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Ophthalmic composition

a technology of ophthalmic composition and composition, which is applied in the field of ophthalmic composition, can solve the problems of general lack of symmetry in the structure of hyperbranched polymers, local irritation, etc., and achieve the effects of improving ophthalmic composition, corneal permeation of active agents, and solubility in water

Inactive Publication Date: 2013-02-28
SENJU USA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The present invention is related to the use of hyperbranched polymers to increase the aqueous solubility and corneal permeability of carbonic anhydrase inhibitors such as Brinzolamide and Dorzolamide, which are used for glaucoma therapy. The inventors found that the addition of hyperbranched polymers to the formulation increased the solubility of the inhibitors in a concentration-dependent manner. The hyperbranched polymers also increased the corneal permeation and partitioning of the inhibitors. Additionally, the inventors found that the use of hyperbranched polymers resulted in no cytotoxicity or eye irritation in in vitro studies.

Problems solved by technology

Consequently, the COSOPT® and TRUSOPT® formulations can lead to local irritation, due to the low pH.
Unlike dendrimers, the structure of hyperbranched polymers generally lacks symmetry, as the base units or monomers used to construct the hyperbranched polymer can be of diverse nature and their distribution is non-uniform.

Method used

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  • Ophthalmic composition
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Examples

Experimental program
Comparison scheme
Effect test

experimental example 1

[0095]pH-solubility profile of Dorzolamide in aqueous solution containing different concentrations of Hyperbranched Polymer (HP) (Lupasol® G20, Lupasol® G 35, Lupasol® PS) and PEG.

Methods

[0096]Suspensions of Dorzolamide hydrochloride in 0.1% (w / v) phosphate buffer solution at pH 5.5, pH 6, pH 6.5, pH 7, pH 7, pH 8 and pH 8.5 were prepared. Similar suspensions were also prepared in aqueous solution containing different concentrations of different HP and PEG with a molecular weight of 8000. A combination of Polysorbate 80 and PEG 8000 was also attempted. The pH was measured accurately with micro-pH electrode (Thermo Scientific). The desired pH was adjusted using either 1 M NaOH or 1 M HCl. The suspension solutions were first stirred for 10 min at room temperature (with heating up to 60° C. for 5 minutes). After allowing the suspensions to equilibrate at room temperature for an additional 30 minutes, the suspension solutions were then sonicated for 10 minutes and finally filtered throu...

experimental example 2

[0101]A simple rheological method for the in vitro assessment of mucin-hyperbranched polymer bioadhesive bond strength.

[0102]A simple viscometric method was adopted to quantify the mucin-polymer bioadhesive bond strength. In order to determine the muco-adhesive properties of commercially available HP called Lupasol® PS, the force of bioadhesion was calculated for different concentrations of HP with porcine gastric mucin at pH 7 in comparison with the market product COSOPT®. Porcine gastric mucin was used as a model mucin. However, since all mucins appear to share general physical, structural, and rheological properties, it is believed that porcine gastric mucin is a satisfactory model for primary evaluation of bioadhesive materials.

Methods

[0103]Brookfield Rotational L VDVE viscometer was employed for all measurements. Spindle with code number 18 was used for all viscosity measurements. A factor of 1.32 was used to convert rpm to shear rate (s−1) as per the manual. A solution of 15% ...

experimental example 3

[0110]Aqueous solubility of Dorzolamide in the presence of Timolol for a novel formulation containing HP (Lupasol® PS) and Polysorbate 80 or a combination of PEG and Polysorbate 80 at pH 5.65 and pH 7.

Methods

[0111]A suspension of Dorzolamide hydrochloride and 0.5% (w / v) Timolol in citrate buffer solution at pH 5.65 was prepared (Control sample). A similar suspension was also prepared in aqueous solution containing 2% (w / v) of HP in citrate buffer of pH 3. The final pH was adjusted to 5.65 with 1 M NaOH after addition of HP (sample 1). The combination of different molecular weight PEG and Polysorbate 80 at pH 5.65 as per Table 3 were also attempted. Table 3 shows all the different test samples suspensions to be prepared in 10 mM citrate buffer.

TABLE 3Different Test formulations prepared at pH 5.65 in citrate buffer, and at pH 7 in phosphate buffer.ContentControl(% v / w)SampleS #1S #2S #3S #4S #5S #6S #7S #8Dorzolamide>2.22>2.22>2.22>2.22>2.22>2.22>2.22>2.22>2.22HClTimolol0.6830.6830.6...

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Abstract

The present invention provides an ophthalmic composition comprising a hyperbranched polyester. The ophthalmic compositions may also comprise carbonic anhydrase inhibitors, wherein the hyperbranched polyester increases the aqueous solubility of the carbonic anhydrase inhibitor, and increases corneal permeation of the active agent. The ophthalmic compositions may also comprise non-ionic surfactants, such as PEG, Polysorbate, HPMC or HEC, and beta-blockers, such as Carteolol, Levobunolol, Betaxolol, Metipranolol, Timolol or Propranolol. The concentration of the hyperbranched polyester in the ophthalmic formulation should be less than or equal to 4% (w / v) in order to avoid any cytotoxic effects on human corneal cells and thus the eye irritation.

Description

FIELD OF THE INVENTION[0001]The present invention relates to an ophthalmic composition comprising a hyperbranched polymer. The hyperbranched polymer of the present invention may be any hyperbranched polymer which is pharmaceutically acceptable, e.g., a hyperbranched polymer with a Polyethyleneimine, Polypropyleneimine or Polyester.BACKGROUND OF THE INVENTION[0002]COSOPT® and TRUSOPT® are commercially available topical ophthalmic solutions developed by Merck for treating an eye disease called glaucoma. In the case of TRUSOPT®, the active ingredient is Dorzolamide exclusively. In the case of COSOPT®, the active ingredients are Dorzolamide and Timolol (beta blocker). Dorzolamide is a carbonic anhydraze inhibitor with the aqueous solubility of 40 mg / mL at pH 4.0-5.5. It is a white to off-white, crystalline powder, which is soluble in water and slightly soluble in methanol and ethanol.[0003]However, these formulations contain 2% (w / v) Dorzolamide, and are prepared at pH 5.65, due to the ...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K47/34A61K31/382A61P27/02A61K47/38A61K47/22A61K31/5377C07C211/02A61K31/542
CPCA61K31/138A61K31/382A61K31/433A61K31/4704A61K31/5377A61K31/542A61K47/34A61K9/0048A61K2300/00A61P27/02A61P27/06A61P43/00A61K31/74
Inventor INOUE, JUNSHAH, TAPAN
Owner SENJU USA
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