Hydroxyl Ethyl Cellulose HHX and Polymethyl Methacrylate Based Site Specific Floating Delivery of Prochlorperazine Maleate

Abstract

Background:Prochlorperazine maleate is a phenothiazine antipsychotic used principally in the treatment of nausea, vomiting and vertigo. Biological half- life of the drug is about 6 to 8 hrs and oral dose is 5 or 10 mg thrice or four times a day. The mean absolute bioavailability for drug is 12.5%. Due to the solubility of drug in acidic pH, it is mainly absorbed from stomach.Objective:Site specific oral floating delivery of prochlorperazine maleate will prolong the gastric retention time, increases the drug bioavailability, reduces frequency of administration and can result in better patient compliance.Method:The tablets were prepared by direct compression technique. Floating drug delivery was developed using gas forming agent and release retarding agenti.e.hydroxyethyl cellulose HHX (Natrosol HHX) and polymethyl methacrylate (PMMA). 32full factorial design was used for optimization. Prepared tablets were evaluated for pre and post compression parameters.Results:From the factorial batches it was observed that formulation containing 68.5% of hydroxyethyl cellulose HHX and 15% of polymethyl methacrylate had shown a drug release of 91.56 ± 2.7% with floating upto 10 hrs following Korsmeyer Peppas release kinetics.Conclusion:In- vivoplacebo X-ray study for optimized batch F6 had shown good gastroretention ability for 6 ± 0.5 hrs.In- vitroandin- vivostudy confirmed the site specific floating delivery for drug.

Pharmacological Treatment of Acute Unilateral Vestibulopathy: A Review

“…Relevant compounds for the treatment of vertigo include promethazine [42], prochlorperazine [51][52][53], and thiethylperazine [54], all of which have anticholinergic properties that result in sedative and anti-emetic effects by acting on the chemoreceptor trigger zone (CTZ) [4,51]. Low-dose promethazine (6.25 mg) has been shown to have anti-emetic effects comparable to 4 mg ondansetron but superior vertigo suppression abilities [42,55].…”