Formulasi Fast Disintegrating Tablet Ekstrak Etanol Daun Salam dengan Kombinasi Crospovidone dan Croscarmellose Sodium sebagai Superdisintegrants

Pengembangan formulasi ekstrak daun Salam (Syzygium polyanthum W.) sebagai antihiperlipidemia yang mampu hancur cepat setelah diletakkan di atas lidah sangat diperlukan untuk mempercepat onset obat dan memberikan kenyamanan terutama pada pasien hiperlipidemia usia lanjut yang sulit menelan obat. Tujuan dari penelitian ini untuk mengetahui komposisi perbandingan superdisintegrants crospovidone dan croscarmellose sodium yang mampu menghasilkan sifat fisik Fast Disintegrating Tablet (FDT) yang optimum. Pembuatan FDT menggunakan metode granulasi basah dengan variasi konsentrasi crospovidone dan croscarmellose sodium dalam rentang 2%-5%. Hasil uji sifat fisik FDT dianalisis menggunakan metode Simplex Lattice Design (SLD) program Design Expert 10.1.). Kombinasi kedua superdisintegrants dapat mempengaruhi respon sifat fisik yaitu mampu menurunkan kekerasan, waktu disintegrasi, waktu pembasahan dan meningkatkan kerapuhan FDT ekstrak daun salam. Formula optimum didapat pada kombinasi crospovidone dan croscarmellose sodium dengan perbandingan 25 mg : 10 mg dalam setiap 500 mg tablet. Formula optimum tersebut memiliki kekerasan 4,21 kg, kerapuhan 0,52%, waktu pembasahan 106,65 detik, dan waktu hancur 55,73 detik. Hasil analisis dengan one sample t-test menunjukkan persamaan SLD valid digunakan untuk menyusun formula yang memberikan parameter-parameter optimum FDT.

Stability Study of fast Disintegrating tablets of Nisoldipine as per ICH Guidelines

The stability study is a critical parameter to be evaluated in a pharmaceutical product development cycle. A pharmaceutical scientist pays a great deal of heed in testing a product stability. The present research work focused on conducting stability study of fast disintegrating tablet batch of Nisoldipine (NFDT). The various parameters evaluated were weight, hardness, friability, disintegration time, drug content and % drug released. The stability study of optimized fast disintegrating tablet batch NFDT was performed according to ICH guidelines. For the study plan, fast disintegrating tablet batch was placed in a wide mouth air tight containers, which were charged into the stability chamber. The temperature was adjusted at 40°C ± 2°C and relative humidity of 75% ± 5%. The study period was of 6 months. The fast disintegrating tablet batch NFDT did not showed any significant difference in weight, hardness, % friability and disintegration time. The drug content was also reported to be in limits of acceptance. The % drug released at various time intervals was insignificantly changed during its storage period. Hence, the prepared tablets were stable during their storage period.

Formulation Development and Evaluation of Fast Disintegrating Sustained Release Pellets Containing Verapamil Hydrochloride Tablets by Fluidized Bed Processor

This study aimed to developed novel fast disintegrating sustained release pellets containing tablet by using Fluidized Bed processor. Verapamil HCl used as a model drug for the formulation. Fluidized bed processor was used for coating of drug and polymer on the sugar spheres. To overcome the problem of swallowing for paediatric, geriatric, psychiatric, bedridden patients, uncooperative patients or for active patients who are busy and travelling and may not access to we aim to formulate the fast-disintegrating tablet. The superdisintigrant are commonly use like cross povidone, sodium starch glycolate which disintegrate tablet rapidly. It is assumed that, after the disintegration of tablets, pellets within tablets which are reside in GIT for several hours and gradually released a drug in controlled way. Eudragit RS 30D and ethyl cellulose were used as a sustained release polymer. Coating of spheres with sustained release film is achieved by bottom spray processor of FBP. Proper pellets coating film thickness, and concentration of polymers’, ensure obtaining desirable VH release profile for extended period of time, was defined. X composition of tablet with pellets were examined in order to obtained formulation, from which VH release would mostly appropriate pellets before compressing. Compression of pellets into tablet, being a modern technological process than enclosing them into hard gelatine capsule. The optimized batch evaluated by studied the effect of compression force, tablet hardness and friability and drug release from the pellets by sustained release manner.

