the inner bottom of the cup body 1, and the lower ends of the two upright columns 3 are inserted into the grooves, so that the release assembly is stably fixed in the cup body 1. A through hole matched with the upright column is formed in each of the fixed ring 4 and the release ring 5, and the two fixed rings are located above and below the release ring 5 respectively. The fixed ring 4 is 20 mm high, 20 mm in inner diameter, and 49 mm in outer diameter.
[0024] In the embodiment, the flexible extrusion block 6 is a sponge or a compressible sponge. The sponge above is 120D in hardness, and the sponge below is 90D in hardness. The flexible extrusion block 6 can also be rubber, silica gel, elastic plastic, etc. Before the dissolution medium is added, the upper and lower placed compressible sponges should be fully saturated in the dissolution medium in advance, so as to prevent the sponge from affecting the determination of the release medium due to water absorption,
[0025] As Figure 5 and Figure 6As shown, the release ring 5 includes an upper convex disc 7 and a lower concave disc 8, a release hole is formed in the middle of the convex disc 7 and the concave disc 8, a downward extending recess is formed at the upper end of the concave disc 8, a downward extending convex part is provided at the lower end of the convex disc 7, the recess is located in the middle of the concave disc 8, the convex part is located in the middle of the convex disc 7, and the size of the release hole is smaller than that of the convex part and the recess. The shape of the recess matches that of the convex part, the screen cage 9 is arranged between the convex part and the recess, the height of the convex part is smaller than the depth of the recess to leave space for placing the screen cage 9. The diameter of the screen cage 9 is adapted to the diameter of the release hole of the convex disc 7 and the concave disc 8. The pore size of the screen cage 9 is smaller than the diameter of the released microspheres. In this embodiment, the screen cage 9 is made of 800 mesh nylon net. The mesh nylon net with the required mesh number can be selected according to the specific experimental needs.
[0026] Corresponding bolt through holes 14 are formed in the convex disc 7 and the concave disc 8, bolts are threaded through the bolt through holes 14, and the convex disc 7 and the concave disc 8 are fixed by the bolts. The convex disc 7 and the concave disc 8 can also be connected by a buckle (not shown), a groove and a protrusion, so that they can be clamped and fixed to each other. The convex disc 7 and the concave disc 8 can also be connected by screw threads (not shown), an external thread is formed on the convex disc 7, an internal thread matched with the external thread is formed on the inner wall of the concave disc 8, and the two are screwed and fixed by the screw threads.
[0027] There are several dissolution cups and extrusion rods 11. The upper end of the extrusion rod 11 is connected with a connecting plate 12, the connecting plate 12 is connected with a telescopic driving element 13, the telescopic driving element 13 drives the connecting plate 12 and the extrusion rod 11 to ascend and descend, and the release degree of the microsphere preparation in multiple dissolution cups can be tested at the same time, thereby improving the efficiency and accuracy of the test. The telescopic driving element 13 can be a pneumatic cylinder, an electric rod, a hydraulic cylinder, a servo motor, etc.
[0028] A pressure head is arranged at the lower end of the extrusion rod 11, the size of the pressure head is the same as that of the sponge, and in this embodiment, the pressure head is a nut (not shown) connected to the lower end of the extrusion rod 11. The extrusion rod 11 and the nut are made of stainless steel, which has good stability and avoids possible reaction with the medicament.
[0029] In use, the dissolution cup is placed in a constant temperature water bath to maintain a constant temperature environment. This helps to simulate the physiological conditions in the human body and improves the accuracy and reliability of the experiment. Then, the screen cage 9 containing the microsphere preparation is placed in the release hole of the release ring 5, and is fixed by the fixing ring 4 and the flexible extrusion block 6. Next, the telescopic driving element 13 is set to an appropriate telescopic speed and stroke. After the telescopic driving element 13 is started, the extrusion rod 11 will repeatedly ascend and descend, and the screen cage 9 is extruded and released by the flexible extrusion block 6, thereby simulating the extrusion and release process of the microsphere preparation by the joint movement. During the test, samples can be taken through the sampling hole 10 at regular intervals to monitor the release of the microsphere preparation.
Claims
1. A microsphere formulation dynamic release assay device, characterized in that, The dissolution cup, the extrusion rod and the release assembly arranged in the dissolution cup, the dissolution cup comprises a cup body and a cup cover, a through hole for inserting the extrusion rod and a sampling hole are opened on the cup cover; the release assembly comprises two vertical columns symmetrically arranged on the inner bottom of the cup body, two fixed rings and a release ring commonly arranged on the two vertical columns, flexible extrusion blocks arranged in the fixed rings and a screen cage arranged in the release ring; the release ring is located between the two fixed rings, the bottom of the flexible extrusion block on the upper fixed ring abuts against the top surface of the screen cage, the top of the flexible extrusion block on the lower fixed ring abuts against the bottom surface of the screen cage, and the bottom of the flexible extrusion block on the lower fixed ring abuts against the inner bottom of the cup body.
2. The microsphere formulation dynamic release assay device of claim 1, wherein, The release ring comprises an upper convex disc and a lower concave disc, a downward extending recess is arranged at the center of the upper end of the concave disc, a downward extending convex part is arranged at the center of the lower end of the convex disc, and the shape of the recess matches that of the convex part.
3. The microsphere formulation dynamic release assay device of claim 2, wherein, The height of the convex part is less than the depth of the recess, the screen cage is arranged between the recess and the convex part, and the diameter of the screen cage is adapted to the diameter of the recess and the convex part.
4. The microsphere formulation dynamic release assay device of claim 2 or 3, wherein, Corresponding bolt through holes are arranged on the convex disc and the concave disc, and bolts are arranged in the bolt through holes.
5. The microsphere formulation dynamic release assay device of claim 3, wherein, The aperture of the screen cage mesh is smaller than the diameter of the released microspheres.
6. The microsphere formulation dynamic release assay device of claim 1, wherein, The dissolution cup and the extrusion rod are both several, the upper end of the extrusion rod is connected with a connecting plate, and a telescopic driving element is connected to the connecting plate.
7. The microsphere formulation dynamic release assay device of claim 6, wherein, The telescopic driving element is a gas cylinder, an electric rod, a hydraulic cylinder or a servo motor.
8. The microsphere formulation dynamic release assay device of claim 1, wherein, The flexible extrusion block is a sponge.