Formulation and Evaluation of Fast Disintegrating Tables of Nifedipine by QbD Approach (original) (raw)
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Formulation and Evaluation of Solid dispersion for Dissolution Enhancement of Nifedipine
Nifedipine, a calcium channel blocker antihypertensive drug, is a poorly water soluble drug and belongs to BCS class II. The objective of the research work was to formulate and optimize solid dispersions (SDs) of a poorly water soluble drug, nifedipine, with sodium starch glycollate, croscarmellose sodium, eudragit E-100. Solid dispersions were prepared by solvent evaporation techniques in different weight ratios of polymers. The results indicated that homogeneous or heterogeneous conditions during the preparation methods employed governed the internal structures of the polymer matrices while retaining the drug in an amorphous form. The physical mixtures and solid dispersions were subjected to drug content and dissolution test. The best formulation, nifedipine with croscarmellose sodium in 1:7 ratio, among all was further adsorbed on neusilin US2 to form ternary mixture. The increased dissolution was achieved by more than 70percent and 30percent comparatively to the nifedipine API and marketed product respectively. The tablet dosage form prepared from ternary mixture was stable at stressed conditions 40±2°C and 75±5% RH. The release kinetics of drug from formulation and marketed product follows peppas model. The similar factor f2 was within limit for the product at stressed conditions with the product at room temperature at the same time.
Formulation and Evaluation of Fast Dissolving Tablet of Nifedipine
2020
In the present study, there was an attempt to make rapidly dissolving tablets using the direct dissolution method containing Nifedipine-Mannitol solid dispersion. The main objective of the work was to prepare nifedipine solid dispersion with Mannitol to initiate action. The solid dispersion was prepared by the solvent evaporation method and evaluated for cumulative drug release. FDT was formulated by a direct compression method using different super Disintegrants such as CCS and SSG in different ranges (1–3 %). Preformation studies were performed on the powder mixture for tablets. The flow properties (F1 – F18) of the mixture were evaluated by determining the Carr's index, the Hausner ratio, and the angle of view. Condensate density, tapped density, Carr's index, Hausner ratio and representation of angles. The formulated tablets were evaluated for thickness, hardness, stability, weight variation, wetting time, drug content uniformity, dissolution time, and invitro dissolutio...
Dhaka University Journal of Pharmaceutical Sciences, 2015
Fast disintegrating tablets of nifedipine prepared by superdisintegrant addition and sublimation methods were evaluated. Twelve batches of tablets were formulated by direct compression using varying concentrations of crospovidone and croscarmellose sodium. Camphor was incorporated into six of the batches. Their granules were evaluated for pre-compression and post-compression parameters. FTIR analysis of the drug and excipients was also carried out. Results obtained showed that their granules were free flowing with angle of repose < 26° and Carr's index < 19 %. The tablets gave hardness of 3.67-5.99 kgf, friability of < 1 %, wetting and disintegration times of < 101 and < 91 secs, respectively. Dissolution profiles showed all the tablets released over 92 % of their drug within 30 mins. FTIR analysis demonstrated no interactions between nifedipine and excipients. The sublimation method in combination with superdisintegrant addition method of formulation yielded fast disintegrating tablets of superior quality than the superdisintegrant addition method alone.
Formulation of solid dispersion and surface solid dispersion of nifedipine: A comparative study
African journal of pharmacy and pharmacology
In this study, an attempt was taken to enhance the solubility and dissolution characteristics of nifedipine, a poorly water soluble calcium channel blocking agent, by preparing solid dispersions (SD) with water soluble carriers; Poloxamer 407, HPMC 5 cPs, polyethylene glycol (PEG) 4000 and 6000 and surface solid dispersions (SSD) with insoluble carriers; sodium starch glycolate (SSG) and croscarmellose sodium (CCS). In vitro dissolution study showed that all the preparations were effective to improve the dissolution of nifedipine to several folds when compared with the drug and physical mixtures (PMs). Drug loading in SDs and SSDs was found uniform and they produced satisfactory results on drug content analysis (95 to 102%), compatibility and thermal analysis. PEG 6000, Poloxamer 407 and SSG were found to be the most effective carriers to enhance the dissolution behavior of nifedipine. SDs with water soluble carriers were found more effective in improving solubility of nifedipine th...
