N-[2-(2-Chloro-phen-yl)-2-hydroxy-ethyl]propan-2-aminium hemioxalate.

The asymmetric unit of the title compound, C(11)H(17)ClNO(+)·0.5C(2)O(4) (2-), consists of one N-[2-(2-chloro-phen-yl)-2-hydroxy-ethyl]propan-2-ammonium cation and one-half of a centrosymmetric oxalate anion. In the cation, the C/C/N plane of the ethyl-ammonium group is almost perpendicular to the benzene ring, with a dihedral angle of 88.72 (17)°. In the crystal structure, the two components are connected by O-H⋯O and N-H⋯O hydrogen bonds, forming a supra-molecular tape along the a axis. Between the tapes, a C-H⋯O inter-action is observed.

[Determination of three formulations of pilocarpine in rabbit ocular aqueous by RP-HPLC].

OBJECTIVE: To develop an RP-HPLC method for assay of pilocarpine in rabbit ocular aqueous humor. METHODS: The RP-HPLC method was performed on a column of ODS-C(18) with the mobile phase consisting of 0.5% of triethylamine (TEA) of phosphate solutions (10 mmol/L, pH 2.5) and acetonitrile (98/2,v/v). The detection wavelength was 215 nm and flow rate was 1.0 ml/min. Ninety albino rabbits were divided into 3 groups (30 in each):group 1 received 50 microl of eye drops containing 1% generic pilocarpine, group 21% mixture pilocarpine solution consisting of aqueous sample and liposome and group 31% liposome pilocarpine, respectively. The aqueous humor was withdrawn at 5, 10, 30, 40, 60, 90, 120, 180, 240 and 360 min. Pilocarpine was extracted from aqueous humor with dichloromethane. RESULT: The linear calibration curve was obtained in the concentration range of 0.1 - 20 microg/ml. The average recovery was (68.1+/-2.7)% (n=9). Inter-day and intra-day RSD were 4.33% and 2.87%, respectively. In three formations 1% liposome pilocarpine was the best for the areas under curve and measurable amounts. CONCLUSION: The RP-HPLC method is simple and reliable for pilocarpine measurement in ocular aqueous. Liposome formulation can significantly increase the bioavailability of pilocarpine in ocular aqueous.

[Action of miosis of 1% pilocarpine liposome in rabbits].

OBJECTIVE: To compare the action of miosis of 1% pilocarpine liposome with 1% pilocarpine solution in rabbits. METHODS: 18 white rabbits were randomly divided into 3 groups. Test group received 1% pilocarpine liposome, positive control group received 1% pilocarpine solution, negative control group received liposome. Each eye drop instilled into left eye of rabbits and sterile saline solution instilled into right eye as control. The pupil diameter was measured at time intervals of beginning, 0.25, 0.5, 1, 2, 3, 4, 5, 7 hours. RESULTS: The mean pupil diameter change of 3 groups in both eyes was not significant (P > 0.05) at beginning. The strongest action of miosis took place 0.25 h in positive control group and 0.5 h in test group after instillation. The dilation of pupil in both groups took place 1 h and 3 h, and the restoration of pupil in both groups took place at 5 h and 7 h. The mean pupil diameter of negative control group was not significant in seven hours. CONCLUSIONS: The results suggest that 1% pilocarpine liposome improves the bioavailability and prolong the duration of its action.

[Peripheral iridoplasty with doubled-frequency Nd:YAG laser as treatment for angle-closure glaucoma]

OBJECTIVE: To examine the effects and safety of doubled-frequency Nd:YAG laser peripheral iridoplasty(LPI) for angle-closure glaucoma (ACG) with relieving the pupillary block. METHODS: Thirty-seven eyes of 29 patients of ACG with mean intraocular pressure (IOP) of (33.5+/-9.3)mmHg, were treated by LPI. In the follow-up of 5 approximate, equals 35 months, the IOP, angle and complications from LPI were examined. RESULTS: The mean IOP of the patients was reduced to (17.2+/-5.3)mmHg (P<0.0001). Thirty-three eyes of 25 patients, who had negative of dark room provocative test, maintained the angle opened without adjunctive antiglaucoma treatment. Four eyes of 4 patients continued to developed angle closure and had a high IOP. CONCLUSION: Peripheral iridoplasty doubled frequency Nd:YAG laser is a safe and effective method for treatment of ACG.