Evaluating the quality consistency of compound Liangmianzhen buccal tablets during accessories replacement by HPLC/UV related with its active profiling and UV dissolution profiles

Compound Liangmianzhen buccal tablet is a drug that exhibits notable effect on cough and diphtheria.Since the accessory has been changed,along with the difficulties in traditional Chinese drug-evaluation,it is imperative to set up a reliable method to evaluate the drug and ensure the quality consistency.First,the content of the Compound Liangmianzhen buccal tablets reflected by fingerprints were evaluated by the comprehensive linearly quantified fingerprint method and systematic quantified fingerprint method,in which thirteen fingerprint peaks was selected and gallic acid was chosen as the reference peak.The results of the two methods showed all batches in grades 1–3 of above good level with the qualitative similarities of Sl and Sm above 0.90,and the quantitative ones of Pl%and Pm%from 80%–120%,indicating all samples far qualified.Second,the measurement of antioxidant effect based on DPPH free radical clearance test has demonstrated the consistency between the old prescription group and the new ones and further dug up the major antioxidant compositions.Third,dissolution profiles at 190 to 400 nm that evaluate the curative effect consistency were evaluated by f2 and the correlation of the dissolution curve.In conclusion,the combination of 3 kinds of analysis methods can comprehensively assess the quality of the traditional Chinese drug and be served as a routine procedure to evaluate the herbal medicine consistency.

Development of Extended-Release Formulation of Ibuprofen Using Blends of Calcium Silicate and Polyvinyl Pyrrolidone as Tablet Matrix

A tablet matrix system was developed for ibuprofen and the influence of the polymer blend and concentration on the release rate of the drug was evaluated.Tablets containing different concentrations of calcium silicate and PVP(polyvinyl pyrrolidone)were prepared using direct compression and the weight uniformity,crushing strength,friability,drug content uniformity,dissolution profile,and in vitro release kinetics were examined.Formulated tablets were found to be within the official acceptable limits of physical and chemical parameters except for the thickness test that was below the conformation of extended-release tablets.The crushing strength of the tablets was in the range of 2.5 to 5.6 kg/f,the weight variations of the tablets of all the formulation was less than±5%.The friability of all the formulations was in the range of 0.6%to 1.83%.Tablet thickness and diameter was in range of 3.18 mm to 4.48 mm and 12.53 mm to 12.64 mm respectively.Absolute drug contents of all the formulations were found to be in range of 83.50%to 98%.The release kinetic of F3 containing 20 mg of calcium silicate,40 mg of PVP as matrix formers showed the best linearity(r^2=0.6975)with%drug release of 96 showing that combination of the two polymers(20 mg calcium silicate and 40 mg PVP)for use as a matrix former is best for extended-release formulation of ibuprofen.

Formulation Development, in Vitro Evaluation and Stability Study of Aceclofenac Tablet

The objective of the study was to develop film coated tablets of aceclofenac using wet granulation technique. Possible drug-excipient interaction was evaluated by HPLC （high performance liquid chromatography） and FTIR （fourier infrared spectroscopy）. The tablets prepared were assessed for their physicochemical, in vitro dissolution at pH 1.2, 4.5, 6.8 and 7.5 and stability characteristics. Comparison with a commercial aceclofenac product was made in vitro and in vitro studies. There was no interaction between aceclofenac and used excipients. Furthermore, the physicochemical properties of the tablets were satisfactory. The dissolution profile of one of the formulated aceclofenac tablets （D07） was statistically similar （p 〈 0.05） to that of the commercial aceclofenac brand in all the dissolution media. The formulated products ware stable and showed no changes in physical appearance, drug content, or dissolution pattern after storage at 40 ℃/75% RH for 6 months. The results indicate that it is feasible to achieve a stable aceclofenac tablet formulation by using wet granulation technique.

