Prepn process of isocollidine for eye

A technology for isoclidine and ophthalmic preparations, which is applied in the field of preparation of isoclidine ophthalmic preparations, can solve problems such as large toxic and side effects, complex eye structure, etc., achieves drug safety, eliminates visual fatigue, and is convenient to use preparations Effect

Inactive Publication Date: 2006-03-01
郭曙平
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Existing ophthalmic preparations of atropine have large toxic and side effects, which limits its application
Isocridine exerts drug effect through systemic administration, but due to the complex structure of the eye, the amount of drug that can reach the eye is very small

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0012] Get isocridine hydrochloride 5g, its parameter is:

[0013] Molecular formula C 20 h 23 NO 4 -HCL

[0014] The molecular weight is 377.5

[0015] Among them, what plays a pharmacological role is isocridine, and its parameters are:

[0016] Molecular formula C 20 h 23 NO 4

[0017] Molecular weight 341.41

[0018] Optical rotation [α] 20 D +195°

[0019] Chemical structure (S)-5,6,6a,7-tetrahydro-1,2,10-trimethoxy-6-methyl-4H-dibenzo[de,g]quinolin-11-ol;

[0020] The isocridine hydrochloride formed by isocridine and hydrochloric acid has better water solubility.

[0021] Add 800mL of water for injection to dissolve; add about 8.5g of osmotic pressure regulator sodium chloride to adjust the osmotic pressure of the solution to about 300mOsm / kg; use 10% hydrochloric acid solution or sodium hydroxide solution to adjust the pH value of the liquid to between 4.0-6.9 Between; add benzalkonium chloride as a bacteriostatic agent, the dosage is 0.005%, if it is packa...

Embodiment 2

[0023] Get isocridine citrate 5.3g, its parameter is:

[0024] Molecular formula (C 20 h 23 NO 4 ) 3 -C 6 h 8 o 7

[0025] Molecular weight 1216.19

[0026] Add 800mL of water for injection to dissolve, add about 8.5g of sodium chloride, and adjust the osmotic pressure of the solution at about 300mOsm / kg; use 10% hydrochloric acid solution or sodium hydroxide solution to adjust the pH value of the liquid between 4.0 and 6.9; Benzalkonium, the dosage is 0.005%, if it is a disposable ophthalmic solution packaging material, it can not be added; stir or heat and stir, add water for injection to 1000mL, sterilize and filter, repack, and get ophthalmic use solution.

Embodiment 3

[0028] Get 5g of isocridine hydrochloride, add 800mL of water for injection to dissolve; add about 8.5g of sodium chloride, and adjust the osmotic pressure of the solution at about 300mOsm / kg; adjust the pH value of the liquid with 10% hydrochloric acid solution or sodium hydroxide solution Between 4.0 and 6.9; add benzalkonium chloride, the dosage is 0.005%; if it is packaged with disposable ophthalmic gel packaging materials, it is not necessary to add; sterilize and filter; add hydroxypropyl methylcellulose 0.2 g, add water for injection to 1000mL; subpackage to obtain ophthalmic gel.

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PUM

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Abstract

The present invention relates to preparation process of isocollidine preparation for eye. Through mixing isocollidine and inorganic acid or organic acid to form soluble isocollidine, dissolving in water, adding osmotic pressure regulator to osmotic pressure 280-320 mOsm/kg, adding hydrochloric acid or sodium hydroxide solution to regulate pH value to 3.0-7.0, adding water via stirring and sterilizing, solution for eye is obtained; or, gel as excipient is further added to obtain gel for eye. The isocollidine preparation for eye may be used to replace atropine, which has serious toxic side effect, for mydriasis, may be used also in regulating eyesight, treating pseudomyopia of teenage and eliminate eye fatigue, and is safe, effective and controllable.

Description

technical field [0001] The invention relates to a preparation method of ophthalmic preparations, in particular to a preparation method of isocridine ophthalmic preparations. Background technique [0002] Before the present invention, isocridine, also known as dextro-isoclidine, is a non-specific smooth muscle antispasmodic drug, which has atropine-like pharmacological effects but no side effects of atropine. In clinical medicine, it is mainly used for the treatment of gastroenteritis, peptic ulcer and peptic pain. The existing atropine ophthalmic preparation has severe side effects, which limits its application. Isocridine exerts drug effect through systemic administration, but due to the complex structure of the eye, the amount of drug that can reach the eye is very small. In order to allow more doses to reach the eyes and achieve an effective therapeutic concentration, the dose must be increased. Thus, various undesirable systemic pharmacological effects are bound to oc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/435A61K9/00A61K9/08A61P27/02
Inventor 王宁馨郭曙平
Owner 郭曙平
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