Optimasi Formula Fast Disintegrating Tablet Domperidone Dengan Amilum Biji Alpukat (Persea Americana Mill.) Sebagai Superdisintegrant

Biji alpukat (Persea americana Mill.) dapat dikembangkan menjadi amilum biji alpukat (Persea americana Mill.) yang dapat digunakan menjadi bahan eksipien formulasi sediaan farmasi. Akan tetapi informasi terkait manfaatnya dalam tablet masih sangat terbatas penggunaannya, sehingga industri farmasi masih jarang menggunakan amilum biji alpukat sebagai alternatif pengganti bahan eksipien dari bahan sintetis superdisintegrant pada fast disintegrating tablet (FDT). Telah dibuat sediaan fast disintegrating tablet dengan variasi konsentrasi amilum biji alpukat (5%, 10% dan 15%) dan pembanding Sodium Starch Glycolate (SSG) konsentrasi 5%. Data yang didapat dianalisis secara statistik menggunakan uji one way ANOVA dan dilanjutkan ke uji tukey (Honestly Significant Difference) HSD. Hasil menunjukkan bahwa variasi konsentrasi amilum biji alpukat terdapat pengaruh pada sifat fisik granul dan sifat fisik tablet, formula III dengan konsentrasi 15% memiliki kriteria yang paling baik sebagai superdisintegrant pada tablet terdisintegrasi cepat. Perlu dilakukan modifikasi lanjutan amilum biji alpukat agar dapat digunakan sebagai superdisintegrant yang lebih efektif dalam formulasi fast disintegrating tablet pada penelitian selanjutnya.

A Novel Pulsatile Release Film Coated Tablet of Zaltoprofen Loaded SNEDDS

The aim of the present study was to formulate pulsatile release film coated tablet of zaltoprofen for the treatment of rheumatoid arthritis. Initially solubility of zaltoprofen was enhanced by formulating self emulsifying fast disintegrating tablet of zaltoprofen. Core fast disintegrating tablet of zaltoprofen was coated with ethyl cellulose and eudragit L100 in various proportions as coating polymer. Ethanol was used as coating solvent and dibutyl phthalate as plasticizer. Film coated tablet with different coating levels were formulated and were evaluated for parameters like lag time, rupture time, in vitro dissolution etc. Amongst the nine different formulations P-4 formulation containing 3:1 ratio of ethyl cellulose and eudragit L100 with 5% coating level gives desired lag time with best drug dissolution profile. Formulated film coated tablet of zaltoprofen can be useful for chronotherapeutic treatment of rheumatoid arthritis.

CHARACTERIZATION AND CONCENTRATION OPTIMIZATION OF HIBISCUS ROSA-SINENSIS L. MUCILAGE POWDER AS SUPERDISINTEGRANT

Objective: The main purpose of this study is to characterize Hibiscus rosa-sinensis L. mucilage (MHR) powder as superdisintegrant and to decide the optimum concentration of Hibiscus rosa-sinensis L. Methods: Characterization was conducted in many tests such as organoleptic, swelling ratio, solubility, polysaccharide, viscosity, particle size distribution, flowability and compressibility index. Next, MHR powder was included in fast disintegrating tablet (FDT) domperidone formulation in several concentrations and compared with FDT domperidone formulation that using sodium starch glycolate as superdisintegrant. Results: The result of characterization of MHR powder were brownish powder, specific smell like traditional medicines, swelling ratio of 24, solubility of 0.426±0.034 mg/ml, positive polysaccharide, the viscosity of 491.33±119.44 cps (2% w/v), 4520.00±1224.42 cps (4% w/v), Dv(10) of 26.2 µm, Dv(50) of 157 µm, Dv(90) of 260 µm, Dv(100) of 380 µm, flowless, and average compressibility index of 26.75±1.79%. The optimum MHR powder concentration was 1% because the average disintegration time was 39.67±4.73 seconds and the average wetting time was 66.33±14.29 seconds. Those times were faster than domperidone FDT that used this superdisintegrant in other concentrations or sodium starch glycolate in the same concentration. Conclusion: Hibiscus rosa-sinensis L. mucilage powder can be used as superdisintegrant in FDT formulation with an optimum concentration of 1%.

