Comparative Study On The Methods Of Checking The Stripping Of Four Drugs

Dissolution refers to the rate and extent of active drug dissolving outfrom the solid formulations like tablets or capsules in a predeterminedsolvent[1]. Dissolution test is an effective means to differentiate theextraneous dissolving rate of solid preparations. The second part of ChinesePharmacopoeia2010version contained the stripping method for thedetermination of3, including the first method (Basket method), secondmethod (Paddle method) and the third method (Cup method). As the thirdmethod for the determination of solubility of some small doses of solidpreparation (Cup method) choice, of which the main source is the limit forsensitivity of ultraviolet visible spectrophotometry detection, people willact second (Paddle method) dissolving medium volume900ml (or1000mL)which is reduced to100~250mL, while the corresponding reduction mixingblade (blade diameter from74mm to45mm) and the realization of thesolubility determination. Method of converting it′s lack of rigorousscientific evidence, is also an unpalatable choice. With the development ofmodern analytical techniques, particularly with the popularity of highperformance liquid chromatography, using second method (Paddle method)instead of the third method (Cup method) is not only necessary, but alsofeasible. Fiber-optic dissolutiom test system set solubility test and detectionin one, through fiber optic stripping cup light signal directly into.According to the spectroscopic characteristics of drug selection suitableprobe, the change of the real-time optical signal was caused by dissolvingdrugs during the change of concentration, the realization of the dissolvingdegree measuring software system after processing. Being real-time, online,fast, accurate and process monitoring and other characteristics, is a development direction and objective method for the determination ofsolubility of drugs.HPLC method was used instead of ultraviolet visiblespectrophotometry in this paper. The Cyproheptadine HydrochlorideTablets, Ketotifen Fumarate Tablets and Chlorphenamine Maleate Tabletssolubility determination method was studied, exploring the third method(Cup method) into the second method (Paddle method) can be the line, theobjective evaluation of the intrinsic quality of3street drugs. Fiber-opticreal-time dissolution apparatus, by changing the optical path and thedetection wavelength of Tinidazole Tablets stripping method was for thedetermination of real-time, online, and were compared with thePharmacopoeia method results.The dissolution of Cyproheptadine Hydyochloride Tablets was withthe second method (Paddle method) and with900mL0.1mol·L-1hydrochloric acid as dissolution medium and rotation speed at50r·min-1.No less than80%of the labeled amount of C21H21N·HCl is dissolved in30min. The Agilent Zorbax SB-C18column(150mm×4.6mm,0.5μm) wasused with methanol-0.1%phosphoric acid (every100mL containing0.1gsodium dodecylsulfonate)(75:25) as mobile phase at30℃. The detectingwave length was230nm. The flowrate was1.0ml·min-1. The results showedthat, using the second method (Paddle method,900mL) according to thecurrent drug standard the third method (Cup method,150mL) examinationin accordance with the provisions of the14batches of samples fordetermination of solubility, a total of6batches ware unqualified.The dissolution of Ketotifen Fumarate Tablets was with the secondmethod (Paddle method) and with900mL water as dissolution medium androtation speed at50r·min-1. No less than80%of the labeled amount ofC23H23NO5S is dissolved in30min. The Zorbax SB-C18column(150mm×4.6mm,0.5μm) was used with methanol-water (every1000mLcontaining0.8ml triethylamine solution)(70:30) as mobile phase at40℃. The detecting wave length was299nm. The flowrate was1.0mL·min-1. Theresults showed that, using the second method (paddle method,900mL)according to the current drug standard the third method (cup method,200mL) examination in accordance with the provisions of the6batches ofsamples for solubility determination, both the test results of two methodswere qualified.The dissolution of Chlorphenamine Maleate Tablets was with thesecond method (Paddle method) and with900mL water as dissolutionmedium and rotation speed at50r·min-1. No less than80%of the labeledamount of C23H23NO5S is dissolved in15min. The Zorbax SB-C18column(150mm×4.6mm,0.5μm) was used with0.5%triethylamine solution(Phosphoric acid is adjusted to pH4.0)-acetonitrile-methanol (68:23.8:8.2)as mobile phase at40℃. The detecting wave length was262nm. Theflowrate was1.0mL·min-1. The results showed that, using the secondmethod (Paddle method,900mL) according to the current drug standard thethird method (Cup method,250mL) examination in accordance with theprovisions of the6batches of samples for determination of solubility, atotal of2batches ware unqualified.The improved second method (Paddle method) is simple, accurate,and can be used for Cyproheptadine Hydrochloride Tablets, KetotifenFumarate Tablets and Chlorphenamine Maleate Tablets solubilitydetermination.The Fiber method for the determination of solubility of TinidazoleTablets by selecting the appropriate probe（0.5mm）and the determinationwavelength (314nm) was studied. The results showed that, compared withthe method in Chinese Pharmacopeia, there is no significant differencebetween the13batches of commercially available Tinidazole Tablets (P>0.05). Fiber method can be used for the determination of solubility ofTinidazole Tablets.