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Ocular delivery of drugs

A drug and composition technology, applied in the field of eye delivery of drugs, can solve problems such as limited shelf life

Inactive Publication Date: 2017-08-29
纳诺莫里克斯有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, these compositions are prone to droplet coalescence, which limits their shelf life

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0091] Materials and methods

[0092] polymer

[0093] N-palmitoyl-N-monomethyl-N,N-dimethyl -N,N,N-Trimethyl-6-O-ethylene glycol chitosan (GCPQ). The GCPQ used in the experiment contained 20.51 Mol% palmitoyl / monomer unit, 11.93 Mol% quaternary ammonium group / monomer unit, and a molecular weight of 9.13 kDa.

[0094] CSA composition

[0095] Compositions comprising CSA were prepared as follows. Phosphate buffered saline (pH=7.4, 20 mL) was added to the weighed polymer sample and the weighed drug sample. The initial polymer / drug weight ratio was 7.5:1, and the drug content was adjusted to concentrations of 0.05%, 0.08%, and 0.1% w / v. The liquid mixture was vortexed for 2 minutes to ensure complete mixing, followed by high pressure homogenization (Avestin Emulsiflex, GCT Technology, UK) at 20,000 psi for 30 cycles.

[0096] CsA preparation stability

[0097] For stability analysis, aliquots of the formulation were stored in triplicate at refrigerated (2-3°C), room temper...

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Abstract

The present invention relates to an aqueous composition comprising a macrolide immunosuppressant drug at a concentration of less than 2% w / v and an amphiphilic carbohydrate compound having a molecular weight in the range 1-50kDa, for use in treatment of an eye disorder by topical application to the eye, wherein the amphiphilic carbohydrate compound is present at a concentration below 10% w / v of the composition. A preferred carbohydrate compound is quaternary ammonium palmitoyl glycol chitosan (GCPQ). Pharmaceutical compositions and methods of treatment are also provided. The treatment may be for instance dry eye syndromes (DES), vernal keratoconjunctivitis (VKC), eczema, atopic keratoconjunctivitis (AKC), Sj gren syndrome, post-operative refractive surgery, corneal transplant or contact lens intolerance.

Description

technical field [0001] The present invention relates to new systems for ocular delivery of drugs. Background technique [0002] Topical ophthalmic formulations are commonly used to treat conditions affecting the front of the eye including, but not limited to, glaucoma, iritis, conjunctival eye infections, and dry eye syndrome (DES). DES refers to a family of ocular surface disorders with multiple etiologies characterized by chronic ocular dryness of the cornea and conjunctiva caused by an improper balance of tear production and drainage or abnormalities in tear composition. In addition, inflammation of the ocular surface often occurs. [0003] T lymphocyte-mediated inflammatory responses have been considered as a possible cause of DES. Therefore, cyclosporine (CSA) and tacrolimus (TAC) have emerged in recent years as local immunosuppressants for the treatment of DES. Such treatment has been shown to reduce the immune response and has also been shown to increase tear produ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K47/36A61K38/13
CPCA61K9/0048A61K9/08A61K38/13A61K47/36A61P27/02A61P37/06A61P37/08
Inventor I·乌切格布A·沙茨林L·卡普雷托
Owner 纳诺莫里克斯有限公司
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