Gingko diterpene lactone ophthalmic preparation as well as preparation method and application thereof

A technology of ginkgo diterpene lactone and ophthalmic preparations, which is applied in the field of ginkgo diterpene lactone ophthalmic preparations and its preparation, can solve the problems of increasing the difficulty of treatment, easy recurrence of chorioretinitis, etc., and achieve improved bioavailability, Conducive to storage and drug administration, the effect of solving solubility problems

Active Publication Date: 2020-03-13
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 recurren

Method used

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  • Gingko diterpene lactone ophthalmic preparation as well as preparation method and application thereof
  • Gingko diterpene lactone ophthalmic preparation as well as preparation method and application thereof
  • Gingko diterpene lactone ophthalmic preparation as well as preparation method and application thereof

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 invention provides an application of gingko diterpene lactone in preparation of optic nerve injury drugs, the gingko diterpene lactone is selected from a composition containing ginkgolide A, ginkgolide B and ginkgolide K, and the ratio of ginkgolide A to ginkgolide B to ginkgolide K is (20-40): (50-75): (0.2-5.0). The gingko diterpene lactone provided by the invention has the effects of expanding blood vessels, increasing blood flow and repairing and protecting optic nerves, can be applied to treatment of optic nerve injury, posterior globular neuritis and retinitis, and can also be applied to relief of asthenopia. The gingko diterpene lactone is prepared into an ophthalmic preparation, so that the problem of low solubility of the gingko diterpene lactone is solved, and the contact time of a medicine and cornea is prolonged by increasing the viscosity, so that the bioavailability can be improved.

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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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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