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Ginkgo diterpene lactone ophthalmic preparation and its preparation method and application

A technology of ginkgo diterpene lactone and ophthalmic preparations, applied in the field of ginkgo diterpene lactone ophthalmic preparations and preparation thereof, can solve the problems of increasing the difficulty of treatment, easy recurrence of chorioretinitis and the like, and achieves improved bioavailability, Solubility problem and the effect of relieving visual fatigue

Active Publication Date: 2022-04-22
JIANGSU KANION PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because chorioretinitis is prone to recurrence, it increases the difficulty of treatment

Method used

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  • Ginkgo diterpene lactone ophthalmic preparation and its preparation method and application
  • Ginkgo diterpene lactone ophthalmic preparation and its preparation method and application
  • Ginkgo diterpene lactone ophthalmic preparation and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1～7

[0053] The prescription composition is shown in Table 2, and the balance is water for injection. The ginkgolides in Examples 1 to 7 are ginkgolide compositions, including ginkgolides A, B, and K, and the dosage ratio is ginkgolide A: ginkgolide B: Ginkgolide K=36:60:3.6 (w / w).

[0054] Table 2 Ginkgolide temperature-sensitive ophthalmic gel prescription (by mass percentage)

[0055]

[0056]

[0057] Examples 1-7 Preparation method: Weigh the ginkgolide composition and borax in the prescribed amount, add water for injection, heat and stir at 70°C to dissolve; filter, put the filtrate in a refrigerator at 4°C to cool, and slowly add poiroxine under magnetic stirring Sham 407 and poloxamer 188 were made to moisten and disperse, placed in a refrigerator at 4°C for more than 24 hours, fully swelled to obtain a clear and uniformly dispersed solution 1, and another borax was added to the same amount of water for injection to dissolve, and the magnetic Slowly add poloxamer P40...

Embodiment 8～14

[0067] The composition of the prescription is shown in Table 4, and the balance is water for injection, wherein the ginkgolides in Examples 8 to 12 are ginkgolides. The composition includes ginkgolides A, B, and K, and the dosage ratio is ginkgolides A: ginkgolides B: ginkgolide K=36:60:3.6 (w / w); the ginkgolide in Example 13 is ginkgolide B; the ginkgolide in Example 14 is ginkgolide K.

[0068] Table 4 Ginkgolide temperature-sensitive ophthalmic gel prescription (by mass percentage)

[0069]

Embodiment 8～10

[0070] Embodiment 8~10 preparation method (same as embodiment 1~7).

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Abstract

The present invention proposes the application of a ginkgo diterpene lactone in the preparation of drugs for optic nerve injury, the ginkgo diterpene lactone is selected from the composition comprising ginkgolides A, B and K, wherein, ginkgolide A: ginkgolide Lactone B: Ginkgolide K = (20-40): (50-75): (0.2-5.0). The ginkgo diterpene lactone proposed by the present invention has the functions of dilating blood vessels, increasing blood flow, repairing and protecting the optic nerve, and can be applied to treating optic nerve injury, retrobulbar neuritis, and retinitis, and can also be applied to relieve visual fatigue. The invention prepares the ginkgo diterpene lactone into an ophthalmic preparation to overcome the problem of low solubility of the ginkgo diterpene lactone, and prolongs the contact time between the medicine and the cornea by increasing the viscosity, thereby improving the bioavailability.

Description

technical field [0001] The invention relates to the technical field of medicines, in particular to a ginkgo diterpene lactone ophthalmic preparation and a preparation method and application thereof. Background technique [0002] Treatment and functional recovery after optic nerve injury is a historical problem in the medical field. Due to the lack of microenvironment required for nerve repair and regeneration after optic nerve injury as part of the central nervous system. Effective neuroprotection, prevention of neuronal death and promotion of neuronal repair are therefore crucial. At present, clinically, due to the lack of timely and effective treatment measures, about half of the patients eventually lose their vision. [0003] Retrobulbar optic neuritis is one of the frequently occurring diseases in ophthalmology, which can lead to irreversible damage to vision or even blindness. It is more common in inflammation of the optic nerve center and mainly invades the papillary...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/365A61K9/06A61K9/08A61K47/40A61P25/00A61P27/02
CPCA61K31/365A61K9/0048A61K9/06A61K9/08A61K47/40A61P25/00A61P27/02A61K2300/00
Inventor 肖伟刘文君杨彪王奎龙曹亮王振中
Owner JIANGSU KANION PHARMA CO LTD
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