RESEARCH ARTCLE Rajashre panigrahi et al, IJRRPAS, 2(1)., 65-81 ISSN 2249-1236 65 Formulation and Evaluation of Fast Dissolving Tablet of Lisinopril Rajeshree Panigrahi 1 , Saiprasanna Behera 1 , P.N.Murthy 2 International Journal of Research and Reviews in Pharmacy and Applied science www.ijrrpas.com Rajeshree Panigrahi lecturer, Royal college of Pharmacy and Health sciences, Andhapasara road, Near new mango market, Berhampur-Ganjam, Pin-760003 Sai prasanna Behera, lecturer Royal college of Pharmacy andhealthsciencesAndhapasara road, Near new mango market , Berhampur-Ganjam, Pin-7600 03, Email:[email protected]P.N.Murthy , Director cum Principal of Royal College of Pharmacy and Health Sciences, Andhapasara ABSTRACT - Orodispersible tablets are useful in patients, such as pediatric, geriatric, bedridden or developmentally disabled, who may face difficulty in swallowing conventional tablets or capsules and liquids orals or syrup, leading to ineffective therapy, with persistent nausea, sudden episodes of allergic attack or coughing for those who have an active life style. Fast onset of action- dispersible tablet has major advantage that the drug product is already in solution at that time it is consumed. Thus the absorption is faster and more complete than with conventional tablet. Lisinopril {(S)-1-[N2-(1-carboxy- 3-phenylpropyl)-L proline] dihydrate} is a lysine analog of enalapril at, the active metabolite of enalapril. It is a long-acting, non sulfhydryl angiotensin-converting enzyme (ACE) inhibitor that is used for the treatment of hypertension and congestive heart failure in daily dosages of 10-80 mg. All the superdisintegrants such as crosscarmellose, crosspovidone, sodium starch glycolate were maintained in different concentrations in all the formulations. Microcrystalline cellulose was used as diluent. Here microcrystalline cellulose was also a superdisintegrant; each formulation was composed of drug and excipients in various proportions. This design techniques was used to optimized and obtain better formulation with respect to in vitro dispersion time , Drug release (% ), Disintegration time. In vitro drug release showed that formula C- 5 (Crosspovidone) and S6 (sodium starch glycolate) had better % drug release as compare to other formulations. The faster disintegration may attribute to its rapid capillary activity and pronounce hydration with little tendency to gel formation. Thus these results can suggest that the disintegration time can be decreased by using wicking type of disintegrants. Keywords: Orodispersible tablets, disintegration time, Crosspovidone, Sodium starch glycolate, Superdisintegrant.
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RESEARCH ARTCLE Rajashre panigrahi et al, IJRRPAS, 2(1)., 65-81 ISSN 2249-1236
65 Available on www.ijrrpas.com
Formulation and Evaluation of Fast Dissolving Tablet of Lisinopril
ABSTRACT - Orodispersible tablets are useful in patients, such as pediatric, geriatric, bedridden or developmentally disabled, who may face difficulty in swallowing conventional tablets or capsules and liquids orals or syrup, leading to ineffective therapy, with persistent nausea, sudden episodes of allergic attack or coughing for those who have an active life style. Fast onset of action- dispersible tablet has major advantage that the drug product is already in solution at that time it is consumed. Thus the absorption is faster and more complete than with conventional tablet. Lisinopril {(S)-1-[N2-(1-carboxy-3-phenylpropyl)-L proline] dihydrate} is a lysine analog of enalapril at, the active metabolite of enalapril. It is a long-acting, non sulfhydryl angiotensin-converting enzyme (ACE) inhibitor that is used for the treatment of hypertension and congestive heart failure in daily dosages of 10-80 mg. All the superdisintegrants such as crosscarmellose, crosspovidone, sodium starch glycolate were maintained in different concentrations in all the formulations. Microcrystalline cellulose was used as diluent. Here microcrystalline cellulose was also a superdisintegrant; each formulation was composed of drug and excipients in various proportions. This design techniques was used to optimized and obtain better formulation with respect to in vitro dispersion time , Drug release (% ), Disintegration time. In vitro drug release showed that formula C- 5 (Crosspovidone) and S6 (sodium starch glycolate) had better % drug release as compare to other formulations. The faster disintegration may attribute to its rapid capillary activity and pronounce hydration with little tendency to gel formation. Thus these results can suggest that the disintegration time can be decreased by using wicking type of disintegrants.
Keywords: Orodispersible tablets, disintegration time, Crosspovidone, Sodium starch glycolate, Superdisintegrant.
RESEARCH ARTCLE Rajashre panigrahi et al, IJRRPAS, 2(1)., 65-81 ISSN 2249-1236
66 Available on www.ijrrpas.com
INTRODUCTION
Oral routes of drug administration have wide acceptance up to 50-60% of total dosage forms. Solid dosage forms are popular because of
ease of administration, accurate dosage, self-medication, Pain avoidance and most importantly the patient compliance [1]. The most
popular solid Dosage forms are being tablets and capsules; one important drawback of this dosage forms for some patients, is the
difficulty to swallow. Drinking water plays an important role in the Swallowing of oral dosage forms. Often times people experience
inconvenience in swallowing conventional dosage forms such as tablet when water is not available, in the case of the motion sickness
(kinetosis) and sudden episodes of coughing during the common cold, allergic condition and bronchitis. For these reason, tablets that can
rapidly dissolve or disintegrate in the oral cavity have attracted a great deal of attention. Dispersible tablets are not only indicated for
people who have swallowing difficulties, but also are ideal for active people.
Fast dissolving tablets (FDT) are also called as mouth-dissolving tablets, melt-in mouth tablets, Orodispersible tablets, rapi-melts, porous
tablets, quick dissolving etc. Fast dissolving tablets are those when put on tongue disintegrate instantaneously releasing the drug which
dissolve or disperses in the saliva [2-6]. The faster the drug into solution, quicker the absorption and onset of clinical effect. Some drugs are
absorbed from the mouth, pharynx and esophagus as the saliva passes down into the stomach. In such cases, bioavailability of drug is
significantly greater than those observed from conventional tablets dosage form. The advantage of mouth dissolving dosage forms are
increasingly being recognized in both, industry and academics. Their growing importance was underlined recently when European
pharmacopoeia adopted the term “or dispersible tablet” as a tablet that to be placed in the mouth where it disperses
Rapidly before swallowing. According to European pharmacopoeia, the ODT should disperse/disintegrate in less than three minutes [7-10].
The basic approach in development of FDT is the use of super disintegrants like cross linked carboxymethyl cellulose (Crosscarmellose),
sodium starch glycolate (primo gel, explotab), polyvinylpyrollidone (Polyplasdone) etc, which provide instantaneous disintegration of
tablet after putting on tongue, their by release the drug in saliva. The bioavailability of some drugs may be increased due to absorption of
drug in oral cavity and also due to pregastric absorption of saliva containing dispersed drugs that pass down into the stomach. More ever,
the amount of drug that is subjected to first pass metabolism is reduced as compared to standard tablet. The technologies used for
RESEARCH ARTCLE Rajashre panigrahi et al, IJRRPAS, 2(1)., 65-81 ISSN 2249-1236