Acetylation of Starch Extracted from Rejected Fruits of <i>Musa ×paradisiaca L.</i>to Obtain a Pharmaceutical Disintegrant

There are many natural sources to obtain pharmaceutical grade starch, one of which is banana (Musa × paradisiaca L.);nevertheless, the use of native starch has certain disadvantages compared to modified starches, whose disintegrating properties are better. In this study, starch extracted from rejected fruits of Musa × paradisiaca L., was modified by acetylation, under the following optimized experimental conditions: 130 mL acetic anhydride, 3 mL sodium hydroxide 50% p/v for each 15 grams of native starch, at 123℃ during 3 hours. The reaction resulted in a modified green banana starch with twice as much swelling capacity compared to unmodified (native) starch;acetylation was verified by infrared spectroscopy and degree of substitution of acetyl groups by back titration. The dissolution profiles of Ibuprofen tablets made with banana modified starch and commercial disintegrant, have no differences according with their similarity factor, f2. It is concluded that it is feasible to use green banana starch modified through acetylation as a pharmaceutical disintegrant.

Preparation of solid pharmaceutical forms of celecoxib with immediate-release and sustained-release by using wet granulation techniques and evaluation of their in vitro characteristics

In the present study,we aimed to formulate matrix tablets of celecoxib with immediate-release(IR)and sustained-release(SR)and evaluate the influence of different types and concentrations of polymers on drug release characteristics in vitro.All formulations were prepared by using the wet granulation technique.One formulation(F5)with the traditional release was composed without release-control polymers.In contrast,four formulations(F1–F4)with prolonged action were designed by using different cellulosic polymers,such as hydroxypropyl methylcellulose polymers(HPMC-K100M and HPMC-Е6),hydroxypropyl cellulose with high viscosity grade(HPCh),carboxymethyl cellulose(CMC),and ethylcellulose(EC-10 cps).All tablet formulations contained sodium lauryl sulfate(SLS),polyvinylpyrrolidone(PVP-k30),microcrystalline cellulose(MCC),and lactose monohydrate.The MCC and PVP-k30 were used in a fixed quantity in all formulations except for formulation F5,which contained 10%and 2.7%of them,respectively.The effects of polymer viscosity grade and its quantity on celecoxib release from two formulations containing the same polymer were studied.Drug release in vitro was evaluated in phosphate buffer(pH=7.4).The amount of celecoxib released in phosphate medium was calculated by preparing a standard series.In vitro profile indicated that formulations F1(HPMC-K100M)and F2(HPMC-E6)extended the drug release for 18 h(82%)and 10 h(96.001%),respectively.Formulations F3and F4 released 72.09%and 59.8%of their contents during 18 h,respectively,and thus their effects could last for more than a day.However,IR formulation(F5)released more than 90%of its content within 1–2 h.MS Excel was used to analyze the dissolution profile data for drug release kinetics,such as first-order,Zero-order,Higuchi,and Korsmeyer-Peppas models.The release mechanism of all formulations was CaseⅡrelaxation release.This study showed that cellulosic derivative polymers could successfully prolong IR of matrix tablet formulation.

Crystalline inclusion complexes formed between the drug diflunisal and block copolymers

The solid form of drugs plays a central role in optimizing the physicochemical properties of drugs,and new solid forms will provide more options to achieve the desirable pharmaceutical profiles of drugs.Recently,certain drugs have been found to form crystalline inclusion complexes（ICs） with multiple types of linear polymers,representing a new subcategory of pharmaceutical solids.In this study,we used diflunisal（DIF） as the model drug host and extended the guest of drug/polymer ICs from homopolymers to block copolymers of poly（ethylene glycol）（PEG） and poly（s-caprolactone）（PCL）.The block length in the guest copolymers showed a significant influence on the formation,thermal stability and dissolution behavior of the DIF ICs.Though the PEG block could hardly be included alone,it could indeed be included in the DIF ICs when the PCL block was long enough.The increase of the PCL block length produced IC crystals with improved thermal stability.The dissolution profiles of DIF/block copolymer ICs exhibited gradually decreased aqueous solubility and dissolution rate with the increasing PCL block length.These results demonstrate the possibility of using drug/polymer ICs to modulate the desired pharmaceutical profiles of drugs in a predictable and controllable manner.

Drug-polymer inclusion complex as a new pharmaceutical solid form

The solid forms of drugs play a central role in controlling their physicochemical properties and consequently the bioavailability. Multiple types of drug solid forms have been developed to achieve the desirable pharmaceutical profiles, but new solid forms will provide more options for the solid-state property optimization and hence are highly desirable. This review focuses on a new pharmaceutical solid form, drug-polymer inclusion complexes （ICs）, and summarizes their structural features, structure- property relationships, as well as potential pharmaceutical applications