The influence excipients on the dissolution profiles of nifedipine tablets
Scripta Scientifica Pharmaceutica, 2014
Currently a large number of generic drugs are registered in Ukraine for medical use. The advantage of generic drugs is the relatively cheapness compared to innovative medicines, because the creation and registration of generic drugs require less research and, consequently, less material costs, which are nec-ABSTRACT PURPOSE: Study of dissolution profiles of nifedipine tablets from different manufacturers to further assess of their equivalence in vitro, as well as study of the dependence of the dissolution profile on the adjuvants composition. MATERIAL AND METHODS: 3 buffer media with pH 1.2 (hydrochloric acid buffer); 4.5 (acetate buffer); 6.8 (phosphate buffer) was used. The absorptions were observed at 343. RESULTS: The dissolution profiles of nifedipine tablets from different manufacturers have been studied and have been founded that the percentage of nifedipine release from the sample B is higher than from "Corinfar", and the percentage of nifedipine release from "Corinfar" is higher than from the sample A. Adjuvants composition of nifedipine tablets have been studied. It is founded that the inclusion of surfactants, solubilizers and emulsifiers into tablets contribute to increasing of active substance release from the dosage form. CONCLUSIONS: Found that the introduction of surfactants into tablets, solubilizers and emulsifiers help to increase the release of active substance from the dosage form.
International Journal of Research in Pharmaceutical Sciences, 2020
Nifedipine has a bioavailability of 45-56 percent and a 2-hour elimination half-life. It has a 50 percent kidney excretion rate and a 5-15 percent bile excretion rate. The intention of this research is to invent and evaluate Nifedipine loaded ODT and to prove the enhancement of bioavailability. The 23 factorial optimization design exposed about the outcome of independent variable on dependent variable throughout the formulation of Nifedipine ODT. From the records, it was accomplished that there was a good correlation between Disintegration time, Dissolution rate and super disintegration concentration. The formulation F4 (Nifedipine ODT) has achieve the goal of ODT drug delivery with desired release characteristics, cost-effective, decreased dose, effective administration and hence improved patient compliance. The invivo pharmacokinetic studies reveals that increase in AUC0-∞; decrease in Tmax; increase in Cmax in Nifedipine ODT shows better bioavailability and faster duration of the...
Tablet among the all dosage form is the common one and in the Pharmacy it is the mother of Pharmacy. Generally tablet are accepted in all category of patient. In children Dispersible form and in female for virginal infection virginal form are the preferred. The most common preferred route is oral rout of administration. In ancient Ayurveda, Unani, Greek, Egyptian remedies drug in the form of Churna, Bhasma, Gutika, Araka, are administered though oral rout. Pills which are coated by natural resinous material are administered in the form of tablet through oral rout. Today oro-dispersible tablet from novel drug delivery system gain importance from patient. Which is administer to the patient to control the various immediate action viz. attack of angina or hypertension in cardiac problems. Orodispersible tablet gets dispersed in oral cavity in absence of water and release fast drug which result fast pharmacological action. In the market drug from Analgesic, Antipyretic, Antihypertensive and many more are available in the form of the orodispersible tablet. Various manufacture are formulated this formulation by various method. The most importance thing in this formulation are masking of taste of drugs. Generally oro-dispersible tablet are prepared by direct compression method. Dry granulation, wet granulation, Spry drying is the various methods for preparation of oro-dispersible tablet. Oro-dispersible tablet generally contains filler, glidant, anti-adherent super disintegrate, Flavoring agent sweetener and resins. Evaluation parameter includes hardness, friability, wetting time, moisture uptake, disintegration test, and dissolution test. Wetting time, Disintegration time, and Dissolution test is directly proportional to the hydrophobic ingredient added for lubrication, anti-adherent, Glidant action. These hydrophobic ingredient are Magnesium Stearate. To oppose the action of magnesium stearate, hydrophilic additives are incorporated viz Sodium lauryl sulphate. From Marketing point of view special Marketing Executive team required to promote the new technique , new formulation with demonstration to the Cardiac Surgeon, Pediatrics, Orthopedics, Gynecologists, Ophthalmologists, Urologist. After demonstration that how to use the Orodispersible tablet these marketing team personally serve to the new admitted patients.
