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A temperature-sensitive recombinant human thymosin β4 ophthalmic in situ gel preparation

A temperature-sensitive, in-situ gel technology, which can be used in medical preparations without active ingredients, medical preparations containing active ingredients, and drug combinations, which can solve problems such as side effects, discomfort, and short residence time

Active Publication Date: 2021-11-16
北京汇恩兰德制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] In addition, clinically used ophthalmic preparations are usually solid and liquid. According to statistics, among the ophthalmic preparations that have been marketed, liquid eye drops account for about 70% of ophthalmic preparations. It is accepted by people, but the liquid stays in the eyes for a short time. When dripping into the eyes, you need to raise your head and keep your posture as much as possible, but the liquid still cannot avoid outflow and affect the efficacy of the medicine. At the same time, the liquid may flow into the throat through the eyes Or nasal cavity, causing discomfort and unnecessary side effects, so ophthalmic drugs for gel preparations have been developed. Ophthalmic gels mainly refer to mixing drugs with excipients that can be prepared into gels to obtain suspensions or semi-solids. and emulsion-type latex-like viscous liquids

Method used

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  • A temperature-sensitive recombinant human thymosin β4 ophthalmic in situ gel preparation
  • A temperature-sensitive recombinant human thymosin β4 ophthalmic in situ gel preparation
  • A temperature-sensitive recombinant human thymosin β4 ophthalmic in situ gel preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Example 1: Packing and comparison of different molar ratios (1:10, 1:20, 1:40) of recombinant human thymosin β4 and hydroxypropyl-β-cyclodextrin

[0028] Methods: Recombinant human thymosin β4 cyclodextrin, hydroxypropyl-β-cyclodextrin and recombinant human thymosin β4 prepared according to different ratios were measured by FT-IR and potassium bromide tablet method respectively. IR of fine clathrate and hydroxypropyl-β-cyclodextrin. Weigh 0.3mg~2mg respectively, add potassium bromide as a carrier, grind evenly with a mortar, press into tablets, put it into a Fourier transform infrared spectrometer, the spectral scanning range is 4000~400cm-1, and measure each group infrared absorption spectrum. According to the change of absorption peak of each substance in the scanning range, the formation of clathrate can be judged.

[0029] Weigh the recombinant human thymosin β4 freeze-dried product, hydroxypropyl-β-cyclodextrin, recombinant human thymosin β4-cyclodextrin inclusio...

Embodiment 2

[0031] Example 2: Effects of different ratios of P407 and P188 on the temperature of thermosensitive gel

[0032] Beroxamer 407 is the most studied temperature-sensitive polymer, and it is the most frequently used polymer excipient in the preparation of temperature-sensitive gels. The 20% to 30% solution of Beroxamer 407 has the property of reverse gelling. Beroxamer 188 will not cause gelation when used alone in the concentration range of 10% to 30%, so the two are usually used in combination. By investigating the relationship between the concentration of poloxamer 407 and boloxamer 188 and the gelation temperature, the experimental results show that as the concentration of P407 increases, the gelation temperature decreases. As the temperature increases, the gelation temperature also gradually increases, as shown in Table 1-1.

[0033] Table 1-1 The influence of the composition concentration of poloxamer on the gelling temperature

[0034]

[0035]

[0036] By compari...

Embodiment 3

[0037] Embodiment three: stability comparison

[0038] The degradation rates of recombinant human thymosin β4 aqueous solution, recombinant human thymosin β4 cyclodextrin inclusion complex aqueous solution prepared in different proportions and recombinant human thymosin β4 cyclodextrin inclusion complex thermosensitive gel solution were compared by content determination.

[0039] Results: Through the experimental investigation on the stability of drugs and preparations, the thermosensitive gel of recombinant human thymosin β4 cyclodextrin inclusion compound has good stability within one month, which is more stable than recombinant human thymosin β4, and the degradation rate is lower than that of recombinant human thymosin. Prime β4 is slow. Comparing the preparations with three ratios, the preparation prepared when the ratio is 1:10 is the most stable.

[0040] 0 1 5 10 30 N1：10 100％ 97.6％ 95.7％ 90.4％ 89.6％ N1：20 100％ 98.2％ 96.5％ 89％ 68.4％ ...

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Abstract

The invention discloses a temperature-sensitive ophthalmic in-situ gel preparation with a suitable phase transition temperature, which contains different types of poloxamers, and the preparation contains poloxamer 407 and poloxamer 188. The in situ gel can be administered in a liquid state at room temperature and forms a gel on the surface of the eye. The invention can enhance the stability of the recombinant human thymosin β4 drug and prolong the efficacy and shelf life of the drug.

Description

technical field [0001] The present invention relates to a new dosage form of ophthalmic drug in the field of pharmaceutical technology-temperature-sensitive ophthalmic in-situ gel preparation, specifically, it is a temperature-sensitive polymer aqueous solution, which is in a liquid state at room temperature and can be administered Afterwards, a gel state is formed in the cornea to delay drug elimination and improve local bioavailability. Background technique [0002] Dry eye syndrome refers to the general term for various diseases caused by abnormal tear quality or quantity or abnormal dynamics caused by any reason, resulting in decreased tear film stability, accompanied by ocular discomfort and (or) ocular surface tissue lesions. Common clinical manifestations are eye dryness, which may be accompanied by eye itching, and eye fatigue after long working hours. When the eyes always secrete a sticky white filamentous substance, when the eyelids are pulled open, some white sub...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/06A61K9/08A61K38/22A61K47/69A61K47/10A61P27/02
CPCA61K9/0048A61K9/06A61K9/08A61K38/2292A61K47/10A61K47/6951A61P27/02
Inventor 许松山聂李亚高中镐
Owner 北京汇恩兰德制药有限公司
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