Pengaruh kombinasi Superdisintegrant Crospovidone dan Croscarmellose Sodium pada sifat fisik dan disolusi Fast Disintegrating Tablet Hidroklorotiazid

Hidroklorotiazid (HCT) merupakan obat lini pertama untuk penanganan hipertensi. HCT memiliki kelemahan terkait bioavailabilitasnya yang rendah dan umumnya tersedia dalam bentuk sediaan tablet konvensional sehingga dapat menimbulkan masalah tersendiri bagi pasien yang tidak mampu menelan tablet. Fast disintegrating tablet (FDT) HCT merupakan tablet yang dapat terdisintegrasi dan terdisolusi dengan cepat di dalam mulut yang memungkinkan obat dapat diabsorpsi di daerah pregastric sehingga meningkatkan bioavailabilitas obat. Penelitian ini bertujuan untuk mendapatkan formula FDT HCT yang menghasilkan sifat fisik optimum dengan kombinasi superdisintegrant crospovidone (CP) dan croscarmellose sodium (CCS). FDT HCT diformulasikan menggunakan kombinasi superdisintegrant CP:CCS pada rentang konsentrasi CP 2-6% dan CCS 1-5%. FDT dibuat dengan metode kempa langsung. Tablet FDT yang dihasilkan, dilakukan uji sifat fisik tablet yaitu kekerasan, kerapuhan, waktu disintegrasi, waktu pembasahan, rasio absorpsi air, dan uji disolusi. Data diolah dengan metode simplex lattice design menggunakan software Design Expert® untuk memprediksi formula optimum. Hasil penelitian menunjukkan bahwa CP berpengaruh signifikan dalam mempercepat waktu pembasahan, waktu disintegrasi, dan disolusi tablet, sedangkan CCS berpengaruh signifikan dalam menurunkan kekerasan, meningkatkan kerapuhan dan rasio absorpsi air.

Pharmacokinetic and bioavailability study of lercanidipine hydrochloride fast disintegrating tablets in rabbits by high-performance liquid chromatography

In the present study, fast disintegrating tablets of Lercanidipine Hydrochloride (LFDT) were tested in vivo in the buccal cavity of the rabbits. Various pharmacokinetic parameters were analysed in the study, including maximum measured plasma concentration (Cmax), time of maximum measured plasma concentration (tmax) and area under the plasma concentration vs time curve (AUC). Also, the comparative study of the Lercanidipine Hydrochloride fast disintegrating tablets (LFDT) was performed with the marketed conventional tablets of the drug (LMKT). The technique selected for the bioanalytical analysis of the blood samples of the rabbits for pharmacokinetic data computation was High-Performance Liquid Chromatography. An already well-established and validated method was used to analyse the blood samples of the rabbits. The results revealed that the rate of absorption was improved for fast disintegrating tablets of Lercanidipine Hydrochloride (LFDT) as compared to the marketed conventional tablets of the drug (LMKT). This indicated that drug was rapidly absorbed from the fast disintegrating tablet and attained elevated plasma concentration in a short interval after dosing than the marketed formulation. However, the value of tmax was drastically shorter for LFDT than the LMKT. The average peak plasma concentration also designated a rise in the extent of absorption (AUC). From the present study, it was concluded that the fast disintegrating tablet batch (LFDT) had much more improved pharmacokinetic parameters as compared to its conventional marketed counterpart (LMKT).