Timolol maleate eye drops and preparation process

Abstract

The invention discloses timolol maleate eye drops and a preparation process. The timolol maleate eye drops are prepared from the following raw materials in parts by weight: 10 to 12 parts of dispersion liquid C, 5 to 7 parts of timolol maleate nanoparticles, 20 to 30 parts of a water-based solvent, 4 to 6 parts of a buffering solution, 100 to 200 parts of a diluting agent and 0.01 to 0.03 part ofbenzalkonium chloride. The timolol maleate eye drops are prepared through the following steps: step 1, preparing the dispersion liquid C; step 2, adding the timolol maleate nanoparticles into the dispersion liquid C prepared by step 1 to prepare a nano mixed solution; and step 3, mixing a glucose solution with the mass percent of 8 percent and the nano mixed solution obtained by step 2, and carrying out vacuum freeze-drying for 8h to 10h; after freeze-drying is finished, adding a solid obtained by the freeze-drying into the buffering solution and the diluting agent; raising the temperature to80 DEG C, and keeping the heat for 30min; then cooling to 40 to 50 DEG C; adding the benzalkonium chloride and stirring and dissolving; filtering by a filter element; filling and sealing.

Description

technical field [0001] The invention belongs to the technical field of preparation of pharmaceutical preparations, and in particular relates to timolol maleate eye drops and a preparation process. Background technique [0002] Glaucoma is an eye disease characterized by optic neuropathy and loss of visual function. Elevated intraocular pressure is the main blinding factor of glaucoma, and drug therapy is the main treatment. At present, the clinical medicine for glaucoma is mainly based on eye drops, including β-receptor antagonists, prostaglandin analogs, carbonic anhydrase inhibitors, adrenergic receptor agonists, choline receptor agonists and optic nerve protection drugs, etc. . The drugs for clinical treatment of glaucoma are still mainly β-receptor antagonists with low price and clear curative effect, among which timolol maleate is the most widely used clinical drug. [0003] Timolol maleate is a non-selective β-adrenoceptor blocker, has no obvious endogenous sympathe...

AI Technical Summary

Problems solved by technology

However, due to the impact of blinking and tear secretion, the retention time of ordinary eye drops in the eyes is short after administration, and the absorbed drug amount usually only accounts for a very small part of the administered dose. The drug dose is usually high, and generally requires repeated administration. , prone to obvious systemic side effects, such as bradycardia, arrhythmia, bronchospasm, etc., and poor patient compliance