Effect of Water-Soluble Carriers on Dissolution Characteristics of Nifedipine Solid Dispersions
Drug Development and Industrial Pharmacy, 2000
T he solid binary systems of aceclofenac (AC) with β-cyclodextrin (βCD) were prepared by co-grinding, kneading, and co-evaporation, and with PEG 6000 were prepared by the melt-solvent method in 1:1 and 1:2 molar and weight ratios, respectively. The phase solubility study with βCD suggested B S type of curve with a possibility of 1:1 inclusion complex. The solid systems were characterized by in vitro release studies, DSC, and SEM. The results of solid state studies revealed that AC was completely dissolved in the carrier matrix in case of the melt-solvent method, which suggested the possible formation of solid solution with AC to be existed in an amorphous state. All the binary systems exhibited improved dissolution as compared to pure drug. However, the best dissolution enhancement was achieved with the binary system AC: PEG 6000 in 1:2 weight ratio using the melt-solvent method which was subjected to tablet preparation by direct compression. The tablets so compressed complied with in-house and compendial specifications. The in vitro dissolution test was carried out for the formulated tablets and three popular marketed brands of conventional AC tablets. None of the commercial brands showed complete drug release but the formulated tablets exhibited almost complete drug release within 50 min. The dissolution data were further characterized using model-independent parameters DP 30 , DE 50 , t 50% , similarity factor f 2 and difference factor f 1. The tablets formulated incorporating the AC: PEG 6000 (1:2) binary system displayed significantly improved dissolution profile as compared to existing immediate release commercial tablets.
Pharmacon: Jurnal Farmasi Indonesia
Nifedipine is a drug that acts as an antihypertensive and anti-angina. Nifedipine is known as a drug with poor water solubility. This characteristic will affect the intrinsic dissolution rate so that it can affect the absorption process and reduce the amount of drug that reaches systemic circulation. One of the strategies to increase the intrinsic dissolution rate is developing nifedipine to solid dispersions form. This study aims to observe the intrinsic dissolution rate of nifedipine after it has been made into a solid dispersion. Four samples were prepared, including three solid dispersions of nifedipine-PVP K-30 and one sample of pure nifedipine. The results of the intrinsic dissolution tests are then interpreted through the intrinsic dissolution rate constant (G). The solid dispersions with concentration of nifedipine-PVP K-30 90%:10%; 75%:25%; 60%:40% (w/w), and pure nifedipine produced G values of 3.63; 9.33; 12.63; and 2.08 µg/mm2. min1, consecutively. It shows that the form...
The effect of some natural polymers on the solubility and dissolution characteristics of nifedipine
International Journal of Pharmaceutics, 1992
The effect of natural polymers, such as eater-soluble gelatin and egg albumin, on the ~lubili~ and di~olution characteristics of nifedipine has been studied. Comparison of such polymers was carried out by complexation with &cyclodextrin. The interaction of nifedipine with these polymers both in aqueous solution and in the solid state was examined by performing solubility analysis, powder X-ray diffractometry and differential scanning calorimetry measurements. In addition, the surface tension of the samples was evaluated. Solid mixtures of nifedipine and polymer in various ratios were prepared by the kneading technique and their dissolution was carried out according to the dispersed amount method. It was found that water-soluble gelatin and P-cyclodextrin resulted in a significant increase in the rate of dissolution of nifedipine as compared to drug alone. Further, water-soluble gelatin may be particularly useful for the enhancement of dissolution of nifedipine.